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Dictionary of drugs:A3

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Dictionary of drugs A page 3

g tumor cells. B7-H4, a member of the B7 family of immune modulators, is upregulated in a variety of tumor cell types and negatively regulates T-cell immune responses.


anti-B7-H4 monoclonal antibody FPA150

A fully human, glycoengineered monoclonal antibody targeting B7-H4 (V-set domain-containing T-cell activation inhibitor 1; VTCN1; B7x; B7S1) with potential antineoplastic and immune checkpoint inhibitory activities. Upon intravenous administration, anti-B7-H4 monoclonal antibody FPA150 binds to B7-H4 on the surface of tumor cells, thereby preventing B7-H4 binding to T cells and abrogating the B7-H4-mediated negative regulation of T-cell activation. This increases a cytotoxic T-lymphocyte (CTL)-mediated immune response against B7-H4-expressing tumor cells. In addition, the afucosylated Fc region of the anti-B7-H4 monoclonal antibody FPA150 enhances its binding affinity for human FcgammaRIIIa receptors (CD16) on natural killer (NK) cells, resulting in enhanced antibody-dependent cellular cytotoxicity (ADCC) against B7-H4-expressing tumor cells. B7-H4, a member of the B7 family of immune modulators, is upregulated in a variety of tumor cell types and negatively regulates T-cell immune responses.


anti-BCMA antibody SEA-BCMA

A humanized, afucosylated monoclonal antibody created using the proprietary, sugar-engineered antibody (SEA) platform and directed against the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; TNFRSF17), with potential immunoadjuvant activity. Upon administration, the anti-BCMA antibody SEA-BCMA targets and binds to BCMA expressed on tumor cells. When administered with antibody-coupled T-cell receptor (ACTR)-expressing T cells, the ACTR-expressing T cells bind, with high affinity, to the anti-BCMA antibody SEA-BCMA. This activates the ACTR T-cells and the T cells induce specific cytotoxic T-lymphocyte (CTL)-mediated cytotoxicity toward BCMA-expressing tumor cells. BCMA, a cell surface protein and member of the tumor necrosis factor (TNF) receptor superfamily that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival.


anti-BCMA antibody-drug conjugate GSK2857916

An antibody-drug conjugate (ADC) consisting of an afucosylated, humanized monoclonal antibody, directed against the B-cell maturation antigen (BCMA), conjugated to the auristatin analogue and microtubule inhibitor monomethyl auristatin phenylalanine (MMAF), with potential antineoplastic activity. The anti-BCMA antibody moiety of anti-BCMA ADC GSK2857916 selectively binds to the BCMA on tumor cell surfaces. Upon internalization, the MMAF moiety binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces tumor cell apoptosis. In addition, GSK2857916 induces antibody-dependent cellular cytotoxicity (ADCC). Altogether, this results in the inhibition of cellular proliferation in tumor cells that overexpress BCMA. BCMA, a receptor for a proliferation-inducing ligand and B-cell activating factor, is a member of the tumor necrosis factor (TNF) receptor superfamily and plays a key role in plasma survival; it is found on the surfaces of plasma cells and overexpressed on malignant plasma cells. Afucosylation of the antibody moiety increases ADCC.


anti-BCMA/CD3 BiTE antibody AMG 701

A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; TNFRSF17), fused to one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-BCMA/CD3 BiTE antibody AMG 701, this bispecific antibody binds to both CD3 on cytotoxic T lymphocytes (CTLs) and BCMA found on BCMA-expressing tumor cells. This activates and redirects CTLs to BCMA-expressing tumor cells, which results in the CTL-mediated cell death of BCMA-expressing tumor cells. BCMA, a member of the tumor necrosis factor receptor superfamily that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival.


anti-BCMA/PBD ADC MEDI2228

An antibody-drug conjugate (ADC) consisting of a fully human monoclonal antibody against the tumor-associated antigen (TAA) B-cell maturation antigen (BCMA, TNFRSF17) that is site-specifically conjugated, via a protease-cleavable linker, to a cytotoxic, DNA minor groove crosslinking agent and pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration of anti-BCMA/PBD ADC MEDI2228, the antibody moiety targets the cell surface antigen BCMA expressed on certain cancer cells. Upon antibody/antigen binding, internalization and lysosome-mediated cleavage, the cytotoxic PBD moiety is released. In turn, the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of BCMA-overexpressing tumor cells. BCMA, a receptor for a proliferation-inducing ligand (APRIL; tumor necrosis factor ligand superfamily member 13; TNFSF13), and B-cell activating factor (BAFF), is a member of the tumor necrosis factor (TNF) receptor superfamily and plays a key role in plasma survival; it is found on the surfaces of plasma cells and is overexpressed on malignant plasma cells.


antibiotic SQ109

An orally available, acid-stable diamine antibiotic, with potential antimicrobial activity against a variety of bacteria including Helicobacter pylori (H. pylori) and Mycobacterium tuberculosis (M. tuberculosis). As an ethambutol analogue with asymmetric structure, SQ109 does not act on the same target as ethambutol. However, this agent interferes with cell wall synthesis, thereby causing weakening of the cell wall and ultimately cell lysis.


antibody-drug conjugate ABBV-085

An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of ABBV-085 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action.


antibody-drug conjugate ABBV-155

An antibody-drug conjugate (ADC) composed of an as of yet undisclosed monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of ABBV-155 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action.


antibody-drug conjugate ABBV-176

An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against the prolactin receptor (PRLR) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of ABBV-176 targets and binds to PRLR expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the PRLR-expressing tumor cells, through an as of yet unknown mechanism of action. PRLR, a tumor-associated antigen (TAA), is overexpressed by a variety of tumor cell types.


antibody-drug conjugate ADC XMT-1536

A proprietary antibody-drug conjugate (ADC) composed of XMT-1535, a proprietary, humanized monoclonal antibody against human sodium-dependent phosphate transport protein 2B (SLC34A2; NaPi2b), site-specifically linked, via a protease cleavable linker, to the proprietary cytotoxic aurastatin derivative auristatin F-HPA (AF-HPA; auristatin F-hydroxypropylamide), with potential antineoplastic activity. XMT-1536 is produced via the proprietary dolaflexin ADC conjugation platform, which promotes the conjugation of between 10 and 15 AF-HPA payload molecules to each XMT-1535 antibody. Upon administration of XMT-1536, the antibody moiety targets and binds to NaPi2b expressed on tumor cells. Upon binding, internalization by endosomes/lysosomes, and enzymatic cleavage, the AF-HPA binds to tubulin and inhibits microtubule polymerization, which results in G2/M phase arrest and apoptosis of NaPi2b-expressing tumor cells. NaPi2b, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer cells and plays a key role in the transport of inorganic phosphate (Pi) and the maintenance of phosphate homeostasis.


antibody-drug conjugate ADCT-402

An antibody-drug conjugate (ADC) consisting of an anti-CD19 humanized monoclonal antibody conjugated, via a cleavable linker comprised of valine-alanine and maleimide, to a cytotoxic, cross-linking agent pyrrolobenzodiazepine (PBD) dimer, which targets DNA minor grooves, with potential antineoplastic activity. Upon administration, the monoclonal antibody portion of anti-CD19-PBD conjugate ADCT-402 targets the cell surface antigen CD19 on various cancer cells. Upon antibody/antigen binding and internalization, the cytotoxic PBD moiety is released. The imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA and inhibits DNA replication, which inhibits the proliferation of CD19-overexpressing tumor cells. CD19, a transmembrane receptor and tumor-associated antigen (TAA), is expressed on a number of B-cell-derived cancer s.


antibody-drug conjugate anti-TIM-1-vcMMAE CDX-014

A human immunoglobulin G1 (IgG1) monoclonal antibody-drug conjugate (ADC) targeting the extracellular domain of T-cell immunoglobulin mucin-1 (TIM-1) (clone CR014) and linked, via a valine-citrulline (vc) peptide linker, to the potent cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of ADC Anti-TIM-1-vcMMAE CDX-014, the monoclonal antibody moiety targets and binds to TIM-1. Upon internalization and proteolytic cleavage, MMAE is released into the cytosol of TIM-1-expressing tumor cells, binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. TIM-1 is upregulated in a variety of cancer cell types while only minimally expressed in healthy tissue. The linkage system in CDX-014 is highly stable in plasma, resulting in cytotoxic specificity for TIM-1-positive cells.


antibody-drug conjugate BAY79-4620

A monoclonal antibody (MoAb) directed against the MN protein with potential antineoplastic activity. Upon administration of BAY79-4620, this MoAb may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response and an antibody mediated cellular cytotoxicity (ADCC) against MN-expressing tumor cells. MN, a transmembrane glycoprotein, is expressed in some human carcinomas and appears to be involved in cancer cell proliferation and transformation.


antibody-drug conjugate DFRF4539A

An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against a specific myeloma antigen and conjugated to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of DFRF4539A selectively binds to a specific protein expressed on the surface of myeloma cells. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and tumor cell apoptosis.


antibody-drug conjugate MEDI7247

An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against an unnamed tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of MEDI7247 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action.


antibody-drug conjugate SC-002

An antibody-drug conjugate (ADC) composed of an as of yet publicly unknown monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-002 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action.  


antibody-drug conjugate SC-003

An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-003 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action.


antibody-drug conjugate SC-004

An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to a currently undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-004 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an unknown mechanism of action.


antibody-drug conjugate SC-005

An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to a currently undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-005 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an unknown mechanism of action.


antibody-drug conjugate SC-006

An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-006 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action.


antibody-drug conjugate SC-007

An antibody-drug conjugate (ADC) composed of a monoclonal antibody against an undisclosed tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-007 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action.  


antibody-like CD95 receptor/Fc-fusion protein CAN-008

A human, soluble fusion protein consisting of the extracellular domain of the CD95 receptor fused to the Fc-domain of the human IgG antibody, with potential antineoplastic activity. Upon administration, antibody-like CD95 receptor/Fc-fusion protein CAN-008 binds to the CD95 ligand (CD95L) and blocks the binding of CD95L to the CD95 receptor. In tumor cells, blockage of CD95L-mediated signaling pathways may prevent cell migration and invasive cell growth; in healthy cells, blockage of CD95L-mediated signaling pathways may prevent apoptosis and may protect cell damage. Activation of the CD95 receptor plays an important role in the initiation of apoptosis in healthy cells or the invasive growth of cancer cells.


anti-C4.4a antibody-drug conjugate BAY1129980

An antibody-drug conjugate (ADC) composed of an antibody against a structural homolog of the urokinase-type plasminogen activator receptor (uPAR) and tumor-associated antigen, C4.4a, and conjugated with a cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, anti-C4.4a antibody-drug conjugate BAY1129980 targets and binds to C4.4a-expressing tumor cells. Upon binding and cell entry, the cytotoxic agent kills the tumor cell. C4.4a, a glycolipid-anchored membrane protein and a member of the Ly-6 family, is overexpressed by a variety of cancer cell types whereas it is minimally expressed on healthy cells.


anti-CA19-9 monoclonal antibody 5B1

A human monoclonal antibody against the carbohydrate antigen sialyl-Lewis A (carbohydrate antigen 19-9; CA19-9), with potential antineoplastic activity. Upon administration, monoclonal antibody 5B1 binds to CA19-9 and kills CA19-9-expressing tumor cells, possibly through the induction of both complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC). CA19-9 is overexpressed on a number of different tumor cell types, and plays a key role in tumor cell survival and metastasis.


anti-CA6-DM4 immunoconjugate SAR566658

An immunoconjugate consisting of a humanized monoclonal antibody against the tumor-associated sialoglycotope CA6 (huDS6) conjugated to the cytotoxic maytansinoid DM4, with potential antineoplastic activity. The anti-CA6 monoclonal antibody moiety of SAR566658 targets and binds to the cell surface antigen CA6. Upon antibody/antigen binding and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CA6-expressing tumor cells. The CA6 epitope is found on a variety of solid tumors, including breast, ovarian, cervical, lung and pancreatic tumors.


anticachexia agent MT-102

A small molecule with potential anticachexia activity. The anticachexia agent MT-102 may increase protein synthesis and decrease muscle protein breakdown. This may result in improved body weight, muscle mass and may improve weakness and fatigue associated with cancer -related cachexia.  


anti-CCR5 monoclonal antibody PRO 140

A humanized immunoglobulin (Ig) G4 monoclonal antibody against CC chemokine receptor 5 (CCR5; CD195), with potential activity as a human immunodeficiency virus (HIV) entry blocker and potential protective activity against graft-versus-host disease (GvHD). Upon administration, PRO 140 targets and binds to CCR5 expressed on T cells. This blocks HIV cell entry, which prevents HIV infection and/or reduces HIV viral load. In addition, blocking CCR5 by PRO 140 decreases CCR5-mediated signaling and the CCR5-induced migration of donor cells into tissues after an allogeneic hematopoietic cell transplantation (HCT). Blocking CCR5 may therefore prevent or reduce GvHD. CCR5, a co-receptor needed for HIV cell entry, plays a key role in immunomodulation. Expressed on monocytes, activated T cells and dendritic cells (DCs), CCR5 can regulate chemotaxis. Lymphocyte trafficking via chemokine receptors, such as CCR5, and recruitment to target organs, plays a critical role in alloreactive responses.


anti-CD123 ADC IMGN632

An antibody-drug conjugate (ADC) consisting of a humanized anti-CD123 (interleukin-3 (IL-3) receptor alpha chain; IL3RA) immunoglobulin G1 (IgG1) monoclonal antibody conjugated, via a cleavable linker, to a cytotoxic, DNA-alkylating payload, which is an indolino-benzodiazepine dimer containing an imine moiety, with potential antineoplastic activity. Upon administration of anti-CD123 ADC IMGN632, the antibody moiety targets the cell surface antigen CD123. Upon antibody/antigen binding, internalization, and lysosome uptake, the cytotoxic moiety is released, and covalently binds to and alkylates DNA with its imine moiety. This results in cell cycle arrest in S-phase, which leads to apoptosis and inhibition of cell growth in cells overexpressing CD123. CD123, the alpha subunit of the IL-3 receptor, regulates the proliferation, survival and differentiation of hematopoietic cells. CD123 is overexpressed on a variety of cancer s.


anti-CD123 monoclonal antibody KHK2823

A fully human monoclonal antibody against CD123 (interleukin-3 receptor alpha chain) with potential antineoplastic activity. Anti-CD123 monoclonal antibody KHK2823 binds to and neutralizes CD123, which is upregulated on leukemic stem cells (LSC) found in myelodysplastic syndrome (MDS) or acute myeloid leukemia (AML). This agent may inhibit IL-3-dependent signaling and proliferation and may prevent the uncontrolled growth and differentiation of mutated LSC.


anti-CD123 x anti-CD3 bispecific antibody XmAb14045

An anti-CD123/anti-CD3 bispecific monoclonal antibody, in which most of the naturally-occurring Fc domain is maintained, with potential immunostimulatory and antineoplastic activities. Anti-CD123/CD3 monoclonal antibody XmAb14045 possesses two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for CD123, a tumor-associated antigen (TAA) overexpressed on the surface of certain tumor cells. Upon administration of XmAb14045, this bispecific antibody simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This may result in potent CTL-mediated cell lysis of CD123-expressing tumor cells. CD123, the interleukin-3 receptor alpha chain, is overexpressed in a variety of hematological malignancies; its expression is low or absent in normal hematopoietic progenitors and stem cells. The Fc domain on the antibody prolongs the half-life of the bispecific antibody and enhances T-cell-mediated tumor cell killing through its binding to the Fc receptors.


anti-CD123/CD3 bispecific antibody APVO436

An immunoglobulin Fc-modified bispecific monoclonal antibody against the tumor-associated antigen (TAA) CD123 and the human T-cell surface antigen CD3 bispecific monoclonal antibody, with potential immunostimulatory and antineoplastic activities. Upon administration, anti-CD123/CD3 monoclonal antibody APVO436 simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This results in the activation and proliferation of T-cells and causes CTL-mediated cell lysis of CD123-expressing tumor cells. CD123, the interleukin-3 receptor alpha chain, is overexpressed in a variety of hematological malignancies; its expression is low or absent in normal hematopoietic progenitors and stem cells. The Fc domain on the antibody prolongs the half-life of the bispecific antibody. Compared to some other CD123 x CD3 targeting bispecific antibodies, APVO436 causes less cytokine release upon T-cell stimulation.


anti-CD123/CD3 bispecific antibody JNJ-63709178

A humanized anti-CD123/anti-CD3 bispecific monoclonal antibody, with potential immunostimulating and antineoplastic activities. Anti-CD123/CD3 bispecific antibody JNJ-63709178 possesses two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for CD123, a tumor-associated antigen (TAA) overexpressed on the surface of certain tumor cells. Upon administration of JNJ-63709178, this bispecific antibody simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This may result in potent CTL-mediated cell lysis of CD123-expressing tumor cells. CD123, the interleukin-3 receptor alpha chain, is overexpressed in a variety of cancer s; its expression is low or absent in normal, healthy cells.


anti-CD123-pyrrolobenzodiazepine dimer antibody drug conjugate SGN-CD123A

An antibody-drug conjugate (ADC) consisting of an anti-CD123 humanized monoclonal antibody conjugated, via a stable maleimidocaproyl-valine-alanine dipeptide protease-cleavable linker, to the cytotoxic, DNA minor-groove crosslinking agent pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration of anti-CD123 ADC SGN-CD123A, the antibody moiety targets the cell surface antigen CD123. Upon antibody/antigen binding, internalization, and lysosome uptake, the cytotoxic PBD moiety is released. In turn, the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of CD123-overexpressing tumor cells. CD123, the alpha subunit of the IL-3 receptor, regulates the proliferation, survival and differentiation of hematopoietic cells. CD123 is overexpressed on a variety of cancer s, including myeloid leukemia, and increased expression of CD123 on leukemic stem cells is associated with poor prognosis. Cysteine engineering of the monoclonal antibody (EC-mAb) allows for a site-specific, stable conjugation and uniform loading of the PBD agent to the antibody.


anti-CD133-CAR vector-transduced allogeneic T lymphocytes

A preparation of allogeneic peripheral blood T lymphocytes (PBTL) that have been genetically modified to express a chimeric antigen receptor (CAR) specific for the chimeric CD (cluster of differentiation) 133 antigen receptor, with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD133-CAR vector-transduced allogeneic T lymphocytes specifically recognize and kill CD133-expressing tumor cells. CD133, a tumor associated antigen (TAA), is overexpressed on a variety of tumor cell types.


anti-CD133-PE38-KDEL fusion protein

A fusion protein consisting of an anti-single-chain variable fragment (scFv) peptide sequence targeting the extracellular domain of human CD133 (prominin-1) (anti-CD133scFV) and a deimmunized truncated form of Pseudomonas exotoxin A (38-kDa derivative of PE; PE38) where the five C-terminal amino acid residues have been replaced with the endoplasmic reticulum (ER) retention signal, KDEL, with potential antineoplastic activity. Upon administration of the anti-CD133-PE38-KDEL fusion protein, the anti-CD133 scFV moiety targets and binds to CD133, which is expressed on a variety of tumor cells. Upon internalization of the receptor-fusion protein complex, the KDEL sequence targets the fusion protein to the ER, where the PE38 exotoxin portion then inhibits protein synthesis, which results in a reduction of proliferation of CD133-expressing tumor cells. CD133, a glycoprotein expressed by a variety of cancer s and especially by cancer stem cells (CSCs), plays a key role in tumor initiation, proliferation and progression.


anti-CD157 monoclonal antibody MEN1112

A humanized, Fc-engineered, de-fucosylated monoclonal immunoglobulin G1 (IgG1) antibody directed against the bone marrow stromal cell antigen 1 (BST1/CD157), with potential antineoplastic activity. Upon intravenous infusion, anti-CD157 monoclonal antibody MEN1112 specifically binds to and induces an antibody-dependent cell cytotoxic (ADCC) response against CD157-expressing tumor cells. CD157, also known as ADP-ribosyl cyclase 2, is a glycosyl-phosphatidylinositol (GPI)-anchored transmembrane protein belonging to the ADP-ribosyl-cyclase family and is overexpressed on certain cancer cell types. Fc-optimization of MEN1112, which involves the removal of fucose residues from its Fc domain, allows for enhanced Fc-gamma receptor binding on effector cells, such as natural killer (NK) cells, and further enhances tumor cell lysis.


anti-CD166 probody-drug conjugate CX-2009

A probody drug conjugate (PDC) composed of a recombinant antibody targeting the tumor-associated antigen (TAA) CD166, which is masked by a cleavable masking peptide, and conjugated to the cytotoxic agent maytansinoid DM4, with potential antineoplastic activity. Upon administration of CX-2009 and migration to the tumor microenvironment (TME), the cleavable masking peptide, which prevent anti-CD166 antibody binding to the CD166 expressed on both normal cells and tumor cells, is proteolytically cleaved by tumor-associated proteases that are specifically present in the TME. This enables the anti-CD166 antibody moiety of CX-2009 to selectively bind to, be internalized by, and deliver DM4 into CD166-expressing tumor cells. Following internalization, DM4 is released, binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CD166-expressing tumor cells. The masking peptide prevents binding of the anti-CD166 antibody to CD166 in normal tissues, thereby minimizing toxicities.


anti-CD19 fully human monoclonal antibody MDX-1342

A fully human anti-CD19 monoclonal antibody directed against the B-cell-specific membrane protein CD-19 with potential antineoplastic activity. Anti-CD19 monoclonal antibody MDX-1342 binds to CD19, depleting and eliminating CD19-expressing B-cells. CD19 is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.


anti-CD19 monoclonal antibody DI-B4

A low-fucosylated, humanized, IgG1 isotype, monoclonal antibody directed against the B-cell-specific membrane protein CD19 with potential immunostimulating and antineoplastic activities. Anti-CD19 monoclonal antibody DI-B4 binds to CD19, which may result in a strong antibody-dependent cellular cytotoxicity (ADCC) directed at CD19-expressing B-cells but with minimal complement dependent cytotoxicity. DI-B4 contains low levels of fucose, which contributes to its enhanced ADCC activity. CD19 is a B-cell specific membrane antigen that is widely expressed during B-cell development and in all B-cell lineage malignancies.


anti-CD19 monoclonal antibody MEDI-551

A humanized immunoglobulin IgG1 kappa monoclonal antibody directed against the B-cell-specific membrane protein CD-19 with potential immunostimulating and antineoplastic activities. Anti-CD19 monoclonal antibody MEDI-551 binds to CD19, which may result in a cytotoxic T-lymphocyte (CTL) response and antibody-dependent cellular cytotoxicity (ADCC) to CD19-expressing B-cells. The Fc portion of MEDI-551 does not contain a fucose sugar moiety, which may contribute to its enhanced ADCC activity. CD19 is a membrane antigen that is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.  


anti-CD19 monoclonal antibody XmAb5574

An Fc engineered, humanized anti-CD19 monoclonal antibody directed against the B-cell-specific membrane protein CD19 with potential immunostimulating and antineoplastic activities. Anti-CD19 monoclonal antibody XmAb5574 targets and binds to CD19, thereby depleting and eliminating CD19-expressing B-cells. The modified Fc region of XmAb5574 increases binding affinity to Fc-gamma receptors of effector cells and thereby enhances antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cell-mediated phagocytosis (ADCP). CD19 is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.


anti-CD19/CD20/CD22/CD30 CAR-T cells

A preparation of human T lymphocytes engineered to express a chimeric antigen receptor (CAR) specific for the tumor-associated antigens (TAAs) cluster of differentiation 19 (CD19), CD20, CD22 and CD30, with potential immunostimulating and antineoplastic activities. Upon administration, the anti-CD19/CD20/CD22/CD30 CAR-T cells target and bind to CD19, CD20, CD22 and CD30 expressed on the surface of certain tumor cells. This induces selective toxicity in tumor cells expressing these TAAs. The TAAs are overexpressed in certain hematologic malignancies.


anti-CD19/CD22 bispecific ligand-directed toxin DT2219ARL

An immunotoxin consisting of two scFv ligands recognizing human CD19 and CD22 linked to the first 389 amino acids of diphtheria toxin (DT), DT 390, with potential antineoplastic activity. The VH and VL regions of anti-CD22 (sFv) and anti-CD19 are reversed and linked by an aggregration stabilizing linker (ARL) consisting of a 20 amino acid segment of human muscle aldolase (hma) and an Xho1 -compatible restriction site; the CDR3 region of the VH of anti-CD22 sFv is mutated to enhance its affinity. The anti-CD19 and anti CD-22 portions of the immunotoxin specifically bind to CD19 and CD22 receptors on tumor B cells. Upon internalization, DT catalyzes ADP ribosylation of elongation factor 2 (EF-2) which may result in the irreversible inhibition of protein synthesis and cell death in CD19- and CD22-expressing tumor cells. CD19 and CD22 transmembrane proteins upregulated on malignant B cells.


anti-CD19/CD3 BiTE antibody AMG 562

A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the B-cell-specific membrane protein CD19, and another that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD19/CD3 BiTE antibody AMG 562 binds to both the CD3 antigen on cytotoxic T lymphocytes (CTLs) and the CD19 antigen expressed on malignant B cells. This activates and redirects CTLs to CD19-expressing tumor cells, resulting in CTL-mediated killing of tumor cells. CD19 is a membrane antigen that is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.


anti-CD19/CD3 tetravalent antibody AFM11

An anti-CD19/anti-CD3 bispecific tetravalent antibody with potential immunostimulatory and antineoplastic activities. Anti-CD19/CD3 tetravalent antibody AFM11 possesses two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for CD19, a tumor-associated antigen (TAA) overexpressed on the surface of B-cells. Upon bolus infusion of AFM11, this bispecific antibody binds to CD3-expressing T-cells and CD19-expressing cancer cells, thereby crosslinking CD19-expressing tumor B-cells and cytotoxic T-lymphocytes (CTLs). This may result in a potent CTL-mediated cell lysis of CD19-expressing B-lymphocytes. CD19, a B-cell specific membrane antigen, is expressed during both B-cell development and B-cell malignant growth.


anti-CD19-CAR FMC63-28Z retroviral vector-transduced allogeneic T lymphocytes

Allogeneic T-lymphocytes derived from peripheral blood mononuclear cells (PBMC) transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) consisting of both the light and heavy chain variable regions of anti-CD19 monoclonal antibody FMC63, coupled to the molecule CD28 and the signaling domain of the zeta chain of the T-cell receptor (TCR) (FMC63-28Z), with potential immunomodulating and antineoplastic activities. Upon transfusion, the anti-CD19-CAR FMC63-28Z retroviral vector-transduced allogeneic T lymphocytes specifically recognize and kill CD19-expressing tumor cells. CD19 antigen is a B-cell specific cell surface antigen, which is expressed in all B-cell lineage malignancies and normal B-cells.


anti-CD19-CAR retroviral vector-transduced autologous T cells

A preparation of autologous peripheral blood T-lymphocytes (PBTL) that have been genetically modified to express a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment); an extracellular portion of human CD28 and the entire transmembrane and cytoplasmic portion of human CD28; and the cytoplasmic portion of the human TCR-[zeta] molecule with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD19-CAR retroviral vector-transduced autologous T cells may stimulate host cytotoxic T lymphocyte (CTL) and antibody responses against CD19-expressing tumor cells, resulting in tumor cell lysis. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3 zeta is one of several membrane-bound polypeptides found in the T-cell receptor (TCR)/CD3 complex and regulates the assembly of complete TCR complexes and their expression on the cell surface. CD28 is essential for CD4+ T-cell proliferation, interleukin-2 production, and T-helper type-2 (Th2) development.


anti-CD19-CAR-CD3zeta-4-1BB-expressing natural killer cells

Allogeneic natural killer (NK) cells transduced with an mRNA expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) and the zeta chain of the TCR/CD3 complex (CD3-zeta), coupled to the signaling domain of 4-1BB (CD137), with potential immunomodulating and antineoplastic activities. NK cells from haploidentical donors are expanded in culture and electroporated with the CAR mRNA. Upon transfusion of the transduced cultured cells, CD19CAR-CD3zeta-4-1BB-expressing allogeneic NK cells bind to and induce selective cytotoxicity in CD19-expressing tumor cells. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19. Its inclusion may also increase antitumor activity, when compared to the inclusion of the CD3-zeta chain alone. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies.


anti-CD19-CD20-CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes

Autologous T lymphocytes that have been transduced with a lentiviral vector to express a chimeric antigen receptor (CAR) consisting of a single chain variable fragment (scFv) of anti-CD19 in tandem with an anti-CD20 scFv, and coupled to the cytoplasmic portion of the zeta chain of the human T-cell receptor (CD3zeta), and the co-stimulatory molecule 4-1BB (CD137), with potential immunostimulating and antineoplastic activities. Upon transfusion, anti-CD19-CD20-CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes recognize and direct T cells to CD19- or CD20-expressing tumor B cells. This results in a cytotoxic T-lymphocyte (CTL) response against CD19- or CD20-expressing tumor cells, and causes tumor cell lysis. Both CD19 and CD20 are B-cell-specific cell surface antigens overexpressed in B-cell lineage malignancies.


anti-CD19-CD28-zeta modified CAR CD3+ T lymphocytes JCAR015

Genetically modified CD3-positive-enriched autologous T lymphocytes transduced with a replication incompetent gamma retroviral vector expressing a chimeric T-cell antigen receptor (CAR) consisting of an anti-CD19 single chain variable fragment (scFv), fused to the extracellular, transmembrane and intracellular signaling domains of the T-cell co-stimulatory receptor CD28 and the cytoplasmic signaling domain of the zeta chain of the TCR/CD3 complex (CD3-zeta) (CAR19-28z), with potential antineoplastic activities. Upon intravenous administration, autologous CD19-28z CAR-expressing CD3+ T lymphocytes are directed to CD19-expressing tumor cells, and, upon binding to the T cells, induce selective toxicity in CD19-expressing tumor cells. CD19 antigen is a B-cell-specific cell surface antigen expressed in all B-cell lineage malignancies. The CD28 co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19. The inclusion of the CD28 signaling domain may increase proliferation of T cells and antitumor activity compared to the inclusion of the CD3-zeta chain alone.


anti-CD19-DM4 immunoconjugate SAR3419

An immunoconjugate consisting of an anti-CD19 monoclonal antibody conjugated to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-CD19-DM4 conjugate SAR3419 targets the cell surface antigen CD19, found on a number of B-cell-derived cancer s. Upon antibody/antigen binding and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CD19-expressing tumor cells.


anti-CD20 B9E9 scFv-streptavidin fusion protein

An Escherichia coli periplasm-expressed tetrameric fusion protein composed of four single-chain variable regions (scFv) of the murine immunoglobulin (Ig) G2a anti-CD20 monoclonal antibody B9E9 fused to the streptavidin (SA) gene of Streptomyces avidinii (scFv-SA), with potential use in pretargeted radioimmunotherapy (PRIT). Upon intravenous administration of the anti-CD20 B9E9 scFv-SA fusion protein, this agent targets and binds to CD20-expressing tumor cells. Subsequently, a biotinylated N-acetylgalactosamine-containing clearing agent is administered, which binds to the streptavidin moiety of the unbound fusion protein and promotes its hepatic excretion. In turn, radiolabeled DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid)-biotin is administered and, due to its small size, quickly distributes. The biotin moiety efficiently binds to the SA moiety of the bound fusion protein, which localizes the biotin-conjugated radionuclide to the tumor site. CD20, a tumor-associated antigen (TAA), is overexpressed on B-cell malignancies. PRIT increases both tumor uptake and renal elimination of the radionuclide conjugate as compared to conventional radioimmunotherapy (RIT), where the radioisotope is bound to the antibody before administration; this increases the dose of radionuclide delivered to the tumor while limiting radiation exposure for normal, healthy tissues.


anti-CD20 monoclonal antibody B001

A recombinant humanized monoclonal antibody directed against human CD20 with potential antineoplastic activity. Upon intravenous administration, anti-CD20 monoclonal antibody B001 specifically binds to CD20 on the surfaces of B cells. Although the exact mechanisms through which B001 exert its effects have not been elucidated, B001 may induce a B-cell-directed cell-mediated immune response against CD20-expressing B cells and/or prevent CD20-medaited signaling. This induces tumor cell apoptosis and inhibits proliferation. CD20 is a non-glycosylated cell surface phosphoprotein which is exclusively expressed on B cells during most stages of B-cell development and which is often overexpressed in B-cell malignancies.  


anti-CD20 monoclonal antibody SCT400

A chimeric monoclonal antibody directed against human CD20, with potential antineoplastic activity. Anti-CD20 monoclonal antibody SCT400 binds to the B cell-specific cell surface antigen CD20, which triggers an immune response against CD20-positive B-cells, leading to apoptosis. CD20, a non-glycosylated cell surface phosphoprotein, is exclusively expressed on B-cells during most stages of B-cell development and is often overexpressed in B-cell malignancies.


anti-CD20 monoclonal antibody TL011

A monoclonal antibody directed against human CD20 with potential antineoplastic activity. Anti-CD20 monoclonal antibody TL011 specifically binds to the B cell-specific cell surface antigen CD20 antigen (MS4A1; membrane-spanning 4-domains, subfamily A, member 1), thereby potentially triggering an immune response against CD20-positive B cells, leading to B cell apoptosis. CD20 is a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B cell development and is often overexpressed in B-cell malignancies.


anti-CD20 monoclonal antibody-interferon alpha fusion protein IGN002

A humanized monoclonal antibody directed against the human B-cell-specific cell surface antigen CD20 and fused to the recombinant cytokine, interferon-alpha (IFN-a), with potential antineoplastic and immunomodulating activities. Upon administration of anti-CD20 monoclonal antibody-interferon alpha fusion protein IGN002, the antibody moiety specifically targets and binds to CD20. In turn, the IFN-a moiety binds to the IFN receptor, and activates IFN-mediated signal transduction, which induces the transcription and translation of genes whose protein products mediate anti cancer effects. This results in the induction of both G2 cell cycle arrest and apoptosis in CD20-expressing tumor cells. In addition, IGN002 causes the induction of complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC) against CD20-expressing B-cells, which leads to B-cell apoptosis and the inhibition of tumor cell proliferation. CD20, a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B-cells during most stages of B-cell development, is often overexpressed in B-cell malignancies.


anti-CD20/CD3 bispecific monoclonal antibody RO7082859

A bispecific monoclonal antibody, with potential antineoplastic activity. Anti-CD20/CD3 monoclonal antibody RO7082859 contains two antigen-recognition sites: one for human CD3, a T-cell surface antigen, and one for human CD20, a tumor-associated antigen (TAA) that is exclusively expressed on B cells during most stages of B-cell development and is often overexpressed in B-cell malignancies. Upon administration, RO7082859 binds to both T cells and CD20-expressing B-lineage tumor cells. The resulting cross-linkage may trigger a potent cytotoxic T-lymphocyte (CTL) response against the CD20-expressing tumor B cells.  


anti-CD20/CD3 monoclonal antibody REGN1979

A bispecific, human monoclonal antibody with potential antineoplastic activity. Anti-CD20/CD3 monoclonal antibody REGN1979 contains two antigen-recognition sites: one for human CD3, a T cell surface antigen, and one for human CD20, a tumor-associated antigen that is exclusively expressed on B-cells during most stages of B-cell development and is often overexpressed in B-cell malignancies. Upon administration, REGN1979 binds to both T-cells and CD20-expressing tumor B-cells, which cross-links the T-cells to tumor cells, and may result in a potent cytotoxic T-lymphocyte (CTL) response against CD20-expressing tumor B-cells.


anti-CD20/CD3 monoclonal antibody XmAb13676

A bispecific, Fc domain-containing, monoclonal antibody with potential antineoplastic activity. Anti-CD20/CD3 monoclonal antibody XmAb13676 contains two antigen-recognition sites: one for human CD3, a T-cell surface antigen, and one for human CD20, a tumor-associated antigen (TAA) that is exclusively expressed on B cells during most stages of B-cell development and is often overexpressed in B-cell malignancies. Upon administration, XmAb13676 binds to both T cells and CD20-expressing B-lineage tumor cells. The resulting cross-linkage may trigger a potent cytotoxic T-lymphocyte (CTL) response against the CD20-expressing tumor B-cells. Inclusion of an Fc domain on the antibody prolongs the half-life of the bispecific antibody and enhances T-cell-mediated tumor cell killing because the agent is able to bind to Fc receptors.


anti-CD20-CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes

A preparation of autologous blood T-lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) consisting of an anti-CD20 scFv (single chain variable fragment); the cytoplasmic portion of the human TCR-[zeta] molecule; and the co-stimulatory molecule 4-1BB (CD137), with potential immunostimulating and antineoplastic activities. Upon transfusion, anti-CD20-CAR-CD3zeta-4-1BB-expressing autologous T-lymphocyte cells direct T-cells to CD20-expressing tumor cells. This results in cytotoxic T lymphocyte (CTL) and antibody responses against CD20-expressing tumor cells, causing tumor cell lysis. The CD20 antigen, a non-glycosylated cell surface phosphoprotein, is a B-cell specific cell surface antigen expressed in B-cell lineage malignancies. CD3 zeta is one of several membrane-bound polypeptides found in the T-cell receptor (TCR)/CD3 complex and regulates the assembly of complete TCR complexes and their expression on the cell surface. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD20; the inclusion of this signaling domain may increase the antitumor activity compared to the inclusion of the CD3-zeta chain alone.


anti-CD20-engineered toxin body MT-3724

An engineered toxin body (ETB) composed of the single-chain variable fragment (ScFv) from an antibody targeting CD20 that is linked to a modified form of the ribosome-inactivating alpha subunit of Shiga-like toxin 1 (Shiga-like Toxin-1 A or SLT-1A), with antineoplastic activity. Upon administration, the ScFv moiety of anti-CD20-engineered toxin body MT-3724 targets and binds to the CD20 antigen expressed on tumor cells. Upon internalization, the SLT-1A moiety is released and acts as an N-glycosidase, which binds to and cleaves an adenine nucleobase in the 28S RNA component of the 60S subunit of ribosomes and prevents ribosome activity. This inhibits protein synthesis and eventually leads to apoptosis of CD20-expressing tumor cells. CD20, a B-cell specific transmembrane protein and tumor-associated antigen (TAA), is expressed during most stages of B-cell development and is often overexpressed in B-cell malignancies.


anti-CD22 ADC TRPH-222

An antibody-drug conjugate (ADC) composed of an anti-CD22 humanized monoclonal antibody site-specifically conjugated, via formylglycine (FG) residues and a protease insensitive 4AP linker, to a cytotoxic microtubule-targeting maytansinoid payload, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of TRPH-222 binds to B-cell-specific CD22 receptors and is rapidly internalized, thereby delivering the payload intracellularly. Upon proteolytic cleavage, the maytansinoid payload binds to tubulin, disrupting microtubule assembly/disassembly dynamics, inhibiting both cell division and tumor cell proliferation. CD22, a cell surface sialoglycoprotein, is expressed on mature B-cells and on most malignant B-cells. The site specific and stable conjugation to the payload allows for a higher drug-to-antibody ratio (DAR) and an enhanced therapeutic index.


anti-CD22 CAR-expressing T lymphocytes

A preparation of human T lymphocytes transduced with a recombinant viral vector encoding a chimeric T-cell receptor (chimeric antigen receptor or CAR) consisting of one or more binding domains targeting the tumor-associated antigen (TAA) CD22 and fused to one or more co-stimulatory, TCR-signaling domains, with potential immunostimulating and antineoplastic activities. Upon administration, the anti-CD22 CAR-expressing T lymphocytes, express anti-CD22-CAR on their cell surfaces and bind to the CD22 antigen on tumor cell surfaces. Subsequently, CD22-expressing B cells are lysed. CD22, a B-lineage-restricted, transmembrane phosphoglycoprotein, is expressed on malignant B cells.


anti-CD22 monoclonal antibody-MMAE conjugate DCDT2980S

An antibody-drug conjugate (ADC) composed of MCDT2219A , a humanized IgG1 anti-CD22 monoclonal antibody covalently linked, via a protease-cleavable peptide linker, to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of DCDT2980S binds to B-cell-specific CD22 receptors and is rapidly internalized, thereby delivering MMAE intracellularly. Upon proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. CD22, a cell surface glycoprotein, is expressed on mature B-cells and on most malignant B-cells.


anti-CD22 scFv TCRz:41BB-CAR lentiviral vector-transduced autologous T lymphocytes

Autologous human T lymphocytes transduced with a recombinant lentiviral vector encoding a chimeric T cell receptor consisting of an anti-CD22 single chain variable fragment (scFv) and the co-stimulatory domain 4-1BB (CD137) coupled to the zeta chain of the TCR/CD3 complex (CD3-zeta), with potential immunostimulating and antineoplastic activities. Autologous peripheral blood lymphocytes (PBLs) from a patient with CD22-positive cancer are transduced with this lentiviral vector that encodes the CAR gene specific for CD22. After isolation, transduction, expansion in culture and reintroduction into the patient, the anti-CD22 scFv TCRz:41BB-CAR lentiviral vector-transduced autologous T lymphocytes express anti-CD22-CAR on their cell surfaces and bind to the CD22 antigen on tumor cell surfaces. Subsequently, CD22-expressing tumor cells are lysed. CD22, a B-lineage-restricted, transmembrane phosphoglycoprotein, is expressed on malignant B cells.


anti-CD22-CAR m971-BBz lentiviral vector-transduced autologous T lymphocytes

Autologous human T-lymphocytes transduced with a recombinant lentiviral vector encoding a chimeric T-cell receptor (chimeric antigen receptor or CAR) consisting of an anti-CD22 single chain variable fragment (scFv) derived from the monoclonal antibody (moAb) 971 (m971), and the co-stimulatory domain 4-1BB (CD137) coupled to the zeta chain of the TCR/CD3 complex (CD3-zeta), with potential immunostimulating and antineoplastic activities. Autologous peripheral blood lymphocytes (PBLs) from a patient with CD22-positive cancer are transduced with this lentiviral vector that encodes the CAR gene specific for CD22. After expansion in culture and reintroduction into the patient, the anti-CD22-CAR m971-BBz lentiviral vector-transduced autologous T-lymphocytes express anti-CD22-CAR on their cell surfaces and bind to the CD22 antigen on tumor cell surfaces. Subsequently, CD22-expressing tumor cells are lysed. CD22, a B-lineage-restricted, transmembrane phosphoglycoprotein, is expressed on malignant B-cells. m971 binds to a membrane proximal epitope on CD22 and has a higher binding affinity compared to any other anti-CD22 moAb.


anti-CD25-PBD antibody-drug conjugate ADCT-301

An immunoconjugate consisting of a human immunoglobulin (Ig) G1 monoclonal antibody directed against the alpha subunit of the interleukin-2 receptor (IL-2R alpha or CD25) and conjugated, via a cleavable linker, to a synthetic, cross-linking agent pyrrolobenzodiazepine (PBD) dimer that targets DNA minor grooves, with potential antineoplastic activity. The monoclonal antibody portion of the anti-CD25 antibody-drug conjugate (ADC) ADCT-301 specifically binds to the cell surface antigen CD25. This causes the internalization of ADCT-301 and the subsequent release of the cytotoxic PBD moiety. The imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA and inhibits DNA replication, which inhibits the proliferation of CD25-overexpressing tumor cells. CD25, a transmembrane receptor and tumor-associated antigen (TAA), is expressed on certain cancer cells.


anti-CD26 monoclonal antibody YS110

A humanized, immunoglobulin G1 (IgG1) monoclonal antibody directed against the extracellular domain of dipeptidyl peptidase 4 (CD26; DPP4; DPP IV), with potential antineoplastic activity. Upon administration of anti-CD26 monoclonal antibody YS110, this antibody targets and binds to CD26 expressed on tumor cells. This inhibits CD26 activity and causes internalization of CD26-YS110. This leads to cell cycle arrest, lysis and inhibition of growth in CD26-positive tumor cells. YS110 also induces antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) against CD26-expressing tumor cells. CD26, a 110-kDa, type II transmembrane glycoprotein, is overexpressed in a variety of cancer cell types while absent in normal, healthy cells and plays a key role in tumor cell growth, migration, invasion and survival. It also plays a major role in the regulation of T-cell activity.


anti-CD27L antibody-drug conjugate AMG 172

An immunoconjugate consisting of a human IgG1 monoclonal antibody directed against CD27L conjugated, via a non-cleavable linker, to the cytotoxic agent maytansinoid DM1, with potential antineoplastic activity. The monoclonal antibody moiety of this immunoconjugate binds to CD27L on tumor cell surfaces. After internalization, the DM1 moiety binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting both cell division and proliferation of cancer cells that express CD27L. CD27L, a type II transmembrane protein and member of the tumor necrosis factor family, is a co-stimulatory molecule constitutively expressed on a subset of activated T-cells, B-cells, and dendritic cells, which is overexpressed in certain tumor cell types.


anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1)

A bivalent recombinant fusion protein immunotoxin derived from the anti-CD3 monoclonal antibody UCHT1 with potential antineoplastic activity. Anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1) consists of 1-390 amino acid residues of chain A diphtheria toxin (DT) joined via a spacer to the Fv fragment of UCHT1, which is connected to a second UCHT1 Fv fragment via a disulfide bond (hence the "bisFv" designation); the addition of the second Fv fragment overcomes the steric hindrance of immunotoxin binding due to the large N-terminal DT domain. Once inside target T cells, the DT moiety catalyzes the transfer of the ADP-ribose moiety of NAD to diphthamide, a posttranslationally modified histidine residue found in elongation factor 2 (EF-2); inactivation of EF-2, disruption of polypeptide chain elongation, and cell death ensue. CD3 is a complex of five cell-surface polypeptides associated with the T cell receptor (TCR) complex.


anti-CD3 x anti-CD20 bispecific antibody-armed activated T cells

Autologous activated T cells that have been coated with bispecific antibodies (BiAb), with potential antineoplastic and immunomodulating activities. In vitro, T cells are activated through exposure to the anti-CD3 murine monoclonal antibody OKT3 and low-dose interleukin 2 (Il-2) for 6-14 days and then armed with anti-CD3 x anti-CD20 bispecific antibody (CD20Bi). Upon administration, anti-CD3 x anti-CD20 bispecific antibody-armed activated T cells (AATC) attach to CD3-expressing T cells and CD20-expressing tumor cells, selectively cross-linking T cells and tumor cells. This may result in the recruitment and activation of cytotoxic T lymphocyte (CTLs), CTL-mediated specific tumor cell lysis, and the secretion of antitumor cytokines and chemokines. CD20, a cell surface phosphoprotein, is found on normal B cells and most B-cell tumors.


anti-CD3/anti-BCMA bispecific monoclonal antibody JNJ-64007957

A bispecific humanized monoclonal antibody against human CD3, a T-cell surface antigen, and human B-cell maturation antigen (BCMA; TNFRSF17), a tumor-associated antigen (TAA) expressed on plasma cells, with potential antineoplastic activity. Upon administration, anti-CD3/anti-BCMA bispecific monoclonal antibody JNJ-64007957 binds to both CD3 on T cells and BCMA expressed on malignant plasma cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against BCMA-expressing plasma cells. BCMA, a member of the tumor necrosis factor receptor superfamily member that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival.


anti-CD3/anti-BCMA bispecific monoclonal antibody PF-06863135

A bispecific monoclonal antibody against human CD3, a T-cell surface antigen, and human B-cell maturation antigen (BCMA; TNFRSF17), a tumor-associated antigen (TAA) expressed on plasma cells, with potential antineoplastic activity. Upon administration, anti-CD3/anti-BCMA bispecific monoclonal antibody PF-06863135 binds to both CD3 on T cells and BCMA expressed on malignant plasma cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against BCMA-expressing plasma cells. BCMA, a member of the tumor necrosis factor receptor superfamily that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival.


anti-CD3/anti-CD20 trifunctional bispecific monoclonal antibody FBTA05

A trifunctional bispecific monoclonal antibody with potential antineoplastic activity. FBTA05 contains two antigen-recognition sites: one for human CD3, a T cell surface antigen; and one for human CD20, a tumor-associated antigen that is exclusively expressed on B cells during most stages of B-cell development and often overexpressed in B-cell malignancies. In addition, the modified Fc portion of this antibody binds Fc receptors on antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs). FBTA05 brings T cells, CD20-expressing tumor B-cells and APCs together into tricellular complexes, which may result in a potent cytotoxic T-lymphocyte (CTL) response against CD20-expressing tumor B-cells. Fc-mediated binding of APCs in the tricellular complex potentiates CD20 antigen presentation to T cells and the activation of anti-tumor cytotoxic T cells.


anti-CD3/anti-GPRC5D bispecific monoclonal antibody JNJ-64407564

A bispecific humanized monoclonal antibody against human CD3, a T-cell surface antigen, and human G-protein coupled receptor family C group 5 member D (GPRC5D), a tumor-associated antigen (TAA), with potential antineoplastic activity. Upon administration, anti-CD3/anti-GPRC5D bispecific monoclonal antibody JNJ-64407564 binds to both CD3 on T cells and GPRC5D expressed on certain tumor cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against GPRC5D-expressing tumor cells. GPRC5D is overexpressed on certain tumors, such as multiple myeloma, while minimally expressed on normal, healthy cells, and plays a key role in tumor cell proliferation.


anti-CD3/CD38 bispecific monoclonal antibody AMG 424

A humanized, bispecific monoclonal antibody (BsAb) targeting CD3, a T-cell surface antigen, and CD38, a human cell surface glycoprotein and tumor-associated antigen (TAA), with potential antineoplastic activity. Upon intravenous administration, anti-CD3/CD38 bispecific monoclonal antibody AMG 424 binds to both CD3 on T cells and CD38 expressed on tumor cells. The resulting cross-linkage may trigger a potent cytotoxic T-lymphocyte (CTL) response against CD38-expressing tumor cells. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies; its expression has been correlated with poor prognosis.


anti-CD3/humanized 3F8 bispecific antibody-activated T lymphocytes

Autologous activated T cells that have been coated with bispecific antibodies (BiAb) comprised of anti-CD3 murine monoclonal antibody OKT3 heteroconjugated to anti-GD2 humanized monoclonal antibody 3F8 (hu3F8), with potential antineoplastic and immunomodulating activities. In vitro, T cells are exposed to OKT3, which binds to the T cell receptor-CD3 complex on the T cell surface, crosslinks the CD3 receptors and leads to T cell activation. In turn, the hu3F8 monoclonal antibody is heteroconjugated to OKT3. Upon administration, anti-CD3 x anti-GD2 bispecific antibody-armed activated T cells attach to GD2-expressing tumor cells, thereby selectively cross-linking T cells and tumor cells. This results in selective cytotoxicity towards the GD2-expressing tumor cells. In addition, cytokine and chemokine secretion by the T cells further activates the immune system, which leads to the recruitment and activation of cytotoxic T lymphocytes (CTLs), and additional CTL-mediated tumor-specific cell lysis. GD2, a disialoganglioside and tumor-associated antigen, is overexpressed in a variety of tumor cell types. CD3 is part of the functional T cell receptor (TCR) complex, which is necessary for antigen recognition by T cells, and is required for signal transduction.


anti-CD3/MUC1 antibody-armed PD-1 inhibitor-induced cytokine-induced killer cells

A preparation of cytokine-induced killer cells (CIKs), which have been exposed, ex vivo, to a specific set of cytokines and a programmed cell death protein 1 (PD-1) inhibitor, mixed with a bispecific anti-cluster of differentiation 3 (CD3)/anti-mucin-1 (MUC1) antibody, with potential anti-tumor cytotoxic activity. Upon administration of the anti-CD3/MUC1 antibody-armed PD-1 inhibitor-induced CIKs, the antibody moiety binds to both CD3 on the CIKs and MUC1 on cancer cells. This crosslinks the CIKs and tumor cells, which allows the CIKs to target and lyse MUC1-expressing cancer cells. PD-1 blockade activates the CIKs. The cytokines used, usually interferon-gamma (IFNg), interleukin 1 (IL-1), and IL-2, stimulate the proliferation and maturation of peripheral blood mononuclear cells (PBMCs) into CIK cells. Anti-CD3 stimulation allows for the CIKs' improved lytic activity.


anti-CD30 monoclonal antibody MDX-1401

A fully human, second-generation, nonfucosylated monoclonal antibody directed against the cell surface receptor CD30 with potential immunomodulating and antineoplastic activities. Anti-CD30 monoclonal antibody MDX-1401 specifically binds to the CD30 antigen, which may result in a cytotoxic T lymphocyte (CTL) response against CD30-expressing tumor cells. CD30, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on activated lymphocytes transiently and is constitutively expressed in hematologic malignancies including Hodgkin's disease and some T-cell non-Hodgkin's lymphomas. Compared to conventional antibodies, deletion of fucose molecules on the antibody backbone, as is done in MDX-1401, may result in an increased affinity for Fc receptors and an enhanced antibody-dependent cellular cytotoxicity (ADCC).


anti-CD30 monoclonal antibody XmAb2513

A humanized monoclonal antibody directed against the cell surface receptor CD30 with potential immunotherapeutic activity. Anti-CD30 monoclonal antibody XmAb2513 specifically binds to the CD30 antigen, which may result in a cytotoxic T lymphocyte (CTL) response against CD30-expressing tumor cells. CD30, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on activated lymphocytes transiently and is constitutively expressed in hematologic malignancies including Hodgkin's disease and some T-cell non-Hodgkin's lymphomas.


anti-CD30/CD16A monoclonal antibody AFM13

A tetravalent bispecific antibody directed against human CD30 and the human low affinity IgG Fc region receptor (FCGR3A; CD16A), with potential immunomodulating and antineoplastic activities. Anti-CD30/CD16A monoclonal antibody AFM13 binds to the CD16A expressed on natural killer (NK) cells with two of its binding sites and to CD30 on CD30-expressing tumor cells with the other two binding sites, thereby selectively cross-linking tumor and NK cells. This may result in NK cell activation, antibody-dependent cellular cytotoxicity (ADCC) and eventually tumor cell lysis. CD30, a cell surface receptor and a member of the tumor necrosis factor (TNF) receptor superfamily, is overexpressed in hematologic malignancies; CD16A is specifically expressed on the surface of NK cells.


anti-CD32B monoclonal antibody BI-1206

A fully human monoclonal antibody targeting the Fc gamma receptor IIB (FcgRIIB; CD32B) with potential immunomodulatory and antineoplastic activities. Upon intravenous administration, anti-CD32B monoclonal antibody BI-1206 selectively binds to CD32B, a receptor expressed on the surface of B-cells. This prevents CD32B-mediated internalization of anti-CD20 monoclonal antibodies, such as rituximab, which abrogates tumor cell resistance caused by CD32B-mediated monoclonal antibody internalization and degradation of CD32B-expressing B-cells. By blocking CD32B, BI-1206 may recover and enhance the activity of rituximab and other anti CD20 monoclonal antibodies. In addition, BI-1206 itself activates the immune system to exert an immune-mediated tumor cell death of B-cells. CD32B, an inhibitory member of the FcgammaR family, is implicated in immune cell desensitization and tumor cell resistance.


anti-CD33 antigen/CD3 receptor bispecific monoclonal antibody AMV564

An anti-CD33/anti-CD3 bispecific tetravalent antibody, with potential immunostimulatory and antineoplastic activities. Anti-CD33/CD3 tetravalent bispecific monoclonal antibody AMV564 possesses two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for CD33, a tumor-associated antigen (TAA) overexpressed on the surface of a variety of tumor cell types. Upon infusion of AMV564, this bispecific antibody binds to CD3-expressing T cells and CD33-expressing tumor cells, thereby crosslinking CD33-expressing tumor cells and cytotoxic T-lymphocytes (CTLs). This may result in a potent CTL-mediated cell lysis of CD33-expressing cells. CD33, a glycoprotein expressed by a variety of cancer s, including the majority of acute myeloid leukemias (AMLs), and normal non-pluripotent hematopoietic stem cells, plays a key role in tumor initiation, proliferation and progression.


anti-CD33 monoclonal antibody BI 836858

An engineered, fully human, immunoglobulin (Ig) G1 anti-CD33 monoclonal antibody, with potential antineoplastic activity. Upon administration, anti-CD33 monoclonal antibody BI 836858 induces an antibody-dependent cellular cytotoxicity (ADCC) against CD33-expressing tumor cells, leading to cell death. CD33, a cell surface antigen expressed on normal non-pluripotent hematopoietic stem cells, is overexpressed on myeloid leukemia cells.


anti-CD33 monoclonal antibody-DM4 conjugate AVE9633

An immunoconjugate consisting of the humanized monoclonal antibody huMy9-6 conjugated to the cytotoxic maytansinoid DM4 with potential antineoplastic activity. The monoclonal antibody portion of anti-CD33 monoclonal antibody-DM4 conjugate AVE9633 specifically binds to the cell surface antigen CD33 expressed on myeloid leukemia cells; upon internalization, the DM4 moiety is released, binds tubulin, and disrupts microtubule assembly/disassembly dynamics, resulting in the inhibition of cell division and cell growth in myeloid leukemia cells that express CD33. CD33 is expressed on normal non-pluripotent hematopoietic stem cells as well as on myeloid leukemia cells.


anti-CD33/CD3 bispecific antibody GEM 333

A bispecific antibody possessing two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for the tumor-associated antigen (TAA) CD33, with potential immunostimulating and antineoplastic activities. Upon administration of anti-CD33/CD3 bispecific antibody GEM 333, this bispecific antibody binds to both the CD3 antigen on cytotoxic T lymphocytes (CTLs) and the CD33 antigen found on CD33-expressing tumor cells, thereby crosslinking tumor cells and CTLs. This activates and redirects CTLs to CD33-expressing tumor cells, which results in the CTL-mediated cell death of CD33-expressing tumor cells. CD33, a myeloid differentiation antigen, is expressed on normal non-pluripotent hematopoietic stem and progenitor cells (HSPCs) and is overexpressed on a variety of cancer cell types, including acute myeloid leukemia (AML). It plays a key role in tumor initiation, proliferation and progression.


anti-CD33/CD3 BiTE antibody AMG 330

A proprietary recombinant bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) CD33 fused to one that is directed against the CD3 antigen found on T-lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-CD33/CD3 BiTE antibody AMG 330, this bispecific antibody binds to both the CD3 antigen on cytotoxic T-lymphocytes (CTLs) and the CD33 antigen found on CD33-expressing tumor cells. This activates and redirects CTLs to CD33-expressing tumor cells, which results in the CTL-mediated cell death of CD33-expressing tumor cells. CD33, a myeloid differentiation antigen, is expressed on normal non-pluripotent hematopoietic stem cells and overexpressed on neoplastic cells in patients with acute myeloid leukemia.


anti-CD33/CD3 BiTE antibody AMG 673

A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) CD33 fused to one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-CD33/CD3 BiTE antibody AMG 673, this bispecific antibody binds to both the CD3 antigen on cytotoxic T lymphocytes (CTLs) and the CD33 antigen found on CD33-expressing tumor cells. This activates and redirects CTLs to CD33-expressing tumor cells, which results in the CTL-mediated cell death of CD33-expressing tumor cells. CD33, a myeloid differentiation antigen, is expressed on normal non-pluripotent hematopoietic stem cells and overexpressed on a variety of cancer cell types, including acute myeloid leukemia (AML). It plays a key role in tumor initiation, proliferation and progression.


anti-CD352 antibody-drug conjugate SGN-CD352A

An antibody-drug conjugate (ADC) consisting of an engineered cysteine humanized monoclonal antibody (EC-mAb) targeting CD352 (SLAM family member 6; SLAM6) that is conjugated to the cytotoxic, DNA minor-groove crosslinking agent pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration of anti-CD352 ADC SGN-CD352A, the antibody moiety targets the cell surface antigen CD352. Upon antibody/antigen binding, internalization, and lysosome uptake, the cytotoxic PBD moiety is released. In turn, the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of CD352-overexpressing tumor cells. CD352, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer s. Cysteine engineering of the monoclonal antibody allows for a site-specific, stable conjugation and uniform loading of the PBD agent to the antibody.


anti-CD37 antibody-drug conjugate IMGN529

An immunoconjugate that consists of a humanized IgG1 antibody K7153A against the cell-surface antigen CD37 that is covalently linked via the uncleavable, maleimide-derived thioether-based linker SMCC to the maytansinoid DM1, with potential pro-apoptotic and cytotoxic activities. The antibody moiety of IMGN529 binds to CD37 on tumor B cells and induces an antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), thereby showing pro-apoptotic activity. In addition, after the internalization of this agent and lysosomal degradation, the DM1 moiety binds to tubulin and inhibits tubulin polymerization and microtubule assembly, resulting in a disruption of microtubule activity and cell division, and eventually causing cell death in CD37-positive B cells. CD37, a transmembrane glycoprotein, is overexpressed in B-cell malignancies. Compared to reducible, cleavable linkers, the non-reducible SMCC linker shows increased stability in plasma.


anti-CD37 monoclonal antibody BI 836826

An Fc-engineered, chimeric immunoglobulin (Ig) G1 monoclonal antibody against the tumor-associated antigen (TAA) CD37, with potential antineoplastic activity. Upon administration, the anti-CD37 monoclonal antibody BI 836826 both activates the immune system to induce an antibody-dependent cell-mediated cytotoxicity (ADCC) against CD37-overexpressing tumor cells and induces apoptosis in these tumor cells. BI 836826 is Fc-engineered to improve ADCC activity and enhance affinity for the receptor Fc-gamma-RIIIa, which is expressed on human natural killer (NK) cells. CD37, a member of the tetraspanin superfamily of cell surface antigens, is overexpressed on a variety of cancer cell types and plays a key role in tumor cell proliferation.


anti-CD38 monoclonal antibody MOR03087

A fully human monoclonal antibody directed against the cell surface glycoprotein CD-38 with potential antineoplastic activity. Anti-CD38 monoclonal antibody MOR03087 specifically binds to CD38 on CD38-positive tumor cells. This may trigger antitumoral antibody-dependent cellular cytotoxicity (ADCC) and may eventually lead to cell lysis in CD38-expressing tumor cells. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies, and its expression has been correlated with poor prognosis.


anti-CD38 monoclonal antibody TAK-079

A human, non-agonistic immunoglobulin G1 (IgG1) monoclonal antibody directed against the cell surface glycoprotein ADP-ribosyl cyclase 1 (CD38) with potential immunomodulating and antineoplastic activities. Anti-CD38 monoclonal antibody TAK-079 specifically binds to CD38 that is expressed on human plasmablasts, plasma cells, NK cells and activated T and B cells. This may trigger antibody-dependent cellular cytotoxicity (ADCC), cell lysis and depletion of CD38-expressing cells. Additionally, TAK-079 does not induce CD38-dependent signaling and does not promote cytokine activation in peripheral blood mononuclear cells (PMBCs). CD38, a type II transmembrane glycoprotein, is overexpressed on cells associated with autoimmune diseases and hematologic malignancies.


anti-CD38/CD3 bispecific monoclonal antibody GBR 1342

A humanized, bispecific monoclonal antibody (BsAb) against human CD3, a T-cell surface antigen, and the human cell surface glycoprotein CD38, a tumor-associated antigen (TAA), with potential antineoplastic activity. Upon administration, anti-CD38/anti-CD3 bispecific monoclonal antibody GBR 1342 binds to both CD3 on T cells and CD38 expressed on certain tumor cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against CD38-expressing tumor cells. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies; its expression has been correlated with poor prognosis. GBR 1342 uses the proprietary bispecific engagement by antibodies based on the T-cell receptor (BEAT) platform.


anti-CD38-targeted IgG4-attenuated IFNa TAK-573

A proprietary preparation composed of an immunoglobulin G4 (IgG4) directed against the cell surface glycoprotein CD-38 (CD38) that is fused to an attenuated form of human interferon alpha (IFN alpha; IFNa), with potential immunomodulating and antineoplastic activities. Upon administration, the IgG4 moiety of the anti-CD38-targeted IgG4-attenuated IFNa TAK-573 specifically targets and binds to CD38 on CD38-positive tumor cells. In turn, the IFNa moiety binds to cell-surface IFN receptors, and activates IFN-mediated signal transduction pathways, which results in the transcription and translation of genes whose products may cause antiproliferative effects in CD38-positive tumor cells. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies, and its expression has been correlated with poor prognosis.


anti-CD40 agonist monoclonal antibody ABBV-927

An agonistic monoclonal antibody directed against the B-cell surface antigen CD40, with potential antineoplastic activity. Upon administration, ABBV-927 binds to CD40 on a variety of immune cell types. This induces CD40-dependent signaling pathways, triggers the proliferation and activation of antigen-presenting cells (APCs), and activates T cells. This results in an enhanced cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. CD40, a cell surface receptor and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on various immune cells and plays a key role in the activation of the immune system.


anti-CD40 agonist monoclonal antibody CDX-1140

A fully human immunoglobulin G2 (IgG2) agonistic monoclonal antibody targeting the B-cell surface antigen CD40, with potential immunostimulatory and antineoplastic activities. Upon administration, CDX-1140 targets and binds to CD40 on a variety of immune cell types. This induces CD40-dependent signaling pathways, triggers the proliferation and activation of antigen-presenting cells (APCs) and activates T cells. This results in an enhanced cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. CD40, a cell surface receptor and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on various immune cells, such as dendritic cells (DCs), macrophages and B cells, and plays a key role in the activation of the immune system.


anti-CD40 monoclonal antibody Chi Lob 7/4

An IgG1 chimeric monoclonal antibody agonist of the cell surface receptor CD40 with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, anti-CD40 monoclonal antibody Chi Lob 7/4 binds to CD40 on a variety of immune cell types, triggering the cellular proliferation and activation of antigen-presenting cells (APCs), activating B cells and T cells, and enhancing the immune response; in addition, this agent binds to the CD40 antigen present on the surfaces of some solid tumor cells, resulting in complement-dependent cytotoxicity (CDC) and antibody-dependent cytotoxicity (ADCC) eventually resulting in decreased tumor growth. CD40, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on various immune cells, many B-cell malignancies, and many solid tumors, mediating both indirect tumor cell death through the activation of the immune system and direct tumor cell apoptosis.


anti-CD40 monoclonal antibody SEA-CD40

A proprietary, non-fucosylated monoclonal antibody directed against the cell surface receptor CD40 with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, anti-CD40 monoclonal antibody SEA-CD40 binds to CD40 on a variety of immune cell types, triggering both cellular proliferation and activation of antigen-presenting cells (APCs), which activates B-cells and T-cells, and enhances the immune response against tumor cells. In addition, this agent binds to the CD40 antigen present on the surfaces of tumor cells, which induces antibody-dependent cytotoxicity (ADCC), and eventually inhibits the proliferation of CD40-expressing tumor cells. CD40, a stimulatory receptor and a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on various immune cells, such as macrophages, dendritic cells and various tumor cell types; it plays a key role in the activation of the immune system. The non-fucosylated antibody shows increased efficacy as compared to its fucosylated counterpart.  


anti-CD40L Fc-fusion protein BMS-986004

A dimeric fusion protein composed of the C-terminus of the domain antibody (dAb) BMS2h-572-633 targeting the CD40 ligand (CD40L or CD154) linked to a modified Fc fragment of immunoglobulin G1 (IgG1), with potential immunomodulatory activity. Upon intravenous administration, the peptide moiety of anti-CD40L antibody BMS-986004 specifically targets and binds to CD40L expressed on T lymphocytes. This prevents the binding of CD40L to its cognate receptor CD40 expressed on B lymphocytes, macrophages, and dendritic cells (DCs). This prevents T-cell mediated proliferation and differentiation of B cells, and prevents the production of antibodies. By inhibiting both the production of anti-glycoprotein (GP) IIb/IIIa antibodies by B cells and GPIIb/IIIa-dependent T-cell proliferation, BMS-986004 may prevent platelet destruction and may increase platelet counts in idiopathic thrombocytopenic purpura (ITP). The direct binding of BMS-986004 to CD40L on platelets further prevents CD40L/CD40-mediated destruction by macrophages and DCs in ITP. The modified Fc domain prevents the binding of BMS-986004 to the Fc receptor FcgammaRIIA on platelets, thereby preventing FcgammaRIIA-dependent platelet activation and anti-CD40L-induced thromboembolism. CD40L, a transmembrane protein of the tumor necrosis factor (TNF) superfamily, is primarily expressed on activated T cells, but is also expressed on eosinophils, basophils, natural killer (NK) cells, mast cells, platelets and activated endothelial cells.


anti-CD44 monoclonal antibody RO5429083

A recombinant, humanized monoclonal antibody targeting the cancer stem cell (CSC) antigen CD44, with potential immunomodulating and antineoplastic activities. Upon administration, RO5429083 binds to the constant region of the extracellular domain of CD44, thereby preventing the activation of various CD44-mediated signal transduction pathways. This may lead to a reduction in the proliferation of CD44-expressing tumor stem cells. CD44, a transmembrane glycoprotein and hyaluronic acid receptor, is expressed in healthy tissue and overexpressed in numerous cancer cell types; it plays a key role in tumor cell proliferation, migration and survival.


anti-CD45 monoclonal antibody

A monoclonal antibody directed against the receptor-like leukocyte cell surface glycoprotein CD45 with leukocyte-depleting activity. Upon administration, anti-CD45 monoclonal antibody binds to leukocyte surface-expressed CD45, which may result in the transient depletion of circulating leukocytes including circulating T cell depletion (TCD). CD45, a receptor-like protein-tyrosine phosphatase that consists of several isoforms, is present on all differentiated hematopoietic cells except erythrocytes and plasma cells and is essential for T cell development and lymphocyte activation.


anti-CD45 monoclonal antibody AHN-12

A high affinity IgG1 monoclonal antibody with potential immunotherapeutic activity. Anti-CD45 monoclonal antibody AHN-12 recognizes CD45, a transmembrane protein tyrosine phosphatase that is expressed on the surface of normal and malignant hematopoietic cells.


anti-CD45 monoclonal antibody BC8

A murine IgG1 anti-CD45 monoclonal antibody (MoAb) with immunotherapeutic activity. CD45 antigen, a receptor protein-tyrosine phosphatase essential for T cell development and lymphocyte activation, is expressed on virtually all leukocytes. MoAb BC8 has specificity for hematopoietic tissues and may be used in targeted immunotherapy.


anti-CD45 monoclonal antibody BC8-streptavidin conjugate

An immunoconjugate containing a monoclonal antibody directed against the CD45 antigen BC8, conjugated to streptavidin, a nonglycosylated homotetrameric protein that has four high affinity binding sites for biotin. Anti-CD45 BC8 antibody-streptavidin conjugate binds to CD45, a transmembrane protein tyrosine phosphatase that is expressed on the surface of normal and malignant hematopoietic cells. Upon administration of a biotin-based radioconjugate, the biotin moiety of the radioconjugate binds to the streptavidin moiety of anti-CD45 BC8 antibody-streptavidin conjugate and, upon cellular internalization, specifically delivers cytotoxic radiation to CD45-expressing tumor cells.


anti-CD46 antibody-drug conjugate FOR46

An antibody-drug conjugate (ADC) composed of a human monoclonal antibody directed against the cluster of differentiation 46 (CD46; membrane cofactor protein; MCP) and conjugated to an as of yet undisclosed cytotoxic payload, with potential antineoplastic activity. Upon administration, anti-CD46 ADC FOR46 specifically targets and binds to a specific conformational epitope on the immune modulatory receptor CD46 expressed on certain tumor cells. Upon binding and internalization, the cytotoxic payload kills the CD46-expressing tumor cells. The conformational epitope of CD46 is highly expressed in multiple tumor cell types while minimally expressed or absent in normal, healthy tissues. FOR46 does not interfere with other CD46-mediated pathways that naturally occur in normal, healthy tissues.


anti-CD47 monoclonal antibody CC-90002

A monoclonal antibody targeting the human cell surface antigen CD47, with potential phagocytosis-inducing and antineoplastic activities. Upon administration, anti-CD47 monoclonal antibody CC-90002 selectively binds to CD47 expressed on tumor cells and blocks the interaction of CD47 with signal regulatory protein alpha (SIRPa), a protein expressed on phagocytic cells. This prevents CD47/SIRPa-mediated signaling and abrogates the CD47/SIRPa-mediated inhibition of phagocytosis. This induces pro-phagocytic signaling mediated by the binding of calreticulin (CRT), which is specifically expressed on the surface of tumor cells, to low-density lipoprotein (LDL) receptor-related protein (LRP), expressed on macrophages. This results in macrophage activation and the specific phagocytosis of tumor cells. In addition, blocking CD47 signaling activates both an anti-tumor T-lymphocyte immune response and T cell-mediated killing of CD47-expressing tumor cells. CD47, also called integrin-associated protein (IAP), is a tumor-associated antigen (TAA) expressed on normal, healthy hematopoietic stem cells (HSC) and overexpressed on the surface of a variety of cancer cells. Expression of CD47, and its interaction with SIRPa, leads to the inhibition of macrophage activation and protects cancer cells from phagocytosis, which allows cancer cells to proliferate.


anti-CD47 monoclonal antibody Hu5F9-G4

A humanized monoclonal antibody targeting the human cell surface antigen CD47, with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD47 monoclonal antibody Hu5F9-G4 selectively binds to CD47 expressed on tumor cells and blocks the interaction of CD47 with its ligand signal regulatory protein alpha (SIRPa), a protein expressed on phagocytic cells. This prevents CD47/SIRPa-mediated signaling, allows the activation of macrophages, through the induction of pro-phagocytic signaling mediated by calreticulin, which is specifically expressed on the surface of tumor cells, and results in specific tumor cell phagocytosis. In addition, blocking CD47 signaling activates an anti-tumor T-lymphocyte immune response and T-cell mediated cell killing. CD47, a tumor associated antigen expressed on normal, healthy hematopoietic stem cells (HSC), is overexpressed on the surface of a variety of cancer cells. Expression of CD47, and its interaction with SIRP-alpha, leads to inhibition of macrophages and protects cancer cells from phagocytosis thereby allowing cancer cells to proliferate.


anti-CD47 monoclonal antibody IBI188

A human immunoglobulin G4 (IgG4) monoclonal antibody targeting leukocyte surface antigen CD47 with potential immunostimulating and antineoplastic activities. Upon intravenous administration, anti-CD47 monoclonal antibody IBI188 selectively binds to CD47 expressed on tumor cells and blocks the interaction of CD47 with signal regulatory protein alpha (SIRPa), a protein expressed on phagocytic cells. This prevents CD47/SIRPa-mediated signaling and abrogates the CD47/SIRPa-mediated inhibition of phagocytosis. This induces pro-phagocytic signaling mediated by the binding of calreticulin (CRT), which is specifically expressed on the surface of tumor cells, to low-density lipoprotein (LDL) receptor-related protein (LRP), expressed on macrophages. This results in macrophage activation and the specific phagocytosis of tumor cells. In addition, blocking CD47 signaling activates both an anti-tumor T-lymphocyte immune response and T cell-mediated killing of CD47-expressing tumor cells. CD47, also called integrin-associated protein (IAP), is a tumor-associated antigen (TAA) expressed on normal, healthy hematopoietic stem cells (HSCs) and overexpressed on the surface of a variety of cancer cells. Expression of CD47, and its interaction with SIRPa, leads to the inhibition of macrophage activation and protects cancer cells from phagocytosis, which allows cancer cells to proliferate.


anti-CD47 monoclonal antibody SRF231

A human monoclonal antibody targeting the human cell surface antigen CD47, with potential phagocytosis-inducing and antineoplastic activities. Upon administration, anti-CD47 monoclonal antibody SRF231 selectively binds to CD47 on tumor cells and blocks the interaction of CD47 with signal regulatory protein alpha (SIRPalpha), an inhibitory protein expressed on macrophages. This prevents CD47/SIRPalpha-mediated signaling and abrogates the CD47/SIRPa-mediated inhibition of phagocytosis. This induces pro-phagocytic signaling mediated by the binding of calreticulin (CRT), which is specifically expressed on the surface of tumor cells, to low-density lipoprotein (LDL) receptor-related protein (LRP), expressed on macrophages. This results in macrophage activation and the specific phagocytosis of tumor cells. In addition, blocking CD47 signaling activates both an anti-tumor T-lymphocyte immune response and T-cell-mediated killing of CD47-expressing tumor cells. CD47, also called integrin-associated protein (IAP), is a tumor-associated antigen (TAA) expressed on normal, healthy hematopoietic stem cells (HSCs) and overexpressed on the surface of a variety of cancer cells. Expression of CD47, and its interaction with SIRPalpha, leads to the inhibition of macrophage activation and protects cancer cells from phagocytosis, which allows cancer cells to proliferate.


anti-CD48/MMAE antibody-drug conjugate SGN-CD48A

An antibody-drug conjugate (ADC) composed of an antibody targeting the cell surface antigen CD48 that is conjugated to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), via a proprietary next-generation PEGylated glucuronide linker, with potential antineoplastic activity. Following intravenous administration, the antibody moiety of anti-CD48 ADC SGN-CD48A binds to CD48 on the surface of tumor cells. Following internalization of the ADC, the MMAE binds to tubulin and inhibits microtubule polymerization, which may result in G2/M phase cell cycle arrest and apoptosis in CD48-expressing tumor cells. CD48, a member of the signaling lymphocyte activation molecule (SLAM) family of immune cell receptors, is involved in T-cell activation and leukocyte trafficking. Additionally, CD48 is expressed on the surface of multiple myeloma cells at significantly higher levels than it is expressed on normal lymphocytes and monocytes. The linkage system in SGN-CD48A improves stability, reduces off-target uptake, and enables conjugation of larger numbers of MMAE/antibody than other systems, resulting in increased specificity against CD48-positive cells.


anti-CD70 antibody-drug conjugate MDX-1203

An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody, directed against the extracellular domain of the human CD70 molecule, conjugated to a prodrug of a CC-1065 (rachelmycin) analogue via a stable peptide-based linker, with potential antineoplastic activity. The anti-CD70 antibody moiety of the anti-CD70 antibody-drug conjugate MDX-1203 selectively binds to the extracellular domain of CD70 on tumor cell surfaces. Upon internalization, the prodrug moiety is released and activated and binds to double-stranded B-DNA within the minor groove, thereby alkylating the –3 position of adenine, which may result in the inhibition of cellular proliferation of tumor cells that overexpress CD70. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on the surfaces of various types of cancer cells. The antitumor antibiotic CC-1065, a DNA minor-groove-binding alkylating agent, was originally isolated from the bacterium Streptomyces zelensis.


anti-CD70 antibody-drug conjugate SGN-CD70A

An antibody-drug conjugate (ADC) containing an engineered cysteine monoclonal antibody (EC-mAb), directed against the extracellular domain of the human CD70 molecule, conjugated to the synthetic, cytotoxic, DNA minor-groove crosslinking agent, pyrrolobenzodiazepine (PBD) dimer, via a stable, protease-cleavable, peptide-based linker, with potential antineoplastic activity. The anti-CD70 antibody moiety of the anti-CD70 antibody-drug conjugate SGN-CD70A selectively binds to the extracellular domain of CD70 on tumor cell surfaces. Upon internalization, the PBD dimer moiety is released and covalently binds, through its imine moieties, to the N2 positions of guanines on opposite strands of DNA. This induces DNA double strand breaks and inhibits DNA replication, which lead to the inhibition of cell growth of tumor cells that overexpress CD70. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on the surfaces of various types of cancer cells. The cysteine moiety of the EC-mAb allows for the stable conjugation of the PBD to the antibody.


anti-CD70 monoclonal antibody ARGX-110

A defucosylated, humanized IgG1 monoclonal antibody directed against the extracellular domain of the human CD70 molecule with potential antineoplastic activity. Upon administration, anti-CD70 monoclonal antibody ARGX-110 selectively binds to, and neutralizes the activity of CD70, which may also induce an antibody-dependent cellular cytotoxicity (ADCC) response against CD70-expressing tumor cells. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on a number of solid and hematological tumors. Its overexpression may play an important role in evasion of immune surveillance.


anti-CD70 monoclonal antibody MDX-1411

A glycoengineered, fully human IgG1 monoclonal antibody directed against the extracellular domain of the human CD70 molecule with potential antineoplastic activity. Anti-CD70 fully human monoclonal antibody MDX-1411 selectivity binds to the extracellular domain of CD70, which may induce an antibody-dependent cellular cytotoxicity (ADCC) response against CD70-expressing tumor cells. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on renal cell carcinoma (RCC) cells among other cancer cell types.


anti-CD71/vcMMAE probody-drug conjugate CX-2029

A probody-drug conjugate (PDC) composed of a monoclonal antibody directed against the transferrin receptor 1 (TFR1; TRP1; CD71), linked to a proprietary masking peptide that covers the active antigen-binding site of the antibody through a protease-cleavable linker, and conjugated, via a valine-citrulline (VC) peptide linker, to the potent cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of the anti-CD71/vcMMAE PDC CX-2029, the anti-CD71 moiety is unable to bind to CD71 antigen, which is highly expressed on both tumor and healthy dividing cells, until the masking peptide that is attached to the anti-CD71 probody is cleaved by tumor-associated proteases upon extravasation into the tumor microenvironment (TME). Local protease-mediated removal of the linker and masking peptide enables specific binding of the unmasked anti-CD71 moiety to CD71 expressed on tumor cells. Upon internalization and proteolytic cleavage, MMAE is released into the cytosol of CD71-expressing tumor cells, binds to tubulin, and inhibits microtubule polymerization, which induces both G2/M phase arrest and tumor cell apoptosis. CD71, a transmembrane glycoprotein, is a highly expressed protein present in a number of solid and hematologic cancer s, but is also expressed on normal, healthy tissues. The peptide masking of CX-2029 minimizes binding of the anti-CD71 antibody moiety to normal, healthy cells and may minimize systemic toxicity, when compared to other anti-CD71 antibody-drug conjugates (ADCs). Tumor-associated proteases are present in high concentrations and aberrantly activated in the TME.


anti-CD73 monoclonal antibody BMS-986179

A monoclonal antibody targeting the ectoenzyme 5'-ecto-nucleotidase (cluster of differentiation 73; CD73; 5'-NT; ecto-5'-nucleotidase; NT5E), with potential immunomodulating and antineoplastic activities. Upon administration, anti-CD73 monoclonal antibody BMS-986179 targets and binds to CD73, leading to clustering and internalization of CD73. This prevents CD73-mediated conversion of extracellular adenosine monophosphate (AMP) to adenosine and decreases the amount of free adenosine. This prevents adenosine-mediated suppression of lymphocyte activity and increases the activity of CD8-positive effector cells. This also activates macrophages, and reduces the activity of both myeloid-derived suppressor cells (MDSCs) and regulatory T lymphocytes. By abrogating the inhibitory effect on the immune system and enhancing the cytotoxic T-cell-mediated immune response against cancer cells, tumor cell growth is decreased. CD73, a plasma membrane protein belonging to the 5'-nucleotidase (NTase) family, is upregulated on a number of cancer cell types and catalyzes the conversion of extracellular nucleotides, such as AMP, to membrane-permeable nucleosides, such as adenosine; it plays a key role in adenosine-mediated immunosuppression within the tumor microenvironment.


anti-CD73 monoclonal antibody CPI-006

A type II humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting the ectoenzyme 5'-ecto-nucleotidase (cluster of differentiation 73; CD73; 5'-NT; ecto-5'-nucleotidase; NT5E), with potential immunomodulating and antineoplastic activities. Upon intravenous administration, anti-CD73 monoclonal antibody CPI-006 targets and binds to CD73 on tumor cells, leading to internalization of CD73. This prevents CD73-mediated conversion of extracellular adenosine monophosphate (AMP) to adenosine, thereby preventing adenosine-mediated suppression of lymphocyte activity and increasing the activity of cytotoxic T lymphocytes (CTLs). This also activates macrophages, and reduces the activity of both myeloid-derived suppressor cells (MDSCs) and regulatory T lymphocytes. By abrogating the inhibitory effect on the immune system and enhancing the CTL-mediated immune response against cancer cells, tumor cell growth is decreased. CD73, a plasma membrane protein belonging to the 5'-nucleotidase (NTase) family, is upregulated on a number of cancer cell types and catalyzes the conversion of extracellular nucleotides, such as AMP, to membrane-permeable nucleosides, such as adenosine; it plays a key role in adenosine-mediated immunosuppression within the tumor microenvironment.


anti-CD98 monoclonal antibody IGN523

A humanized, monoclonal antibody targeting the CD98 (gp125) antigen, with potential immunomodulatory and antineoplastic activities. Upon intravenous administration, IGN523 binds to CD98 expressed on the tumor cell surface and elicits both natural killer (NK)-cell mediated antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity towards CD98-expressing tumor cells. In addition, IGN523 inhibits essential amino acid uptake by rapidly proliferating tumor cells. CD98, a type II transmembrane glycoprotein, is involved in both integrin signaling and amino acid transport processes; it is overexpressed in certain cancer cells and plays a key role in the proliferation, survival, and metastasis of tumor cells.


anti-CDH6 antibody-drug conjugate HKT288

An immunoconjugate consisting of a human monoclonal antibody directed against the tumor-associated antigen (TAA) cadherin-6 (CDH6; CDH-6) conjugated to a maytansine-based cytotoxic agent, with potential antineoplastic activity. The monoclonal antibody moiety of HKT288 targets and binds to CDH6 located on tumor cell surfaces. After internalization, the maytansine moiety binds to tubulin, which disrupts microtubule assembly/disassembly dynamics and inhibits both division and proliferation of CDH6-expressing tumor cells. CDH6, a member of the cadherin family and overexpressed by a variety of cancer s, plays a key role in tumor cell proliferation.


anti-CEA BiTE monoclonal antibody AMG211

A recombinant, proprietary bispecific T-cell engagers (BiTE) antibody directed against human carcinoembryonic antigen (CEA), with potential immunostimulating and antineoplastic activities. Anti-CEA BiTE monoclonal antibody MEDI-565 possesses two antigen-recognition sites, one for CEA and one for the CD3 complex, a group of T cell surface glycoproteins that complex with the T cell receptor (TCR). This bispecific monoclonal antibody brings CEA-expressing tumor cells and cytotoxic T lymphocytes (CTLs) and helper T lymphocytes (HTLs) together, which may result in the CTL- and HTL-mediated cell death of CEA-expressing cells. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancer s.


anti-CEA IgCD28TCR-transduced autologous T cells

A population of autologous tumor infiltrating lymphocytes (TIL) transduced with a retroviral vector encoding the chimeric gene IgCD28TCR with potential immunostimulating and antineoplastic activities. The chimeric IgCD28TCR gene consists of portions of CD28, the zeta chain of the T-cell receptor (TCRzeta), and a single chain antibody domain (sFv) specific for the tumor-associated antigen CEA. Upon administration, these gene-modified TIL bind to tumor cells expressing CEA, which may result in activation and proliferation of TIL and an enhanced cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells. CEA may be overexpressed in various gastrointestinal and breast cancer s. CD28, a T-cell surface-associated co-stimulatory molecule, is required for full T-cell activation, proliferation, and survival; expression of the CD28 fragment in this chimeric gene construct may impede activation-induced cell death (AICD) of TIL.


anti-CEA TCR retroviral vector-transduced autologous lymphocytes

Autologous human peripheral blood lymphocytes (PBLs), transduced with a retroviral vector encoding both the alpha and beta chains of a T cell receptor (TCR) specific for the carcinoembryonic antigen (CEA), with potential immunostimulating and antineoplastic activities. After transduction, expansion in culture, and reintroduction into the patient, anti-CEA TCR retroviral vector-transduced autologous lymphocytes bind to tumor cells expressing CEA, which may result in cytokine expression, activation and proliferation of T-cells, and a specific cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells. The tumor-associated antigen (TAA) CEA is overexpressed by a variety of cancer cell types, including those of the gastrointestinal tract, lung , and breast.


anti-CEA/anti-DTPA-In (F6-734) bispecific antibody

A bispecific monoclonal antibody (BsMAb) consisting of the Fab fragment of an anti-CEA monoclonal antibody (F6) coupled to the Fab fragment of an anti-DTPA-In monoclonal antibody (734) with potential radioimmunotherapeutic activity. In a two-step "pretargeted" radioimmunotherapeutic approach, this BsMAb, localizing to CEA-expressing tumor cells via the F6 Fab fragment, is introduced into patient first, followed by injection of indium 131-radiolabeled DTPA, which is recognized by the 734 Fab fragment of the BsMAb. Accordingly, a potentially lethal dose of indium 131 is delivered specifically to CEA-expressing tumor cells while minimizing radiotoxicity to normal tissues. CEA (carcinoembryonic antigen) is a tumor antigen overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancer s. DTPA (diethylenetriaminepentaacetic acid) is a bivalent hapten.


anti-CEA/anti-HSG bispecific monoclonal antibody TF2

A tri-Fab bispecific monoclonal antibody (BiMoAb) divalent for the carcinoembryonic antigen (CEA) and monovalent for histamine-succinyl-glycine (HSG) peptide-hapten. Anti-CEA/anti-HSG bispecific monoclonal antibody TF2 binds to the tumor associated antigen (TAA) CEA on CEA-expressing tumor cells. Subsequently, an HSG peptide-hapten carrying a radionuclide is administered, binding to the anti-HSG binding fragment on the BiMoAb. Depending on the characteristics of the radionuclide used, CEA-expressing tumor cells may then be radioimaged and/or treated radioimmunotherapeutically.


anti-CEA/CD3 bispecific antibody RO6958688

An anti-carcinoembryonic antigen (CEA)/anti-CD3 bispecific monoclonal antibody with potential antineoplastic activity. Anti-CEA/CD3 monoclonal antibody RO6958688 contains two antigen-recognition sites: one for human CD3, a T-cell surface antigen, and one for human CEA, a tumor-associated antigen that is specifically expressed on certain tumor cells. Upon intravenous administration, RO6958688 binds to both T-cells and CEA-expressing tumor cells, which cross-links the T-cells with the tumor cells. This may result in a potent cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells. CEA is overexpressed in many cancer cell types.


anti-CEACAM1 monoclonal antibody CM-24

A humanized monoclonal immunoglobulin G4 (IgG4) antibody targeting the anti-carcinoembryonic antigen (CEA)-related cell adhesion molecule 1 (CEACAM1; CD66a), with potential immunomodulating and antineoplastic activities. Upon administration of anti-CEACAM1 monoclonal antibody CM-24, this agent binds to CEACAM1 on cancer cells and certain immune cells. This blocks the binding of CEACAM1-expressing cancer cells to CEACAM1-expressing immune cells and abrogates CEACAM1-mediated immunosuppression. This enhances the activation of cytotoxic T-lymphocytes (CTLs) and natural killer (NK) cells and increases CTL- and NK-mediated killing of CEACAM1-overexpressing cancer cells. CEACAM1, a member of the CEA family of proteins that plays a key role in cell migration, cell invasion, and cell adhesion, is overexpressed by a variety of cancer cell types. Its overexpression is correlated with both immunosuppression and poor prognosis.


anti-CEACAM5 antibody-drug conjugate SAR408701

An immunoconjugate consisting of anti-carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5) conjugated to a cytotoxic agent, with potential antineoplastic activity. Upon administration of anti-CEACAM5 antibody-drug conjugate SAR408701, the antibody moiety targets CEACAM5 on tumor cells. Upon antibody/antigen binding and internalization, the immunoconjugate releases the cytotoxic agent, which results in tumor cell death. CEACAM5, a member of the CEA family of proteins that plays a key role in cell migration, cell invasion, and cell adhesion, is overexpressed by a variety of cancer cell types.  


anti-CEACAM6 AFAIKL2 antibody fragment/Jack Bean urease immunoconjugate L-DOS47

A lyophilized formulation of DOS47, an immunoconjugate composed of AFAIKL2, a recombinant camelid single-domain antibody which recognizes carcinoembryonic antigen-related cell adhesion molecule 6 (CEACAM6), and the enzyme urease derived from the plant Canavalia ensiformis (Jack bean), with potential antineoplastic activity. Upon intravenous administration, the AFAIKL2 antibody fragment moiety of L-DOS47 specifically targets and binds to CEACAM6 expressed on certain tumor cells. In turn, the urease moiety of L-DOS47 catalyzes the hydrolysis of urea into ammonia, which is further hydrolyzed to produce hydroxyl ions, and causes a locally increased concentration of the toxic waste product ammonia, which under normal conditions is converted into the nontoxic substance urea via the urea cycle. This increases the pH of the tumor microenvironment and alkalinizes the highly acidic environment that is needed for cancer cell survival and proliferation. In addition, the ammonia diffuses into cancer cells and exerts a cytotoxic effect. Altogether, this leads to cell death of CEACAM6-expressing cancer cells. The naturally-occurring enzyme urease catalyzes the hydrolysis of urea into ammonia and carbon dioxide. CEACAM6, a tumor-associated antigen and CEA family member, is overexpressed in a variety of tumor cells and plays a key role in tumor initiation, progression, metastasis and survival.


anti-CEA-CAR autologous T lymphocytes

Autologous lymphocytes transduced with a retroviral vector encoding a chimeric antigen receptor (CAR) specific for the tumor-associated antigen human carcinoembryonic antigen (CEA), with potential immunostimulating and antineoplastic activities. Upon administration, the anti-CEA-CAR autologous T-lymphocytes target and bind to tumor cells expressing CEA, which results in the cytotoxic T-lymphocyte (CTL)-mediated cell killing of CEA-expressing tumor cells. CEA is overexpressed in various tumor cell types.


anti-c-fms monoclonal antibody AMG 820

A fully human IgG2 monoclonal antibody against the colony-stimulating factor-1 (CSF-1 or M-CSF) receptor c-fms (or CSFR1), with potential antineoplastic activity. Upon administration, anti-c-fms monoclonal antibody AMG 820 binds to and blocks c-fms, thereby blocking CSF-1 binding to its receptor and suppressing CSF-1-induced c-fms signaling. This results in the suppression of recruitment and activation of tumor associated macrophages (TAM) within the tumor microenvironment. This eventually leads to a decrease in tumor growth. c-fms, a transmembrane protein belonging to the tyrosine kinase family, is overexpressed in certain tumor cell types and plays an essential role in macrophage differentiation and regulation of cell proliferation. The presence of TAM is correlated with tumor proliferation, invasion and a poor prognosis.


anti-c-KIT monoclonal antibody KTN0158

A humanized immunoglobulin (Ig) G1 monoclonal antibody against the stem cell factor receptor c-Kit (SCFR; KIT; CD117), with potential antineoplastic and anti-allergic activities. Upon administration, the anti-c-KIT monoclonal antibody KTN0158 binds to and inhibits the activation of the cell surface antigen c-Kit. This leads to an inhibition of the activation of c-KIT-mediated signal transduction pathways and inhibits cell proliferation in cancer cells expressing c-Kit. In mast cells, inhibition of c-KIT and c-KIT-mediated signaling prevents mast cell activation, degranulation and subsequent cytokine release. c-Kit, a transmembrane protein and receptor tyrosine kinase, is overexpressed in various cell types, including certain cancer cells and mast cells; it plays a key role in the regulation of cell differentiation and proliferation.


anti-CLDN6 monoclonal antibody IMAB027

A monoclonal antibody directed against the cell surface protein claudin 6 (CLDN6), with potential immunostimulating and antineoplastic activities. Upon administration, the anti-CLDN6 monoclonal antibody IMAB027 binds to CLDN-6 and may stimulate the immune system to exert both an antibody-dependent cellular cytotoxicity (ADCC) and a complement-dependent cytotoxicity (CDC)-mediated immune response against CLDN-6-expressing tumor cells. This may inhibit tumor cell growth. CLDN-6, a tight-junction protein and embryonic antigen, is expressed on a variety of tumor cells but is not expressed on normal, healthy adult cells.


anti-CLEC12A/CD3 bispecific antibody MCLA117

An immunoglobulin G1 (IgG1) bispecific human monoclonal antibody against human CD3, a T-cell surface antigen, and human C-type lectin domain family 12 member A (CLEC12A), a tumor-associated antigen (TAA) overexpressed on certain tumor cells, with potential antineoplastic activity. Upon administration, anti-CLEC12A/CD3 bispecific antibody MCLA117 binds to both CD3 on T cells and CLEC12A expressed on malignant cells, such as myeloid blasts, atypical progenitor cells and leukemic stem cells (LSCs). This results in the cross-linking of T cells with tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against CLEC12A-expressing tumor cells. CLEC12A, a myeloid differentiation antigen and member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily, is overexpressed on myeloid leukemia cells, but not on normal early hematopoietic progenitors, including hematopoietic stem cells (HSCs).


anti-c-Met antibody-drug conjugate HTI-1066

An antibody-drug conjugate (ADC) composed of a monoclonal antibody against the tumor-associated antigen (TAA) the proto-oncogene c-Met (hepatocyte growth factor receptor; HGFR) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of HTI-1066 targets and binds to c-Met expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the c-Met-expressing cancer cells, through an as of yet unknown mechanism of action. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays key roles in tumor cell proliferation, survival, invasion, metastasis and tumor angiogenesis.


anti-c-Met monoclonal antibody ABT-700

A monoclonal antibody directed against human hepatocyte growth factor receptor (HGFR or c-Met), with potential antineoplastic activity. Anti-c-Met monoclonal antibody ABT-700 binds to c-Met, thereby preventing c-Met binding to its ligand, HGF and the subsequent activation of the HGF/c-Met signaling pathway. This may cause cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.


anti-c-Met monoclonal antibody ARGX-111

A human monoclonal antibody targeting c-Met, with potential antineoplastic activity. Anti-c-Met monoclonal antibody ARGX-111 binds to c-Met, and blocks both ligand-dependent and -independent activation of c-Met-mediated signaling pathways. In addition, this agent enhances antibody-dependent cellular cytotoxicity (ADCC). This leads to a reduction in cell proliferation of c-Met-expressing cancer cells. c-Met, a receptor tyrosine kinase overexpressed in certain cancer cell types, is involved in cell proliferation, angiogenesis and metastasis in multiple solid tumors. Compared to other c-Met targeting monoclonal antibodies, ARGX-111 shows increased antibody circulation time, enhanced tissue distribution and increased efficacy. ARGX-111 is obtained through active immunization with C-met antigen in Camelids and utilizes the Camelid V-domains fused with human antibody backbones.


anti-c-MET monoclonal antibody LY2875358

A humanized IgG4 monoclonal antibody directed against human hepatocyte growth factor receptor (HGFR or c-MET) with potential antineoplastic activity. Anti-c-MET monoclonal antibody LY2875358 binds to c-MET, thereby preventing the binding of HGF to its receptor c-Met and subsequent activation of the HGF/c-Met signaling pathway. This may result in cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.


anti-C-met monoclonal antibody SAIT301

A humanized monoclonal antibody targeting the alpha chain of the extracellular domain of human hepatocyte growth factor receptor (HGFR or c-Met), with potential antineoplastic activity. Anti-c-Met monoclonal antibody SAIT301 binds to c-Met, thereby preventing both binding of its ligand, HGF, and the subsequent activation of the HGF/c-Met signaling pathway. In addition, SAIT301 induces c-Met internalization and subsequent degradation, which further inhibits c-Met-mediated signaling. This leads to a reduction in the proliferation of c-Met-expressing cancer cells. c-Met, a proto-oncogene receptor tyrosine kinase overexpressed in certain cancer cell types, is involved in various tumors.


anti-CSF1 monoclonal antibody PD-0360324

A humanized immunoglobulin (Ig) G2 monoclonal antibody (mAb) directed against the cytokine colony stimulating factor 1 (CSF1; CSF-1; macrophage colony-stimulating factor; M-CSF), with potential immunomodulating and antineoplastic activities. Upon administration, anti-CSF1 monoclonal antibody PD-0360324 targets, binds to and neutralizes CSF1. This prevents the binding of CSF1 to its receptor CSF1R (CD115; M-CSFR), which is expressed on various immune cells, such as monocytes and macrophages. This prevents CSF1R activation and CSF1R-mediated signaling in these cells, leading to inhibition of monocyte differentiation, blocking the activity of macrophages, and reducing their production of inflammatory mediators, which reduces inflammation. By blocking the activity and proliferation of CSF1R-dependent tumor-associated macrophages (TAMs) in the tumor microenvironment, PD-0360324 reduces TAM-mediated immune suppression, decreases regulatory T cells (Tregs), re-activates the immune system, and improves anti-tumor cell responses mediated by increasing infiltration by cytotoxic T cells. TAMs play key roles in immune suppression, and tumor cell proliferation and survival. CSF-1 plays a key role in the regulation of the proliferation, differentiation and survival of monocytes and macrophages.


anti-CSF-1R monoclonal antibody IMC-CS4

A monoclonal antibody directed against colony stimulating factor 1 receptor (CSF1R) with potential antineoplastic activity. CSF1R monoclonal antibody IMC-CS4 binds to CSF1R which may trigger antitumoral antibody-dependent cell-mediated cytotoxicity (ADCC) in tumor cells overexpressing CSF1R. CSF1R, also known as macrophage colony-stimulating factor receptor (M-CSFR) and CD115 (cluster of differentiation 115), is a cell-surface receptor for its ligand colony stimulating factor 1 (CSF1); this receptor is overexpressed or mutated in certain tumor cell types and plays major roles in tumor cell proliferation and metastasis.


anti-CSF-1R monoclonal antibody SNDX-6352

A humanized immunoglobulin (Ig) G4 monoclonal antibody directed against colony-stimulating factor 1 receptor (CSF-1R), with potential antineoplastic activity. Upon intravenous administration, anti-CSF1R monoclonal antibody SNDX-6352 binds to the ligand binding domain of CSF-1R, preventing binding and consequent activation by its natural ligands, IL-34 and colony-stimulating factor 1 (CSF-1). Inhibition of CSF-1R activation may disrupt the activity of tumor-associated macrophages (TAMs), which promote initiation and metastasis of tumor cells, inhibit T-cell responses, and stimulate tumor angiogenesis and disease progression. CSF-1R, also known as macrophage colony-stimulating factor receptor (M-CSFR) and cluster of differentiation 115 (CD115), is a tyrosine-protein kinase that plays an essential role in the regulation, proliferation, survival and differentiation of tissue macrophages as well as TAMs.


anti-CTGF monoclonal antibody FG-3019

A human monoclonal antibody targeting connective tissue growth factor (CTGF) with potential anti-fibrotic and antineoplastic activities. FG-3019 binds to CTGF thereby preventing the binding of the ligand to the receptor and subsequent receptor activation. As CTGF enhances the production of collagen and fibronectin, FG-319 may prevent and reverse fibrosis. In addition, FG-3019 may prevent tumor cell proliferation in CTGF-expressing tumor cells. CTGF, a member of the CCN family (CTGF, CYR61/CEF and NOV), is expressed in a variety of tumor cell types and is involved in processes such as cell proliferation, cell migration, cell adhesion, differentiation and angiogenesis.


anti-CTLA4 mAb RNA/GITRL RNA-transfected autologous dendritic cell vaccine

An autologous dendritic cell (DC) cancer vaccine with potential immunostimulatory activity. Anti-CTLA4 MoAb RNA/GITRL RNA-transfected DC vaccine is prepared by transfecting DCs with RNAs encoding humanized heavy and light chains of the anti-CTLA4 (cytotoxic T-Lymphocyte-Associated Antigen 4) monoclonal antibody and tumor necrosis factor (ligand) superfamily, member 18 (TNFSF18 or GlTRL); expression of anti-CTLA4 blocks the inhibitory effect of CTLA4 on the activation of T-lymphocytes, while expression of GlTRL modulates T lymphocyte survival in peripheral tissues. Co-vaccination of this vaccine with melanoma antigen specific vaccine may eliminate the adverse effects associated with systemic administration of immune modulators, while also enhancing vaccine-induced immune responses.


anti-CTLA-4 mAb RNA-transfected autologous dendritic cell vaccine

An autologous dendritic cell (DC) cancer vaccine with potential immunostimulatory activity. Anti-CTLA4 MoAb RNA-transfected autologous DC vaccine is prepared by transfecting DCs with RNAs encoding humanized heavy and light chains of the anti-CTLA4 (cytotoxic T-Lymphocyte-Associated Antigen 4); expression of anti-CTLA4 blocks the inhibitory effect of CTLA4 on the activation of T-lymphocytes. Co-vaccination of this vaccine with melanoma antigen specific vaccine may eliminate the adverse effects associated with systemic administration of immune modulators, while also enhancing vaccine-induced immune responses.


anti-CTLA-4 monoclonal antibody AGEN1884

A recombinant human monoclonal antibody directed against the human T-cell receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4), with immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-CTLA4 monoclonal antibody AGEN1884 binds to CTLA4 expressed on T cells and inhibits the CTLA4-mediated downregulation of T-cell activation. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells. CTLA4, an inhibitory receptor and member of the immunoglobulin superfamily, plays a key role in the downregulation of the immune system.


anti-CTLA4 monoclonal antibody BMS-986218

A Fc-modified monoclonal antibody directed against the human T-cell receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-CTLA4 monoclonal antibody BMS-986218 targets and binds to CTLA4 expressed on T cells and inhibits the CTLA4-mediated downregulation of T-cell activation. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells. CTLA4, an inhibitory receptor and member of the immunoglobulin superfamily, plays a key role in the downregulation of the immune system. Removal of the fucose sugar units from the antibody's Fc region, enhances its activity and decreases the toxicity of BMS-986218.


anti-CTLA-4 monoclonal antibody MK-1308

A monoclonal antibody directed against the human T-cell-expressed receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-CTLA4 monoclonal antibody MK-1308 targets and binds to CTLA4 expressed on T cells and inhibits the CTLA4-mediated downregulation of T-cell activation. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells. CTLA4, an inhibitory receptor and member of the immunoglobulin superfamily, plays a key role in the downregulation of the immune system.


anti-CTLA-4/OX40 bispecific antibody ATOR-1015

A bispecific antibody consisting of a cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) inhibitory protein fused to an OX40 agonistic human immunoglobulin G1 (IgG1) antibody, with potential immunostimulating and antineoplastic activities. Upon administration, anti-CTLA-4/OX40 bispecific antibody ATOR-1015 simultaneously binds to CTLA-4 and OX40, which may inhibit CTLA-4-mediated downregulation of T-cell activation and induce proliferation of memory and effector T lymphocytes via OX40 activation. Both CTLA-4, an inhibitory receptor and member of the immunoglobulin superfamily (IgSF), and OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor superfamily (TNFRSF), are overexpressed by regulatory T cells (Tregs) in the tumor microenvironment. ATOR-1015 may reduce the number of Tregs and promote the activation of effector T cells, thereby enhancing the immune-mediated anti-tumor response.


anti-CXCR4 monoclonal antibody PF-06747143

A humanized immunoglobulin (Ig) G1 monoclonal antibody (mAb) against C-X-C chemokine receptor type 4 (CXCR4), with potential antineoplastic activity. Upon administration, anti-CXCR4 mAb PF-06747143 binds to CXCR4, thereby preventing the binding of stromal cell-derived factor-1 (SDF-1 or CXCL12) to CXCR4 and inhibiting CXCR4 activation. This results in decreased proliferation and migration of CXCR4-expressing tumor cells. In addition, PF-06747143 promotes cell death through the induction of both complement-dependent cytotoxicity (CDC) and antibody-dependent cellular cytotoxicity (ADCC). CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) family, is upregulated in several tumor cell types and plays an important role in cancer cell proliferation, survival, and chemotaxis, and in tumor angiogenesis.


anti-denatured collagen recombinant monoclonal antibody TRC093

A humanized, affinity-matured IgG1k antibody directed against denatured collagens (I-IV) with potential antiangiogenic and antineoplastic activities. Anti-denatured collagen recombinant monoclonal antibody TRC093 binds to multiple epitopes on denatured collagens, inhibiting proteolytic collagen-mediated signaling in the extracellular matrix (ECM) that is important to tumor angiogenesis, tumor growth, and metastasis. The epitopes on denatured collagen bound by this antibody are considered "cryptic" because, in vivo, they are accessible only on the subendothelial basement membrane of tumors or in normal tissues undergoing neovascularization.


 

anti-DKK1 monoclonal antibody BHQ880

A humanized monoclonal antibody directed against Wnt antagonist Dickkopf-1 (DKK1) with potential anti-osteolytic activity. Anti-DKK1 monoclonal antibody BHQ880 binds to and inhibits DKK1, enhancing signaling through the Wnt pathway, which may result in osteoblast differentiation and activation within the bone matrix and the reversal of tumor-induced osteolytic disease. DKK! is a potent Wnt signaling pathway antagonist.


anti-DKK-1 monoclonal antibody LY2812176

A human monoclonal antibody directed against the WNT antagonist dickkopf homolog 1 (DKK1), with potential anti-osteolytic activity. Anti-DKK1 monoclonal antibody LY2812176 binds to and inhibits DKK1, thereby restoring signaling through the WNT pathway, which may result in osteoblast differentiation and activation within the bone matrix and the reversal of tumor-induced osteolytic disease. DKK1, overexpressed by myeloma cells, is an inhibitor of the WNT signaling pathway and prevents the mediated formation of bone.


anti-DLL3/CD3 BiTE antibody AMG 757

A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) delta-like protein 3 (DLL3) fused to one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-DLL3/CD3 BiTE antibody AMG 757, this bispecific antibody binds to both the CD3 antigen on cytotoxic T lymphocytes (CTLs) and the DLL3 antigen found on DLL3-expressing tumor cells. This activates and redirects CTLs to DLL3-expressing tumor cells, which results in the CTL-mediated cell death of DLL3-expressing tumor cells. DLL3, a Notch pathway protein, is overexpressed on a variety of cancer cell types. It plays a key role in embryonic development and in tumor initiation and proliferation.


anti-DLL4 monoclonal antibody MEDI0639

An immunoglobulin G1 lambda monoclonal antibody directed against the Notch ligand delta-like 4 (DLL4) with potential antineoplastic activity. Anti-DLL4 monoclonal antibody MEDI0639 specifically binds to DLL4 and prevents its interaction with Notch receptors, thereby inhibiting Notch-mediated signaling and gene transcription, which may block tumor angiogenesis and eventually the inhibition of tumor cell growth. Activation of Notch receptors by DLL4 stimulates proteolytic cleavage of the Notch intracellular domain (NICD); after cleavage, NICD is translocated to the nucleus and mediates the transcriptional regulation of a variety of genes involved in vascular development. The expression of DLL4 is highly restricted to the vascular endothelium; DLL4/Notch signaling is required for the development of functional tumor blood vessels.


anti-DLL4 monoclonal antibody REGN421

A human monoclonal antibody directed against Delta-like ligand-4 (DLL4) with potential antineoplastic activity. Anti-DLL4 monoclonal antibody REGN421 specifically binds to human DLL4, preventing its binding to Notch receptors and inhibiting Notch signaling, which may result in defective tumor vascularization and, so, the inhibition of tumor cell growth. DLL4 is the only Notch ligand selectively expressed on endothelial cells; DLL4/Notch signaling is required for the development of functional tumor blood vessels.


anti-DLL4/VEGF bispecific monoclonal antibody OMP-305B83

A bispecific monoclonal antibody directed against both the Notch ligand delta-like 4 (DLL4) and the human tyrosine kinase vascular endothelial growth factor (VEGF), with potential anti-angiogenic and antineoplastic activities. The anti-DLL4 moiety of anti-DLL4/VEGF monoclonal antibody OMP-305B83 specifically binds to DLL4, prevents its interaction with Notch receptors, and inhibits Notch-mediated signaling and gene transcription, which may both block tumor angiogenesis and inhibit tumor cell growth. The anti-VEGF moiety binds to VEGF and prevents the binding of VEGF to its receptor, which blocks VEGF-mediated signaling and further inhibits the growth and maintenance of tumor blood vessels. The expression of DLL4 is highly restricted to the vascular endothelium; DLL4/Notch signaling is required for the development of functional tumor blood vessels. The expression of the pro-angiogenic growth factor VEGF is associated with tumor angiogenesis and tumor cell proliferation and invasion.


anti-DR5 agonist monoclonal antibody TRA-8

An agonist mouse monoclonal antibody directed against TRAIL death receptor type 5 (DR5) with potential antineoplastic activity. Anti-DR5 agonist monoclonal antibody TRA-8 binds DR5, which may induce apoptosis in DR5-expressing tumor cells. DR5 is a tumor cell surface ligand that crosslinks with death receptor type 4 (DR4) when bound by TRAIL [Tumor necrosis (TNF)-related apoptosis-inducing ligand], triggering apoptosis via a death receptor signaling pathway. The apoptotic activity of this antibody may not require DR4/DR5 crosslinking.


anti-DR5 agonistic monoclonal antibody INBRX-109

A recombinant, humanized, agonistic, tetravalent monoclonal antibody directed against human death receptor type 5 (DR5), also called tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) receptor 2 (TRAILR2), with potential pro-apoptotic and antineoplastic activities. Upon administration, INBRX-109 specifically binds to exactly four DR5 receptors per molecule, which mimics the interaction of DR5 with its natural ligand TRAIL. This activates DR5 and the death receptor signaling pathway, which results in the activation of caspase cascades, the induction of tumor cell apoptosis and a reduction in proliferation of DR5-expressing tumor cells. Utilizing a tetravalent monoclonal antibody may overcome the challenge of generating effective DR5 clustering while avoiding toxicities associated with anti-drug antibody (ADA) hyper-clustering. DR5, a member of the TNF receptor superfamily (TNFRSF), is expressed on the surfaces of a variety of tumor cells and plays a key role in the induction of tumor cell apoptosis.


anti-EGFL7 monoclonal antibody MEGF0444A

A humanized IgG1 monoclonal antibody directed against the epidermal growth factor-like domain multiple 7 (EGFL7) with potential antineoplastic activity. Anti-EGFL7 monoclonal antibody MEGF0444A binds to EGFL7, thereby preventing the activities of EGFL7 on endothelial cells and inhibiting the survival and migration of endothelial cells during angiogenesis. EGFL7, a vascular-restricted extracellular matrix protein which is upregulated during angiogenesis and which regulates vascular development, may be overexpressed on the cell surfaces of various solid tumor cell types.


anti-EGFR fluorescence imaging agent ABY-029

A fluorescence imaging and contrast agent composed of an epidermal growth factor receptor (EGFR)-targeting affibody tracer molecule and labeled, through maleimide, with a near-infrared (NIR) fluorescent probe, IRDye 800CW, with potential use in the imaging of EGFR-overexpressing cells. Upon administration, ABY-029 targets and binds to EGFR-overexpressing tumor cells. Upon fluorescent imaging, the fluorescent dye can be visualized and EGFR-positive tumor cells can be detected.


anti-EGFR monoclonal antibody ABT-806

A humanized monoclonal antibody (MoAb) against human epidermal growth factor receptor (EGFR) with antineoplastic activity. MoAb ABT-806 targets the EGFR deletion variant, de2-7 EGFR as well as wild-type EGFR expressed in cells overexpressing the receptor, thereby preventing the activation and subsequent dimerization of the receptor; the decrease in receptor activation and dimerization result in an inhibition in signal transduction and anti-proliferative effects. This MoAb targets cells expressing aberrant EGFR, hence making it an ideal candidate for generation of radioisotope or toxin conjugates.


anti-EGFR monoclonal antibody CPGJ 602

A recombinant, human-mouse chimeric monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Upon intravenous administration, anti-EGFR monoclonal antibody CPGJ 602 targets and binds to EGFR, which prevents receptor dimerization and activation. This leads to an inhibition of EGFR-dependent downstream pathways and EGFR-dependent tumor cell proliferation and metastasis. EGFR, a receptor tyrosine kinase, may be overexpressed on the surfaces of various tumor cell types.


anti-EGFR monoclonal antibody GC1118

A recombinant, human monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Upon intravenous administration, GC1118 binds to and blocks the ligand binding site of EGFR, which prevents receptor dimerization and activation. This may lead to an inhibition of both EGFR-dependent downstream pathways and EGFR-dependent tumor cell proliferation and metastasis. EGFR, a receptor tyrosine kinase, may be overexpressed on the surfaces of various tumor cell types.


anti-EGFR monoclonal antibody mixture MM-151

An oligoclonal therapeutic composed of three fully human monoclonal antibodies targeting epidermal growth factor receptor (EGFR or ErbB1), with potential antineoplastic activity. Upon administration of MM-151, the three antibodies bind to distinct, non-overlapping epitopes of EGFR, thereby preventing the binding of a full range of both high and low affinity EGFR ligands and inhibiting EGFR-ERK-mediated signaling. This eventually inhibits tumor cell proliferation in EGFR-overexpressing tumor cells. Furthermore, multi antibody-antigen bindings cause crosslinking of EGFR and downregulate receptor signalings that are mediated via heterodimerization of EGFR with other members of the EGFR family. EGFR, a receptor tyrosine kinase overexpressed in a variety of cancer cell types, is a key regulator of cancer cell proliferation, apoptosis, invasion, and metastasis.


anti-EGFR monoclonal antibody mixture sym004

A mixture of two recombinant IgG1 antibodies directed against different epitopes in the epidermal growth factor receptor (EGFR) extracellular domain III, with potential antineoplastic activity. Anti-EGFR monoclonal antibody mixture Sym004 binds to the extracellular domain of EGFR, thereby preventing ligand binding. This may prevent activation and subsequent dimerization of the receptor; the decrease in receptor activation may result in an inhibition of downstream ERK and JNK signaling pathways and thus inhibition of EGFR-dependent tumor cell proliferation and metastasis. In addition, binding of Sym004 to EGFRs causes EGFR internalization and degradation. EGFR, a receptor tyrosine kinase, often is overexpressed on the cell surfaces of various solid tumor cell types.


anti-EGFR monoclonal antibody RO5083945

A glycoengineered monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. anti-EGFR monoclonal antibody RO5083945 binds to the extracellular domain of EGFR, preventing the activation and subsequent dimerization of the receptor; the decrease in receptor activation and dimerization may result in an inhibition of downstream ERK and JNK signaling pathways and so inhibition of EGFR-dependent tumor cell proliferation and metastasis. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surfaces of various solid tumor cell types.


anti-EGFR monoclonal antibody SYN004

A glyco-engineered monoclonal antibody directed against the receptor tyrosine kinase epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon administration, anti-EGFR monoclonal antibody SYN004 binds to the extracellular domain of EGFR, which prevents ligand binding and the subsequent activation and dimerization of the receptor. This inhibits the activation of EGFR-mediated signaling pathways and inhibits EGFR-dependent tumor cell proliferation. EGFR, a member of the EGFR receptor tyrosine kinase family, may be overexpressed on the cell surfaces of various tumor cell types.  


anti-EGFR TAP antibody-drug conjugate IMGN289

A targeted antibody payload (TAP)-based immunoconjugate consisting of a human monoclonal antibody directed against the epidermal growth factor receptor (EGFR) conjugated, via a nonreducible thioether linker (succinimidyl trans-4-(maleimidylmethyl)cyclohexane-1-carboxylate or SMCC), to the cytotoxic agent maytansinoid mertansine (DM1), with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of immunoconjugate IMGN289 binds to and inhibits EGFR on tumor cell surfaces. Inhibition of EGFR prevents EGFR-mediated signaling and may inhibit tumor cell proliferation. After internalization, the mertansine moiety binds to tubulin and interferes with microtubule assembly/disassembly dynamics. This inhibits both cell division and the proliferation of cancer cells that express EGFR. EGFR, overexpressed by a variety of cancer s, plays a key role in tumor cell proliferation and survival. Linkage of the antibody and drug, through a nonreducible linker, appears to contribute to the improved efficacy and reduced toxicity of this antibody-drug conjugate (ADC) compared to similar ADCs constructed with reducible linkers.


anti-EGFR/c-Met bispecific antibody JNJ-61186372

A human bispecific antibody targeting both epidermal growth factor receptor EGFR and hepatocyte growth factor receptor (HGFR; cMet), with potential antineoplastic activity. Upon administration, anti-EGFR/c-Met bispecific antibody JNJ-61186372 simultaneously targets and binds to wild-type or certain mutant forms of both EGFR and cMet expressed on cancer cells, thereby preventing receptor phosphorylation. This prevents the activation of both EGFR- and cMet-mediated signaling pathways. In addition, binding results in receptor degradation, which further inhibits EGFR- and cMet-mediated signaling. JNJ-61186372 also causes antibody-dependent cellular cytotoxicity (ADCC). Altogether, this results in the inhibition of tumor cell proliferation. EGFR and cMet, both upregulated or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation.


anti-EGFR/DM1 antibody-drug conjugate AVID100

A targeted antibody drug conjugate (ADC) consisting of a human monoclonal antibody directed against the epidermal growth factor receptor (EGFR) conjugated to the cytotoxic agent maytansinoid mertansine (DM1), with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of AVID100 binds to and inhibits EGFR on tumor cell surfaces. Inhibition of EGFR prevents EGFR-mediated signaling and may inhibit tumor cell proliferation. Following receptor internalization, the mertansine moiety binds to tubulin and interferes with microtubule assembly/disassembly dynamics. This inhibits both cell division and proliferation of cancer cells that express EGFR. EGFR, overexpressed by a variety of cancer s, plays a key role in tumor cell proliferation and survival.


anti-EGFR/HER2/HER3 monoclonal antibody mixture Sym013

An antibody mixture composed of six humanized, immunoglobulin G1 (IgG1) monoclonal antibodies directed against three members of the human epidermal growth factor receptor (EGFR; HER) family: EGFR (HER1; ErbB1), HER2 (ErbB2) and HER3 (ErbB3), with potential antineoplastic activity. Upon administration of anti-EGFR/HER2/HER3 monoclonal antibody mixture Sym013, the six antibodies bind to non-overlapping epitopes on EGFR, HER2 and HER3, which prevents both ligand binding and receptor activation, and induce simultaneous down-modulation of EGFR, HER2 and HER3. This inhibits the activation of HER-dependent signaling pathways and HER-dependent tumor cell proliferation. Overexpression of the HER family plays a key role in many cancer s; targeting multiple HER family members simultaneously may increase therapeutic efficacy.


anti-EGFR/HER3 monoclonal antibody MEHD7945A

An immunoglobulin (Ig) G1 monoclonal antibody directed against both human epidermal growth factor receptor 3 (HER3 or ERBB3) and human epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Anti-EGFR/HER3 monoclonal antibody MEHD7945A binds to both EGFR and HER3 and inhibits their activation. This may prevent EGFR/HER3-mediated signaling and inhibit EGFR/HER3-dependent tumor cell proliferation. In addition, MEHD7945A induces antibody-dependent cell-mediated cytotoxicity (ADCC) against EGR/HER3-expressing tumor cells. EGFR and HER3, members of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, are frequently overexpressed in tumors; their expression is associated with both poor prognosis and drug resistance.


anti-EGFR/PBD antibody-drug conjugate ABBV-321

An antibody drug conjugate (ADC) consisting of ABT-806 AM1, an affinity-matured humanized monoclonal antibody directed against the epidermal growth factor receptor (EGFR), and conjugated to the cytotoxic, DNA minor groove crosslinking agent, pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon intravenous administration of anti-EGFR/PBD ADC ABBV-321, the monoclonal antibody moiety of ABBV-321 targets and binds to EGFR on tumor cell surfaces. Following receptor internalization and lysosome-mediated cleavage, the cytotoxic PBD moiety is released. In turn, the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death and inhibits the proliferation of EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase (RTK) that is overexpressed by a variety of cancer s, plays a key role in tumor cell proliferation and survival.


anti-EGFRvIII antibody drug conjugate AMG 595

An immunoconjugate consisting of a human monoclonal antibody directed against the deletion-mutant of epidermal growth factor receptor, EGFRvIII, conjugated via a non-cleavable linker to the cytotoxic agent maytansinoid DM1, with potential antineoplastic activity. The monoclonal antibody moiety of this immunoconjugate binds to EGFRvIII on tumor cell surfaces. After internalization, the DM1 moiety binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that express the EGFRvIII mutant. EGFRvIII, a deletion mutation of exons 2-7 in the epidermal growth factor receptor gene, is overexpressed by a variety of cancer s, including glioblastoma multiforme, non-small cell lung carcinoma, and breast carcinoma.


anti-EGFRvIII CAR-transduced allogeneic T lymphocytes

Allogeneic human T lymphocytes transduced with a retroviral vector encoding an anti-epidermal growth factor receptor (EGFR) variant III (EGFRvIII) mutant chimeric T-cell receptor (chimeric antigen receptor or CAR) gene coupled to the signaling domains from CD8, CD28, 4-1BB (CD137) and CD3 zeta, with potential immunostimulatory and antineoplastic activities. Upon administration, the anti-EGFRvIII CAR-transduced allogeneic T lymphocytes bind to the EGFRvIII antigen on tumor cell surfaces; subsequently, EGFRvIII-expressing tumor cells may be lysed. EGFRvIII, an in-frame deletion of exons 2-7 in the EGFR gene, is overexpressed by a variety of cancer cell types and absent in normal, healthy cells; it plays a key role in tumor cell proliferation, tumor angiogenesis and radio- and chemoresistance.


anti-EGFRvIII immunotoxin MR1-1

A recombinant immunotoxin consisting of single-chain variable domain fragment antibody directed against the tumor-specific antigen EGFRvIII (MR1scFv) fused to domains II and III of the Pseudomonas exotoxin (PE38KDEL), with potential antineoplastic activity. Upon administration, the antibody moiety of anti-EGFRvIII immunotoxin MR1-1 binds to EGFRvIII; upon internalization, the exotoxin portion inhibits protein synthesis, resulting in a reduction in tumor cell proliferation of EGFRvIII- expressing tumor cells. EGFRvIII, a type III in-frame deletion mutation of the epidermal growth factor receptor (EGFR) gene, is expressed by a variety of cancer s, including glioblastoma multiforme, non-small lung carcinoma, and breast carcinoma. Compared to intact IgG antibodies, single-chain antibodies such as MR1scFv are smaller and may penetrate tumors better. Pseudomonas exotoxin PE38KDEL was modified to remove the natural cell binding domain.


anti-EGFRvIII/CD3 BiTE antibody AMG 596

A proprietary recombinant bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one that is directed against a tumor-associated antigen (TAA), the epidermal growth factor receptor (EGFR) deletion-mutant form, EGFR variant III (EGFRvIII), and one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-EGFRvIII/CD3 BiTE antibody AMG 596, the bispecific antibody binds to both the CD3 antigen on cytotoxic T lymphocytes (CTLs) and EGFRvIII found on EGFRvIII-expressing tumor cells. This activates and crosslinks CTLs with EGFRvIII-expressing tumor cells, which results in the CTL-mediated cell death of EGFRvIII-expressing tumor cells. EGFRvIII, a mutation in the EGFR gene where exons 2-7 have been deleted, is overexpressed by a variety of cancer s, but is absent in normal, healthy cells. It plays a key role in tumor cell proliferation, tumor angiogenesis and resistance to both radio- and chemotherapy.


anti-EGP-2 immunotoxin MOC31-PE

An immunotoxin consisting of a monoclonal antibody directed against epithelial glycoprotein-2 (EP-2, or epithelial cell adhesion molecule (EpCAM)) conjugated to the bacterial toxin Pseudomonas exotoxin A (PE) with potential antineoplastic activity. Upon administration of anti-EGP-2 immunotoxin MOC31-PE, the monoclonal antibody moiety targets and binds to EP-2. Upon internalization, the Pseudomonas exotoxin A moiety then inactivates elongation factor 2 (EF-2) through ADP ribosylation, resulting in inhibition of protein synthesis in EP-2-expressing cells. EP-2, a tumor-associated antigen, is overexpressed in a variety of cancer cell types.


anti-endosialin/TEM1 monoclonal antibody MORAb-004

A humanized IgG1 monoclonal antibody directed against human endosialin/TEM1 (tumor endothelial marker;CD248) with potential anti-angiogenic and antineoplastic activities. Anti-endosialin/TEM1 monoclonal antibody MORAb-004 binds to and inhibits the activity of cell surface protein endosialin/TEM1, which may result in the inhibition of angiogenesis, tumor cell proliferation and metastasis. Endosialin/TEM1 plays a key role in angiogenesis and may be overexpressed on tumor stromal cells and endothelial cells.


anti-ENPP3 antibody-drug conjugate AGS-16C3F

An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody (AGS-16C) directed to the ectonucleotide pyrophosphatase/phosphodiesterase family member 3 (ENPP3), conjugated via a non-cleavable linker to monomethyl auristatin F (MMAF), an auristatin derivative and a potent microtubule inhibitor, that has potential antineoplastic activity. Upon intravenous administration of ADC AGS-16C3F, the monoclonal antibody moiety of this conjugate selectively binds to ENPP3 then is internalized and undergoes proteolytic cleavage to release MMAF. MMAF binds to and inhibits tubulin polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. While normally expressed at low levels in the proximal tubules of the kidney, the type II transmembrane glycoprotein ENPP3 has been found to be overexpressed in renal neoplasms.


anti-Ep-CAM monoclonal antibody ING-1

An engineered monoclonal antibody (MAb) directed against the tumor-associated antigen (TAA) human epithelial cell adhesion molecule (Ep-CAM; EpCAM; CD326), with potential antitumor activity. Upon administration, anti-Ep-CAM monoclonal antibody ING-1 binds to Ep-CAM, which may result in a cytotoxic T-lymphocyte (CTL)-mediated immune response against Ep-CAM-expressing tumor cells. Ep-CAM, a cell surface protein upregulated on many tumor cell types, promotes the proliferation, migration and invasiveness of tumor cells.


anti-EphA2 antibody-directed liposomal docetaxel prodrug MM-310

A formulation containing nanoparticles composed of liposomes that are conjugated to scFv antibody fragments directed against the ephrin receptor A2 (EphA2; Ephrin A2) and a proprietary prodrug of docetaxel, a poorly water-soluble, second-generation taxane analog, with potential antineoplastic activity. Upon intravenous administration of the anti-EphA2 antibody-directed liposomal docetaxel prodrug MM-310, the anti-EphA2 moiety selectively targets and binds to cells expressing EphI3:I12A2. Following accumulation of MM-310, docetaxel is slowly released from MM-310 and accumulates at the tumor site due to the unique characteristics of the tumor vasculature. In turn, docetaxel is taken up by tumor cells, where it binds to and stabilizes the beta-subunit of tubulin, thereby stabilizing microtubules and inhibiting microtubule disassembly. This results in cell cycle arrest and the induction of cell death. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) that are involved in mammalian development, is overexpressed by a variety of cancer cell types and plays an important role in tumor growth; its expression is associated with poor prognosis. Compared to free docetaxel, MM-310 increases docetaxel's half-life, and provides enhanced and specific accumulation in EphA2-expressing tumors, thereby increasing docetaxel's efficacy while lowering its systemic toxicity.


anti-EphA2 monoclonal antibody DS-8895a

A monoclonal antibody directed against the ephrin receptor A2 (EphA2), with potential antineoplastic activity. Upon administration, anti-EphA2 monoclonal antibody DS-8895a selectively binds to cells expressing the EphA2 receptor. This blocks EphA2 activation and EphA2-mediated signaling. In addition, DS-8895a may activate an immune response against EphA2-expressing tumor cells. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) that are involved in mammalian development, is overexpressed by a variety of cancer cell types and plays an important role in tumor growth.


anti-EphA2 monoclonal antibody-MMAF immunoconjugate MEDI-547

An auristatin analogue immunoconjugate directed against Eph receptor A2 (EphA2)-positive cancer cells with potential antineoplastic activity. Anti-EphA2 monoclonal antibody-MMAF immunoconjugate MEDI-547 is generated by conjugating the fully human IgG1 anti-EphA2 monoclonal antibody (1C1) to the small-molecule microtubule inhibitor monomethyl auristatin phenylalanine (MMAF) via the stable linker maleimidocaproyl (mc) (1C1-mcMMAF). The monoclonal antibody moiety of this agent selectively binds to cells expressing the EphA2 receptor. After internalization and enzymatic cleavage of the immunoconjugate within the tumor cell cytosol, free MMAF binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) involved in mammalian development, is overexpressed by a variety of different cancer cell types.


anti-EphA3 monoclonal antibody KB004

A non-fucosylated monoclonal antibody directed against the ephrin receptor A3 (EphA3), with potential antineoplastic activity. Upon administration, anti-EphA3 monoclonal antibody KB004 selectively binds to tumor cells expressing EphA3. This blocks both EphA3 activation and EphA3-mediated signaling, and induces apoptosis in EphA3-expressing tumor cells. In addition, KB004 can stimulate antibody dependent cell-mediated cytotoxicity (ADCC) against EphA3-expressing tumor cells. This agent also prevents tumor cell proliferation by inhibiting both EphA3 signaling and proliferation of endothelial cells in the tumor vasculature. The cell-surface receptor EphA3, a member of the ephrin family of receptor tyrosine kinases (RTKs) that are involved in mammalian development, is overexpressed by a variety of tumor types but is not expressed in normal healthy adult tissues. It plays an important role in tumor cell proliferation. Non-fucosylation of the antibody enhances its ADCC activity.


anti-epidermal growth factor receptor 2 antibody expressing pluripotent killer T lymphocytes

A specific population of pluripotent killer (PIK) T cells that have been induced to express high levels of antibodies against human epidermal growth factor receptor 2 (ERBB2; HER2), with potential antitumor activity. Although the exact mechanism(s) of action through which PIK-HER2 cells exert their effects has yet to be elucidated, upon infusion, these cells secrete antibodies targeting HER2 expressed on the surface of tumor cells. This may inhibit HER2-dependent signaling, which may lead to inhibition of cellular proliferation and differentiation. Additionally, these cells may stimulate the host immune system to mount both a highly-specific cytotoxic T-lymphocyte (CTL) response and antibody-dependent cell cytotoxicity (ADCC) directed against HER2-overexpressing tumors, which leads to tumor cell lysis. HER2 is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases and is frequently overexpressed in solid tumors.


anti-ErbB2/anti-ErbB3 bispecific monoclonal antibody MM-111

A bispecific monoclonal antibody directed against the human epidermal growth factor receptors ErbB2 (Her2) and ErbB3 (Her3) with potential antineoplastic activity. The anti-ErB2 targeting arm of anti-ErbB2/anti-ErbB3 bispecific monoclonal antibody MM-111 binds to ErbB2 on tumor cells with high affinity while the anti-Erb3 therapeutic arm binds to ErbB3, which may result in the inhibition of cellular proliferation and differentiation in ErbB2-overexpressing tumor cells via inhibition of ErbB3-dependent signal transduction pathways. ErbB2 and ErB3 are members of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases and are frequently overexpressed in solid tumors.


anti-ErbB3 monoclonal antibody AV-203

A humanized monoclonal antibody (MoAb) directed against the human receptor tyrosine-protein kinase ErbB-3 (HER3) with potential antineoplastic activity. Anti-ErbB3 MoAb AV-203 binds to and inhibits both ligand neuregulin-1 (NRG-1)-dependent and ligand-independent ErbB3 activation, which may result in inhibition of ErbB3-dependent PI3K/Akt signaling and may lead to inhibition of cellular proliferation and differentiation. ErbB3, a member of the epidermal growth factor receptor (EGFR) family, is frequently overexpressed in solid tumors and its overexpression generally correlates with poor prognosis and tumor resistance; it has no active kinase domain itself but is activated through heterodimerization with other members of the EGFR receptor family that do.


anti-ErbB3 monoclonal antibody CDX-3379

A human monoclonal antibody directed against the human epidermal growth factor receptor ErbB3 (HER3), with potential antineoplastic activity. Upon administration, the anti-ErbB3 monoclonal antibody CDX-3379 targets and binds to a unique epitope on ErbB3, thereby preventing ErbB3 phosphorylation and both ligand-dependent and ligand-independent ErbB3 signaling. This inhibits cellular proliferation and survival of ErbB3-expressing tumor cells. ErbB3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in a variety of tumors and its overexpression generally correlates with poor prognosis and tumor resistance.


anti-ErbB3 monoclonal antibody REGN1400

A human monoclonal antibody directed against the human epidermal growth factor receptor ErbB3 (Her3) with potential antineoplastic activity. Anti-ErbB3 receptor monoclonal antibody REGN1400 binds to ErbB3 and prevents neuregulin 1 ligand binding to ErbB3, which may result in an inhibition of ErbB3-dependent phosphatidylinositol-3 kinase (PI3K)/Akt signaling. This eventually leads to the inhibition of cellular proliferation and differentiation. ErbB3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in a variety of solid tumors and its overexpression generally correlates with poor prognosis and tumor resistance.


anti-ErbB3/anti-IGF-1R bispecific monoclonal antibody MM-141

A bispecific monoclonal antibody directed against the human epidermal growth factor receptor ErbB3 (Her3) and the human insulin-like growth factor-1 receptor (IGF-1R), with potential antineoplastic activity. The anti-IGF-1R targeting arm of anti-IGF-1R/anti-ErbB3 bispecific monoclonal antibody MM-141 binds to IGF-1R on tumor cells thereby preventing the binding of the natural ligands IGF-1, 2 and heregulin (HRG) to IGF-1R; the anti-ErbB3 therapeutic arm prevents the binding of neuregulin (NRG) to ErbB3. This prevents the activation of the PI3K/AKT signal transduction pathway and may result in both the induction of apoptosis and a decrease in cellular proliferation in IGF-1R and ErbB3-overexpressing tumor cells. IGF-1R, a receptor tyrosine kinase of the insulin receptor superfamily, and ErB3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, are frequently overexpressed in solid tumors.


anti-FAP/interleukin-2 fusion protein RO6874281

A recombinant fusion protein comprised of a human monoclonal antibody directed against fibroblast activation protein-alpha (FAP) linked to an engineered, variant form of interleukin-2 (IL-2v), with potential immunostimulating and antineoplastic activities. Upon administration of RO6874281, the monoclonal antibody moiety recognizes and binds to FAP, thereby concentrating IL-2 in FAP-expressing tumor tissue. Subsequently, the IL-2 moiety of this fusion protein may stimulate a local immune response and activate natural killer (NK) cells and cytotoxic T-cells. FAP is a cell surface protein that is expressed on a wide variety of cancer cells. IL-2v cannot bind to IL-2 receptor-alpha (CD25, IL2Ra) and does not activate regulatory T-cells (Tregs).


anti-FCRH5/CD3 BiTE antibody BFCR4350A

A proprietary recombinant bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) Fc receptor-like protein 5 (FCRH5; CD307; FCRL5; IRTA2; BXMAS1) and one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-FCRH5/CD3 BiTE antibody BFCR4350A, the bispecific antibody binds to both the CD3 antigen on cytotoxic T lymphocytes (CTLs) and FCRH5 found on FCRH5-expressing tumor cells. This activates and crosslinks CTLs with FCRH5-expressing tumor cells, which results in the CTL-mediated cell death of FCRH5-expressing tumor cells. FCRH5, an immune receptor translocation-associated protein/Fc receptor homolog (IRTA/FCRH) family member and a B-cell lineage marker, is overexpressed on myeloma cells.


anti-FcRn monoclonal antibody SYNT001

A monoclonal antibody that targets the neonatal crystallizable fragment receptor (FcRn), with potential immunomodulating activity. Upon administration, SYNT001 targets and binds to FcRn at the immunoglobulin G (IgG) binding site, thereby preventing the interaction between FcRn and the serum protein IgG. By preventing FcRn/IgG binding, SYNT001 blocks the FcRn-mediated rescue of IgG, enables IgG degradation and prevents IgG-mediated inflammation. IgG plays a key role in many autoimmune diseases and is an important factor in inflammatory processes.


anti-FGFR2 antibody BAY1179470

An antibody against the fibroblast growth factor receptor type 2 (FGFR2), with potential antineoplastic activity. Upon administration, the anti-FGFR2 antibody BAY1179470 binds to and inhibits FGFR2, which may result in the inhibition of both FGFR2 phosphorylation and FGFR2-mediated signal transduction pathways. This results in the inhibition of cell proliferation and the induction of cell death of FGFR2-expressing tumor cells. FGFR2, upregulated in many tumor cell types, is a receptor tyrosine kinase, which is essential to tumor cellular proliferation, differentiation and survival.


anti-FGFR3 antibody-drug conjugate LY3076226

An antibody-drug conjugate (ADC) composed of a human monoclonal antibody against the fibroblast growth factor receptor type 3 (FGFR3) and conjugated to an as of yet not publicly known cytotoxic agent, with potential antineoplastic activity. Upon administration, the antibody moiety of anti-FGFR3 ADC LY3076226 binds to FGFR3. Upon internalization, the cytotoxic moiety causes cell death in FGFR3-expressing tumor cells. FGFR3, a receptor tyrosine kinase upregulated or mutated in many tumor cell types, plays a key role in tumor cell proliferation.


anti-FGFR3 monoclonal antibody B-701

A human immunoglobulin G1 (IgG1) monoclonal antibody directed against the fibroblast growth factor receptor type 3 (FGFR3), with potential antineoplastic activity. Upon intravenous administration, the anti-FGFR3 monoclonal antibody B-701 specifically binds to and inhibits both wild-type and mutated forms of FGFR3. This may result in the inhibition of FGFR3 phosphorylation, thereby preventing its activation and FGFR3-mediated signal transduction pathways. This results in the inhibition of cell proliferation and the induction of cell death in FGFR3-expressing tumor cells. FGFR3, a receptor tyrosine kinase upregulated or mutated in many tumor cell types, plays a key role in tumor cell proliferation.


anti-FGFR3 monoclonal antibody MFGR1877S

A human monoclonal antibody against the fibroblast growth factor receptor type 3 (FGFR3), with potential antineoplastic activity. Upon administration, the anti-FGFR3 antibody MFGR1877S binds to and inhibits FGFR3, which may result in the inhibition of both FGFR3 phosphorylation and FGFR3-mediated signal transduction pathways. This results in the inhibition of cell proliferation and the induction of cell death in FGFR3-expressing tumor cells. FGFR3, upregulated or mutated in many tumor cell types, is a receptor tyrosine kinase, and plays a key role in tumor cell proliferation.


anti-FGFR4 monoclonal antibody U3-1784

A human monoclonal antibody against human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, U3-1784 specifically binds to and blocks FGFR4. This prevents the activation of FGFR4, inhibits FGFR4-mediated signaling and leads to an inhibition of cell proliferation in FGFR4-overexpressing tumor cells. FGFR4, a receptor tyrosine kinase overexpressed by certain tumor cell types, is involved in tumor cell proliferation, differentiation, angiogenesis, and survival.  


anti-FLT-1 ribozyme

A nuclease-stabilized synthetic ribozyme (ribonucleic acid enzyme) with potential anti-angiogenesis activity. Ribozyme RPI.4610 specifically recognizes the mRNA for FLT1 (vascular endothelial growth factor receptor 1; VEGFR1), and hydrolyzes the mRNA, thereby preventing VEGFR1 proteins from being made. This may prevent VEGF-stimulated angiogenesis in cancer ous tissue and metastasis.


anti-FLT3 monoclonal antibody 4G8-SDIEM

A human, Fc-optimized, immunoglobulin G1 (IgG1) monoclonal antibody directed against the FLT3 tyrosine kinase receptor (CD135), with potential antineoplastic activity. Upon binding to FLT3, anti-FLT3 monoclonal antibody 4G8-SDIEM blocks FLT3 ligand binding to FLT3 and subsequent phosphorylation of FLT3, which may result in the inhibition of FLT3-mediated signal transduction pathways. In addition, this agent may stimulate an anti-FLT3 antibody-dependent cell-mediated cytotoxicity (ADCC) against FLT3-expressing tumor cells, which may lead to the inhibition of cellular proliferation and decreased survival in FLT3-expressing cells. FLT3 (FLK2), a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias.


anti-FLT3 monoclonal antibody IMC-EB10

A fully human, IgG1 monoclonal antibody directed against the FLT3 tyrosine kinase receptor (CD135) with potential antineoplastic activity. Upon binding to FLT3, anti-FLT3 monoclonal antibody IMC-EB10 blocks FLT3 ligand binding to FLT3 and subsequent FLT3 phosphorylation, which may result in the inhibition of FLT3-mediated signal transduction pathways. In addition, this agent may stimulate an anti-FLT3 antibody-dependent cell-mediated cytotoxicity (ADCC) against FLT3-expressing tumor cells, which may result in the inhibition of cellular proliferation and survival in FLT3-expressing cells. FLT3 (FLK2), a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias.


anti-FLT3/CD3 BiTE antibody AMG 427

A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) FLT3 tyrosine kinase receptor (Fms-like tyrosine kinase 3; FLT3; FLT-3; CD135; fetal liver kinase-2; FLK2), fused to one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-FLT3/CD3 BiTE antibody AMG 427, this bispecific antibody binds to both CD3 on cytotoxic T lymphocytes (CTLs) and FLT3 found on FLT3-expressing tumor cells. This activates and redirects CTLs to FLT3-expressing tumor cells, which results in the CTL-mediated cell death of FLT3-expressing tumor cells. FLT3, a cytokine receptor belonging to the class III tyrosine kinase receptors, is overexpressed or mutated in most B-lineage and acute myeloid leukemias (AMLs).


anti-folate receptor-alpha antibody drug conjugate STRO-002

An antibody drug conjugate (ADC) composed of SP8166 (H01), an anti-folate receptor alpha (FolRa; FOLR1) human immunoglobulin G1 (IgG1) antibody, conjugated to a proprietary cleavable drug linker, SC239, containing a tubulin-targeting 3-aminophenyl hemiasterlin warhead, SC209, with potential antineoplastic activity. Upon intravenous administration, the SP8166 antibody moiety targets and binds to FolRa expressed on certain tumor cells. Upon binding, internalization, and enzymatic cleavage, the cytotoxic SC209 moiety induces tumor cell death in FolRa-expressing cells. FolRa is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancer s including serous and epithelial ovarian cancer , endometrial adenocarcinoma, non-small cell lung cancer and triple negative breast cancer . In contrast, FolRa expression is limited in normal tissues.


anti-fucosyl-GM1 monoclonal antibody BMS-986012

A monoclonal antibody directed against the ganglioside fucosyl-GM1, with potential antineoplastic and immunomodulating activities. Upon administration, anti-fucosyl-GM1 monoclonal antibody BMS-986012 binds to fucosyl-GM1 on cancer cells and may activate both antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity against the bound tumor cells. This may inhibit the proliferation of GM1-expressing tumor cells. Fucosyl-GM1, a sphingolipid monosialoganglioside and tumor-associated antigen (TAA), is overexpressed on the surface of many cancer cells while its expression is minimal or non-existent in normal tissues.


antifungal agent F901318

A systemic antifungal agent that can potentially be used in the treatment of systemic fungal infections.


antifungal agent VL-2397

A cyclic hexapeptide and natural compound isolated from the Malaysian leaf litter fungus, Acremonium persicinium MF-347833, with potential antifungal activity against various invasive fungal infections including invasive aspergillosis (IA). Upon administration, VL-2397, by resembling the siderophore ferrichrome, is specifically taken up by fungal cells through the membrane-bound transporter siderophore iron transporter 1 (Sit; Sit1). Upon fungal cell entry, VL-2397 targets and binds to an as of yet undisclosed intracellular site, thereby killing fungal cells. Since mammalian cells lack the Sit1 transporter, VL-2397 is not taken up by human cells.


anti-ganglioside GM2 monoclonal antibody BIW-8962

A humanized anti-ganglioside GM2 (GM2) monoclonal antibody with potential antineoplastic and immunomodulating activities. Upon administration, anti-ganglioside GM2 monoclonal antibody BIW-8962 may activate an antibody dependent cellular cytotoxicity (ADCC) against GM2-expressing tumor cells. GM2 is a tumor associated antigen (TAA) overexpressed on the surface of many cancer cells, such as multiple myeloma (MM) cells and neuroblastoma cells.


anti-GCC antibody-drug conjugate MLN0264

An antibody-drug conjugate (ADC) containing a monoclonal antibody directed against guanylyl cyclase C (GCC or GUCY2C) conjugated to monomethylauristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. The monoclonal antibody moiety of MLN0264 selectively binds to GCC, a transmembrane receptor normally found on intestinal cells and dopamine neurons in the brain, but is also overexpressed on the surface of gastrointestinal cancer s. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis in GCC-expressing tumor cells.


anti-GCC antibody-drug conjugate TAK-164

An antibody-drug conjugate (ADC) comprised of a full-length, fully-human immunoglobulin G1 (IgG1) monoclonal antibody (mAb) directed against the extracellular domain of guanylyl cyclase C (GCC; GUCY2C), conjugated using the peptide-linked indolino-benzodiazepine DNA alkylator DGN549 (IGN-P1), with potential antineoplastic activity. Upon intravenous administration of TAK-164, the antibody moiety selectively binds to GCC-expressing cells. Upon antibody/antigen binding and internalization, the cytotoxic DGN549 payload is released and binds to guanine residues on opposing strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of GCC-expressing cells. GCC, a transmembrane receptor normally found on intestinal cells and dopamine neurons in the brain, is overexpressed on the surface of certain tumor cells.


anti-GD2 monoclonal antibody hu14.18K322A

A monoclonal antibody directed against human glycosphingolipid GD2 with potential antineoplastic activity. Upon binding to the GD2 antigen, anti-GD2 monoclonal antibody hu14.18K322A triggers a host immune response against GD2-expressing tumor cells, which may result in tumor cell death. GD2, an O-acetylated disialoganglioside with expression in normal tissues restricted primarily to the cerebellum and peripheral nerves, is commonly expressed at high levels on tumors of neuroectodermal origins such as melanomas and neuroblastomas.


anti-GD2 monoclonal antibody MORAb-028

A human IgM monoclonal antibody directed against disialoganglioside GD2 with potential immunomodulating activity. Upon administration, anti-GD2 monoclonal antibody MORAb-028 may stimulate the immune system to exert a complement-mediated cytotoxic response against GD2-expressing tumor cells. The glycosphingolipid GD2 is a tumor associated antigen (TAA) overexpressed on the surface of many cancer cells.


anti-GD3 antibody-drug conjugate PF-06688992

An antibody-drug conjugate (ADC) composed of a monoclonal antibody against the ganglioside GD3, a surface antigen expressed on many malignant melanoma cells, and linked to an as of yet not fully elucidated chemotherapeutic agent, with potential antineoplastic activity. Upon administration of the ADC PF-06688992, the antibody moiety targets and binds to GD3 expressed on melanoma cells. Upon internalization, the chemotherapeutic agent specifically kills the GD3-positive cells. GD3 represents a major surface marker on most human melanoma cells and is not expressed on most other types of normal, healthy cells.


antigen-targeted personalized breast cancer vaccine

An individualized, therapeutic cancer vaccine (IVAC) composed of liposomes containing RNA encoding two or three tumor-associated antigens (TAAs) that are specifically expressed in the patient's individual cancer selected from a warehouse (“off the shelf”) and p53 RNA, with potential immunostimulatory and antineoplastic activities. Upon administration, the antigen-targeted personalized breast cancer vaccines are translated by antigen presenting cells (APCs) and the expressed protein is presented via major histocompatibility complex (MHC) molecules on the surface of the APCs. This leads to an induction of both cytotoxic T-lymphocyte (CTL) and memory T-cell immune responses against the TAAs. The RNAs in the vaccine are specifically selected for an individual patient after RNA profiling of the patient’s tumor.


anti-GITR agonistic monoclonal antibody INCAGN01876

An anti-human glucocorticoid-induced tumor necrosis factor receptor (tumor necrosis factor superfamily, member 18; TNFRSF18; GITR; CD357) agonistic humanized monoclonal antibody, with potential immune checkpoint modulating activity. Anti-GITR antibody INCAGN01876 binds to and activates GITRs found on multiple types of T cells. This stimulates the immune system, induces both the activation and proliferation of tumor-antigen-specific T-effector cells (Teffs), and suppresses the function of activated T-regulatory cells (Tregs). This leads to tumor cell eradication. GITR, a member of the TNF receptor superfamily and T-cell receptor co-stimulator, is expressed on the surface of multiple immune cell types, including Tregs, Teffs, B-cells, and natural killer (NK) cells. Inappropriately activated Tregs suppress Teffs and suppress T-cell receptor (TCR) signaling.


anti-GITR agonistic monoclonal MS-986156

An anti-human glucocorticoid-induced tumor necrosis factor receptor (GITR; tumor necrosis factor superfamily member 18; TNFRSF18; CD357) agonistic monoclonal antibody, with potential immune checkpoint modulating activity. Anti-GITR antibody BMS-986156 binds to and activates GITR, which is expressed on the cell surface of multiple types of T cells. This stimulates the immune system, induces both the activation and proliferation of tumor antigen-specific T-effector cells (Teffs), and suppresses the function of activated T-regulatory cells (Tregs). This leads to tumor cell eradication. GITR, a member of the TNF receptor superfamily and T-cell receptor co-stimulator, is expressed on the surface of multiple immune cell types, including Tregs, Teffs, B cells, and natural killer (NK) cells. Inappropriately activated Tregs suppress both Teffs and T-cell receptor (TCR) signaling.


anti-GITR monoclonal antibody GWN 323

An anti-human glucocorticoid-induced tumor necrosis factor receptor (tumor necrosis factor superfamily, member 18; TNFRSF18; GITR; CD357) agonistic monoclonal antibody, with potential immune checkpoint modulating activity. Anti-GITR antibody GWN 323 binds to and activates GITRs found on multiple types of T-cells. This stimulates the immune system, induces both the activation and proliferation of tumor-antigen-specific T effector cells (Teff), and suppresses the function of activated T regulatory cells (Tregs). This leads to tumor cell eradication. GITR, a member of the TNF receptor superfamily and T-cell receptor-co-stimulator, is expressed on the surface of multiple immune cell types, including Tregs, Teffs, B-cells, and natural killer (NK) cells. Inappropriately activated Tregs suppress both Teffs and T-cell receptor (TCR) signaling.


anti-GITR monoclonal antibody MK-4166

An anti-human glucocorticoid-induced tumor necrosis factor receptor (GITR) agonistic monoclonal antibody (MoAb) with potential immunomodulating activity. Anti-GITR monoclonal antibody MK-4166 binds to and activates GITRs found on multiple types of T-cells. This stimulates the immune system and induces both the activation and proliferation of tumor-antigen-specific T effector cells, and suppresses the function of activated T regulatory cells. This leads to tumor cell eradication. Also, this agent is shown to act synergistically with chemotherapeutic drugs in multiple cancer models. GITR, a member of the TNF receptor superfamily, is expressed on the surface of multiple types of immune cells, including regulatory T-cells, effector T-cells, B-cells, and natural killer (NK) cells.


anti-globo H monoclonal antibody OBI-888

A monoclonal antibody targeting the hexasaccharide glycosphingolipid antigen Globo H with potential immunostimulating, anti-angiogenic and antineoplastic activities. Upon infusion, anti-Globo H monoclonal antibody OBI-888 may induce tumor cell destruction via the activation of antibody dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), and complement-dependent cytotoxicity (CDC), and may reduce immunosuppression. Globo H is a tumor-associated antigen (TAA) expressed on the surface of various types of cancer cells.


anti-glypican 3-scFvGC33-CAR-expressing T lymphocytes

A preparation of autologous T lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) containing a single chain variable fragment (scFv) derived from the anti-glypican-3 (GPC3) monoclonal antibody GC33 (scFvGC33), with potential immunostimulating and antineoplastic activities. Upon administration, anti-GPC3-scFvGC33-CAR autologous T lymphocytes specifically target and bind to GPC3-expressing tumor cells, resulting in tumor cell lysis. GPC3, a heparan sulfate proteoglycan and a member of the glypican family, is overexpressed on certain tumor cell types while minimally expressed in normal, healthy cells.. GPC3 plays an important role in cellular proliferation and differentiation.  


anti-GnRH vaccine PEP223

A peptide vaccine derived from the synthetic peptide pyroEHWSYGLRPG, corresponding to amino acids 22-31 of mouse gonadotropin releasing hormone (GnRH), with potential immunocastration activity. PEP223 is dimerized and contains a D-lysine (k) substitution at position 6 (pyroEHWSYkLRPG) to increase its immunogenicity. Anti-GnRH vaccine PEP223 may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against GnRH, neutralizing its activity. In turn, testosterone production and tumor cell growth may be inhibited in testosterone-sensitive tumors.


anti-gpA33/CD3 monoclonal antibody MGD007

An anti-glycoprotein A33 (gpA33)/anti-CD3 bispecific humanized monoclonal antibody with potential immunostimulatory and antineoplastic activities. Anti-gpA33/CD3 monoclonal antibody MGD007 possesses two antigen-recognition sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for gpA33, a tumor-associated antigen (TAA) overexpressed on the surface of certain tumor cells. Upon administration of MGD007, this bispecific antibody simultaneously binds to both CD3-expressing T-cells and gpA33-expressing cancer cells, thereby crosslinking cytotoxic T-lymphocytes (CTLs) to gpA33-expressing tumor cells. This may result in CTL-mediated cell lysis of the crosslinked tumor cells. The gpA33 antigen, a member of the immunoglobulin superfamily, is expressed in certain malignancies, including colon and gastrointestinal cancer s.


anti-GPC3 monoclonal antibody GC33

A humanized monoclonal antibody directed against the cell surface oncofetal protein glypican-3 (GPC3) with potential antineoplastic activity. Anti-GPC3 monoclonal antibody GC33 binds to GPC3 and triggers a host immune response against GPC3-expressing tumor cells, which may result in tumor cell death. GPC3, a heparin sulfate proteoglycan, is frequently upregulated in hepatocellular carcinoma and mesoderm-derived organs such as the liver, lungs, and kidney.


anti-GPC3-CAR autologous T lymphocytes

A preparation of autologous T-lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) specific for glypican-3 (GPC3), with potential immunostimulating and antineoplastic activities. Upon administration, anti-GPC3-CAR autologous T-lymphocytes specifically target and bind to GPC3-expressing tumor cells, resulting in tumor cell lysis. GPC3, a heparan sulfate proteoglycan and a member of the glypican family, is overexpressed on certain tumor cell types while minimally expressed in normal, healthy cells; GPC3 plays an important role in cellular proliferation and differentiation.


anti-GRP78 monoclonal antibody PAT-SM6

A IgM monoclonal antibody (MoAb) against 78-kDa glucose-regulated protein (GRP78; also called BiP or HSPA5), with potential proapoptotic and antineoplastic activities. Upon intravenous administration of the anti-GRP78 monoclonal antibody PAT-SM6, the MoAb strongly binds to GRP78, thereby preventing the activation of multiple GRP78-mediated pathways and blocking the GRP78-induced suppression of apoptotic pathways. This eventually leads to the induction of tumor cell apoptosis and a reduction in tumor cell proliferation. GRP78, the endoplasmic reticulum (ER) chaperone and unfolded protein response (UPR) regulator, is overexpressed on the surface of a variety of cancer cell types; its expression is associated with increased tumor cell survival and proliferation, as well as angiogenesis and resistance to chemotherapy.


anti-HA epitope monoclonal antibody MEDI8852

A human immunoglobulin (Ig) G1 kappa monoclonal antibody (mAb) targeting a unique epitope in the stalk of the influenza A hemagglutinin (HA) protein, with broad influenza A virus neutralization activity. MEDI8852 was derived from an antibody isolated from human memory B cells from patients previously infected with influenza caused by type A strains that was further optimized to increase neutralization potential. Upon infusion, MEDI8852 targets and binds to a region within the stalk of the HA protein that is highly conserved amongst all influenza A virus subtypes. This neutralizes and prevents essential steps of the viral lifecycle, thereby blocking infectivity of all influenza A virus subtypes. HA, a glycoprotein found on the surface of the influenza virus, plays a key role in viral attachment and cell entry.


anti-HB-EGF monoclonal antibody KHK2866

A proprietary fucose-free monoclonal antibody directed against human heparin-binding EGF-like growth factor (HBEGF) with potential antineoplastic activity. Anti-HB-EGF monoclonal antibody KHK2866 binds to HBEGF, thereby blocking its binding to the EGF receptors. This prevents EGF receptor activation and the subsequent induction of cell growth signaling. HBEGF is mitogenic for fibroblasts and smooth muscle and may be involved in macrophage-mediated cellular proliferation. The fucose-free monoclonal antibodies enhance antigen dependent cellular cytotoxicity (ADCC), and increase binding affinity to the Fc receptor to overcome genetic polymorphism.


anti-HBEGF monoclonal antibody U3-1565

A humanized monoclonal antibody directed against human heparin-binding EGF-like growth factor (HBEGF) with potential antineoplastic activity. Anti-HBEGF monoclonal antibody U3-1565 binds to HBEGF and blocks the binding of HBEGF to the EGF receptors. This prevents EGF receptor activation and the subsequent induction of cell growth signaling. HBEGF is mitogenic for fibroblasts and smooth muscle and may be involved in macrophage-mediated cellular proliferation.


anti-hCD70-CAR retroviral vector-transduced autologous PBLs

A preparation of autologous human peripheral blood lymphocytes (PBLs) transduced with a retroviral vector encoding for a T-cell chimeric antigen receptor (CAR) gene specific for the human cluster of differentiation 70 (CD70), with potential immunostimulatory and antineoplastic activities. Autologous PBLs from a patient with CD70-positive cancer are transduced with a retroviral vector that encodes the CAR gene specific for CD70. After expansion in culture and reintroduction into the patient, anti-hCD70-CAR retroviral vector-transduced autologous PBLs bind to the CD70 antigen on tumor cell surfaces; subsequently, CD70-expressing tumor cells are lysed. CD70, the ligand for the costimulatory receptor CD27, is overexpressed on the surfaces of various cancer cell types.


anti-HCV E2 monoclonal antibody MBL-HCV1

A neutralizing, human monoclonal antibody against the hepatitis C virus (HCV) E2 envelope glycoprotein, with potential immunomodulatory and antiviral activities against HCV. Upon administration, anti-HCV E2 monoclonal antibody MBL-HCV1 recognizes and binds to the E2 glycoprotein of HCV. This suppresses HCV load and provides passive immunization against HCV. This may prevent both infection by HCV in immunocompromised patients and hepatitis C-related liver disease. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family.


antihemophilic factor, human recombinant

The recombinant form of human antihemophilic factor (AH) (Factor VIII) with coagulation promoting activity. Antihemophilic factor binds to factor IXa in the coagulation cascade along with calcium and phospholipid. This complex converts factor X to the activated form, factor Xa. In turn, factor Xa/Va complex activates thrombin, which cleaves fibrinogen into fibrin, eventually resulting in blood clot formation.  


anti-HER2 ADC DS-8201a

An antibody-drug conjugate (ADC) composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2; EGFR2; HER2) conjugated to a derivative of the camptothecin analog exatecan (DXd; DX-8951 derivative), a DNA topoisomerase 1 (topoisomerase I; Top1) inhibitor, with potential antineoplastic activity. Upon administration of anti-HER2 ADC conjugate DS-8201a, the antibody moiety targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, the DX-8951 derivative moiety binds to and inhibits Top1-DNA complexes, which results in an inhibition of DNA replication, cell cycle arrest and tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. In addition, DS-8201a induces antibody-dependent cell-mediated cytotoxicity (ADCC) and causes a bystander killing effect, thereby killing neighboring HER2-expressing tumor cells.


anti-HER2 antibody-drug conjugate A166

An antibody-drug conjugate (ADC) composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) and conjugated to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon administration of anti-HER2 ADC A166, the antibody moiety targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, the cytotoxic agent induces tumor cell apoptosis, through an as of yet not publicly known mechanism. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.


anti-HER2 antibody-drug conjugate ARX788

An antibody-drug conjugate (ADC) composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2) site-specifically conjugated, via the non-natural amino acid linker para-acetyl-phenylalanine (pAcF), to the auristatin analog and potent microtubule inhibitor monomethyl auristatin F (MMAF), with potential antineoplastic activity. Upon administration of anti-HER2 ADC ARX788, the antibody moiety targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, MMAF binds to and inhibits tubulin polymerization, which results in G2/M phase arrest and tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. The site-specific conjugation of the cytotoxic agent to the antibody improves the biophysical properties of ARX788, increases payload stability and optimizes its efficacy.


anti-HER2 antibody-drug conjugate MEDI4276

An antibody-drug conjugate (ADC) composed of a bispecific antibody against the extracellular domain of human epidermal growth factor receptor 2 (HER2; ERBB2) comprised of the single-chain variable fragment (scFv) of the anti-HER2 monoclonal antibody trastuzumab, which binds to domain IV of HER2, fused to the heavy chains of the anti-HER2 monoclonal antibody 39S, which binds to domain II of HER2, and conjugated, via a cleavable linker, to the cytotoxic anti-microtubule agent tubulysin, with potential antineoplastic activity. Upon administration of MEDI4276, the anti-HER2 bispecific antibody specifically targets and binds to HER2 on the surface of certain cancer cells. Upon binding, crosslinking and internalization of antibody-HER2 complexes occurs and MEDI4276 is transported to the lysosome where the linker is cleaved, thereby delivering tubulysin inside HER2-expressing cancer cells. Tubulysin binds to tubulin and inhibits microtubule polymerization, which blocks cell division. This results in G2/M phase arrest, tumor cell apoptosis, and decreased proliferation of HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.


anti-HER2 antibody-drug conjugate RC48

An antibody-drug conjugate (ADC) composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2) and conjugated to an as-of-yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon administration of anti-HER2 ADC RC48, the antibody moiety targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, the cytotoxic agent induces tumor cell apoptosis, through an as of yet not publicly known mechanism. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.


anti-HER2 bi-specific monoclonal antibody ZW25

An engineered bi-specific monoclonal antibody that targets two different epitopes of the human tumor-associated antigen (TAA) epidermal growth factor receptor 2 (HER2) with potential immunomodulating and antineoplastic activities. After binding to HER2 on the tumor cell surface, anti-HER2 bispecific monoclonal antibody ZW25 induces a cytotoxic T-lymphocyte (CTL) response and antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. Antibody-dependent cellular phagocytosis (ADCP) is also induced and further stimulates the immune system to kill HER2-overexpressing tumor cells. In addition, binding of ZW25 to HER2 induces receptor internalization, which inhibits HER2 activation, HER2-mediated signaling and HER2-mediated tumor cell growth. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.


anti-HER2 monoclonal antibody CT-P6

A monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2) with potential immunomodulating and antineoplastic activity. After binding to HER2 on the tumor cell surface, anti-HER2 monoclonal antibody CT-P6 may induce a cytotoxic T-lymphocyte (CTL) as well as an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.


anti-HER2 monoclonal antibody/anti-CD137 anticalin bispecific fusion protein PRS-343

A bivalent, bispecific fusion protein comprised of an anti-human epidermal growth factor receptor (HER2) monoclonal antibody linked to a CD137-targeting anticalin with potential immunostimulatory and antineoplastic activities. Upon administration of anti-HER2 monoclonal antibody/anti-CD137 anticalin bispecific fusion protein PRS-343, CD137 clustering is promoted by bridging CD137-positive T cells with HER2-positive tumor cells, leading to the recruitment of tumor antigen-specific cytotoxic T lymphocytes (CTLs). This may result in potent CTL-mediated lysis of HER2-expressing tumor cells. HER2 plays a key role in tumor cell proliferation and tumor vascularization. CD137 is a costimulatory immunoreceptor and a member of the tumor necrosis factor receptor superfamily (TNFRSF). Anticalins are synthetic antigen-binding proteins derived from lipocalins. Structurally dissimilar to antibodies, anticalins are able to bind to smaller antigens and exhibit improved tissue penetration.


anti-HER2/Anti-CD3 bispecific monoclonal antibody BTRC 4017A

An anti-human epidermal growth factor receptor 2 (HER2)/anti-CD3 T-cell-dependent bispecific (TDB) monoclonal antibody with potential immunostimulatory and antineoplastic activities. Upon administration, anti-HER2/anti-CD3 bispecific monoclonal antibody BTRC4017A possesses two antigen recognition sites, one for HER2, a tyrosine kinase receptor overexpressed by many cancer cell types, and one for the CD3 complex, a group of T-cell surface glycoproteins that interact with the T-cell receptor (TCR). Upon administration of BTRC4017A, this bispecific monoclonal antibody simultaneously binds to both CD3-expressing T cells and HER2-expressing cancer cells, thereby crosslinking HER2-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This may result in potent CTL-mediated lysis of HER2-expressing tumor cells. HER2 plays a key role in tumor cell proliferation and tumor vascularization.


Anti-HER2/Anti-CD3 Bispecific monoclonal antibody GBR 1302

An anti-human epidermal growth factor receptor 2 (HER2)/anti-CD3 bispecific monoclonal antibody with potential immunostimulatory and antineoplastic activities. Anti-HER2/Anti-CD3 bispecific monoclonal antibody GBR 1302 possesses two antigen recognition sites, one for HER2, a tyrosine kinase receptor overexpressed by many cancer cell types, and one for the CD3 complex, a group of T-cell surface glycoproteins that interact with the T-cell receptor (TCR). Upon administration of GBR 1302, this bispecific monoclonal antibody simultaneously binds to both CD3-expressing T cells and HER2-expressing cancer cells, thereby crosslinking HER2-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This may result in potent CTL-mediated lysis of HER2-expressing tumor cells. HER2 plays a key role in tumor cell proliferation and tumor vascularization.


anti-HER2/Anti-HER3 bispecific monoclonal antibody MCLA-128

A full-length IgG1 bispecific antibody with enhanced antibody-dependent cellular cytotoxicity (ADCC) directed against human epidermal growth factor receptor 2 (HER2; EGFR2, ERBB2) and human epidermal growth factor receptor 3 (HER3; ErbB3), with potential antineoplastic activity. Upon intravenous administration, the bispecific antibody docks on HER2, and subsequently blocks heregulin-stimulated proliferation of tumor cells by binding HER3. In addition to inhibiting HER3-dependent signaling, simultaneous targeting of HER2 and HER3 by MCLA-128 may overcome a common resistance mechanism driven by heregulin-mediated dimerization of HER2 and HER3. MCLA-128 is expected to eliminate tumor cells by recruiting natural killer (NK) cells to tumor cells coated with the bispecific antibody.


anti-HER2/auristatin payload antibody-drug conjugate XMT-1522

An antibody-drug conjugate (ADC) composed of HT-19, a monoclonal antibody directed against the human epidermal growth factor receptor 2 (ERBB2; HER2), conjugated, via a proprietary biodegradable, hydrophilic polymer backbone and various linkers, to proprietary auristatin-derived payload molecules (about 15 per antibody), with potential antineoplastic activity. Upon administration of anti-HER2/auristatin payload ADC XMT-1522, the antibody moiety targets and binds to a unique epitope in the extracellular domain (ECD) of HER2. Upon internalization, cleavage and release of the cytotoxic molecules, the auristatin-derived molecules bind to tubulin and inhibit its polymerization, which results in G2/M phase arrest and induces apoptosis of HER2-expressing tumor cells. The attachment of multiple auristatin molecules to the backbone enables XMT-1522 to effectively kill tumors that express relatively low amounts of the HER2 protein; therefore, this agent shows increased therapeutic potential in tumors with low HER2 expression compared to other anti-HER2 antibody-based therapies. The polymer-based proprietary platform optimizes delivery of the cytotoxic drug payload and improves drug solubility.


anti-HER2/PBD-MA antibody-drug conjugate DHES0815A

An antibody-drug conjugate (ADC) consisting of a monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2; EGFR2; HER2) linked to a DNA minor groove crosslinking agent pyrrolo[2,1- c][1,4]benzodiazepine monoamide (PBD-MA), with potential antineoplastic activity. Upon intravenous administration of ADC DHES0815A, the monoclonal antibody moiety targets and binds to HER2 expressed on tumor cells. Following receptor internalization and lysosome-mediated cleavage, the cytotoxic PBD-MA moiety is released. In turn, the imine groups of the PBD-MA moiety bind to and crosslink specific sites of DNA, resulting in DNA strand breaks, cell cycle arrest, and cell death in HER2 expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.


anti-HER2-CAR autologous CMV-specific cytotoxic T lymphocytes

Autologous human cytomegalovirus (CMV)-specific human cytotoxic T lymphocytes (CTLs) transduced with a retroviral vector encoding a human anti-HER2 (epidermal growth factor receptor 2) chimeric T cell receptor (CAR) gene with potential immunostimulatory and antineoplastic activities. Autologous CTLs from a patient with HER2- and CMV-positive glioblastoma multiforme (GBM) are genetically modified to express CAR gene specific for HER2 on their cell surfaces. After expansion in culture and reintroduction into the patient, the anti-HER2-CAR autologous CMV-specific CTLs bind to HER2 antigen on tumor cell surfaces; subsequently, HER2-positive tumor cells and stem cells may be lysed. HER2 (ErbB2), a receptor tyrosine kinase (RTK) overexpressed by a variety of cancer cell types, plays key roles in tumor cell proliferation and tumor angiogenesis. CMV is present in the majority of GBM tumors.


anti-Her-2-CAR retroviral vector-transduced autologous peripheral blood lymphocytes

Autologous human peripheral blood lymphocytes (PBLs) transduced with a retroviral vector encoding an anti-Her-2 (epidermal growth factor receptor 2) chimeric T cell receptor (chimeric antigen receptor or CAR) gene with potential immunostimulatory and antineoplastic activities. Autologous PBLs from a patient with Her-2-positive cancer are pulsed with a retroviral vector that encodes the CAR gene specific for Her-2. After expansion in culture and reintroduction into the patient, anti-Her-2-CAR retroviral vector-transduced autologous peripheral blood lymphocytes, expressing anti-Her-2-CAR on their cell surfaces, bind to Her-2 antigen on tumor cell surfaces; subsequently, Her-2-expressing tumor cells may be lysed. Her-2 (ErbB-2), a receptor tyrosine kinase (RTK) overexpressed by a variety of cancer cell types, belongs to the EGFR superfamily and plays key roles in tumor cell proliferation and tumor angiogenesis.


anti-HER2-vc0101 ADC PF-06804103

A proprietary antibody-drug conjugate (ADC) composed of a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) site-specifically linked, via a protease cleavable linker, to an analog of dolastatin 10, Auristatin-0101, with potential antineoplastic activity. Upon administration, anti-HER2-vc0101 ADC PF-06804103 targets HER2 expressed on tumor cells. Upon binding, internalization and cleavage, Auristatin-0101 binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and apoptosis of HER2-expressing tumor cells. HER2, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer cells.


anti-HER3 antibody-drug conjugate U3 1402

An antibody-drug conjugate (ADC) composed of patritumab, a monoclonal antibody directed against the human epidermal growth factor receptor HER3 (ErbB3),linked to the topoisomerase I inhibitor DX 8951, a semisynthetic, water-soluble derivative of camptothecin, with potential antineoplastic activity. Upon administration of the anti-HER3 ADC U3 1402, the patritumab moiety targets and binds to HER3. After internalization, DX 8951 inhibits topoisomerase I activity by stabilizing the complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors.


anti-HER3 monoclonal antibody GSK2849330

A monoclonal antibody directed against the human epidermal growth factor receptor 3 (HER3; ERBB3) with potential antineoplastic activity. Anti-HER3 monoclonal antibody GSK2849330 binds to HER3 and inhibits its activation. This may prevent HER3-mediated signaling and inhibit HER3-dependent tumor cell proliferation and differentiation. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors and is associated with poor prognosis and drug resistance; it has no active kinase domain but is activated through heterodimerization with other members of the EGFR receptor family, such as HER2.


anti-HER3 monoclonal antibody LJM716

A human monoclonal antibody directed against the human epidermal growth factor receptor HER3 (ErbB3) with potential antineoplastic activity. Anti-HER3 monoclonal antibody LJM716 possesses a novel mechanism of action; LJM716 binds to and locks HER3 in the inactive conformation and does not interfere with its interaction with neuregulin (NRG). The inactivated form of HER3 blocks the PI3K/Akt signaling pathway, thereby inhibiting cellular proliferation in HER2 or NRG expressing tumor cells. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors; it has no active kinase domain but is activated through heterodimerization with other members of the EGFR receptor family, such as HER2.


anti-HGF monoclonal antibody TAK-701

A humanized monoclonal antibody directed against human hepatocyte growth factor (HGF) with potential antineoplastic activity. Anti-HGF monoclonal antibody TAK-701 binds to the soluble ligand HGF, preventing HGF binding to and activation of the HGF receptor c-Met and so the activation of the c-Met signaling pathway; this may result in the induction of cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in a variety of tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.


anti-HIF-1alpha LNA antisense oligonucleotide EZN-2968

A synthetic antisense oligodeoxynucleotide (AS ODN) targeting hypoxia-inducible factor-1alpha (HIF-1alpha) with potential antineoplastic activity. Anti-HIF-1alpha LNA antisense oligonucleotide EZN-2968 hybridizes with HIF-1alpha mRNA and blocks t HIF-1 alpha protein expression, which may result in the inhibition of angiogenesis, the inhibition of tumor cell proliferation, and apoptosis. HIF-1alpha, normally activated in response to hypoxia-induced stress, is a key transcription regulator of a large number of genes important in cellular adaptation to low-oxygen conditions, including angiogenesis, cell proliferation, apoptosis, and cell invasion.


anti-HLA-A2/NY-ESO-1 TCR-transduced autologous T lymphocytes

Autologous human peripheral blood T lymphocytes transduced with a lentiviral or retroviral vector encoding a human leukocyte antigen A2 (HLA-A2)-restricted anti- cancer -testis antigen 1 (NY-ESO-1) T-cell receptor (TCR) gene, with potential antineoplastic activity. Following leukapheresis, isolation of lymphocytes, expansion ex vivo, transduction, and re-introduction into the patient, the anti-HLA-A2/NY-ESO-1 TCR-transduced autologous T lymphocytes recognize and bind to NY-ESO-1/HLA-A2-positive tumor cells. This results in cytotoxic T-lymphocyte (CTL)-mediated elimination of NY-ESO-1-positive cancer cells. NY-ESO-1, a tumor-associated antigen (TAA), is found in normal testis and on the surface of various tumor cell types.


anti-HLA-DR monoclonal antibody IMMU-114

A humanized IgG4 monoclonal antibody that targets the human leukocyte antigen HLA-DR, with potential antineoplastic activity. Upon administration, anti-HLA-DR monoclonal antibody IMMU-114 binds to HLA-DR on HLA-DR-expressing tumor cells and, although the exact mechanism has yet to be fully elucidated, appears to induce hyperactivation of ERK- and JNK-dependent mitogen activated protein kinase signaling pathways. This may lead to mitochondrial membrane depolarization and reactive oxygen species (ROS) generation. This eventually leads to an induction of tumor cell apoptosis and a reduction in tumor cell proliferation. IMMU-14 may be beneficial in the treatment of graft versus host disease (GVHD) as it appears to suppress T-lymphocyte proliferation and natural killer (NK) cell activation. As the Fc region of the orgnial IgG1 MoAb was replaced with the IgG4 isotype, IMMU-114 does not induce a complement cytotoxicity (CDC) or an antibody-dependent cell-mediated cytotoxicity (ADCC) . HLA-DR, a MHC class II molecule, is found on various B-cell hematologic malignancies and in autoimmune diseases as well as on normal cells.


anti-human chorionic gonadotropin vaccine

A peptide vaccine consisting of the whole or partial beta subunit of human chorionic gonadotrophin hormone (hCG), linked to an adjuvant carrier of bacterial or viral origin, with anti-fertility activity. Anti-human chorionic gonadotropin vaccine blocks the activity of hCG which is naturally produced by the trophectoderm of the pre-implantation embryo within a few days of fertilization. hCG is required for the maintenance of the corpus luteum in the ovary thus ensuring its continued production of progesterone, which is required for the successful completion of implantation of the blastocyst. Without progesterone, the corpus luteum regresses, and menstruation is initiated.


anti-human GITR monoclonal antibody TRX518

A humanized, Fc disabled anti-human glucocorticoid-induced tumor necrosis factor receptor (GITR) monoclonal antibody (MoAb) with immunomodulating activity. Anti-human GITR MoAb TRX518 blocks the interaction of GITR, found on multiple types of T cells, with its ligand, thereby inducing both the activation of tumor-antigen-specific T effector cells, as well as abrogating the suppression induced by inappropriately activated T regulatory cells. This agent is shown to act synergistically with chemotherapeutic drugs in multiple cancer models.


anti-human integrin alpha v subunit monoclonal antibody EMD 525797

A humanized monoclonal antibody directed against the human alpha v integrin subunit with potential antiangiogenic and antineoplastic activities. Anti-human integrin alpha v subunit monoclonal antibody EMD 525797, a chimeric antibody which includes the antigen binding sites of the anti-integrin mouse antibody 17E6, binds to and inhibits the activity of alphavbeta3 integrin (vitronectin receptor); this may result in the inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, and integrin-mediated tumor angiogenesis and metastasis in alphavbeta3-expressing tumor cells. Alphavbeta3 integrin, a cell adhesion and signaling receptor, is expressed on the surface of tumor vessel endothelial cells and plays a crucial role in endothelial cell adhesion and migration.


anti-ICAM-1 monoclonal antibody BI-505

A fully human IgG1 monoclonal antibody directed against intercellular adhesion molecule-1 (ICAM-1 or CD54), with potential antineoplastic activity. Anti-ICAM-1 monoclonal antibody BI-505 selectively binds to the adhesion protein ICAM-1, which may result in antibody-dependent cellular cytotoxicity (ADCC), hyper-cross-linking-induced apoptosis, and a decrease in cellular proliferation of ICAM-1-expressing tumor cells. ICAM-1, normally expressed on leukocytes and endothelial cells, may be overexpressed in a variety of cancer s.


anti-ICOS agonist antibody GSK3359609

An agonistic antibody for the inducible T-cell co-stimulator (ICOS; CD278), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-ICOS agonist antibody GSK3359609 targets and binds to ICOS expressed on tumor infiltrating CD4-positive T cells. This stimulates ICOS-positive T-cell proliferation, enhances cytotoxic T-lymphocyte (CTL) survival and increases CTL-mediated immune responses against tumor cells. ICOS, a T-cell specific, CD28-superfamily costimulatory molecule and immune checkpoint protein, is normally expressed on certain activated T cells and plays a key role in the proliferation and activation of T cells.


anti-ICOS agonist monoclonal antibody BMS-986226

An agonistic monoclonal antibody that recognizes inducible T-cell co-stimulator (ICOS; CD278), with potential immunomodulating and antineoplastic activities. Upon administration, anti-ICOS agonist monoclonal antibody BMS-986226 targets and binds to ICOS expressed on certain T cells. This stimulates ICOS-mediated signaling, induces proliferation of ICOS-positive T cells, enhances cytotoxic T lymphocyte (CTL) survival and augments the CTL-mediated immune response against tumor cells. ICOS, a T-cell-specific, CD28-superfamily co-stimulatory molecule and immune checkpoint protein, is normally expressed on certain activated T cells and plays a key role in the proliferation and activation of T cells.


anti-ICOS agonist monoclonal antibody JTX-2011

An agonistic humanized monoclonal antibody that recognizes inducible T-cell co-stimulator (ICOS; CD278), with potential antineoplastic activity. Upon administration, anti-ICOS agonist monoclonal antibody JTX-2011 targets and binds to ICOS expressed on certain T cells. This stimulates ICOS-mediated signaling, induces proliferation of ICOS-positive T cells, enhances cytotoxic T-lymphocyte (CTL) survival and augments the CTL-mediated immune response against tumor cells. ICOS, a T-cell specific, CD28-superfamily co-stimulatory molecule and immune checkpoint protein, is normally expressed on certain activated T cells and plays a key role in the proliferation and activation of T cells.


anti-ICOS monoclonal antibody MEDI-570

An Fc-optimized humanized immunoglobulin (Ig) G1 monoclonal antibody (MoAb) directed against the inducible T-cell co-stimulator (ICOS, CD278), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-ICOS MoAb MEDI-570 targets and binds to ICOS expressed on tumor infiltrating CD4-positive T-cells. This prevents the interaction between ICOS-positive T-cells and plasmacytoid dendritic cells (pDCs), which express the ICOS ligand (ICOSL). Blocking ICOS activation prevents the pDC-induced proliferation and accumulation of regulatory ICOS-positive T-cells (ICOS+ Tregs) and inhibits interleukin-10 (IL-10) secretion by CD4+ infiltrating T-cells. This may abrogate Treg-mediated immune suppression and may enhance cytotoxic T-lymphocyte (CTL)-mediated immune responses against tumor cells. Fc optimization enhances antibody-dependent cellular cytotoxicity (ADCC). ICOS, a T-cell specific, CD28-superfamily costimulatory molecule and immune checkpoint protein, plays a key role in the proliferation and activation of T-cells. It is normally expressed on both activated CD4+ T-cells, which is a subset of memory T-cells (Tm), and follicular helper T-cells (Tfh). ICOS is highly expressed on Tregs infiltrating various tumors and its expression is associated with a poor prognosis; ICOS-positive Tregs play a key role in immune suppression and tumor immune evasion.


anti-IGF1/2 monoclonal antibody MEDI-573

A humanized monoclonal antibody directed against insulin-like growth factors 1 and 2 (IGF-1/2) with potential antineoplastic activity. Anti-IGF1/2 monoclonal antibody MEDI-573 inhibits IGF1- and IGF2-stimulated activation of membrane-bound IGF receptors and the subsequent triggering of proliferation and survival signaling pathways. This may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF1/2 ligands stimulate cell proliferation, enable oncogenic transformation, and suppress apoptosis; IGF1/2 signaling has been highly implicated in tumorigenesis and metastasis.


anti-IGF-1R monoclonal antibody AVE1642

A humanized monoclonal antibody directed against the human insulin-like growth factor-1 receptor (IGF-1R/CD221) with potential antineoplastic activity. Anti-IGF-1R monoclonal antibody AVE1642 specifically binds to and blocks membrane-bound IGF-1R, preventing the binding of the natural ligand IGF-1 and the subsequent activation of PI3K/AKT signal transduction, which may result in the induction of apoptosis and a decrease in cellular proliferation. Activation of IGF-1R , a receptor tyrosine kinase of the insulin receptor superfamily overexpressed by various cancer cell types, stimulates cell proliferation, promotes angiogenesis, enables oncogenic transformation, and suppresses apoptosis.


anti-IGF-1R recombinant monoclonal antibody BIIB022

A recombinant, human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Anti-IGF-1R recombinant monoclonal antibody BIIB022 binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; inhibition of this survival signaling pathway may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. The activation of IGF-1R, a tyrosine kinase and a member of the insulin receptor family, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis.


anti-IL-1 alpha monoclonal antibody CA-18C3

A "true human" (cloned from human B lymphocytes) monoclonal antibody directed against interleukin-1 alpha (IL1a) with potential antineoplastic activity. Anti-IL-1 alpha monoclonal antibody CA-18C3 binds to IL1a and may block the activity of IL1a. IL1a, an inflammatory mediator, plays a key role in interleukin-mediated tumor cell activity such as angiogenesis, tissue matrix remodeling, metastasis and tumor cell invasion.


anti-IL-13 humanized monoclonal antibody TNX-650

A humanized monoclonal antibody directed against interleukin-13 (IL-13) with potential antineoplastic activity. Anti-IL-13 humanized monoclonal antibody TNX-650 binds to and blocks the activity of IL-13, which may result in the inhibition of Hodkin lympoma cell proliferation. IL-13 cytokine, an important mediator in allergic inflammation, may be an autocrine growth factor for Hodgkin lymphoma cells.  


anti-IL-15 monoclonal antibody AMG 714

A human immunoglobulin G1 (IgG1) monoclonal antibody directed against the human pro-inflammatory cytokine interleukin-15 (IL-15), with potential anti-inflammatory, immunomodulating and antineoplastic activities. Upon administration, anti-IL-15 monoclonal antibody AMG 714 binds to and neutralizes IL-15, thereby preventing IL-15-mediated pro-inflammatory signaling. By inhibiting IL-15-mediated immune responses, AMG 714 decreases natural killer (NK) cell activation and proliferation, reduces T-cell infiltration, increases T-cell apoptosis, and may prevent the growth of IL-15-driven cancer cells. IL-15 plays a key role in inflammation and is associated with a variety of autoimmune and inflammatory disorders as well as with cell proliferation in certain cancer types, such as T-cell lymphomas. IL-15 is required for the proliferation of certain T-cells and NK cells.


anti-IL17A monoclonal antibody CJM112

A human immunoglobulin G1 (IgG1) monoclonal antibody against the pro-inflammatory cytokine interleukin 17A (IL-17A; IL-17), with potential anti-inflammatory activity. Upon subcutaneous administration, anti-IL17A monoclonal antibody CJM112 selectively targets and binds to IL-17A, thereby neutralizing the IL-17A protein. This prevents binding of IL-17A to the IL-17 receptor (IL-17R), and inhibits IL-17A/IL-17R-mediated signaling and inflammation mediated by this pathway. IL-17A is mainly produced by inflammatory T helper 17 cells (Th17), and certain lymphocytes. IL-17A production is upregulated in many immune-mediated inflammatory diseases, such as psoriasis and multiple sclerosis (MS), and plays a key role in the development of inflammation and the immune response.


anti-IL-4/IL-13 combination agent QBX258

A combination agent composed of the two human monoclonal antibodies VAK694 (VAK296), targeting interleukin-4 (IL-4), and dectrekumab, targeting IL-13, that can potentially be used to block signaling mediated by IL-4 and IL-13. Upon intravenous administration of the anti-IL-4/IL-13 combination agent QBX258, the two antibodies VAK694 and dectrekumab target and block the activity of the two cytokines IL-4 and IL-13, respectively, which prevents IL-4/IL-13-mediated signaling. In patients with breast cancer related lymphedema (BCRL), this agent may prevent lymphedema-associated effects, such as fibrosis, hyperkeratosis, the deposition of fibroadipose tissue, fluid accumulation, limb swelling, reduction of skin elasticity, and pain. By reducing the excess volume, QBX258 may improve lymphatic and arm functions. The development of lymphedema after lymphatic injury is associated with tissue inflammation, the infiltration of CD4-positive cells and their differentiation to the type 2 helper T-cell (Th2) phenotype. Th2 cells produce IL-4 and IL-13 that play a key role in the development of lymphedema-associated symptoms as well as other Th2-mediated diseases.


anti-IL-8 monoclonal antibody HuMax-IL8

A human monoclonal antibody against the pro-inflammatory mediator interleukin-8 (IL-8; CXCL8), with potential antineoplastic activities. Upon administration, HuMax-IL8 directly binds to IL-8, thereby inhibiting the binding of IL-8 to its receptors CXCR1 and CXCR2. This inhibits activation of IL-8-mediated signaling transduction pathways, which decreases proliferation of susceptible tumor cells. Also, HuMax-IL8 effectively blocks binding of IL-8 to neutrophils and inhibits neutrophil activation and recruitment towards sites of inflammation, which reduces inflammation. IL-8, a member of the CXC chemokine family, is upregulated in a variety of cancer cell types and inflammatory diseases; it plays a key role in tumor cell proliferation, endothelial cell proliferation, and cancer stem cell (CSC) renewal.


anti-ILDR2 monoclonal antibody BAY 1905254

A mouse/human cross-reactive immunoglobulin G2 (IgG2) monoclonal antibody against the immune checkpoint immunoglobulin-like domain containing receptor 2 (ILDR2; Chromosome 1 Open Reading Frame 32; C1orf32), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, BAY 1905254 targets, binds to and inhibits ILDR2, thereby blocking the immunosuppressive activity of ILDR2. This prevents ILDR2-mediated inhibition of T-cell activities and induces a cytotoxic T-lymphocyte (CTL) response against tumor cells. ILDR2, a type I transmembrane protein belonging to the B7 family of immunomodulatory receptors, negatively regulates T-cell responses.


anti-inflammatory antibody ALXN1007

A proprietary antibody that targets the complement inflammatory pathway with potential immunomodulating and anti-inflammatory activities. Upon intravenous administration, anti-inflammatory antibody ALXN1007 modulates the complement inflammatory pathway through binding to an as of yet undisclosed target. This may help in the treatment of certain inflammatory-mediated disorders, such as antiphospholipid syndrome (APS). This agent may also influence the progression of graft-versus-host disease (GvHD).


anti-inflammatory/antimicrobial/analgesic aqueous mouth rinse

A water-based proprietary mouthwash with anti-inflammatory, antimicrobial and analgesic activities. Upon rinsing with this mouthwash, the unspecified ingredients may help prevent or reduce the symptoms and severity of mucositis.


anti-integrin monoclonal antibody-DM4 immunoconjugate IMGN388

An immunoconjugate consisting of an anti-integrin monoclonal antibody covalently attached to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-integrin monoclonal antibody-DM4 immunoconjugate IMGN388 binds to tumor cell surface integrins; upon internalization, the DM4 moiety is released from the immunoconjugate, binding to tubulin and disrupting microtubule assembly/disassembly dynamics, which may result in inhibition of cell division and cell growth of integrin-expressing tumor cells. Integrins, a class of transmembrane cell surface receptors, link the extracellular matrix (ECM) to intracellular signaling pathways that control cell proliferation and differentiation.


anti-interleukin 6 monoclonal antibody ALD518

A humanized monoclonal antibody directed against the pro-inflammatory cytokine interleukin-6 (Il-6) with potential immunomodulating activity. Upon administration, anti-interleukin 6 monoclonal antibody ALD518 binds to and blocks the activity of IL-6, which may mitigate the catabolic effects of IL-6.


anti-interleukin-1 alpha monoclonal antibody MABp1

A human IgG1 monoclonal antibody targeting the inflammatory cytokine interleukin-1 alpha (IL1a) with potential antineoplastic, anti-cachectic and anti-angiogenic activities. Anti-IL1a monoclonal antibody MABp1 targets and binds to IL1a and prevents IL1a activity. This prevents IL1a-mediated tumorigenesis and angiogenesis. In addition, MABp1 abrogates IL1a-mediated cachexia. IL1a, an inflammatory mediator expressed on monocytes, platelets and overexpressed by certain tumors, plays a key role in the promotion of tumor cell growth, metastasis and invasion. In addition, IL1a stimulates metabolic activity in the central nervous system.


anti-KIR monoclonal antibody IHP 2101

A human monoclonal antibody directed against the human inhibitory killer IgG-like receptor (KIR) with potential immunostimulating and antineoplastic activities. Anti-KIR monoclonal antibody IPH 2101 binds to the KIR receptor expressed on human natural killer (NK) cells, which may prevent KIR-mediated inhibition of NK cells and permit NK cell-mediated anti-tumor cytotoxicity. KIRs are surface glycoproteins that bind to major histocompatibility complex (MHC)/human leukocyte antigen (HLA) class I subtypes on target cells; binding of KIRs inhibits NK cell-mediated cytotoxicity.


anti-KIR3DL2 monoclonal antibody IPH4102

A humanized monoclonal antibody against the immune receptor human killer cell immunoglobulin-like receptor, three domains, long cytoplasmic tail, 2 (KIR3DL2), with potential immunomodulating and antineoplastic activities. Upon administration, the anti-KIR3DL2 monoclonal antibody IPH4102 binds to KIR3DL2 expressed on certain tumor cells. This recruits natural killer (NK) cells and leads to lysis of KIR3DL2-expressing tumor cells. In addition, IPH4102 induces antibody-dependent cellular cytotoxicity (ADCC), thereby further eliminating tumor cells. KIR3DL2, a tumor-associated antigen (TAA) and inhibitory receptor of the KIR family, is specifically expressed in most subtypes of cutaneous T-cell lymphomas (CTCL) and expressed only on a fraction of normal NK cells.


anti-K-RAS G12D mTCR-transduced autologous peripheral blood lymphocytes

Autologous peripheral blood lymphocytes (PBLs) transduced with a retroviral vector encoding for an HLA class I histocompatibility antigen A*11:01 (HLA-A1101)-restricted murine T-cell receptor (mTCR) that recognizes the glycine (Gly, G) to aspartic acid (Asp, D) point mutation at position 12 (G12D) variant of K-RAS (KRAS), with potential immunomodulating and antineoplastic activities. HLA-A1101-positive PBLs are harvested from a K-RAS G12D-expressing cancer patient and transfected with a retroviral vector that encodes anti-K-RAS G12D mTCR. The transduced PBLs are then expanded in culture. When reintroduced to the patient, these anti-K-RAS G12D mTCR-expressing PBLs target and bind to K-RAS G12D-overexpressing tumor cells, which results in both cytokine secretion, including interferon-gamma (IFN-g), and tumor cell lysis. K-RAS, a member of the RAS family of oncogenes, serves an important role in cell signaling, division and differentiation. Mutation of K-RAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.


anti-K-RAS G12V mTCR-transduced autologous peripheral blood lymphocytes

Autologous peripheral blood lymphocytes (PBLs) transduced with an HLA class I histocompatibility antigen A*11:01 (HLA-A1101)-restricted murine T-cell receptor (mTCR) that recognizes the glycine to valine point mutation at position 12 (G12V) variant of K-RAS, with potential antineoplastic activity. HLA-A1101 positive PBLs are harvested from a K-RAS G12V-expressing cancer patient and transfected with a retroviral vector that encodes anti-K-RAS G12V mTCR. The transduced PBLs are then expanded in culture. When reintroduced to the patient, these anti-K-RAS G12V mTCR-expressing PBLs target and bind to K-RAS G12V-overexpressing tumor cells, which results in both cytokine secretion and tumor cell lysis. K-RAS, a member of the RAS family of oncogenes, serves an important role in cell signaling, division and differentiation. Mutation of K-RAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.


anti-LAG-3 monoclonal antibody BI 754111

A monoclonal antibody directed against the antigen lymphocyte-activation gene 3 (LAG-3; CD223).


anti-LAG-3 monoclonal antibody LAG525

A humanized monoclonal antibody directed against the inhibitory receptor lymphocyte activation gene-3 (LAG-3), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-LAG-3 monoclonal antibody LAG525 binds to LAG-3 expressed on tumor-infiltrating lymphocytes (TILs) and blocks its binding with major histocompatibility complex (MHC) class II molecules expressed on tumor cells. This activates antigen-specific T-lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which leads to a reduction in tumor growth. LAG-3, a member of the immunoglobulin superfamily (IgSF) and expressed on various immune cells, negatively regulates cellular proliferation and activation of T-cells. Its expression on TILs is associated with tumor-mediated immune suppression.  


anti-LAG3 monoclonal antibody MK-4280

A humanized, immunoglobulin G4 (IgG4) monoclonal antibody (MAb) directed against the inhibitory receptor lymphocyte activation gene-3 protein (LAG3), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-LAG3 monoclonal antibody MK-4280 binds to LAG3 expressed on tumor-infiltrating lymphocytes (TILs) and blocks its binding with major histocompatibility complex (MHC) class II molecules expressed on tumor cells. This activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which leads to a reduction in tumor growth. LAG3, a member of the immunoglobulin superfamily (IgSF), is expressed on various immune cells, and negatively regulates both proliferation and activation of T cells. Its expression on TILs is associated with tumor-mediated immune suppression.


anti-LAG-3 monoclonal antibody REGN3767

A monoclonal antibody directed against the inhibitory receptor lymphocyte activation gene-3 protein (LAG-3; LAG3; CD223), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-LAG-3 monoclonal antibody REGN3767 binds to LAG-3 expressed by tumor infiltrating lymphocytes (TILs) and blocks LAG-3 binding to tumor cells expressing major histocompatibility complex (MHC) class II molecules. This may activate antigen-specific T lymphocytes and enhance cytotoxic T-lymphocyte (CTL)-mediated tumor cell lysis, which leads to a reduction in tumor growth. LAG-3, a member of the immunoglobulin superfamily (IgSF), is expressed on various immune cells; its expression on TILs is associated with tumor-mediated immune suppression and the negative regulation of both cellular proliferation and T-cell activation.


anti-LAG-3 monoclonal antibody Sym022

A recombinant, human Fc-inert monoclonal antibody targeting lymphocyte-activation gene 3 protein (LAG-3; LAG3), with potential immune checkpoint inhibitory and antineoplastic activities. Upon intravenous administration, monoclonal antibody Sym022 binds to human LAG-3 and blocks the interaction between LAG-3 and major histocompatibility complex class II (MHCII) molecules on the surface of antigen-presenting cells (APCs) and tumor cells. This prevents the negative regulation of T-cell activity that occurs via LAG-3-MHCII binding and enhances a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. Additionally, Sym022 decreases LAG-3 surface levels through internalization and shredding. LAG-3 plays a key role in the activation of T cells and natural killer (NK) cells.


anti-LAG3 monoclonal antibody TSR-033

A humanized, immunoglobulin G4 (IgG4) monoclonal antibody directed against the inhibitory receptor lymphocyte activation gene 3 protein (LAG3; LAG-3), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-LAG3 monoclonal antibody TSR-033 binds to LAG3 expressed on tumor-infiltrating lymphocytes (TILs) and blocks its binding with major histocompatibility complex (MHC) class II molecules expressed on tumor cells. This activates antigen-specific T-lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which leads to a reduction in tumor growth. LAG3, a member of the immunoglobulin superfamily (IgSF), is expressed on various immune cells, and negatively regulates both proliferation and activation of T-cells. Its expression on TILs is associated with tumor-mediated immune suppression.


anti-LAG-3/PD-L1 bispecific antibody FS118

A bispecific antibody directed against two immune checkpoint proteins, the inhibitory receptor lymphocyte activation gene 3 protein (LAG3; LAG-3) and the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. FS118 is generated by incorporating an anti-LAG-3 Fc-region with antigen binding (Fcab) into a PD-L1-specific antibody. Upon administration, FS118 simultaneously targets and binds to LAG3 expressed on T-cells in the tumor microenvironment (TME) and PD-L1 expressed on tumor cells. This prevents LAG3- and PD-L1-mediated signaling, reverses T-cell inactivation, activates the immune system and enhances cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune responses against PD-L1-expressing tumor cells, which together lead to a reduction in tumor growth. LAG3, a member of the immunoglobulin superfamily (IgSF) negatively regulates both proliferation and activation of T-cells. Its expression is associated with tumor-mediated immune suppression. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to its receptor programmed death 1 (PD-1; PDCD1; CD279) on activated T-cells inhibits the expansion and survival of CD8-positive T-cells, suppresses the immune system and results in immune evasion.


anti-LAMP1 antibody-drug conjugate SAR428926

An antibody-drug conjugate (ADC) consisting of a monoclonal antibody against lysosome-associated membrane protein 1 (LAMP1) conjugated, via the disulfide-containing cleavable linker N-succinimidyl-4-(2-pyridyldithio)butyrate (SPDB), to the cytotoxic maytansinoid DM4, with potential antineoplastic activity. Upon administration of anti-LAMP1 ADC SAR428926, the anti-LAMP1 monoclonal antibody moiety targets and binds to the cell surface antigen LAMP1. After antibody-antigen interaction and internalization, the SPDB linker is selectively cleaved by proteases in the cytosol and the DM4 moiety is released. DM4 binds to tubulin and disrupts microtubule assembly/disassembly dynamics, thereby inhibiting both cell division and cell growth of LAMP1-expressing tumor cells. LAMP1, overexpressed on a variety of cancer cells, plays a key role in cell-cell adhesion and migration. The SPDB linker is resistant to cleavage in the bloodstream, which may increase stability and reduce toxicity.


anti-LeY-CAR-transduced autologous T lymphocytes

Genetically modified, autologous T lymphocytes transduced with a retroviral vector encoding a chimeric antigen receptor (CAR) specific for the tumor-associated antigen (TAA) Lewis-Y (LeY), with potential immunomodulating and antineoplastic activities. Upon intravenous administration, anti-LeY-CAR-transduced autologous T lymphocytes specifically target and induce selective toxicity in LeY-expressing tumor cells. LeY, a difucosylated carbohydrate antigen, is overexpressed by a variety of cancer cell types.


anti-LGR5 monoclonal antibody BNC101

A humanized monoclonal antibody targeting leucine-rich repeat-containing G-protein coupled receptor 5 (LGR5), with potential antineoplastic activity. Upon administration, the anti-LGR5 humanized monoclonal antibody BNC101 targets and binds to LGR5, thereby inhibiting LGR5-mediated signal transduction pathways. This prevents proliferation of LGR5-expressing tumor cells. LGR5, a member of the Wnt signaling pathway, is a cancer stem cell (CSC) receptor overexpressed on certain cancer cells; it plays a key role in CSC proliferation and survival.


anti-LIF monoclonal antibody MSC-1

A humanized immunoglobulin G1 (IgG1) monoclonal antibody against leukemia inhibitory factor (LIF), with potential immunomodulating and antineoplastic activities. Upon intravenous administration, monoclonal antibody MSC-1 binds to LIF and inhibits LIF signaling by blocking the recruitment of glycoprotein 130 (gp130) to the LIF-LIF receptor (LIFR)-gp130 signaling complex. This inhibits signal transducer and activator of transcription 3 (STAT3) signaling and inhibits tumor cell growth. In addition, the inhibition of LIF signaling abrogates the immunosuppressive tumor microenvironment (TME) by decreasing immunosuppressive M2 macrophages and allows for the activation of natural killer (NK) cells and cytotoxic T lymphocytes (CTLs) against tumor cells. LIF, a member of the interleukin-6 (IL-6) family of cytokines, is involved in many physiological and pathological processes and plays an important role in both creating the TME and promoting the activity of cancer -initiating cells (CICs). LIF is overexpressed in many tumor cell types and its expression correlates with poor prognosis.


anti-LIV-1 monoclonal antibody-MMAE conjugate SGN-LIV1A

An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed against the anti-solute carrier family 39 zinc transporter member 6 (SLC39A6; LIV-1; ZIP6) protein that is conjugated, via a protease-cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration and internalization by LIV-1-positive tumor cells, anti-LIV-1 antibody-drug conjugate SGN-LIV1A undergoes enzymatic cleavage to release MMAE into the cytosol. In turn, MMAE binds to and inhibits tubulin polymerization, which may result in G2/M phase cell cycle arrest and apoptosis in LIV-1-expressing tumor cells. LIV-1, a member of the zinc transporter family, is expressed in several types of solid tumors and plays a key role in tumor cell progression and metastasis. The linkage system in SGN-LIV1A is highly stable in plasma, resulting in cytotoxic specificity against LIV-1-positive cells.


anti-LOXL2 monoclonal antibody GS-6634

A humanized monoclonal antibody against lysyl oxidase-like 2 (LOXL2), with potential antineoplastic activity. Anti-LOXL2 monoclonal antibody AB0024 targets and specifically binds to the scavenger receptor cysteine rich domain 4 (SRCR-4) on LOXL2, thereby preventing the crosslinking of collagen and inhibiting the recruitment and activation of fibroblasts. Inhibiting fibroblast activation and the subsequent production of growth factors and chemokines may lead to an inhibition of tumor cell proliferation. LOXL2, a member of the lysyl oxidase (LO) gene family, is an extracellular, copper-dependent enzyme overexpressed in a variety of tumor cell types, and contributes to tumor cell invasion and metastasis.


anti-Ly6E antibody-drug conjugate DLYE5953A

An antibody-drug conjugate (ADC) composed of an antibody against the tumor-associated antigen (TAA) lymphocyte antigen 6 complex locus E (Ly6E) and linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the antibody moiety of DLYE5953A targets and binds to Ly6E expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills, through an as of yet unknown mechanism of action, the Ly6E-expressing cancer cells. Ly6E, an interferon (IFN)-inducible glycosylphosphatidylinositol (GPI)-linked cell membrane protein, is expressed on a variety of tumor cell types.


anti-MASP-2 monoclonal antibody OMS721

A monoclonal antibody against mannan-binding lectin (MBL)-associated serine protease-2 (MASP-2), with potential anti-thrombotic and immunomodulating activities. Upon subcutaneous administration, OMS721 binds to and inhibits MASP-2. This prevents the activation of MASP-2, the cleavage of certain complement components, and the activation of the complement lectin pathway. This inhibits complement deposition and complement-induced thrombus formation. MASP-2, a pro-inflammatory protein, plays a key role in the activation of the lectin complement pathway, which is a key component in the immune system, and is associated with complement-mediated diseases, such as thrombotic microangiopathies (TMAs), which includes hematopoietic stem cell transplant (HSCT)-related TMA, atypical hemolytic uremic syndrome (aHUS), and thrombotic thrombocytopenic purpura (TTP).


Anti-M-CSF monoclonal antibody MCS110

A humanized monoclonal antibody directed against macrophage colony-stimulating factor (M-CSF) with potential anti-osteolytic activity. Anti-M-CSF monoclonal antibody MCS110 binds to M-CSF and blocks M-CSF-mediated signaling through the M-CSF receptor CD116 expressed on osteoclasts, which may result in inhibition of M-CSF-induced osteoclast differentiation and so osteoclastic bone resorption. Osteoclasts are derived through the fusion of cells of the monocyte/macrophage lineage. Osteoblasts and stromal cells may react to bone metastases by producing M-CSF and its osteoclastogenic cofactor RANKL (receptor activator of NF-kappaB ligand).


anti-mesothelin antibody-drug conjugate BMS-986148

An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against the cell surface glycoprotein mesothelin and conjugated to an as of yet undisclosed cytotoxic drug, with potential antineoplastic activity. The monoclonal antibody moiety of anti-mesothelin ADC BMS-986148 targets and binds to the tumor-associated antigen mesothelin. Upon internalization, the cytotoxic agent kills or prevents cellular proliferation of mesothelin-expressing tumor cells through an as of yet undescribed mechanism of action. Mesothelin is overexpressed by all mesotheliomas and a variety of other cancer s, while it is minimally expressed in normal tissue.


anti-mesothelin CAR vector-transduced autologous T lymphocytes

Genetically modified, autologous T lymphocytes transduced with a retroviral vector encoding a chimeric antigen receptor (CAR) consisting of an anti-human tumor-associated antigen (TAA) mesothelin single chain variable fragment (scFv), the intracellular CD3 zeta T-cell receptor domain and the 4-1BB (cd137) costimulatory domain, with potential immunomodulating and antineoplastic activities. After isolation, transduction, expansion in culture, and reintroduction into the patient, the anti-mesothelin CAR vector-transduced autologous T lymphocytes specifically target and kill mesothelin-expressing tumor cells. Mesothelin, a cell surface glycoprotein involved in cell adhesion, is overexpressed in a variety of cancer cell types.


anti-mesothelin cytolytic fusion protein LMB-100

An anti-mesothelin (MSLN) recombinant cytolytic fusion protein (cFP) composed of a humanized Fab fragment of anti-MSLN monoclonal antibody SS1 linked to a truncated and de-immunized 24 kDa fragment of the Pseudomonas exotoxin (PE) (PE24), with potential antineoplastic activity. Upon intravenous administration of anti-MSLN-PE24 cFP LMB-100, the anti-MSLN moiety targets and binds to MSLN-expressing tumor cells. Upon binding and internalization through endocytosis, the toxin moiety ADP-ribosylates and inactivates eukaryotic elongation factor 2 (eEF2), preventing the elongation step of protein synthesis and leading to both an inhibition of protein synthesis and an induction of MSLN-expressing tumor cell apoptosis. MSLN, a tumor-associated antigen overexpressed in a variety of cancer cell types, plays a key role in tumor cell proliferation and migration. The engineered PE24 portion of LMB-100 does contain the targeting domain and furin cleavage site, which are needed for cytotoxicity, but most of the translocation domain II is deleted and the catalytic domain III contains point mutations, which result in the deletion and silencing of most T- and B-cell epitopes; therefore, the immunogenicity and toxicity is reduced compared to non-engineered PE toxin, which allows for the administration of larger doses of LMB-100.


anti-mesothelin iCasp9M28z CAR-transduced autologous T lymphocytes

Genetically modified, autologous T lymphocytes transduced with a retroviral vector encoding a chimeric antigen receptor (CAR) specific for mesothelin linked to the signaling domains for the co-stimulatory molecules CD28 and CD3 zeta, as well as the suicide gene inducible caspase 9 (iCasp9 or iC9), with potential immunomodulating and antineoplastic activities. Upon intravenous administration, anti-mesothelin iCasp9M28z CAR-transduced autologous T lymphocytes specifically target and kill mesothelin-expressing tumor cells. iCasp9 consists of a human FK506 drug-binding domain with an F36V mutation (FKBP12-F36V) linked to human caspase 9. If administration of the T cells lead to unacceptable side effects, a dimerizing agent can be administered which binds to the FKBP12-F36V drug-binding domain and activates caspase 9, resulting in the apoptosis of the administered T-cells. Mesothelin, a tumor-associated antigen, is overexpressed in a variety of cancer cell types.


anti-mesothelin-CAR mRNA-transduced autologous T lymphocytes

Autologous chimeric immune receptor (CIR) T cells transfected with anti-mesothelin chimeric T cell receptor mRNA, with potential antineoplastic activity. The anti-mesothelin mRNA encodes a single chain antibody variable fragment (ScFv), the intracellular CD 3 zeta T cell receptor domain and the 4-1BB (cd137) costimulatory domain. Upon intravenous administration, the anti-mesothelin-CAR mRNA-transduced autologous T lymphocytes may attach to cancer cells expressing mesothelin. This may stimulate the secretion of multiple cytokines and may result in cell lysis of mesothelin-expressing cancer cells. Mesothelin is a cell surface glycoprotein involved in cell adhesion and is overexpressed in many epithelial-derived cancer s.


anti-Met monoclonal antibody mixture Sym015

A mixture of two humanized immunoglobulin G1 (IgG1) monoclonal antibodies, Hu9006 and Hu9338, which recognize non-overlapping epitopes in the extracellular domain of the human hepatocyte growth factor receptor (MET; HGFR; c-Met), with potential antineoplastic activity. Upon administration, anti-MET monoclonal antibody mixture Sym015 targets and binds to the extracellular domain of MET, thereby preventing the binding of its ligand, hepatocyte growth factor (HGF). This may prevent activation of the receptor and MET-mediated signal transduction pathways. This inhibits MET-dependent tumor cell proliferation. MET, a receptor tyrosine kinase, is overexpressed on the cell surfaces of various solid tumor cell types; it plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.


anti-Met/EGFR monoclonal antibody LY3164530

A monoclonal antibody (MoAb) against human epidermal growth factor receptor (EGFR) and human hepatocyte growth factor receptor (HGFR or c-Met), with potential antineoplastic activity. Upon administration, anti-Met/EGFR MoAb LY3164530 targets and prevents the activation of EGFR and c-Met. This leads to a downstream inhibition of EGFR/c-Met-mediated signal transduction pathways, and prevents cellular proliferation in tumor cells overexpressing EGFR and c-Met. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surface of various solid tumor cell types. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.


antimetabolite FF-10502

An antimetabolite with potential antineoplastic activity. Upon administration, FF-10502 is able to enter the nucleus where it inhibits DNA polymerases, thereby preventing DNA synthesis and halting tumor cell proliferation.


anti-minor histocompatibility complex donor T lymphocytes

A preparation of allogeneic, donor-derived T lymphocytes that are specific for a unique set of minor histocompatibility complex antigens (MiHA) exclusively found on the surface of malignant cells, with potential immunomodulating and antineoplastic activities. T lymphocytes are derived from an allogeneic hematopoietic cell transplant (AHCT) donor. Ex vivo, these T cells are exposed to and primed against a select set of host-specific hematopoietic tissue-restricted MiHAs that are expressed on leukemic cells. Then the cells are subsequently expanded. After AHCT and infusion of the anti-MiHA T lymphocytes, these cells target and bind to MiHA antigens expressed on the host's leukemia cells, thereby killing these cancer cells. MiHA are small, cell-surface peptides that are associated with graft-versus-host disease (GvHD). The selected set of MiHAs is expressed mainly, or only, by hematopoietic cells, and overexpressed on leukemic cells.


anti-MMP-9 monoclonal antibody GS-5745

A humanized monoclonal antibody against matrix metalloproteinase 9 (MMP-9), with potential antineoplastic activity. Upon administration, anti-MMP-9 monoclonal antibody GS-5745 binds to MMP-9 and inhibits its enzymatic activity. This results in an inhibition of extracellular matrix protein degradation and, potentially, the inhibition of angiogenesis, tumor growth, invasion, and metastasis. MMP-9, a protein belonging to the MMP family, plays a key role in the degradation of collagens and proteoglycans; increased activity of MMP-9 has been associated with increased invasion and metastasis of cancer .


anti-MUC1 CAR-transduced autologous T lymphocytes

Autologous T lymphocytes transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) consisting of a single chain variable fragment (scFv) against the human tumor-associated epithelial antigen mucin 1 (MUC1), with potential immunomodulating and antineoplastic activities. Autologous PBLs from a patient with MUC1-positive cancer are transduced with a retroviral vector that encodes the CAR gene specific for MUC1. After expansion in culture and reintroduction into the patient, anti-MUC1 CAR-transduced autologous T lymphocytes target and induce selective toxicity in MUC1-expressing tumor cells. MUC-1 is a human, hypoglycosylated tumor-associated antigen (TAA) overexpressed by epithelial cancer cells.


anti-MUC16/CD3 BiTE antibody REGN4018

A human bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) human mucin 16 (MUC16; cancer antigen 125; CA125; FLJ14303), and one directed against human CD3, a T-cell surface antigen found on T lymphocytes, with potential antineoplastic activity. Upon administration, anti-MUC16/CD3 BiTE antibody REGN4018 binds to both CD3 on T cells and MUC16 expressed on tumor cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against MUC16-expressing tumor cells. MUC16, a member of the mucin family of glycoproteins, is overexpressed in a variety of tumor cells and plays a key role in tumor cell proliferation.


anti-MUC16/MMAE antibody-drug conjugate DMUC4064A

An antibody-drug conjugate (ADC) composed of a monoclonal antibody against human mucin 16 (MUC16; cancer antigen 125; CA125; FLJ14303) conjugated to monomethyl auristatin E (MMAE), an auristatin derivative and potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration, anti-MUC16/MMAE ADC DMUC4064A binds to MUC16 located on the tumor cell surface. After internalization of the agent, the MMAE moiety is released and binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and apoptosis. MUC16, a member of the mucin family glycoproteins, is overexpressed in a variety of tumor cells and plays a key role in tumor cell proliferation.


anti-myeloma monoclonal antibody-DM4 immunoconjugate BT-062

An immunoconjugate consisting of a monoclonal antibody directed against a highly-expressed myleoma cell surface antigen covalently attached to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-myeloma monoclonal antibody-DM4 immunoconjugate BT-062 binds to an unspecified cell surface antigen highly expressed on myeloma cells; upon internaliization the DM4 moiety is released, binding to tubulin and disrupting microtubule assembly/disassembly dynamics, which may result in the inhibition of cell division and cell growth of myeloma tumor cells.


anti-myostatin monoclonal antibody LY2495655

A monoclonal antibody against myostatin (MSTN) with potential anti-cachexia activity. Upon administration, anti-myostatin monoclonal antibody LY2495655 binds to and neutralizes the MSTN protein, thereby blocking the MSTN signalling pathway. This may help decrease muscle protein breakdown and muscle weakness and may attenuate cancer cachexia. MSTN, a member of the transforming growth factor-beta (TGF-beta) superfamily, is a negative regulator of muscle growth and development.


anti-NaPi2b monoclonal antibody XMT-1535

A proprietary humanized monoclonal antibody against human sodium-dependent phosphate transport protein 2B (SLC34A2; NaPi2b), with potential antineoplastic activity. Upon administration of XMT-1535, the antibody targets and binds to NaPi2b expressed on tumor cells. Although the tumor cell killing effects of XMT-1535 are not established, this binding may induce an antibody-dependent cellular cytotoxicity (ADCC)-mediated immune response against NaPi2b-expressing tumor cells, and/or may inhibit NaPi2b-mediated sodium and phosphate ion cotransport activity and ion-dependent tumor cell signaling. NaPi2b, a tumor-associated antigen (TAA), is overexpressed on a variety of tumor cells. It plays a key role in the transport of inorganic phosphate (Pi) and the maintenance of phosphate homeostasis.


anti-NaPi2b/MMAE antibody-drug conjugate DNIB0600A

An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against the sodium-dependent phosphate transport protein 2B (NaPi2b), and covalently linked to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of DNIB0600A binds to NaPi2b-expressing tumor cells and is internalized, thereby delivering MMAE intracellularly. Proteolytic cleavage releases MMAE, which then binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. NaPi2b, a tumor-associated antigen (TAA), overexpressed in a variety of cancer cell types, plays a key role in transport of inorganic phosphate and the maintenance of phosphate homeostasis.


anti-Nectin-4 monoclonal antibody-drug conjugate AGS-22M6E

An antibody drug conjugate (ADC) containing a fully human monoclonal antibody AGS-22 targeting the cell adhesion molecule nectin-4 and conjugated, via a proprietary enzyme-cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE) (AGS-22M6E), with potential antineoplastic activity. The monoclonal antibody moiety of AGS-22M6E selectively binds to nectin-4. After internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis in nectin-4 overexpressing tumor cells. Nectin-4, a tumor associated antigen belonging to the nectin family, is overexpressed in a variety of cancer s, including breast, bladder, lung and pancreatic cancer .


antineoplastic agent combination SM-88

An orally bioavailable, proprietary combination of four agents with potential antineoplastic activity. Although the four agents and their exact mechanisms of action are not publicly known, the components of SM-88 appear, upon oral administration, to work synergistically to increase the amount of free radicals in cancer cells, thereby inducing oxidative stress and selective killing of the cancer cells.


antineoplastic agent TRX-818

An orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities. Although the exact multiple mechanisms of action through which this agent exerts its effects have yet to be fully elucidated, TRX-818, upon oral administration appears to induce cancer cell apoptosis and inhibits cancer cell proliferation. This agent also prevents tumor cell VM by blocking the formation of vasculogenic-like tubular structures through an as of yet undetermined mechanism of action.


antineoplaston A10

A piperidinedione antineoplaston with potential antineoplastic activity. Antineoplaston A10 was originally isolated from human urine but is now synthetically derived. This agent intercalates into DNA, resulting in cell cycle arrest in G1 phase, reduction of mitosis, and decreased protein synthesis. Antineoplaston A10 may also inhibit ras-oncogene expression and activate tumor suppressor gene p53, leading to cell differentiation and apoptosis.


antineoplaston AS2-1

A 4:1 mixture of phenylacetate and phenylacetylgluatmine, degradation products of the antineoplaston agent A10. Antineoplaston AS2-1 inhibits the incorporation of L-glutamine into tumor-cell proteins, leading to cell cycle arrest in the G1 phase and inhibition of mitosis. This agent may also inhibit RAS oncogene expression and activate tumor suppressor gene p53, resulting in cell differentiation and apoptosis.


anti-neuropilin-1 monoclonal antibody MNRP1685A

A human IgG1 monoclonal antibody directed against neuropilin-1 (NRP1), with potential antiangiogenic and antineoplastic activities. Upon intravenous administration, MNRP1685A specifically targets and binds to NRP1; the antibody-NRP1 complex prevents the subsequent coupling of NRP1 to VEGFR2, thereby potentially inhibiting VEGF-mediated signaling and potentially preventing angiogenesis. In combination with other anti-VEGF therapies, MNRP1685A may enhance their anti-angiogenic effect. NRP1 is a membrane-bound co-receptor normally expressed by endothelial cells and overexpressed by certain tumor cells, and plays a role in angiogenesis, cell survival, migration, and invasion.


anti-nf-P2X7 antibody ointment BIL-010t

An ointment formulation composed of a purified sheep immunoglobulin G (IgG) antibody against the non-functional form of the purinergic P2X7 receptor (nf-P2X7), with potential antineoplastic activity. Upon topical application of the anti-nf-P2X7 antibody ointment BIL-010t, the antibody binds to nf-P2X7 and inhibits its antiapoptotic activity. This may induce apoptosis and inhibit the growth of nf-P2X7-overexpressing cancer cells. P2X7, an ATP-gated cation-selective channel, plays a role in the induction of apoptosis; nf-P2X7, is upregulated in a variety of cancer cell types while not expressed on normal, healthy cells and is unable to form a large transmembrane, apoptotic pore upon exposure to ATP and prevents apoptosis.  


anti-nucleolin aptamer AS1411

A 26-base guanine-rich oligodeoxynucleotide aptamer with potential apoptotic induction activity. Upon administration, anti-nucleolin aptamer AS1411 targets and binds to nucleolin, a nucleolar phosphoprotein which is overexpressed on the surface of certain cancer cells. Via binding to cell surface nucleolin, AS1411 is internalized and may prevent nucleolin from binding to and stabilizing mRNA of the anti-apoptotic BCL2, thereby destabilizing BCL2 mRNA, leading to a reduction in BCL2 protein synthesis. This may lead to the induction of apoptosis.


anti-NY-ESO-1 TCR LV-transduced autologous T cells TAEST16001

A preparation of human autologous T lymphocytes that are transduced with a lentiviral vector (LV) encoding an affinity-enhanced T-cell receptor (TCR) specific for the cancer -testis antigen NY-ESO-1, with potential immunostimulating and antineoplastic activities. Upon isolation, transduction, expansion ex vivo, and reintroduction into the patient, the anti-NY-ESO-1 TCR LV-transduced autologous T cells TAEST16001 recognize and bind to NY-ESO-1-overexpressing tumor cells. This may result in a specific cytotoxic T-lymphocyte (CTL)-mediated killing of NY-ESO-1-positive tumor cells. NY-ESO-1, a tumor-associated antigen (TAA), is found in normal testis and on the surface of various tumor cell types, and is not, or is minimally, expressed in normal, healthy cells.


anti-NY-ESO1 TCR-transduced autologous CD62L+-derived T lymphocytes

Human autologous CD62L-positive T lymphocytes transduced with a retroviral vector encoding a T cell receptor (TCR) specific for the cancer -testis antigen NY-ESO-1, with potential antineoplastic activity. Following leukapheresis, isolation of lymphocytes, expansion ex vivo, transduction, and reintroduction into the patient, the anti-NY-ESO1 TCR-transduced autologous CD62L+-derived T lymphocytes bind to NY-ESO-1-overexpressing tumor cells. This may result in cytotoxic T-lymphocyte (CTL)-mediated elimination of NY-ESO-1-positive cancer cells. NY-ESO-1, a tumor associated antigen (TAA), is found in normal testis and on the surface of various tumor cell types. CD62L, also called L-selectin, is a lymphoid homing receptor and differentiation marker and is expressed on a subset of CD8-positive T-lymphocytes; it is involved in the migration of T-lymphocytes to lymph nodes and may improve the efficacy for ex vivo-expanded T-cells following adoptive cell therapy.


anti-NY-ESO1/LAGE-1A TCR/scFv anti-CD3 IMCnyeso

A bispecific molecule composed of a soluble, affinity-enhanced T-cell receptor (TCR) specific for human leukocyte antigen A2 (HLA-A2)-restricted cancer -testis antigens (CTAs) NY-ESO-1 and L antigen family member 1 isoform A (LAGE-1A; LAGE-A1; CT6.2a), fused to a single-chain variable fragment (scFv) specific for the T-cell surface antigen CD3, with potential immunomodulating and antineoplastic activities. Upon infusion, anti-NY-ESO1/LAGE-1A TCR/scFv anti-CD3 IMCnyeso specifically targets and binds with its TCR moiety to NY-ESO-1 and/or LAGE-1A expressed on tumor cells and with its scFv moiety to CD3 expressed on T-cells. This crosslinks tumor cells and T-cells, re-directs and activates T cells, and results in a cytotoxic T-lymphocyte (CTL)-mediated destruction of NY-ESO-1 and/or LAGE-1A-positive tumor cells. NY-ESO-1 and LAGE-1A, members of the cancer -testis antigen (CTA) family, are overexpressed on the surface of various tumor cell types; they share a specific HLA-A*0201 epitope, 157-165, which is expressed on certain tumor cell types while its expression is not found on normal, healthy cells.


anti-OX40 antibody BMS 986178

An agonistic monoclonal antibody against the co-stimulatory receptor OX40 (CD134; TNFRSF4), with potential immunostimulatory activity. Upon administration, anti-OX40 monoclonal antibody BMS 986178 selectively binds to and activates the OX40 receptor, by mimicking the action of the endogenous OX40 ligand (OX40L). OX40 receptor activation induces proliferation of memory and effector T-lymphocytes. In the presence of tumor-associated antigens (TAAs), this may promote an immune response against the TAA-expressing tumor cells. OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor family (TNFRSF), is expressed on T-lymphocytes and provides a co-stimulatory signal for the proliferation and survival of activated T-cells.


anti-OX40 antibody PF-04518600

An agonistic antibody that recognizes the co-stimulatory receptor OX40 (CD134;TNFRSF4), with potential immunostimulatory activity. Upon administration, anti-OX40 antibody PF-04518600 selectively binds to and activates OX40; which induces proliferation of memory and effector T-lymphocytes. In the presence of tumor-associated antigens (TAAs), this may promote a T-cell-mediated immune response against TAA-expressing tumor cells. OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T-lymphocytes and plays an essential role in T-cell activation.


anti-OX40 monoclonal antibody

An agonistic monoclonal antibody against receptor OX40 (CD134), with potential immunostimulatory activity. Mimicking the natural OX4 ligand (OX40L), anti-OX40 monoclonal antibody selectively binds to and activates the OX40 receptor. Receptor activation induces proliferation of memory and effector T lymphocytes. In the presence of tumor associated antigens (TAAs), this may promote an immune response against the TAA-expressing tumor cells. OX40, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) receptor family, is expressed by CD4 T cells and provides a costimulatory signal for T cell activation.


anti-OX40 monoclonal antibody MEDI0562

An agonistic, humanized monoclonal antibody against receptor OX40 (CD134), with potential immunostimulatory activity. Upon administration, anti-OX40 monoclonal antibody MEDI0562 selectively binds to and activates the OX40 receptor. OX40 receptor activation induces proliferation of memory and effector T-lymphocytes. In the presence of tumor-associated antigens (TAAs), this agent may promote an immune response against TAAs-expressing tumor cells. OX40, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) receptor family, is expressed on T-lymphocytes and provides a co-stimulatory signal for the proliferation and survival of activated T-cells.


anti-OX40 monoclonal antibody MOXR0916

An agonistic humanized monoclonal antibody against the receptor, OX40 (CD134), with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, anti-OX40 monoclonal antibody MOXR0916 selectively binds to and activates OX40, by mimicking the action of endogenous OX40 ligand (OX40L). OX40 activation induces proliferation of effector T lymphocytes and inhibits the activity of regulatory T cells. In the presence of tumor-associated antigens (TAAs), this may promote an immune response against the TAA-expressing tumor cells. OX40, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on T lymphocytes and provides a co-stimulatory signal for the proliferation and survival of activated T cells.


anti-p53 T-cell receptor-transduced peripheral blood lymphocytes

Human autologous peripheral blood lymphocytes (PBLs) transduced with an anti-p53 T cell receptor gene with potential antineoplastic activity. PBLs are harvested from a patient and pulsed with a retroviral vector that encodes the T-cell receptor gene specific for a mutated form of p53. The transduced PBLs are then expanded in culture. When reintroduced to the patient, these modified PBLs express the anti-p53 T cell receptor which binds to mutant p53-overexpressing tumor cells; PBL-mediated tumor growth inhibition may follow. Many tumor cell types overexpress mutant p53 proteins, which are associated with the loss of apoptosis regulation and abnormal cell proliferation.


anti-PD-1 checkpoint inhibitor PF-06801591

An inhibitor of the human inhibitory receptor programmed cell death 1 (PD-1; PDCD1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 checkpoint inhibitor PF-06801591 targets and binds to PD-1 and blocks the interaction between PD-1 and its ligands, PD-1 ligand 1 (PD-L1) and PD-1 ligand 2 (PD-L2). This prevents the activation of PD-1 and its downstream signaling pathways. This may restore immune function through the activation of natural killer (NK) cells and cytotoxic T-lymphocytes (CTLs) against tumor cells. PD-1, an inhibitory receptor belonging to the B7-receptor family, is expressed on activated T-lymphocytes, B-cells and NK cells; it functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands, and plays an important role in tumor evasion from host immunity.


anti-PD-1 fusion protein AMP-224

A recombinant B7-DC Fc-fusion protein composed of the extracellular domain of the PD-1 ligand programmed cell death ligand 2 (PD-L2, B7-DC) and the Fc region of human immunoglobulin (Ig) G1, with potential immune checkpoint inhibitory and antineoplastic activities. Anti-PD-1 fusion protein AMP-224 specifically binds to PD-1 on chronically stimulated T-cells and reduces their proliferation. This may restore immune function and may result in the activation of cytotoxic T-cells and cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein of Ig superfamily and inhibitor receptor expressed on activated T-cells, negatively regulates T-cell activation and effector function when activated by its ligands, and plays an important role in tumor evasion from host immunity. AMP-224 does not bind normal activated T-cells.


anti-PD1 monoclonal antibody ABBV-181

A monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1, PCD-1; PDCD1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody ABBV-181 targets and binds to PD-1, thereby blocking its binding to the PD-1 ligand, programmed cell death-1 ligand 1 (PD-L1), and preventing the activation of PD-1/PD-L1 downstream signaling pathways. This may restore immune function through the activation of cytotoxic T lymphocytes (CTLs). PD-1, a transmembrane protein in the immunoglobulin superfamily expressed on activated T cells, negatively regulates T-cell activation and effector function when activated by its ligand; it plays an important role in tumor evasion from host immunity.


anti-PD1 monoclonal antibody AGEN2034

A monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1, PCD-1; PDCD1) protein, with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody AGEN2034 binds to PD-1, and thereby blocks its binding to the PD-1 ligand programmed cell death-1 ligand 1 (PD-L1), and prevents the activation of its downstream signaling pathways. This may restore immune function through the activation of cytotoxic T cells. PD-1, a transmembrane protein in the immunoglobulin superfamily expressed on activated T cells, negatively regulates T-cell activation and effector function when activated by its ligand; it plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody AK105

A monoclonal antibody directed against the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody AK105 targets, binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells and T-cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death-1 ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody BCD-100

A monoclonal antibody directed against the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody BCD-100 binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells and cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death-1 ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody BI 754091

A monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death protein 1 (PD-1; PDCD1), with immune checkpoint inhibitory and antineoplastic activities. Upon administration, BI 754091 selectively binds to and blocks the activation of PD-1, an immunoglobulin (Ig) superfamily transmembrane protein, by its ligands programmed cell death ligand 1 (PD-L1), which is overexpressed on certain cancer cells, and programmed cell death ligand 2 (PD-L2), which is primarily expressed on antigen-presenting cells (APCs). This results in the activation of T cells and T-cell-mediated immune responses against tumor cells. Activated PD-1 negatively regulates T-cell activation and plays a key role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody HLX10

A humanized monoclonal antibody directed against the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody HLX10 targets, binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells and T-cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death-1 ligand 1 (PD-L1) and 2 (PD-L2); it plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody JTX-4014

A human immunoglobulin G4 (IgG4) monoclonal antibody directed against the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody JTX-4014 targets, binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells and T-cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death-1 ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody LZM009

A recombinant, humanized monoclonal antibody directed against the negative immunoregulatory human cell surface receptor, programmed cell death 1 (PD-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon intravenous administration, LZM009 binds to PD-1 and inhibits the binding of PD-1 to the PD-1 ligands, programmed cell death-1 ligand 1 (PD-L1) and PD-1 ligand 2 (PD-L2). This prevents the activation of PD-1 and its downstream signaling pathways, leading to the activation of both T cells and T-cell-mediated immune responses against tumor cells. PD-1 is a transmembrane protein in the immunoglobulin (Ig) superfamily expressed on activated T cells that negatively regulates T-cell activation and effector function when activated by its ligands. PD-1 plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody MEDI0680

A humanized immunoglobulin (Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody MEDI0680 binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T-cells and cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the Ig superfamily expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody MGA012

A proprietary humanized monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody MGA012 binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells and cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody Sym021

A humanized monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1 , PCD-1; PDCD1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody Sym021 binds to and inhibits PD-1 activation and its downstream signaling pathways. This may restore immune function through the activation of T cells and cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF), is expressed on T cells and functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death ligand 1 (PD-L1) or 2 (PD-L2). Activated PD-1 plays an important role in tumor evasion from host immunity.


anti-PD-1 monoclonal antibody TSR-042

A humanized monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1; programmed death-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody TSR-042 binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells. PD-1, a transmembrane protein in the Ig superfamily expressed on T cells, functions as an immune checkpoint protein that negatively regulates T-cell activation and T-cell-mediated immune responses when activated by its ligands programmed cell death receptor ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.


anti-PD-1/anti-LAG-3 DART protein MGD013

An Fc-bearing, humanized antibody-like protein that specifically recognizes the immune checkpoint molecules programmed cell death 1 (PD-1; PD1; PDCD1; CD279; Programmed Death 1) and lymphocyte activation gene-3 (LAG-3; LAG3; CD223), with potential T-lymphocyte immunomodulatory and antineoplastic activities. Upon administration, the anti-PD-1/anti-LAG-3 dual-affinity re-targeting (DART) protein MGD013 specifically binds to both PD-1 and LAG-3, which are both expressed on T cells. The dual blockade of the PD-1 and LAG-3 pathways enables potent activation of a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. PD-1 and LAG-3 play key roles in suppressing T-cell activation.


anti-PD-1/CTLA-4 bispecific antibody AK104

A bispecific antibody directed against the human negative immunoregulatory checkpoint receptors programmed cell death protein 1 (PD-1; PDCD1; CD279) and cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1/CTLA4 bispecific antibody AK104 targets and binds to both PD-1 and CTLA4 expressed on tumor-infiltrating T lymphocytes (TILs), and inhibits the PD-1- and CTLA4-mediated downregulation of T-cell activation and proliferation. This restores immune function and activates a sustained cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. Both PD-1 and CTLA4 are selectively expressed on TILs in the tumor microenvironment (TME) and negatively regulate the activation and effector functions of T cells. They play key roles in the downregulation of the immune system and tumor evasion from host immunity. Dual checkpoint blockade of PD-1 and CTLA4 with AK104 may enhance T-cell activation and proliferation more than the blockade of either immune checkpoint receptor alone.


anti-PD1/CTLA4 bispecific antibody XmAb20717

A Fc-engineered bispecific antibody directed against the human negative immunoregulatory checkpoint receptors programmed cell death protein 1 (PD-1; PDCD1; CD279) and cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD1/CTLA4 bispecific antibody XmAb20717 targets and binds to both PD-1 and CTLA4 expressed on tumor-infiltrating T lymphocytes (TILs) and inhibits the PD-1- and CTLA4-mediated downregulation of T-cell activation and proliferation. This restores immune function and activates a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. Both PD-1 and CTLA4 are selectively expressed on TILs in the tumor microenvironment (TME) and negatively regulate the activation and effector functions of T cells. They play key roles in the downregulation of the immune system and tumor evasion from host immunity. Dual checkpoint blockade of PD1 and CTLA4 with XmAb20717 may enhance T-cell activation and proliferation more than the blockade of either immune checkpoint receptor alone. The engineered Fc domain increases the stability and half-life of the antibody.


anti-PD1/ICOS bispecific monoclonal antibody XmAb23104

A humanized, Fc-engineered bispecific monoclonal antibody directed against both the human negative immunoregulatory checkpoint receptor, programmed cell death protein 1 (PD-1; PCD-1; CD279), and inducible T-cell co-stimulator (ICOS; CD278), with potential immunomodulating and antineoplastic activities. Upon administration, anti-PD1/ICOS bispecific monoclonal antibody XmAb23104 targets and binds to both PD-1 and ICOS expressed on certain T cells, including tumor-infiltrating lymphocytes (TILs). This prevents the activation of PD-1 by its ligands, programmed cell death-1 ligand 1 (PD-L1) and PD-1 ligand 2 (PD-L2), and stimulates ICOS-mediated signaling, which promotes the activation of T cells and enhances T-cell-mediated immune responses against tumor cells. Combined PD-1 blockade and ICOS stimulation may enhance T-cell activation and proliferation more than targeting each receptor individually. The engineered Fc domain increases the stability and half-life of the antibody.


anti-PDCD1 monoclonal antibody JNJ-63723283

A monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 protein (PD-1, PCDC-1), with potential immune checkpoint inhibitory and antineoplastic activity. Upon administration, anti-PD-1 monoclonal antibody JNJ-63723283 binds to PD-1, and inhibits the interaction with its ligands, programmed cell death 1 ligand 1 (PD-L1, PD-1L1) and PD-1 ligand 2 (PD-L2, PD-1L2). The inhibition of ligand binding prevents PD-1-mediated signaling and results in both T-cell activation and the induction of T-cell-mediated immune responses against tumor cells. PD-1, an immunoglobulin (Ig) superfamily transmembrane protein and inhibitory receptor, negatively regulates T-cell activation.


 

anti-PDGFR alpha monoclonal antibody MEDI-575

A humanized monoclonal antibody directed against the platelet-derived growth factor receptor (PDGFR) alpha with potential antineoplastic activity. Anti-PDGFR alpha monoclonal antibody MEDI-575 inhibits activation of the cell-surface tyrosine kinase PDGFR alpha subunit and subsequent triggering of mitogenic signaling pathways, including the JAK/STAT, PI3K/Akt, and MAP kinase pathways. PDGFR alpha acts as a mitogenic signaling receptor for cells of mesenchymal origin and inhibition of receptor activity may inhibit tumor cell proliferation.


anti-PD-L1 monoclonal antibody BCD-135

A monoclonal antibody directed against the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-L1 monoclonal antibody BCD-135 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed death 1 (PD-1). This reverses T-cell inactivation caused by PD-1/PD-L1 signaling and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response against PD-L1-expressing tumor cells. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T-cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein belonging to the immunoglobulin superfamily expressed on activated T cells, is a negative regulator of the immune system that limits the expansion and survival of CD8-positive T cells.


anti-PD-L1 monoclonal antibody BGB-A333

A humanized immunoglobulin G1 (IgG1)-variant monoclonal antibody directed against the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-L1 monoclonal antibody BGB-A333 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor, programmed cell death 1 (PD-1; PDCD1; CD279; programmed death-1). This reverses T-cell inactivation caused by PD-L1/PD-1 signaling, increases T-cell expansion and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response against PD-L1-expressing tumor cells. In addition, BGB-A333 blocks the interaction between PD-L1 and its other receptor, the immunostimulatory molecule cluster of differentiation 80 (CD80; B7-1). This prevents PD-L1/CD80 signaling and inhibits the induction of PD-L1-induced apoptosis of activated CD8+ T cells and increases T-cell proliferation. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on activated T cells suppresses the immune system and results in immune evasion. PD-1 negatively regulates T-cell activation.


anti-PD-L1 monoclonal antibody CBT-502

A humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the immunosuppressive ligand programmed cell death-1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-L1 monoclonal antibody CBT-502 specifically targets and binds to PD-L1, preventing the binding and subsequent activation of its receptor, programmed cell death 1 (PD-1; PDCD1; CD279; programmed death-1). This reverses T-cell inactivation caused by PD-L1/PD-1 signaling, increases T-cell expansion and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response against PD-L1-expressing tumor cells. PD-L1, a transmembrane protein expressed on activated T cells, is overexpressed in some cancer types and plays a significant role in immune evasion by tumor cells.


anti-PD-L1 monoclonal antibody CK-301

An immunoglobulin G1 (IgG1), human monoclonal antibody directed against the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-L1 monoclonal antibody CK-301 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed cell death protein 1 (PD-1; PDCD1; CD279; programmed death-1). This reverses T-cell inactivation caused by PD-1/PD-L1 signaling and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response against PD-L1-expressing tumor cells. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein belonging to the immunoglobulin superfamily expressed on activated T cells, is a negative regulator of the immune system that limits the expansion and survival of CD8-positive T cells.  


anti-PD-L1 monoclonal antibody CS1001

A fully human monoclonal antibody directed against the immunosuppressive ligand, programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-L1 monoclonal antibody CS1001 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor, programmed cell death 1 (PD-1). This reverses T-cell inactivation caused by PD-1/PD-L1 signaling and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response against PD-L1-expressing tumor cells. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein belonging to the immunoglobulin superfamily expressed on activated T cells, is a negative regulator of the immune system that limits the expansion and survival of CD8-positive T cells. Anti-PD-L1 monoclonal antibody CS1001 mirrors natural immunoglobulin G4 (IgG4), potentially reducing immunogenicity and other toxicities.


anti-PD-L1 monoclonal antibody FAZ053

A monoclonal antibody directed against programmed cell death-1 ligand 1 (PD-L1), with immune checkpoint inhibitory and potential antineoplastic activities. Upon administration, anti-PD-L1 monoclonal antibody FAZ053 binds to PD-L1, blocking its binding to and activation of its receptor programmed death 1 (PD-1), which may enhance the T-cell-mediated anti-tumor immune response and reverse T-cell inactivation. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein expressed on activated T cells, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells.


anti-PD-L1 monoclonal antibody KN035

An injectable formulation of a monoclonal antibody directed against programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with immune checkpoint inhibitory and potential antineoplastic activities. Upon subcutaneous administration, anti-PD-L1 monoclonal antibody KN035 binds to PD-L1, blocking its binding to and activation of its receptor programmed death 1 (PD-1), which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T-cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein expressed on activated T-cells, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells.


anti-PD-L1 monoclonal antibody MDX-1105

A fully human monoclonal antibody directed against programmed cell death-1 ligand 1 (PD-L1) with immune checkpoint inhibitory and potential antineoplastic activities. Anti-PD-L1 monoclonal antibody MDX-1105 binds to PD-L1, blocking its binding to and activation of its receptor programmed death 1 (PD-1), which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T-cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein expressed on activated T-cells, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells.


anti-PD-L1 monoclonal antibody MSB2311

A second-generation, humanized monoclonal antibody directed against the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. The anti-PD-L1 monoclonal antibody MSB2311 contains a unique, not as of yet elucidated, pH-dependent antigen binding property allowing the antibody to only bind to PD-L1 within the acidic tumor microenvironment (TME), while it is not able to bind to PD-L1 in normal, healthy tissue. Upon administration, once able to bind to PD-L1 in the TME, MSB2311 blocks the binding of PD-L1 to and activation of its receptor, programmed cell death 1 (PD-1; PDCD1; CD279; programmed death-1). This reverses T-cell inactivation caused by PD-L1/PD-1 signaling, increases T-cell expansion and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response against PD-L1-expressing tumor cells. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on activated T cells suppresses the immune system and results in immune evasion. PD-1 negatively regulates T-cell activation.


anti-PD-L1 monoclonal antibody SHR-1316

An immunoglobulin G4 (IgG4), humanized monoclonal antibody directed against the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-L1 monoclonal antibody SHR-1316 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed death 1 (PD-1). This reverses T-cell inactivation caused by PD-1/PD-L1 signaling and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response against PD-L1-expressing tumor cells. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein belonging to the immunoglobulin superfamily expressed on activated T cells, is a negative regulator of the immune system that limits the expansion and survival of CD8-positive T cells.


anti-PD-L1/CTLA-4 bispecific antibody KN046

A bispecific monoclonal antibody directed against both the immunosuppressive ligand, programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), and cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-L1/CTLA-4 bispecific monoclonal antibody KN046 targets and binds to both PD-L1 expressed on tumor cells and CTLA-4 expressed on T cells. This prevents the binding of PD-L1 to its receptor, programmed cell death protein 1 (PD-1, CD279), and inhibits the PD-1 and CTLA-4-mediated downregulation of T-cell activation and proliferation. This restores immune function and activates a sustained cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. Both PD-L1, which is overexpressed in many human cancer cell types, and CTLA-4, an inhibitory T-cell receptor, play a role in the downregulation of the immune system and tumor evasion from host immunity.


anti-PD-L1/TGFbetaRII fusion protein M7824

A bifunctional fusion protein composed of avelumab, an anti-programmed death ligand 1 (PD-L1) human monoclonal antibody, bound to the soluble extracellular domain of human transforming growth factor beta (TGFbeta) receptor type II (TGFbetaRII), with potential antineoplastic and immune checkpoint modulating activities. Upon administration, the TGFbetaRII moiety of M7824 binds to and neutralizes TGFbeta while the avelumab moiety simultaneously binds to PD-L1. This prevents TGFbeta- and PD-L1-mediated signaling, and increases natural killer (NK) cell and cytotoxic T-lymphocyte (CTL) activities. This inhibits tumor cell proliferation in susceptible tumor cells. TGFbeta and PD-L1 are both upregulated in certain types of cancer s; their overexpression is associated with increased evasion of immune surveillance and contributes to poor prognosis.


anti-PD-L1/TIM-3 bispecific antibody LY3415244

A bispecific antibody directed against the inhibitory T-cell receptor T-cell immunoglobulin and mucin domain-containing protein 3 (TIM-3; TIM3; hepatitis A virus cellular receptor 2; HAVCR2) and the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, LY3415244 simultaneously targets and binds to TIM-3 expressed on certain T cells, including tumor-infiltrating lymphocytes (TILs), and PD-L1 expressed on tumor cells. This blocks the interaction of TIM-3 with some of its physiologic ligands and prevents PD-L1 from binding to and activating its receptor, programmed cell death 1 (PD-1; PDCD1; CD279; programmed death-1). This abrogates T-cell inhibition, activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which may lead to a reduction in tumor growth. TIM-3, a transmembrane protein and immune checkpoint receptor, is often co-expressed with PD-1 on tumor-antigen-specific T cells. PD-L1 binding to PD-1 on activated T cells inhibits the expansion and survival of CD8-positive T cells, suppresses the immune system and results in immune evasion.


antiperspirant cream F511

A cream formulation containing aluminum chlorohydrate with astringent and antiperspirant activities. Upon topical application of F511 cream, aluminium chlorohydrate forms a gel matrix in the sweat gland which subsequently reduces, then stops the flow of water. In addition, this agent exerts an astringent effect, thereby further preventing sweat formation. Hyperhidrosis appears to play a role in the development of certain mucocutaneous reactions, such as palmar-plantar erythrodysesthesia (PPE), upon administration of chemotherapeutic agents such as doxorubicin, 5-fluorouracil, and capecitabine.  


anti-PGF monoclonal antibody RO5323441

A humanized IgG1 monoclonal antibody directed against the placenta growth factor (PGF), with potential anti-angiogenic and antineoplastic activities. Anti-PGF monoclonal antibody RO5323441 binds to both PGF-1 and -2, thereby inhibiting the binding of PGF-1 and -2 to the vascular endothelial growth factor receptor-1 (VEGFR-1) and subsequent VEGFR-1 phosphorylation. This may result in the inhibition of tumor angiogenesis and tumor cell proliferation. PGF, a member of the VEGF sub-family and a key molecule in angiogenesis and vasculogenesis, is upregulated in many cancer s.


anti-PKN3 siRNA Atu027

A lipoplexed formulation consisting of short-interfering RNAs (siRNAs) directed against protein kinase N3 (PKN3) encapsulated in catiogenic and fusiogenic lipids with potential antineoplastic activity. Upon administration, catiogenic and fusiogenic lipids promote anti-PKN3 siRNA Atu02 uptake by tumor cells; the siRNAs moieties are subsequently released once inside the cell. The siRNAs bind to PKN3 mRNAs, which may result in the inhibition of translation and expression of the PKN3 protein and, so, growth inhibition of tumor cells that overexpress PKN3. The protein kinase C-related molecule PKN3, downstream in the phosphoinositide-3-kinase (PI3K) signaling pathway, is upregulated in many tumor cells and plays an important role in invasive cell growth and metastasis.


anti-PLGF monoclonal antibody TB-403

A humanized monoclonal antibody directed against placental growth factor (PLGF) with potential anti-angiogenic and antineoplastic acivities. Anti-PLGF monoclonal antibody TB-403 binds to PLGF, inhibiting the binding of PLGF to the vascular endothelial growth factor receptor, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. PLGF is a protein that belongs to the family of vascular endothelial growth factors (VEGFs).


anti-PR1/HLA-A2 monoclonal antibody Hu8F4

A T-cell receptor (TCR)-like monoclonal antibody against PR1, a 9 amino-acid (VLQELNVTV) human leukocyte antigen (HLA)-A2-restricted leukemia-associated antigen (LAA) derived from the myeloid leukemia-associated antigens proteinase 3 (P3) and neutrophil elastase (NE), with potential immunostimulating and antineoplastic activities. Upon administration, anti-PR1/HLA-A2 monoclonal antibody Hu8F4 selectively binds to a combined epitope of the PR1/HLA-A2 complex expressed on acute myeloid leukemia (AML) blasts and leukemic stem cells (LSC), and prevents PR1/HLA-A2-mediated signaling. This induces complement-dependent cytotoxicity (CDC), to a lesser extent, antibody-dependent cell-mediated cytotoxicity (ADCC), and CDC/ADCC-independent cytolysis of myeloid leukemia cells. This results in a reduction of cellular proliferation in PR1/HLA-A2-overexpressing leukemic cells. PR1 in combination with the HLA-A2 molecule is highly expressed on AML blasts and LSCs.


anti-PRL-3 monoclonal antibody PRL3-zumab

A humanized monoclonal antibody against phosphatase of regenerating liver 3 (PRL-3; PTP4A3), with potential immunomodulating and antineoplastic activities. Upon administration, anti-PRL-3 monoclonal antibody PRL3-zumab targets, binds to and blocks PRL-3 expressed on tumor cells. Although the exact mechanism of action through which this antibody kills tumor cells has yet to be fully elucidated, PRL3-zumab binds to PRL-3. This prevents PRL-3-mediated signaling in, inhibits the proliferation of and induces apoptosis in PRL-3-expressing tumor cells. PRL-3, a member of the PRL family of protein tyrosine kinases, is upregulated in a variety of tumor cells. Its expression is associated with increased invasiveness, higher metastatic potential, increased tumor cell survival and poor prognosis.


anti-programmed cell death protein 1 antibody expressing pluripotent killer T lymphocytes

A specific population of pluripotent killer (PIK) T cells that have been induced to express high levels of antibodies against the negative immunoregulatory human cell surface receptor programmed cell death protein 1 (PD-1; PDCD1; CD279), with potential antitumor activity. Although the exact mechanism(s) of action through which PIK-PD-1 cells exert their effects has yet to be elucidated, upon infusion, these cells secrete antibodies that target PD-1 expressed on the surface of activated T cells and tumor cells. This may block the interaction of PD-1 with its ligands, programmed cell death 1 ligand 1 (PD-L1, PD-1L1; CD274) and PD-1 ligand 2 (PD-L2, PD-1L2; CD273). The inhibition of ligand binding prevents PD-1-mediated signaling and results in both T-cell activation and the induction of T-cell-mediated immune responses against tumor cells. PD-1, an immunoglobulin (Ig) superfamily transmembrane protein and inhibitory receptor, negatively regulates T-cell activation; PD-L1 is overexpressed on certain cancer cells, and PD-L2 is primarily expressed on antigen presenting cells (APCs).


anti-prolactin receptor antibody LFA102

A neutralizing antibody against the prolactin receptor (PRLR) with potential antineoplastic activity. Upon administration, anti-prolactin receptor antibody LFA102 binds to PRLR and prevents the binding of the peptide hormone prolactin (PRL) to its receptor. This binding induces an antibody-dependent cellular cytotoxicity (ADCC) and may eventually prevent tumor cell proliferation in PRLR-positive cancer cells. PRLR/PRL signaling pathway is frequently overexpressed in breast and prostate cancer .


anti-PSCA fully human monoclonal antibody AGS-1C4D4

An IgG1k fully human monoclonal antibody directed against the human prostate stem cell antigen (PSCA) with potential antineoplastic activity. Anti-PSCA fully human monoclonal antibody AGS-1C4D4 selectively targets and binds to PSCA, triggering complement-dependent cell lysis and antibody-dependent cell-mediated cytotoxicity in tumor cells expressing PSCA. PSCA is a glycosyl-phosphatidylinositol (GPI)-linked cell surface antigen found in cancer s of the bladder, pancreas, and prostate.


anti-PSMA monoclonal antibody MDX1201-A488

A recombinant, human monoclonal antibody targeting an extracellular epitope of human prostate specific membrane antigen (PSMA) that is conjugated with a fluorescent dye A488, with potential imaging activity. Upon intravenous administration, the MDX1201 moiety of anti-PSMA monoclonal antibody MDX1201-A488 targets PSMA expressed on cancer cells. Subsequently, the A488 moiety can then be visualized by fluorescence-based imaging and the amount of PSMA-expressing tumor cells can be assessed. A488 is a photostable fluorescent dye with a high quantum yield. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.


anti-PSMA monoclonal antibody-MMAE conjugate

An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody directed against prostate-specific membrane antigen (PSMA), conjugated via a stable, enzyme-cleavable linker to monomethylauristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. The monoclonal antibody moiety of this conjugate selectively binds to PSMA, a protein which is abundantly expressed on the surface of metastatic and hormone-refractory prostate cancer cells. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis.


anti-PSMA/CD3 BiTE antibody AMG 160

A half-life extended (HLE), bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) human prostate specific membrane antigen (PSMA), fused to one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-PSMA/CD3 BiTE antibody AMG 160, this bispecific antibody binds to both CD3 on cytotoxic T lymphocytes (CTLs) and PSMA found on PSMA-expressing tumor cells. This activates and redirects CTLs to PSMA-expressing tumor cells, which results in the CTL-mediated cell death of PSMA-expressing tumor cells. PSMA, a tumor associated antigen, is overexpressed on the surface of metastatic and hormone-refractory prostate cancer cells.


anti-PSMA/CD3 BiTE monoclonal antibody MT112

A recombinant T-cell engaging bispecific monoclonal antibody (BiTE) directed against human prostate specific membrane antigen (PSMA) and the CD3 epsilon subunit of the T cell receptor complex, with potential immunostimulating and antineoplastic activities. Anti-PSMA/CD3 BiTE monoclonal antibody MT112 possesses two antigen-recognition sites, one for PSMA, and one for the CD3 complex, a group of T cell surface glycoproteins that complex with the T cell receptor (TCR). This bispecific monoclonal antibody brings PSMA-expressing tumor cells and cytotoxic T lymphocytes (CTLs) together, which may result in the CTL-mediated cell death of PSMA-expressing cells. PSMA, a tumor associated antigen, is overexpressed on the surface of metastatic and hormone-refractory prostate cancer cells.


anti-PSMA/CD3 monoclonal antibody MOR209/ES414

An anti-prostate specific membrane antigen (PSMA)/anti-CD3 bispecific humanized monoclonal antibody, with potential immunostimulatory and antineoplastic activities. Anti-PSMA/CD3 monoclonal antibody MOR209/ES414 possesses two antigen-recognition sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for PSMA, a tumor-associated antigen (TAA) overexpressed on the surface of prostate tumor cells. Upon intravenous administration of MOR209/ES414, this bispecific antibody simultaneously binds to both CD3-expressing T-cells and PSMA-expressing cancer cells, thereby crosslinking PSMA-expressing tumor cells and cytotoxic T-lymphocytes (CTLs). This results in CTL-mediated cancer cell lysis of prostate cancer cells expressing PSMA.


anti-PSMA/PBD ADC MEDI3726

An antibody-drug conjugate (ADC) consisting of an engineered version of anti-human prostate-specific membrane antigen (PSMA) monoclonal antibody J591 conjugated, via a valine-alanine dipeptide linker, to tesirine, a cytotoxic, DNA minor groove crosslinking agent and pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration of anti-PSMA/PBD ADC MEDI3726, the antibody moiety targets the cell surface antigen PSMA, which is found on prostate cancer cells. Upon antibody/antigen binding, internalization and lysosome-mediated cleavage of the dipeptide linker, the cytotoxic PBD moiety is released. In turn, the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of PSMA-overexpressing tumor cells. PSMA is overexpressed by prostate cancer s; its expression is associated with poor prognosis and metastasis.


anti-PTK7/Auristatin-0101 antibody-drug conjugate PF-06647020

An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody against human inactive tyrosine-protein kinase 7 (PTK7) linked, via a cleavable valine-citrulline linker, to an analog of the auristatin microtubule inhibitor dolastatin 10, auristatin-0101, with potential antineoplastic activity. Upon administration, anti-PTK7/Auristatin-0101 ADC PF-06647020 targets and binds to PTK7 expressed on tumor cells. Upon binding, internalization and cleavage, auristatin-0101 binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and apoptosis of PTK7-expressing tumor cells. PTK7, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer cells.


anti-PVRIG monoclonal antibody COM701

A humanized, hybridoma monoclonal antibody against the poliovirus receptor-related immunoglobulin (PVRIG; PVR Related Immunoglobulin Domain Containing Protein; CD112R), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PVRIG monoclonal antibody COM701 targets and binds to PVRIG expressed on cytotoxic T lymphocytes (CTLs) and natural killer (NK) cells within the tumor microenvironment (TME). This blocks the interaction of PVRIG with its ligand nectin cell adhesion molecule 2 (poliovirus receptor-related 2; PVRL2; CD112), which is overexpressed on a variety of tumor cell types. Inhibiting the activation of PVRIG, abrogates the PVRIG-induced inhibition of T-lymphocyte and NK-cell activation. This activates CTLs and NK cells, enhances anti-tumor responses and immune-mediated tumor cell killing, and inhibits tumor cell proliferation. PVRIG, a member of the B7/CD28 family and immune checkpoint receptor that, upon activation, negatively regulates the activation of various immune cells. It plays a key role in immunosuppression.


anti-ROR1 ADC VLS-101

An antibody-drug conjugate (ADC) composed of a monoclonal antibody against the tumor-associated antigen (TAA) receptor tyrosine kinase-like orphan receptor 1 (ROR1) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of VLS-101 targets and binds to ROR1 expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the ROR1-expressing cancer cells, through an as of yet unknown mechanism of action. ROR1, also known as neurotrophic tyrosine kinase, receptor-related 1 (NTRKR1), is expressed during embryogenesis and by certain leukemias. It plays key roles in tumor cell proliferation and survival.


anti-RSPO3 monoclonal antibody OMP-131R10

An immunoglobulin (Ig) G1 humanized monoclonal antibody targeting human R-spondin 3 (RSPO3), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, the anti-RSPO3 monoclonal antibody OMP-131R10 targets and binds to RSPO3 expressed on tumor cells. This prevents the activation of RSPO3, and inhibits both the binding of RSPO3 to leucine-rich repeat-containing G-coupled receptors (LGRs) and the activation of the RSPO-LGR pathway. This may result in an inhibition of both cancer stem cell (CSC) survival and the proliferation of cancer cells in which this pathway is overactivated. The RSPO-LGR pathway is a CSC pathway activated in a variety of cancer cell types.


anti-RSV nanobody ALX-0171

A trivalent nanobody composed of three monovalent Nb017 moieties linked with glycine-serine (GS) linkers, directed against the fusion protein (F protein) of human respiratory syncytial virus (RSV), with potential activity against RSV infections. Upon administration via nebulization and inhalation, the anti-RSV nanobody ALX-0171 targets and binds to RSV F protein, neutralizing the virus, and preventing viral entry into host cells. RSV F protein is a small envelope glycoprotein required for cytopathic syncytia formation that results from cell-to-cell fusion.


anti-S15 monoclonal antibody NC318

A humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting sialic acid binding Ig-like lectin 15 (Siglec-15; SIGLEC15; S15), a member of the sialic acid-binding immunoglobulin type lectins, with potential antineoplastic and immunomodulatory activities. Upon administration, anti-S15 monoclonal antibody NC318 targets and binds to S15 on the surface of tumor-associated macrophages (TAMs) and certain tumor cells. Binding to S15 may disrupt TAM-mediated activities such as promotion of tumor initiation and metastasis of tumor cells, inhibition of T-cell responses, and stimulation of tumor angiogenesis and disease progression. S15, a highly conserved type 1 cell surface protein, normally involved in osteoclast differentiation and bone remodeling, may play a role in the survival and differentiation of TAMs.


anti-sCLU monoclonal antibody AB-16B5

A humanized, immunoglobulin (Ig) G2 monoclonal antibody against the secreted form of human clusterin (sCLU) expressed by tumor cells, with potential antineoplastic and anti-metastatic activities. Upon administration, anti-sCLU monoclonal antibody AB-16B5 specifically binds to tumor-associated sCLU and inhibits its activity. This inhibits both the sCLU-mediated signal transduction pathways and epithelial-to-mesenchymal transition (EMT), which leads to the inhibition of tumor cell migration and invasion. In addition, AB-16B5 enhances chemo-sensitivity. sCLU, a heterodimeric disulfide-linked glycoprotein overexpressed by various types of cancer cells, contributes to proliferation and survival of cancer cells, and stimulates tumor cell EMT.


anti-SEMA4D monoclonal antibody VX15/2503

A humanized IgG4 monoclonal antibody against the semaphorin 4D (SEMA4D; CD100) with potential immunomodulating and antineoplastic activities. Upon administration, anti-SEMA4D monoclonal antibody VX15/2503 binds to and neutralizes SEMA4D, thereby preventing binding of SEMA4D to its receptor plexin-B1 (PLXNB1). By blocking the interaction of SEMA4D and PLXNB1, VX15/2503 may cause an inhibition of endothelial cell activation and migration, eventually leading to an inhibition of angiogenesis and tumor cell proliferation. Semaphorin 4D, a large cell surface antigen found on the resting T-cell and overexpressed in a variety of tumor cell types, plays an important role in vascular growth, tumor progression, invasion and immune cell regulation.


anti-SIRPa monoclonal antibody CC-95251

A monoclonal antibody targeting signal-regulatory protein alpha (SIRPa; CD172a) with potential immunostimulating and antineoplastic activities. Upon intravenous administration, anti-SIRPa monoclonal antibody CC-95251 targets and binds to SIRPa, a cell surface protein expressed on macrophages, thereby blocking the interaction between SIRPa and cluster of differentiation 47 (CD47) expressed on tumor cells. This prevents CD47/SIRPa-mediated signaling and abrogates the CD47/SIRPa-mediated inhibition of phagocytosis. This induces pro-phagocytic signaling mediated by the binding of calreticulin (CRT), which is specifically expressed on the surface of tumor cells, to low-density lipoprotein (LDL) receptor-related protein (LRP), expressed on macrophages. This results in macrophage activation and the specific phagocytosis of tumor cells. In addition, blocking CD47/SIRPa-mediated signaling activates both an anti-tumor T-lymphocyte immune response and T-cell-mediated killing of CD47-expressing tumor cells. SIRPa, also known as tyrosine-protein phosphatase non-receptor type substrate 1, mediates negative regulation of phagocytosis, mast cell activation and dendritic cell activation. CD47, also called integrin-associated protein (IAP), is a tumor-associated antigen (TAA) expressed on normal, healthy hematopoietic stem cells (HSCs) and overexpressed on the surface of a variety of cancer cells. Expression of CD47, and its interaction with SIRPa, leads to the inhibition of macrophage activation and protects cancer cells from phagocytosis, which allows cancer cells to proliferate.


anti-SLITRK6 monoclonal antibody-MMAE conjugate AGS15E

An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against SLIT and NTRK-like protein 6 (SLITRK6), covalently linked to the cytotoxic agent monomethyl auristatin E (MMAE), an auristatin derivative and a potent inhibitor of microtubule polymerization, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of AGS15E binds to SLITRK6 expressed on tumor cells, which facilitates both AGS15E internalization and the intracellular delivery of MMAE. Upon cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and tumor cell apoptosis. SLITRK6, a member of the Slitrk family of leucine-rich repeat (LRR) neuronal transmembrane proteins, is minimally expressed in normal tissue but overexpressed in a variety of cancer s, including bladder cancer , some forms of lung cancer , breast cancer and glioblastoma.


anti-SSTR2/CD3 monoclonal antibody XmAb18087

A humanized, Fc domain-containing, bispecific monoclonal antibody targeting human CD3, a T-cell surface antigen, and somatostatin receptor 2 (SSTR2), a tumor-associated antigen (TAA) expressed on certain cancer cells, with potential antineoplastic activity. Upon administration, anti-SSTR2/CD3 monoclonal antibody XmAb18087 binds to both T cells and SSTR2-expressing cancer cells. The resulting cross-linkage may trigger a potent cytotoxic T-lymphocyte (CTL) response against the SSTR2-expressing cancer cells. The inclusion of an Fc domain on the antibody prolongs the half-life of the bispecific antibody.


anti-TAG-72 monoclonal antibody CC49-streptavidin conjugate

An immunoconjugate containing CC49, a monoclonal antibody (MAb) directed against the tumor-associated antigen (TAA) tumor-associated glycoprotein 72 (TAG-72), conjugated to streptavidin, a nonglycosylated homotetrameric protein that has four high affinity binding sites for biotin, with potential use in pre-targeted radioimmunotherapy (PRIT). Upon administration of anti-TAG-72 MAb CC49-streptavidin conjugate, the MAb moiety targets and binds to TAG-72 expressed on cancer cells. Upon subsequent administration of a biotin-based radioconjugate, such as yttrium Y 90 DOTA-biotin, the biotin moiety of the radioconjugate binds to the streptavidin moiety of MAb CC49-streptavidin conjugate, which localizes the biotin-conjugated radionuclide to the tumor site. Upon cellular internalization, a cytotoxic does of radiation may be specifically delivered to TAG-72-expressing tumor cells. TAG-72, a human pancarcinoma antigen, is overexpressed on a variety of cancer cell types.


anti-TF monoclonal antibody ALT-836

A recombinant human-mouse chimeric monoclonal antibody against human tissue factor (TF), with potential antiangiogenic, anticoagulant and anti-inflammatory activities. Upon administration, anti-TF monoclonal antibody ALT-836 binds to TF or the TF-Factor VIIa (FVIIa) complex preventing binding and activation of Factor X (FX) and Factor IX (FIX). This may prevent thrombin formation and cancer -associated venous thromboembolism, and may inhibit angiogenesis and tumor cell proliferation. TF, a transmembrane protein and procoagulant, is overexpressed in many tumor cell types, and is correlated with metastasis, angiogenesis, tumor growth and tumor-associated thrombosis.


anti-TGF-beta monoclonal antibody NIS793

A monoclonal antibody directed against human transforming growth factor beta (TGF-beta), with potential antineoplastic activity. Anti-TGF-beta monoclonal antibody NIS793 specifically targets and binds to TGF-beta, thereby preventing the activation of TGF-beta-mediated signaling pathways. TGF-beta, a pro-inflammatory mediator that is mutated and/or overexpressed in a number of cancer cell types, is involved in cancer cell proliferation and migration, and tumor progression.


anti-TGF-beta monoclonal antibody SAR-439459

A monoclonal antibody (mAb) directed against human transforming growth factor beta (TGF-beta; TGFb), with potential antineoplastic activity. Upon administration, anti-TGF-beta monoclonal antibody SAR-439459 specifically targets and binds to TGF-beta, thereby preventing the activation of TGF-beta-mediated signaling pathways. This may inhibit the proliferation of tumor cells in which TGF-beta is overactivated. TGF-beta, a pro-inflammatory mediator that is mutated and/or overexpressed in a variety of cancer cell types, is involved in cancer cell proliferation and migration, and in tumor progression.


anti-TGF-beta RII monoclonal antibody IMC-TR1

A monoclonal antibody directed against transforming growth factor-beta receptor type II (TGF-beta RII) with potential antineoplastic activity. Anti-TGF-beta RII monoclonal antibody IMC-TR1 specifically targets and binds to TGF-beta R11, thereby preventing the activation of TGF-beta RII-mediated signaling pathways. TGF-beta RII is mutated in a number of cancer cell types and is involved in cancer cell proliferation and tumor progression.


anti-thymocyte globulin

A purified gamma immunoglobulin (IgG) with immunosuppressive activity. Obtained from rabbits that have been immunized with human thymocytes, antithymocyte globulin specifically recognizes and destroys T lymphocytes. Although the exact mechanism of action is not completely understood, it appears to involve T lymphocyte clearance from the circulation and modulation of T lymphocyte activity. Administering antithymocyte globulin with chemotherapy prior to stem cell transplantation may reduce the risk of graft-versus-host disease.


anti-thyroglobulin mTCR-transduced autologous peripheral blood lymphocytes

Peripheral blood lymphocytes (PBLs) transduced with a gene encoding for a thyroglobulin (TG)-specific murine T-cell receptor (mTCR), with potential antineoplastic activity. PBLs are harvested from a thyroid cancer patient, and transfected with a retroviral vector that encodes the mTCR gene specific for the human TG antigen. The transduced PBLs are then expanded in culture. When reintroduced to the patient, these anti-TG mTCR-expressing PBLs target and bind to TG-overexpressing tumor cells, which results in both cytokine secretion and tumor cell lysis. TG is a thyroid-specific protein.


anti-TIGIT monoclonal antibody BMS-986207

A human monoclonal antibody targeting the co-inhibitory molecule and immune checkpoint inhibitor T-cell immunoreceptor with immunoglobulin (Ig) and immunoreceptor tyrosine-based inhibitory motif (ITIM) domains (TIGIT), with potential immune checkpoint inhibitory activity. Upon administration, anti-TIGIT monoclonal antibody BMS-986207 binds to TIGIT expressed on various immune cells, particularly on tumor-infiltrating T lymphocytes (TILs), thereby preventing the interaction of TIGIT with its ligands CD112 (nectin-2; poliovirus receptor related-2; PVRL2) and CD155 (poliovirus receptor; PVR; nectin-like protein 5; NECL-5). This enhances the interaction of CD112 and CD155 with the costimulatory receptor CD226 (DNAX Accessory molecule-1; DNAM-1), which is expressed on immune cells, such as natural killer (NK) cells and CD8+ T cells, and leads to CD226 dimerization and CD226-mediated signaling. This activates the immune system to exert a T-cell-mediated immune response against cancer cells. TIGIT, a member of the Ig super family and an immune inhibitory receptor, plays a key role in the suppression of T-cell proliferation and activation; it is involved in tumor cell immune evasion, and the inhibition of antiviral immune responses.  


anti-TIGIT monoclonal antibody OMP-313M32

A monoclonal antibody targeting the human co-inhibitory molecule and immune checkpoint inhibitor T-cell immunoreceptor with immunoglobulin (Ig) and immunoreceptor tyrosine-based inhibitory motif (ITIM) domains (TIGIT), with potential immune checkpoint inhibitory activity. Upon administration, anti-TIGIT monoclonal antibody OMP-313M32 binds to TIGIT expressed on various immune cells, including T cells, and prevents the interaction of TIGIT with its ligands CD112 (nectin-2; poliovirus receptor related-2; PVRL2) and CD155 (poliovirus receptor; PVR; nectin-like protein 5; NECL-5). This enhances the interaction of CD112 and CD155 with the costimulatory receptor CD226 (DNAX Accessory molecule-1; DNAM-1), which is expressed on immune cells, such as natural killer (NK) cells and CD8-positive T cells, and leads to CD226 dimerization and CD226-mediated signaling. This activates the immune system to exert a T-cell-mediated immune response against cancer cells. TIGIT, a member of the Ig super family and an immune inhibitory receptor, plays a key role in the suppression of T-cell proliferation and activation; it is involved in tumor cell immune evasion and the inhibition of antiviral immune responses.


anti-TIM-3 antibody BMS-986258

An antibody against the inhibitory T-cell receptor T-cell immunoglobulin and mucin domain-containing protein 3 (TIM-3; TIM3; hepatitis A virus cellular receptor 2; HAVCR2), with potential immune checkpoint inhibitory and antineoplastic activities. Following administration, anti-TIM-3 antibody BMS-986258 binds to TIM-3 that is expressed on certain T cells, including tumor infiltrating lymphocytes (TILs). This abrogates T-cell inhibition, activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which together result in decreased tumor growth. TIM-3, a transmembrane protein and immune checkpoint receptor, is associated with tumor-mediated immune suppression.


anti-TIM-3 monoclonal antibody BGB-A425

A humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the inhibitory T-cell receptor T-cell immunoglobulin and mucin domain-containing protein 3 (TIM-3; TIM3; hepatitis A virus cellular receptor 2; HAVCR2), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, BGB-A425 binds to TIM-3 expressed on certain T cells, including tumor-infiltrating lymphocytes (TILs), thereby preventing the engagement of TIM-3 by its ligands, phosphatidylserine (PtdSer) and galectin-9. This abrogates T-cell inhibition, activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which results in a reduction in tumor cell proliferation. TIM-3, a transmembrane protein and immune checkpoint receptor, is associated with tumor-mediated immune suppression.  


anti-TIM3 monoclonal antibody LY3321367

A monoclonal antibody against the inhibitory T-cell receptor T-cell immunoglobulin and mucin domain-containing protein 3 (TIM-3; TIM3; hepatitis A virus cellular receptor 2; HAVCR2), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-TIM-3 monoclonal antibody LY3321367 binds to TIM-3 expressed on certain T cells, including tumor-infiltrating lymphocytes (TILs). This abrogates T-cell inhibition, activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which results in a reduction in tumor growth. TIM-3, a transmembrane protein and immune checkpoint receptor, is associated with tumor-mediated immune suppression.  


anti-TIM-3 monoclonal antibody Sym023

A recombinant, fully human monoclonal antibody against the inhibitory T-cell receptor T-cell immunoglobulin and mucin domain-containing protein 3 (TIM-3; TIM3; hepatitis A virus cellular receptor 2; HAVCR2), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-TIM-3 monoclonal antibody Sym023 binds to TIM-3 expressed on certain T cells, including tumor infiltrating lymphocytes (TILs). This abrogates T-cell inhibition, activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which results in a reduction in tumor cell proliferation. TIM-3, a transmembrane protein and immune checkpoint receptor, is associated with tumor-mediated immune suppression.


anti-TIM-3 monoclonal antibody TSR-022

A monoclonal antibody against the inhibitory T-cell receptor, T-cell immunoglobulin and mucin domain-containing protein 3 (TIM-3; TIM3; hepatitis A virus cellular receptor 2; HAVCR2), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-TIM-3 monoclonal antibody TSR-022 binds to TIM-3 expressed on certain T cells, including tumor infiltrating lymphocytes (TILs). This abrogates T-cell inhibition, activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which results in a reduction in tumor growth. TIM-3, a transmembrane protein and immune checkpoint receptor, is associated with tumor-mediated immune suppression.  


anti-tissue factor monoclonal antibody MORAb-066

A humanized monoclonal antibody against human tissue factor (TF), with potential antiangiogenic, anticoagulant and anti-inflammatory activities. Upon administration, anti-TF monoclonal antibody MORAb-066 binds to TF and prevents Factor VIIa (FVIIa) from binding, thereby interfering with the activation of Factor X (FX) into FXa. This may prevent thrombin formation and cancer -associated venous thromboembolism, and may inhibit angiogenesis and tumor cell proliferation. TF, a transmembrane protein and initiator of the coagulation cascade, is overexpressed in many tumor cells and tumor endothelial cells; its expression is correlated with metastasis, angiogenesis, tumor cell growth and tumor-associated thrombosis.  


anti-TLR2 monoclonal antibody OPN-305

A humanized immunoglobulin (Ig) G4 monoclonal antibody directed against toll-like receptor type 2 (TLR2), with potential anti-inflammatory and antineoplastic activities. Upon intravenous administration, OPN-305 binds to the ligand-binding site on the TLR2 receptor and blocks the activation of TLR2-mediated innate immunity signaling. This prevents the TLR2-mediated production of pro-inflammatory mediators and prevents inflammation. TLR2, a member of the TLR family primarily found on leukocytes, plays a key role in the activation of innate immunity; it is overexpressed in various inflammatory diseases and in certain types of cancer .


anti-transthyretin siRNA ALN-TTR02

A lipid nanoparticle (LNP)-based formulation consisting of small-interfering RNAs (siRNAs) directed against transthyretin (TTR)-encapsulated in lipids, which has potential use in the treatment of TTR-mediated amyloidosis (ATTR). Upon intravenous administration of ALN-TTR02, the lipid formulation promotes the uptake by cells. The siRNAs bind to TTR mRNAs, which may result in the inhibition of both the translation and expression of the TTR protein. ATTR is caused by mutations in the TTR gene and results in the formation of abnormal amyloid proteins that accumulate in and cause damage to various body organs and tissues.


anti-TROP2/DXd antibody-drug conjugate DS-1062a

An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody against tumor-associated antigen (TAA) trophoblast cell surface protein 2 (calcium signal transducer 2; TROP2; TROP-2; TACSTD2) conjugated, via an enzymatically cleavable tetrapeptide-based linker, to the cytotoxic DNA topoisomerase I inhibitor and exatecan (DX-8951) derivative DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration of the anti-TROP2/DXd ADC DS-1062a, the anti-TROP2 antibody targets and binds to TROP2 expressed on tumor cells. Upon cellular uptake and lysosomal degradation of the linker, DXd targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication and apoptosis. This inhibits tumor cell proliferation of TROP2-expressing tumor cells. TROP2 is a transmembrane protein overexpressed in various tumors while its expression is low and/or restricted in normal, healthy tissues. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival. The ADC allows for reduced systemic exposure and enhanced delivery of the cytotoxic agent DXd.  


antitumor B key active component-alpha

An orally available concentrated preparation of antitumor B (ATB, Zeng Sheng Ping), a Chinese herbal formula comprised of Sophora tonkinensis, Polygonum bistorta, Prunella vulgaris, Sonchus brachyotus, Dictamnus dasycarpus, and Dioscorea bulbifera, with potential antineoplastic activity. Upon administration, antitumor B key active component-alpha (ATB-KAC-alpha) may, through a not yet fully elucidated mechanism, inhibit tumorigenesis and prevent the development of certain cancer s.


anti-TWEAK monoclonal antibody RO5458640

A humanized monoclonal antibody directed against the apoptotic ligand TNF-like weak inducer of apoptosis (TWEAK) with potential antineoplastic activity. Anti-TWEAK monoclonal antibody RO5458640 binds to TWEAK and prevents the binding of TWEAK to its receptor, FGF-inducible molecule 14 (Fn14), thereby blocking the TWEAK/Fn14 signaling. This may prevent tumor cell proliferation, invasion, migration and angiogenesis. TWEAK has pleiotropic effects, mediating proinflammatory and pro-angiogenic activity as well as stimulation of invasion, migration, and survival mediated via its receptor Fn14; Fn14 is expressed at relatively low levels in normal tissues, but is elevated in tumor cells and locally in injured and diseased tissues.


anti-VEGF anticalin PRS-050-PEG40

A pegylated, proprietary lipocalin that targets human vascular endothelial growth factor (VEGF), with potential antineoplastic activity. Pegylated anti-VEGF anticalin PRS-050 specifically targets and binds to VEGF receptor 2 (VEGFR2 or KDR), thereby preventing its activity. This may inhibit angiogenesis and eventually reduce tumor cell growth.


anti-VEGF monoclonal antibody hPV19

A humanized monoclonal antibody directed against human vascular endothelial growth factor (VEGF), with potential anti-angiogenic and antineoplastic activities. Upon administration, anti-VEGF monoclonal antibody hPV19 targets and binds to VEGFR at a unique binding site and inhibits VEGF binding to its receptors, VEGFR1 and VEGFR2, thereby preventing VEGF/VEGFR-mediated signaling. This prevents the growth and maintenance of tumor blood vessels. This decreases nutrient supply to tumor cells, resulting in tumor cell death. Increased VEGF/VEGFR signaling is associated with increased invasiveness and decreased survival.


anti-VEGF/ANG2 nanobody BI 836880

A nanobody directed against angiopoietin-2 (Ang2; ANGPT2)- and vascular endothelial growth factor (VEGF)-derived peptides, with potential antiangiogenic and antineoplastic activities. Anti-VEGF/ANG2 nanobody BI 836880 binds to Ang2 and VEGF and inhibits receptor binding; this prevents Ang2- and VEGF-mediated signaling and inhibits both tumor angiogenesis and tumor cell proliferation. Both VEGF and Ang2 are upregulated in a variety of cancer cell types and each plays a crucial role in angiogenesis. The nanobody is based on functional fragments of single-chain antibodies.


anti-VEGF-C monoclonal antibody VGX-100

A fully human monoclonal antibody directed against the human vascular endothelial growth factor C (VEGFC or Flt4 ligand) with potential antiangiogenic activity. Anti-VEGFC monoclonal antibody VGX-100 specifically binds to and inhibits VEGFC protein, thereby preventing its binding to VEGFR3 (FLT4) or VEGFR2 (KDR or FLK1). This may prevent VEGFC-mediated signaling and may lead to the inhibition of vascular and lymphatic endothelial cell proliferation. The inhibition of tumor angiogenesis and lymphangiogenesis may eventually decrease tumor cell proliferation and prevent metastasis. VEGFC is overexpressed in a variety of cancer cells, and is associated with increased invasiveness and decreased survival.


anti-VEGFR2 monoclonal antibody HLX06

A fully human monoclonal antibody directed against human vascular endothelial growth factor receptor 2 (VEGFR-2) with potential anti-angiogenesis and antineoplastic activities. Upon administration, anti-VEGFR2 monoclonal antibody HLX06 specifically binds to and inhibits VEGFR-2, which may inhibit tumor angiogenesis and tumor cell proliferation. VEGFR-2, a tyrosine-protein kinase that plays an essential role in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells, is overexpressed in certain tumor types.


anti-VEGFR2-CAR retroviral vector-transduced autologous T lymphocytes

Autologous human CD8-positive T-lymphocytes transduced with a recombinant retroviral vector encoding a chimeric T cell receptor (chimeric antigen receptor or CAR) consisting of an anti-vascular endothelial growth factor receptor type 2 (VEGFR2) scFv (single chain variable fragment), linked to the transmembrane domain of human CD8alpha and coupled to the costimulatory signaling domains of both CD28 and 4-1BB (CD137), and the CD3 zeta chain of the T-cell receptor (TCR), with potential immunostimulating and antineoplastic activities. Autologous peripheral blood lymphocytes (PBLs) from a patient with VEGFR2-positive cancer are pulsed with a retroviral vector that encodes the CAR gene specific for VEGFR2. After expansion in culture and reintroduction into the patient, the anti-VEGFR2 CAR-gene engineered CD8+ lymphocytes express anti-VEGFR2-CAR on their cell surfaces and bind to the VEGFR2 antigen on tumor cell surfaces. Subsequently, VEGFR2-expressing tumor cells are lysed. VEGFR2, a receptor tyrosine kinase (RTK) overexpressed by a variety of cancer cell types, belongs to the VEGFR superfamily and plays key roles in tumor cell proliferation, survival, invasion and tumor angiogenesis. The co-stimulatory molecules are required for optimal T-cell activation.


anti-VEGFR3 monoclonal antibody IMC-3C5

A fully-human monoclonal antibody directed against human vascular endothelial growth factor receptor 3 (VEGFR-3; Flt-4) with antiangiogenic activity. Anti-VEGFR-3 monoclonal antibody IMC-3C5 specifically binds to and inhibits VEGFR-3, which may result in inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR-3 plays a critical role in the embryonic vascular system development but is restricted postnatally to endothelial cells of lymphatic vessels and found to be expressed in many solid and hematologic malignancies.


Antivert

(Other name for: meclizine hydrochloride)


antiviral agent CSJ148

An antiviral agent that can potentially be used to prevent replication of human cytomegalovirus (HCMV).


anti-VISTA monoclonal antibody JNJ 61610588

A human monoclonal antibody against the protein V-domain immunoglobulin (Ig) suppressor of T-cell activation (VISTA; programmed death 1 homolog; PD1H; PD-1H), with potential negative checkpoint regulatory and antineoplastic activities. Upon administration, JNJ 61610588 targets and binds to VISTA. This inhibits VISTA signaling, abrogates the VISTA-induced suppression of T-lymphocyte-mediated immune responses, enhances cytotoxic T-cell responses against tumor cells and inhibits tumor cell growth. VISTA, mainly expressed on hematopoietic cells, plays a key role in immunosuppression.


anti-von Willebrand factor nanobody

A humanized, bivalent anti-von Willebrand factor (VWF) nanobody with potential anti-platelet activity. Anti-von Willebrand factor nanobody specifically binds to the A1 domain of the VWF molecule, thereby inhibiting and neutralizing VWF activity. This prevents the interaction of VWF with the platelet glycoprotein (Gp)Ib-IX-V receptor and prevents VWF-mediated platelet aggregation. VWF is a glycoprotein and plays a key role in blood coagulation. Increased VWF, which is seen in a number of diseases, is associated with an increased risk in thrombosis. The nanobody formulation allows for rapid distribution, onset of action and clearance. The nanobody is based on the smallest functional fragments of single-chain antibodies that naturally occur in the Camelidae family.


Antrin

(Other name for: motexafin lutetium)


Antrodia cinnamomea supplement

A dietary supplement containing extract from the medicinal fungus Antrodia cinnamomea with potential antiangiogenic, hepatoprotective and antioxidant activities. The components in Antrodia cinnamomea supplement are rather complex, however, rich in triterpenoids, polysaccharides, nucleosides (adenosine) nucleic acids, superoxide dismutase, other small molecular weight proteins and steroid like compounds. Neutral sugars in this supplement show inhibitory activity on endothelial tube formation, while maleimide and maleic anhydride derivative components in the extract, such as antrodin B and antrodin C and their metabolites, exhibit significant cytotoxic effects on tumor cells and hepatitis C virus.


AO+ Mist

(Other name for: topical ammonia-oxidizing bacteria-based probiotic solution)


apalutamide

A small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity. Apalutamide binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells.


apatinib

An orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.


apatorsen

A second-generation antisense oligonucleotide targeting heat shock protein 27 (Hsp27) with potential antitumor and chemosensitizing activities. Apatorsen suppresses tumor cell expression of Hsp27, which may induce tumor cell apoptosis and enhance tumor cell sensitivity to cytotoxic agents. Hsp27, a chaperone belonging to the small heat shock protein (sHsp) group of proteins, is a cytoprotective protein that supports cell survival under conditions of stress; it has been found to be over-expressed in a variety of human cancer s.


apaziquone

An indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic and radiosensitization activities. Apaziquone is converted to active metabolites in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. The active metabolites alkylate DNA, resulting in apoptotic cell death. This agent displays activity towards both hypoxic solid tumors, which exhibits higher expression of cytochrome P450 reductase, and well-oxygenated malignant cells that overexpress the bioreductive enzyme NQO1 (NAD(P)H: quinone oxidoreductase). Apaziquone may selectively sensitize hypoxic tumor cells to radiocytotoxicity.


APC8015F

A cell-based vaccine composed of previously frozen autologous antigen-presenting peripheral blood mononuclear cells (enriched for a dendritic cell fraction) that have been exposed to a recombinant protein consisting of granulocyte-macrophage colony-stimulating factor (GM-CSF) fused to prostatic-acid phosphatase (PAP), a protein expressed by prostate cancer cells. Upon administration, the vaccine may stimulate an antitumor T-cell response against tumor cells expressing PAP.


APE1/Ref-1 redox inhibitor APX3330

An orally bioavailable inhibitor of apurinic/apyrimidinic endonuclease 1/reduction-oxidation (redox) effector factor-1 (APE1/Ref-1; APEX1), with potential anti-angiogenic and antineoplastic activities. Upon administration, the APE1/Ref-1 Inhibitor APX3330 selectively targets and binds to APE1/Ref-1. This inhibits the redox-dependent signaling activity of APE1/Ref-1, by preventing the reduction and activation of numerous APE1/Ref-1-dependent oncogenic transcription factors (TFs), such as nuclear factor kappa B (NF-kB), AP-1, STAT3, p53, NRF2 and HIF-1alpha, that are involved in signaling, cell proliferation, tumor progression and survival of cancer cells. Therefore, this agent inhibits the activation of multiple TF-mediated signaling pathways and inhibits tumor cell proliferation and survival. APE1/Ref-1, a multifunctional protein overexpressed in many cancer cell types, plays a key role as a redox regulator of transcription factor activation and in base excision repair upon DNA damage. It drives cancer cell proliferation, migration, drug resistance, angiogenesis and inflammation and its expression level correlates with increased tumor aggressiveness and decreased patient survival. APX3330 specifically blocks the redox activity of APE1/Ref-1 and does not affect its ability to act as a DNA repair endonuclease.


APF530

A controlled-release formulation of the 5-hydroxytryptamine 3 (5-HT3) antagonist granisetron, in which granisteron is encapsulated in a biodegradable poly(ortho ester) polymer, with antiemetic activity. Upon subcutaneous administration, APF530 slowly erodes and releases the active ingredient granisetron over a period of approximately 5 days. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-HT3 receptors, resulting in the suppression of nausea and vomiting.


apilimod dimesylate capsule

A capsule containing the dimesylate salt form of apilimod, an inhibitor of the class III PI kinase phosphatidylinositol-3-phosphate 5-kinase (PIKfyve), with potential antineoplastic and immunomodulatory activities. Upon oral administration of apilimod dimesylate capsule, apilimod selectively binds to and inhibits PIKfyve. The inhibition leads to disruption of PIKfyve-mediated signal transduction pathways and eventually inhibits tumor cell growth in PIKfyve-overexpressing tumor cells. Also, PIKfyve inhibition by apilimod inhibits the toll-like receptor (TLR)-induced production of various cytokines, including interleukin-12 (IL-12) and IL-23, thereby preventing IL-12/IL-23-mediated immune responses. PIKfyve, a lipid kinase dysregulated in various tumor types, plays a key role in TLR signaling and tumor cell migration, proliferation and survival.


apixaban

An orally active inhibitor of coagulation factor Xa with anticoagulant activity. Apixaban directly inhibits factor Xa, thereby interfering with the conversion of prothrombin to thrombin and preventing formation of cross-linked fibrin clots.


Aplenzin

(Other name for: bupropion hydrochloride controlled-release)


Aplidin

(Other name for: plitidepsin)


apolizumab

A humanized monoclonal antibody directed against 1D10, a polymorphic determinant on the HLA-DR beta chain that is expressed on normal and neoplastic B cells. Apolizumab induces complement-mediated cytotoxicity, antibody-dependent cell-mediated cytotoxicity, and apoptosis of 1D10 antigen-positive B cells in vitro.


apomab

A fully human monoclonal antibody directed against human death receptor 5 (DR5; TRAIL-R2; TNFRSF10B) with potential proapoptotic and antineoplastic activities. Mimicking the natural ligand TRAIL (tumor necrosis factor-related apoptosis inducing ligand), apomab binds to DR5, which may directly activate the extrinsic apoptosis pathway and indirectly induce the intrinsic apoptosis pathway in tumor cells. DR5 is a cell surface receptor of the TNF-receptor superfamily and is expressed in a broad range of cancer s.


apoptosis inducer BZL101

An orally active aqueuous extract derived from the plant Scutellaria barbata with potential antineoplastic activity. Sparing normal cells, apoptosis inducer BZL101 specifically facilitates translocation of the protein apoptosis-inducing factor (AIF) from the mitochondrial membrane into the nucleus in tumor cells, thereby causing tumor cell-specific chromatin condensation and DNA degradation followed by the induction of caspase-independent apoptosis. AIF is both a mitochondrial intermembrane flavoprotein with oxidoreductase activity and a caspase-independent death effector that, similar to cytochrome c, is released from mitochondria early in the apoptotic process.


apoptosis inducer GCS-100

A galectin-binding polysaccharide derived from citrus pectin with potential antineoplastic activity. Apoptosis inducer GCS-100 binds to the carbohydrate-binding domain of the lectin galectin-3, which may result in apoptosis mediated through mitochondria/caspase activation cascades; this agent may overcome tumor growth mediated through anti-apoptotic protein Bcl-2, heat shock protein-27 (Hsp-27), and nuclear factor-kappa B (NF-kB). Galectin-3, a chimeric molecule consisting of both carbohydrate recognition and collagen-like domains, interacts with a variety of carbohydrate and protein ligands to form pentamers with unique crosslinking abilities; this lectin also exhibits anti-apoptotic properties, perhaps, in part, through the regulation of intracellular signaling pathways.


apoptosis inducer MPC-2130

A broad-acting, apoptosis-inducing, small molecule with potential antineoplastic activity. Although the exact mechanism of action has yet to be fully elucidated, apoptosis inducer MPC-2130 exhibits proapoptotic activities in tumor cells, including membrane phosphatidylserine externalization, release of cytochrome C from mitochondria, caspase activation, cell condensation, and DNA fragmentation. In addition, because this agent is not a substrate for several types of multidrug resistance (MDR) ABC superfamily transporters, such as P-glycoprotein 1 (MDR-1), multidrug resistance-associated protein 1 (MRP1), and breast cancer resistance protein 1 (BCRP1/ABCG2), it may be useful in treating MDR tumors that express these particular MDR efflux pumps.


apoptotic autologous tumor cells-pulsed alpha-type-1 polarized dendritic cells

A cell-based cancer vaccine composed of mature polarized dendritic cells (DCs) and pulsed with apoptotic autologous tumor cells that has potential immunostimulating and antineoplatic activities. Dendritic cells (DCs) were treated with interleukin-1 beta, tumor necrosis factor alpha, interferon-alpha (IFN-a), IFN-gamma and polyinosinic:polycytidylic acid (p-I:C) to produce mature alpha type-1 polarized DCs (alphaDC1) that are capable of producing high levels of interleukin-12p70 (IL-12p70). The alphaDC1 are subsequently pulsed with apoptotic autologous tumor cells. Upon administration, these DCs are able to induce a potent cytotoxic T lymphocyte (CTL) response against tumor associated antigens (TAAs), resulting in tumor cell lysis and inhibition of tumor cell growth. Apoptotic tumor cells contain an array of TAAs.


APOTONE

(Other name for: androstane steroid HE3235)


aprepitant

A small molecule, high-affinity substance P antagonist (SPA) with antiemetic activity. Crossing the blood brain barrier, aprepitant binds selectively to the human substance P/neurokinin 1 receptor in the central nervous system (CNS), thereby inhibiting receptor binding of endogenous substance P and substance P-induced emesis. This agent has little or no affinity for serotonin type 3 (5-HT3), dopamine, and corticosteroid receptors.


apricoxib

An orally bioavailable nonsteroidal anti-inflammatory agent (NSAID) with potential antiangiogenic and antineoplastic activities. Apricoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), thereby inhibiting the conversion of arachidonic acid into prostaglandins. Apricoxib-mediated inhibition of COX-2 may induce tumor cell apoptosis and inhibit tumor cell proliferation and tumor angiogenesis. COX-related metabolic pathways may represent crucial regulators of cellular proliferation and angiogenesis.


Apriso

(Other name for: mesalamine)


aprotinin bovine

A single chain polypeptide isolated from bovine lung with antifibrinolytic and anti-inflammatory activities. As a broad-spectrum serine protease inhibitor, aprotinin bovine competitively and reversibly inhibits the activity of a number of different esterases and proteases, including trypsin, chymotrypsin, kallikrein, plasmin, tissue plasminogen activator, and tissue and leukocytic proteinases, resulting in attenuation of the systemic inflammatory response (SIR), fibrinolysis, and thrombin generation. This agent also inhibits pro-inflammatory cytokine release and maintains glycoprotein homeostasis.


aprutumab ixadotin

An antibody-drug conjugate (ADC) directed against the fibroblast growth factor receptor type 2 (FGFR2) and conjugated to an as of yet unidentified toxin, with potential antineoplastic activity. Upon intravenous administration, aprutumab ixadotin binds to FGFR2. Upon binding, the toxin selectively induces cell death, through an as of yet undisclosed mechanism of action, in FGFR2-expressing tumor cells. FGFR2, a receptor tyrosine kinase upregulated in many tumor cell types, plays an essential role in tumor cell proliferation, differentiation and survival.


Aptosyn

(Other name for: exisulind)


Aquacel AG with Hydrofiber

(Other name for: ionic silver-impregnated sodium carboxymethyl cellulose antimicrobial dressing)


Aquacel Dressing

(Other name for: sodium carboxymethylcellulose dressing)


Aquadiol

(Other name for: therapeutic estradiol)


Aquaphor

(Other name for: petrolatum-mineral oil-lanolin-ceresin ointment)


AR antagonist BMS-641988

A nonsteroidal androgen receptor (AR) antagonist with anti-androgenic and potential antineoplastic activities. AR antagonist BMS-641988 binds to ARs in target tissues and prevents AR activation, which may result in the inhibition of AR-mediated transcriptional activity and tumor cell death in susceptible tumor cell populations. Global gene expression analysis has shown that exposure to this agent may result in a phenotype that is closer to a castration phenotype than is achievable with other antiandrogens such as bicalutamide.


Aralast

(Other name for: alpha-1-proteinase inhibitor human)


Aranelle

(Other name for: ethinyl estradiol/norethindrone)


Aranesp

(Other name for: darbepoetin alfa)


Arava

(Other name for: leflunomide)


Archexin

(Other name for: Akt antisense oligonucleotide RX-0201)


arcitumomab

A murine IgG monoclonal Fab fragment antibody labeled with technetium-99m directed against carcinoembryonic antigen (CEA), a protein that is overexpressed by many tumor cell types. For tumors that overexpress CEA, arcitumomab may be used as an adjunct diagnostic imaging tool to obtain prognostic information following resection and to monitor for recurrent disease.


Arcoxia

(Other name for: etoricoxib)


Aredia

(Other name for: pamidronate disodium)


arfolitixorin

The R-isomer of folitixorin, a reduced folate-based biomodulator and active metabolite of folate drugs leucovorin (LV) and levoleucovorin (l-LV) that can be used to increase the efficacy of certain antimetabolites, such as the cytotoxic agent 5-fluorouracil (5-FU), and reduce as well as protect against certain antimetabolite-associated adverse effects, such as those seen with high-dose (HD) methotrexate. Upon administration of arfolitixorin, 5,10-methylenetetrahydrofolate (MTHF) is a reduced folate substrate for the enzyme thymidylate synthase (TS) and stabilizes, upon co-administration of 5-FU, the covalent binding of the 5-FU metabolite 5-fluoro-2'-deoxyuridine-5'-monophosphate (FdUMP), instead of deoxyuridine monophosphate (dUMP), to its target enzyme TS, which results in an inhibition of TS. This inhibits the synthesis of deoxythymidine monophosphate (dTMP) and leads to the depletion of thymidine triphosphate (TTP), which is a necessary constituent of DNA. This inhibits DNA synthesis, which leads to an inhibition of cellular proliferation and induces tumor cell death. As MTHF is able to stabilize and strengthen the ternary complex, co-administration of arfolitixorin enhances the inhibition of DNA synthesis and increases the cytotoxic effect of 5-FU. As MTHF is the active form of folate and the active metabolite of LV and l-LV, arfolitixorin does not need to be converted to an active metabolite to become activated. In DNA synthesis, a ternary complex is formed between the reduced folate substrate MTHF, the TS enzyme and dUMP in order to convert dUMP to the DNA building block dTMP, which is necessary for DNA synthesis.


arginase inhibitor INCB001158

An orally available inhibitor of arginase, a manganese-dependent enzyme that hydrolyzes the amino acid arginine to form ornithine and urea, with potential immunomodulating and antineoplastic activities. Upon administration, arginase inhibitor INCB001158 inhibits the breakdown of arginine by arginase, which is produced by myeloid cells, and restores arginine levels. This allows arginine to stimulate the synthesis of nitric oxide and the secretion of pro-inflammatory cytokines and chemokines, which induces the proliferation and activation of T cells. Therefore, this agent may prevent the immunosuppressive effects of tumor-infiltrating myeloid cells and promote lymphocyte-mediated immune responses against tumor cells. Arginase is produced by neutrophils, macrophages and myeloid-derived suppressor cells (MDSC) and plays a role in inflammation-associated immunosuppression.


arginine butyrate

The butyric acid salt of the amino acid arginine. In EBV-related lymphomas, arginine butyrate induces EBV thymidine kinase transcription and may act synergistically with the antiviral agent ganciclovir to inhibit cell proliferation and decrease cell viability. In addition, the butyrate moiety inhibits histone deacetylase, which results in hyperacetylation of histones H3 and H4. Acetylated histones have a reduced affinity for chromatin; this reduced histone-chromatin affinity may allow chromosomal unfolding, potentially enhancing the expression of genes related to tumor cell growth arrest and apoptosis.


arginine hydrochloride

The hydrochloride salt form of arginine, an essential amino acid in juvenile humans. Arginine is a complex amino acid, often found at active sites in proteins and enzymes due to its amine-containing side chain. Arginine may prevent or treat heart and circulatory diseases, combat fatigue, and stimulate the immune system. It also boosts production of nitric oxide, relaxing blood vessels, and treating angina and other cardiovascular problems. Arginine is also an important intermediate in the urea cycle and in detoxification of nitrogenous wastes.


arginine/omega-3 fatty acids/nucleotides oral supplement

An oral nutritional supplement, containing substantial amounts of polyunsaturated fatty acids, arginine, and nucleotides, with potential immunostimulating activity. Omega-3 fatty acids/arginine/nucleotides oral supplement may enhance activities of key components of the immune system, including lymphocytes, antigen presenting cells (APCs), and various cytokines.


ArginMax

(Other name for: L-arginine/Korean ginseng/ Gingko biloba/damiana-based supplement)


Aricept

(Other name for: donepezil hydrochloride)


Arimidex

(Other name for: anastrozole)


Aristocort

(Other name for: triamcinolone)


Aristocort A

(Other name for: triamcinolone acetonide)


Arixtra

(Other name for: fondaparinux sodium)


armodafinil

The R-enantiomer of the racemic synthetic agent modafinil with central nervous system (CNS) stimulant and wakefulness-promoting activities. Although the exact mechanism of action has yet to be fully elucidated, armodafinil appears to inhibit the reuptake of dopamine by binding to the dopamine-reuptake pump, which leads to an increase in extracellular dopamine levels in some brain regions. This agent does not bind to or inhibit several receptors and enzymes that may be involved in sleep/wake regulation and is not a direct- or indirect-acting dopamine receptor agonist. Armodafinil has a longer half-life than modafinil.


Arnebia Indigo Jade Pearl topical cream

A proprietary multiherbal topical cream based on Chinese herbal medicine with potential antineoplastic, antiviral, antibacterial and immunostimulatory activities. Arnebia Indigo Jade Pearl topical cream contains 12 ingredients including 9 herbs infused in sesame oil, with an additional three powdered ingredients and beeswax added to the infused oil to create the salve. The purported mechanism(s) of action is unclear due to the complexity of the herbal mixture.


Aromasin

(Other name for: exemestane)


Aroplatin

(Other name for: liposomal NDDP)


Arranon

(Other name for: nelarabine)


arsenic trioxide

A small-molecule arsenic compound with antineoplastic activity. The mechanism of action of arsenic trioxide is not completely understood. This agent causes damage to or degradation of the promyelocytic leukemia protein/retinoic acid receptor-alpha (PML/RARa) fusion protein; induces apoptosis in acute promyelocytic leukemia (APL) cells and in many other tumor cell types; promotes cell differentiation and suppresses cell proliferation in many different tumor cell types; and is pro-angiogenic.


arsenic trioxide capsule formulation ORH 2014

An orally bioavailable capsule formulation of the inorganic toxic compound arsenic trioxide (As2O3), with potential antineoplastic activity. Although the mechanism of action (MoA) of As2O3 is not well understood, upon oral administration of ORH 2014, As2O3 appears to bind to DNA, prevent DNA synthesis, and cause DNA fragmentation, which leads to an induction of apoptosis in proliferating cells, including tumor cells. In addition, As2O3 causes damage to and induces degradation of the promyelocytic leukemia protein/retinoic acid receptor-alpha (PML/RARa) fusion protein, and inhibits the activity of the enzyme thioredoxin reductase.


artemether sublingual spray

A sublingual spray containing artemether, a semisynthetic derivative of artemisinin, an endoperoxide extracted from the Chinese herb qinghaosu (Artemisia annua or annual wormwood), with antiparasitic and potential antineoplastic activity. Upon sublingual application of the spray, artemether exerts its antineoplastic activity through as of yet not fully elucidated mechanism(s) of action. This agent binds to heme molecules inside cells, thereby inducing reactive oxygen species (ROS)-mediated damage which selectively kills cancer cells. In addition, artemether appears to target and modulate the expression of various proteins involved in cancer cell proliferation, angiogenesis, invasion and metastasis. Also, this agent depletes T regulatory cells, and modulates the production of inflammatory cytokines, such as interleukin-4 and interferon-gamma. Altogether, this inhibits tumor cell proliferation. The sublingual spray allows faster absorption of a higher percentage of the artemether dose, when compared to the oral form, as it avoids first pass metabolism; this results in an increased efficacy.


artesunate

A water-soluble, semi-synthetic derivative of the sesquiterpine lactone artemisinin with anti-malarial, anti-shistosomiasis, antiviral, and potential anti-neoplastic activities. Upon hydrolysis of artesunate’s active endoperoxide bridge moiety by liberated heme in parasite-infected red blood cells, reactive oxygen species and carbon-centered radicals form, which have been shown to damage and kill parasitic organisms. Additionally, in vitro studies demonstrate that this agent induces DNA breakage in a dose-dependent manner. Artesunate has also been shown to stimulate cell differentiation, arrest the cell cycle in the G1 and G2/M phases, inhibit cell proliferation, and induce apoptosis through mitochondrial and caspase signaling pathways. Artemisinin is isolated form the plant Artemisia annua.


artichoke whole phytocomplex concentrate

A whole phytocomplex concentrate (W.P.C.) composed of a standardized extract of the Cynara scolymus (artichoke) leaf with potential antioxidant, protective and chemopreventive activities. Artichoke W.P.C. is high in flavonoids and polyphenols, such as caffeoylquinic acids, which are mainly responsible for the pharmacological effects of the extract. Artichoke W.P.C. also contains protein, fiber, vitamins, minerals, numerous enzymes, volatile oils, phytosterols and polyunsaturated fatty acids.


artificial saliva spray

A spray formulation containing a saliva substitute, composed of potassium chloride, sodium chloride, magnesium chloride, calcium chloride, dipotassium phosphate and monopotassium phosphate, that has potential anti-xerostomia activity. Upon direct oral application of the artificial saliva spray, a protective film of moisture is deposited over the mucous membranes of the mouth, which relieves dryness of the mucous membranes and increases salivary flow. In addition, artificial saliva may help prevent chemotherapy- or radiotherapy-induced oral mucositis.


Arzerra

(Other name for: ofatumumab)


arzoxifene hydrochloride

The hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist. In comparison to other selective estrogen receptor modulators (SERMs), arzoxifene exhibits greater bioavailability and higher anti-estrogenic potency in the breast than raloxifene; it exhibits reduced estrogenicity in the uterus compared with either tamoxifen or raloxifene. This agent may have beneficial effects on bone and the cardiovascular system.


AS03-adjuvanted H1N1 pandemic influenza vaccine

A split-virus, inactivated influenza A (H1N1) vaccine containing H1N1 immunizing antigen combined with the adjuvant AS03, with potential immunostimulating activity. Upon intramuscular vaccination, AS03-adjuvanted H1N1 influenza vaccine may elicit an immune response against the H1N1 virus and the production of anti-H1N1 antibodies. AS03 is a stabilized oil-in-water emulsion adjuvant containing DL-alpha-tocopherol, squalene and polysorbate 80 that non-specifically stimulates cell-mediated immune antigen responses.


Asacol

(Other name for: mesalamine)


asaley

An L-leucine derivative of melphalan with antineoplastic activity. Asaley alkylates and crosslinks DNA, resulting in disruption of DNA synthesis.


asciminib

An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, asciminib binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies. The Bcr-Abl fusion protein tyrosine kinase is an abnormal enzyme produced by leukemia cells that contain the Philadelphia chromosome.


ascorbic acid

A natural water-soluble vitamin (Vitamin C). Ascorbic acid is a potent reducing and antioxidant agent that functions in fighting bacterial infections, in detoxifying reactions, and in the formation of collagen in fibrous tissue, teeth, bones, connective tissue, skin, and capillaries. Found in citrus and other fruits, and in vegetables, vitamin C cannot be produced or stored by humans and must be obtained in the diet.


ashwagandha root powder extract

A dietary supplement containing an extract powder derived from the root of the ashwagandha shrub with potential antineoplastic, antioxidant, immunostimulating and anti-angiogenic activities. Ashwagandha root powder extract contains numerous alkaloids, including withanine as the primary alkaloid, and steroidal lactone withanolides. The withanolides in this agent may suppress nuclear factor-kappaB activation and nuclear factor-kappaB-regulated gene expression, potentiating apoptosis and inhibiting tumor cell invasion. Cultivated in India and North America, ashwagandha (Withania somnifera Dunal or Indian ginseng) belongs to the Solanaceae (nightshade) family.


Asian ginseng

The aromatic root of perennial herbs of Panax ginseng. Ginseng, used in traditional Chinese medicine and available as a nutritional supplement, is classified as an adaptogenic herb with multiple effects, many of them are regulatory in nature. It contains a complex mixture of saponins, ginsenosides and panaxosides. Although the mechanism of action is unclear, ginseng is reported to enhance the immune system and reduce fatigue.


ASK1 inhibitor GS-4997

An orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Upon oral administration, ASK1 inhibitor GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. This prevents the phosphorylation of downstream kinases, such as c-Jun N-terminal kinases (JNKs) and p38 mitogen-activated protein kinase (p38 MAPK). By preventing the activation of ASK1-dependent signal transduction pathways, GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation. ASK1, also called mitogen-activated protein kinase kinase kinase 5 (MAP3K5), is activated in response to oxidative and endoplasmic reticulum (ER) stress, calcium influx and infection. It plays a key role in the development of certain cardiovascular and neurodegenerative diseases, diabetes, as well as certain types of cancer .


ASONEP

(Other name for: sonepcizumab)


Asorbicap

(Other name for: ascorbic acid)


ASP4132

A molecule with potential antineoplastic activity. Upon oral administration, ASP4132 affects oxidative phosphorylation in mitochondria of metabolically-active tumor cells, which reduces both energy production and tumor cell proliferation. Mitochondrial oxidative phosphorylation is hyperactivated in tumor cells and plays a key role in the promotion of tumor cell proliferation.


ASP9853

An orally bioavailable small molecule, with potential antineoplastic activity.


asparaginase

An enzyme isolated from the bacterium Escherichia coli or the bacterium Erwinia carotovora with antileukemic activity. Asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia in leukemic cells, resulting in the depletion of asparagine, inhibition of protein synthesis, cell cycle arrest in the G1 phase, and apoptosis in susceptible leukemic cell populations. Asparagine is critical to protein synthesis in leukemic cells; some leukemic cells cannot synthesize this amino acid de novo due to the absent or deficient expression of the enzyme asparagine synthase. The E. carotovora-derived form of asparaginase is typically reserved for cases of asparaginase hypersensitivity.


asparaginase Erwinia chrysanthemi

An enzyme isolated from the bacterium Erwinia chrysanthemi (E. carotovora). Asparagine is critical to protein synthesis in leukemic cells, which cannot synthesize this amino acid due to the absence of the enzyme asparagine synthase. Asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia, thereby depleting leukemic cells of asparagine and blocking protein synthesis and tumor cell proliferation, especially in the G1 phase of the cell cycle. This agent also induces apoptosis in tumor cells. The Erwinia-derived product is often used for those patients who have experienced a hypersensitivity reaction to the E. Coli formulation.


Asparlas

(Other name for: calaspargase pegol-mknl)


Aspergum

(Other name for: acetylsalicylic acid)


astatine At 211 anti-CD45 monoclonal antibody BC8-B10

A radioimmunoconjugate containing the murine IgG1 anti-CD45 monoclonal antibody (MAb) BC8 where the lysine side groups have been conjugated with decaborate (closo-decaborate; B10) and labeled with astatine (At) 211, with potential immunotherapeutic activity. Astatine At 211 anti-CD45 monoclonal antibody BC8-B10 binds to CD45 antigen, a receptor protein-tyrosine phosphatase expressed on the surface of both normal and malignant hematopoietic cells. After binding and internalization by CD45-expressing tumor cells, this agent may deliver a cytotoxic dose of alpha radiation. Additionally, the radiolabel can be leveraged to assay the biodistribution and/or pharmacokinetics (absorption, distribution, metabolism and excretion) for this agent. The use of B10 rather than other labeling methods increases the therapeutic efficacy while decreasing the toxicity of the radioconjugate.


Astragalus membranaceus/Angelica gigas/Trichosanthes kirilowii Maximowicz mixed herbal extract SH003

A traditional Chinese medicine (TCM)-based herbal extract composed of Astragalus membranaceus (Am), Angelica gigas (Ag) and Trichosanthes kirilowii Maximowicz (Tk), with potential anti-angiogenic and antineoplastic activities. Upon administration, the active ingredients in Am/Ag/Tk mixed herbal extract SH003 work synergistically to exert a number of activities through various mechanisms of action (MOA); although, not all of the MOAs are fully elucidated. SH003 blocks the binding of vascular endothelial growth factor (VEGF) to its receptor VEGF receptor 2 (VEGFR2; KDR), thereby inhibiting VEGF/VEGFR2-mediated signaling and VEGF-induced tumor endothelial cell migration, invasion and tube formation. This inhibits tumor angiogenesis. In addition, SH003 inhibits signal transducer and activator of transcription 3 (STAT3) activation and STAT3-mediated signaling, decreases the production of the pro-inflammatory cytokine interleukin-6 (IL-6) and the expression of STAT3 target genes. This induces apoptosis in, and reduces proliferation and metastasis of, cancer cells in which STAT3 signaling is overactivated. STAT3 activation contributes to inflammation in the cancer environment and tumor cell proliferation.


Astragalus-based formulation Qing Shu Yi Qi Tang

An herbal remedy containing Astragalus membranaceus, Panax ginseng, Atractylodes chinensis Koidz, Cimicifuga foetida, A. macrocephala Koidz, Alisma orientale Juzep, and Citrus reticulata Blanco, with potential immunomodulating, anti-oxidant and anticachexia activities. Upon oral consumption, the ingredients in this herbal supplement may modulate the activity of the immune system through a decrease in both the expression of nuclear factor-kappa B (NF-κB) and he production of pro-inflammatory cytokines such as interleukin-1beta (Il-1b), IL-6, and tumor necrosis factor-alpha (TNF-alpha). Increased levels of pro-inflammatory cytokines are correlated with decreased appetite and weight loss; thus, this herbal remedy may improve immune function, appetite and weight gain, which could prevent cachexia.


Astugenal

(Other name for: antineoplaston AS2-1)


astuprotimut-R

A cancer vaccine consisting of a recombinant form of human melanoma antigen A3 (MAGE-A3) combined with a proprietary adjuvant with potential immunostimulatory and antineoplastic activities. Upon administration, astuprotimut-R may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the MAGE-A3 antigen, resulting in tumor cell death. MAGE-A3, a tumor-associated antigen (TAA) originally discovered in melanoma cells, is expressed by various tumor types. The proprietary immunostimulating adjuvant in this agent is composed of a specific combination of immunostimulating compounds selected to increase the anti-tumor immune response to MAGE-A3.


asulacrine isethionate

The isethionate salt of an amsacrine analogue with antineoplastic properties. Asulacrine inhibits the enzyme topoisomerase ll, thereby blocking DNA replication and RNA and protein synthesis.


asunaprevir

An orally bioavailable inhibitor of the nonstructural protein 3 (NS3), with potential activity against hepatitis C virus (HCV). Upon administration, asunaprevir binds to the active center of the HCV NS3 and prevents NS3 protease-mediated polyprotein maturation. This disrupts the processing of viral proteins required for HCV replication. NS3, a serine protease, is essential for the proteolytic cleavages within the HCV polyprotein and plays a key role during HCV viral RNA replication. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family.


ASV

(Other name for: neoantigen-HSP70 peptide cancer vaccine)


Atacand

(Other name for: candesartan cilexetil)


atamestane

A synthetic steroidal substance with antineoplastic activity. Atamestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens.


Atengenal

(Other name for: antineoplaston A10)


atenolol

A synthetic isopropylamino-propanol derivative used as an antihypertensive, hypotensive and antiarrhythmic. Atenolol acts as a peripheral, cardioselective beta blocker specific for beta-1 adrenergic receptors, without intrinsic sympathomimetic effects. It reduces exercise heart rates and delays atrioventricular conduction, with overall decreasing oxygen requirements.


atezolizumab

A humanized, Fc optimized, monoclonal antibody directed against the protein ligand PD-L1 (programmed cell death-1 ligand 1), with potential immune checkpoint inhibitory and antineoplastic activities. Atezolizumab binds to PD-L1, blocking its binding to and activation of its receptor programmed death 1 (PD-1) expressed on activated T-cells, which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation. In addition, by binding to PD-L1, atezolizumab also prevents binding of this ligand to B7.1 expressed on activated T cells, which further enhances the T-cell-mediated immune response. PD-L1 is overexpressed on many human cancer cell types and on various tumor-infiltrating immune cells. PD-L1 binding to PD-1 on T-cells suppresses the immune system and results in increased immune evasion. PD-1, a transmembrane protein, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells. The Fc region of atezolizumab is modified in such a way that it does not induce either antibody-dependent cytotoxicity (ADCC) or complement-dependent cytotoxicity (CDC).  


ATGAM

(Other name for: anti-thymocyte globulin)


Atgam

(Other name for: horse anti-thymocyte globulin)


atiprimod

An orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.


Ativan

(Other name for: lorazepam)


ATM inhibitor M 3541

An orally bioavailable inhibitor of ataxia telangiectasia mutated kinase (ATM), with potential chemo-/radio-sensitizing and antineoplastic activities. Upon oral administration, M 3541 targets and binds to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. In addition, M 3541 sensitizes tumor cells to chemo- and radiotherapy. ATM, a serine/threonine protein kinase, is upregulated in a variety of cancer cell types; it is activated in response to DNA damage and plays a key role in DNA-strand repair.


ATM kinase inhibitor AZD0156

An orally bioavailable ataxia telangiectasia mutated (ATM) kinase inhibitor, with potential chemo-/radio-sensitizing and antineoplastic activities. Upon oral administration, AZD0156 targets and binds to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. In addition, AZD0156 sensitizes tumor cells to chemo- and radiotherapy. ATM, a serine/threonine protein kinase, is upregulated in a variety of cancer cell types; it is activated in response to DNA damage and plays a key role in DNA-strand repair.


ATN-161

A small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for integrin alpha5beta1, thereby preventing integrin alpha5beta1 binding. This receptor blockade may result in inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, angiogenesis, and tumor progression. Integrin alpha5beta1 is expressed on endothelial cells and plays a crucial role in endothelial cell adhesion and migration.


atomoxetine hydrochloride

The hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft; the effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.


atorvastatin calcium

The calcium salt of atorvastatin, a synthetic lipid-lowering agent. Atorvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent increases the number of LDL receptors on hepatic cell surfaces, enhancing the uptake and catabolism of LDL and reducing LDL production and the number of LDL particles, and lowers plasma cholesterol and lipoprotein levels. Like other statins, atorvastatin may also display direct antineoplastic activity, possibly by inhibiting farnesylation and geranylgeranylation of proteins such as small GTP-binding proteins, which may result in the arrest of cells in the G1 phase of the cell cycle. This agent may also sensitize tumor cells to cyctostatic drugs, possibly through the mTOR-dependent inhibition of Akt phosphorylation.


ATR kinase inhibitor AZD6738

An orally available morpholino-pyrimidine-based inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor AZD6738 selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. In addition, AZD6738 sensitizes tumor cells to chemo- and radiotherapy. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression, and survival; it is activated by DNA damage caused during DNA replication-associated stress.


ATR kinase inhibitor BAY1895344

An orally available ataxia telangiectasia and Rad3-related (ATR)-specific kinase inhibitor, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor BAY1895344 selectively binds to and inhibits the activity of ATR, which prevents ATR-mediated signaling. This inhibits DNA damage checkpoint activation, disrupts DNA damage repair and induces apoptosis in ATR-overexpressing tumor cells. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression and cell survival.


ATR kinase inhibitor VX-970

An inhibitor of ataxia telangiectasia and rad3-related (ATR) kinase, a DNA damage response kinase, with potential antineoplastic activity. ATR kinase inhibitor VX-970 selectively inhibits ATR kinase activity and prevents ATR-mediated signaling in the ATR-checkpoint kinase 1 (Chk1) signaling pathway. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis. In addition, VX-970 sensitizes tumor cells to chemo- and radiotherapy. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression, and survival; it is activated by DNA damage caused during DNA replication-associated stress.


ATR-101

An orally bioavailable agent that is selective towards adrenal cortex cells with potential antitumor activity. Upon administration, ATR-101 selectively kills adrenal and adrenal cancer cells, through an unknown mechanism.


Atragen

(Other name for: liposomal tretinoin)


atrasentan hydrochloride

The orally available hydrochloride salt of pyrrolidine-3-carboxylic acid with potential antineoplastic activity. As a selective antagonist of the endothelin-A (ETA) receptor, atrasentan binds selectively to the ETA receptor, which may result in inhibition of endothelin-induced angiogenesis and tumor cell proliferation.


Atromid-S

(Other name for: clofibrate)


atropine sulfate

The sulfate salt of atropine, a naturally-occurring alkaloid isolated from the plant Atropa belladonna. Atropine functions as a sympathetic, competitive antagonist of muscarinic cholinergic receptors, thereby abolishing the effects of parasympathetic stimulation. This agent may induce tachycardia, inhibit secretions, and relax smooth muscles.


attenuated chimpanzee adenovirus 5T4 vaccine

A cancer vaccine comprised of a recombinant, attenuated, replication-defective simian adenovirus vector (ChAdOx1) encoding the human 5T4 fetal oncoprotein (ChAdOx1.5T4), with potential immuno-activating and antineoplastic activities. Upon administration of the recombinant attenuated chimpanzee adenovirus 5T4 vaccine, the viral vector expresses 5T4 and stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing 5T4, which results in tumor cell lysis. 5T4, a transmembrane glycoprotein, is overexpressed by a variety of cancer cell types; its expression is correlated with increased invasiveness.


attenuated Listeria monocytogenes CRS-100

A live-attenuated strain of the Gram-positive bacterium Listeria monocytogenes (Lm) with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, attenuated Listeria monocytogenes CRS-100 may accumulate in and infect liver cells where it may activate a potent innate immune response and an adaptive immune response involving the by recruitment and activation of T lymphocytes. This agent may potentiate the immune response to vaccines against various liver neoplasms.


Augmentin

(Other name for: amoxicillin-clavulanate potassium)


auranofin

An orally available, lipophilic, organogold compound, used to treat rheumatoid arthritis, with anti-inflammatory and potential antineoplastic activities. Auranofin interacts with selenocysteine residue within the redox-active domain of mitochondrial thioredoxin reductase (TrxR), thereby blocking the activity of TrxR. As a result, this agent induces mitochondrial oxidative stress leading to the induction of apoptosis. Furthermore, this agent strongly inhibits the JAK1/STAT3 signal transduction pathway, thereby suppressing expression of immune factors involved in inflammation. TrxR, overexpressed in many cancer cell types, inhibits apoptosis, promotes cell growth and survival and plays a role in resistance to chemotherapy; TrxR catalyzes the reduction of oxidized thioredoxin (Trx) and plays a central role in regulating cellular redox homeostasis.


Aurimmune

(Other name for: colloidal gold-bound tumor necrosis factor)


Aurixim

(Other name for: rituximab conjugate CON-4619)


Aurolate

(Other name for: gold sodium thiomalate)


Aurora A kinase inhibitor TAS-119

An orally bioavailable inhibitor of the serine/threonine protein kinase aurora A, with potential antimitotic and antineoplastic activities. Upon intravenous administration, aurora A kinase inhibitor TAS-119 binds to and inhibits aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, inhibition of cell division and the induction of apoptosis in cells overexpressing aurora A kinase. Aurora A kinase localizes to the spindle poles and to spindle microtubules during mitosis; it plays an essential role in the regulation of spindle assembly. Aurora kinase A is overexpressed in a wide variety of cancer s.


Aurora A kinase/tyrosine kinase inhibitor ENMD-2076

An orally bioavailable synthetic small molecule with potential antiangiogenic and antineoplastic activities. Aurora A kinase/tyrosine kinase inhibitor ENMD-2076 selectively binds to and inhibits non-specified tyrosine kinases and Aurora kinases (AKs). The inhibition of AKs may result in the inhibition of cell division and proliferation and may induce apoptosis in tumor cells that overexpress AKs; antiangiogenic activity is related to the inhibition of angiogenic tyrosine kinases. AKs are serine-threonine kinases that play an essential role in mitotic checkpoint control during mitosis and are important regulators of cell division and proliferation.


Aurora B kinase inhibitor TAK-901

A small-molecule inhibitor of the serine-threonine kinase Aurora B with potential antineoplastic activity. Aurora B kinase inhibitor TAK-901 binds to and inhibits the activity of Aurora B, which may result in a decrease in the proliferation of tumor cells that overexpress Aurora B. Aurora B is a positive regulator of mitosis that functions in the attachment of the mitotic spindle to the centromere; the segregation of sister chromatids to each daughter cell; and the separation of daughter cells during cytokinesis. This serine/threonine kinase may be amplified and overexpressed by a variety of cancer cell types.


Aurora B/C kinase inhibitor GSK1070916A

An ATP-competitive inhibitor of the serine/threonine kinases Aurora B and C with potential antineoplastic activity. Aurora B/C kinase inhibitor GSK1070916A binds to and inhibits the activity of Aurora kinases B and C, which may result in inhibition of cellular division and a decrease in the proliferation of tumor cells that overexpress the Aurora kinases B and C. Aurora kinases play essential roles in mitotic checkpoint control during mitosis, and are overexpressed by a wide variety of cancer cell types.


Aurora kinase inhibitor AMG 900

A small-molecule inhibitor of Aurora kinases A, B and C with potential antineoplastic activity. Aurora kinase inhibitor AMG 900 selectively binds to and inhibits the activities of Aurora kinases A, B and C, which may result in inhibition of cellular division and proliferation in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis and are overexpressed by a wide variety of cancer cell types.


Aurora kinase inhibitor BI 811283

A small molecule inhibitor of the serine/threonine protein kinase Aurora kinase with potential antineoplastic activity. Aurora kinase inhibitor BI 811283 binds to and inhibits Aurora kinases, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation.


Aurora kinase inhibitor MLN8054

An orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. Aberrant expression of Aurora kinases occurs in a wide variety of cancer s, including colon and breast cancer s.


Aurora kinase inhibitor PF-03814735

An orally bioavailable, ATP-competitive, reversible small-molecule Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor PF-03814735 binds to and inhibits Aurora kinases A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis.


Aurora kinase inhibitor SNS-314

A synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs. AKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis.


Aurora kinase inhibitor TTP607

A small-molecule pan-Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor TTP607 selectively binds to and inhibits Aurora kinases A, B and C, which may result in the disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cellular division and proliferation in Aurora kinase-overexpressing tumor cells. Aurora kinases A, B and C, are serine/threonine kinases that play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of tumor cell types.


Aurora kinase/VEGFR2 inhibitor CYC116

An orally bioavailable small molecule multi-kinase inhibitor with antineoplastic activity. Aurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis. Aurora kinases are serine/threonine protein kinases that are only expressed in actively dividing cells and are critical in division or mitosis. VEGFR2 is a receptor tyrosine kinase that appears to account for most of the mitogenic and chemotactic effects of vascular endothelial growth factor (VEGF) on adult endothelial cells.


autologous ACTR-CD16-CD28-expressing T lymphocytes ACTR707

A preparation of autologous T lymphocytes that have been genetically modified, using proprietary Antibody-Coupled T-cell Receptor (ACTR) technology, to express a chimeric protein containing, at least, the extracellular Fc receptor domain of CD16, normally found on certain immune cells, such as natural killer (NK) cells, coupled to the co-stimulatory signaling domain of CD28, with potential immunostimulating and antineoplastic activities. Upon reintroduction into the patient with co-administration of a cancer -specific antibody, the co-administered antibody targets and binds to the tumor-associated antigen (TAA) expressed on the tumor cell. In turn, the autologous ACTR-CD16-CD28-expressing T lymphocytes ACTR707 bind to the antibody, become activated and induce the destruction of the tumor cells by a) releasing cytotoxins that directly kill cancer cells; b) releasing cytokines that trigger an immune response and recruit other immune-mediated killer cells to kill the tumor cells; c) targeting and killing adjacent tumor cells that are not bound to the antibody; d) inducing T-cell proliferation and thereby further enhancing the T-cell mediated tumor cell attack. Compared to other T-cell products, ACTR-based products do not target a specific TAA and can potentially be used in a variety of tumors because targeting is based on the specificity of the co-administered antibody.  

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