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Antineoplastic agents a4

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  • Anti-denatured collagen 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. DKK1 is a potent Wnt signaling pathway antagonist.
  • 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-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 antibody ds-8273a - An agonistic monoclonal antibody directed against human death receptor type 5 (DR5), also called tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) receptor 2, with potential pro-apoptotic and antitumor activities. Upon administration, anti-DR5 agonistic antibody DS-8273a mimics the natural receptor ligand TRAIL and binds to DR5. This activates DR5 and leads to the activation of the death receptor signal 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. DR5, a member of the TNF receptor superfamily, is expressed on the surfaces of a variety of tumor cells and plays a key role in the induction of tumor cell apoptosis.
  • 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-egfr car-transduced il-12-expressing t-lymphocytes - A preparation of human T-lymphocytes transduced with a retroviral vector encoding an anti-epidermal growth factor receptor (EGFR) chimeric antigen receptor (CAR) gene coupled to the signaling domains from CD28, 4-1BB (CD137) and CD3 zeta, and modified to express the cytokine interleukin-12 (IL-12), with potential immunostimulatory and antineoplastic activities. Upon administration, the anti-EGFR CAR-transduced IL-12-expressing T-lymphocytes target and bind to the EGFR antigen on tumor cell surfaces; subsequently, EGFR-expressing tumor cells may be lysed. IL-12 expression activates the immune system by promoting the secretion of interferon-gamma (IFNg), activating natural killer cells (NKs), and inducing cytotoxic T-cell responses, which may result in both decreased cell proliferation and increased cell death for the EGFR-overexpressing tumor cells. EGFR, overexpressed by a variety of cancer cell types, plays a key role in tumor cell proliferation, tumor angiogenesis and radio- and chemoresistance.
  • 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 emd 55900 - A murine monoclonal antibody targeting the epidermal growth factor receptor (EGFR) exhibiting anti-tumor activity. EMD 55900 antibody binds to the extracellular domain of EGFR close to the EGF binding domain and does not induce any tyrosine kinase activity on its own. As a result, EMD 55900 binding inhibits receptor activation by natural ligands thereby interrupting activation of downstream signaling cascade, required for tumor cell growth and proliferation.
  • 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 gt-mab 5.2-gex - A glycoengineered form of a human monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Anti-EGFR monoclonal antibody GT-MAB 5.2-GEX specifically binds to the extracellular domain of EGFR, thereby potentially inducing an antibody-dependent cell-mediated cytotoxicity (ADCC) against EGFR-expressing tumor cells, eventually leading to tumor cell apoptosis and an inhibition of tumor cell growth. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, is overexpressed on the cell surfaces of various solid tumors. This antibody has a specific glycosylation profile that may enhance its ADCC response against EGFR-expressing tumor cells.
  • 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 sct200 - A recombinant monoclonal antibody against human epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Upon administration, anti-EGFR monoclonal antibody SCT200 targets EGFR, prevents the activation and subsequent dimerization of this receptor and inhibits both EGFR-mediated signal transduction and cellular proliferation of EGFR-expressing tumor cells. In addition, SCT200 may induce antibody-dependent cell-mediated cytotoxicity (ADCC) against EGFR-expressing tumor cells. EGFR, a member of the epidermal growth factor receptor family, is overexpressed on the cell surfaces of various solid tumors.
  • 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/cd16a bispecific antibody afm24 - A human, tetravalent, bispecific antibody targeting both the epidermal growth factor receptor (EGFR) and the human low affinity IgG Fc region receptor IIIA (FCGR3A; CD16A), with potential immunomodulating and antineoplastic activities. Upon administration, anti-EGFR/CD16A bispecific antibody AFM24 simultaneously targets and binds to the CD16A expressed on natural killer (NK) cells and macrophages, and to EGFR on EGFR-expressing tumor cells, thereby selectively cross-linking EGFR-expressing tumor cells with NK cells and macrophages. This may result in NK cell and macrophage activation, antibody-dependent cellular cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), and eventually tumor cell lysis. EGFR, a receptor tyrosine kinase upregulated or mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. CD16A is specifically expressed on the surface of NK cells and macrophages.
  • Anti-egfr/c-met bispecific antibody emb-01 - A human, Fabs-in-tandem immunoglobulin (FIT-Ig)-based, tetravalent, bispecific antibody targeting both the epidermal growth factor receptor EGFR and the hepatocyte growth factor receptor (HGFR;; cMet; c-Met), with potential antineoplastic activity. Upon administration, anti-EGFR/c-Met bispecific antibody EMB-01 simultaneously targets and binds to wild-type or certain mutant forms of both EGFR and c-Met expressed on cancer cells, thereby preventing receptor phosphorylation. This prevents the activation of both EGFR- and c-Met-mediated signaling pathways and results in the inhibition of tumor cell proliferation. EGFR and c-Met, both upregulated or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation. In EMB-01, the two antigen-binding fragments (Fabs) are fused directly in a crisscross orientation resulting in four active and independent antigen binding sites.
  • 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 cancers, 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 cancers; targeting multiple HER family members simultaneously may increase therapeutic efficacy.
  • 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 cancers, including glioblastoma multiforme, non-small 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 cancers, 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 cancers, 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-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-enpp3/mmaf antibody-drug conjugate ags-16m8f - An antibody-drug conjugate (ADC) containing a human immunoglobulin (Ig) G2k monoclonal antibody (AGS-16C) directed against the ectonucleotide pyrophosphatase/phosphodiesterase family member 3 (ENPP3, NPP3, B10, PDNP3 CD203c, or PD-IBETA ), conjugated, via the non-cleavable maleimidocaproyl (mc) linker, to monomethyl auristatin F (MMAF), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. Upon intravenous administration of anti-ENPP3/MMAF ADC AGS-16M8F, the monoclonal antibody moiety selectively binds to ENPP3 expressed on tumor cells; upon internalization, the ADC is degraded by lysosomal proteases and MMAF is released. In turn, MMAF binds to and inhibits tubulin polymerization, which results 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 is overexpressed in most renal neoplasms and some liver cancers.
  • 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-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 antibody isu104 - A fully human antibody directed against the receptor tyrosine-protein kinase erbB-3 (ErbB3; HER3) with potential antineoplastic activity. Upon intravenous administration, anti-ErbB3 antibody ISU104 targets and binds to domain 3 and weakly interacts with domain 1 of ErbB3. This prevents heregulin (HRG) binding and blocks dimerization of ErbB3, thereby inactivating ErbB3 downstream signaling. ISU104 may also elicit the internalization of ErbB3 from the plasma membrane and downregulate ErbB3 expression. 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 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. Upon administration, anti-ErbB3 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-etbr/mmae antibody-drug conjugate dedn6526a - An antibody-drug conjugate (ADC) composed of a humanized immunoglobulin (Ig) G1 monoclonal antibody against anti-endothelin B receptor (ETBR) 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 DEDN6526A binds to ETBR-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. ETBR, a G-protein coupled receptor that can activate RAF/MEK signaling, is overexpressed in a variety of tumor cell types and plays a key role in tumor cell proliferation, invasion, epithelial-mesenchymal transition (EMT) and angiogenesis.
  • 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) that is conjugated to an undisclosed 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-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-fl(fitc-e2) car t cells - A preparation of genetically modified T-cells transduced with a replication incompetent, self-inactivating (SIN) lentiviral vector expressing a second generation chimeric antigen receptor (CAR) consisting of an anti-fluorescein (anti-FL) fluorescein isothiocyanate (FITC)-E2 single chain variable fragment (scFv), that is coupled, via an immunoglobulin G4 (IgG4) hinge-CH2(L295D)-CH3 spacer, to the costimulatory signaling molecules CD28, CD137 (4-1BB), and CD3 zeta, and linked to a truncated form of the human epidermal growth factor receptor (EGFRt), with potential immunostimulating and antineoplastic activities. Prior to the administration of anti-FL(FITC-E2) CAR T-cells, the CAR-T adaptor molecule (CAM) EC17 is administered. EC17 is a bispecific molecule that is composed of folic acid conjugated to FITC (folate-FITC). EC17 targets and binds with its folate moiety with high affinity to folate receptor (FR)-expressing tumor cells. Upon administration of the anti-FL(FITC-E2) CAR T-cells, these cells are attracted by and bind to the FITC antigen moiety of EC17. Upon binding to EC17, the T-cells induce specific tumor cell lysis, cytokine secretion, and proliferation, and activate a robust immune response against the EC17-bound, FR-expressing tumor cells. FR is overexpressed in various tumor cell types and is associated with increased leukemic cell proliferation and aggressiveness. The co-stimulatory molecules are required for full T-cell activation and enhance both proliferation of T-cells and antitumor activity. EGFRt both facilitates detection of the administered T-cells in vivo and can promote elimination of those cells following a cetuximab-induced antibody-dependent cellular cytotoxicity (ADCC) response. The reactivity of the anti-FL(FITC-E2) CAR T-cells is dependent on dosing of EC17, and therefore allows CAR T-cell activity to be controlled by dosing of EC17.
  • Anti-flt3 antibody-drug conjugate ags62p1 - An antibody-drug conjugate (ADC) composed of a human monoclonal antibody directed against the extracellular domain of receptor-type tyrosine-protein kinase FLT3 (FLT-3; FMS-like tyrosine kinase 3; CD135; fetal-liver kinase 2; FLK2) and conjugated, via an oxime linker and the site-directed non-natural amino acid linker para-acetyl-phenylalanine (pAcF), to a microtubule-disrupting cytotoxic agent, with potential antineoplastic activity. Upon administration of ADC AGS62P1, the antibody moiety targets and binds to FLT3. Upon antibody/antigen binding and internalization, the microtubule-targeting agent binds to and inhibits tubulin polymerization, which results in G2/M phase arrest and tumor cell apoptosis. The site-specific conjugation of the cytotoxic agent to the antibody, through pAcF, improves the biophysical properties of AGS62P1, increases payload distribution and stability, and optimizes its efficacy. FLT3, a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage, acute lymphoblastic leukemias and acute myeloid leukemias.
  • 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 cancers 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-fra/eribulin antibody-drug conjugate morab-202 - An antibody drug conjugate (ADC) composed of farletuzumab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the folate receptor alpha (FRA; FolRa; FOLR1), and conjugated, via a cathepsin B-cleavable linker, to the microtubule-targeting agent (MTA) eribulin, a derivative of the macrocyclic polyether natural product halichondrin B, with potential antineoplastic activity. Upon administration of MORAb-202, the farletuzumab moiety targets and binds to FRA expressed on certain tumor cells. Upon binding, internalization, and enzymatic cleavage, eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assembly of microtubules, resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest at G2/M phase, and the induction of tumor cell death in FRA-expressing cells. FRA is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers while its 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.
  • 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-garp monoclonal antibody abbv-151 - A humanized monoclonal antibody directed against the transforming growth factor beta (TGFbeta) activator, glycoprotein A repetitions predominant (GARP; leucine-rich repeat-containing protein 32; LRRC32), with potential immunomodulating and antineoplastic activities. Upon administration, anti-GARP monoclonal antibody ABBV-151 selectively targets and binds to GARP which interferes with the production and release of active TGFbeta by regulatory T-cells (Tregs). Selective inhibition of the release of TGFbeta from Tregs leads to a reversal of immunosuppression thereby increasing the immune response to tumor cells. GARP, a leucine-rich repeat-containing protein, is essential for the expression of TGFbeta on the cell surface of activated Tregs; it plays an important role in regulation of the immune cell function.
  • 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 hu3f8/anti-cd3 huokt3 bispecific antibody - A bispecific antibody comprised of a humanized anti-CD3 OKT3 (huOKT3) single chain variable fragment (scFv), linked to the carboxyl end of a humanized anti-GD2 3F8 (hu3F8) immunoglobulin G1 (IgG1) light chain, with potential antineoplastic activity. Upon intravenous administration, the anti-GD2 hu3F8/anti-CD3 huOKT3 bispecific antibody binds to CD3 on T-cells and disialoganglioside GD2 expressed on certain tumor cells, thereby cross-linking T-cells with GD2-expressing tumor cells. This promotes a selective cytotoxic T-lymphocyte (CTL) response against GD2-expressing cells. The Fc region of the anti-GD2 hu3F8/anti-CD3 huOKT3 bispecific antibody has two amino acid substitutions, N297A and K322A, which may prevent cytokine release syndrome and other unwanted side effects including complement-mediated pain. GD2, a disialoganglioside and tumor-associated antigen (TAA), 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-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-presenting cells-expressing hpv16 e6/e7 sqz-pbmc-hpv - A preparation of antigen presenting cells (APCs) specific for human papillomavirus (HPV) type 16 E6 and E7 proteins, with potential immunomodulating and antineoplastic activities. Autologous peripheral blood mononuclear cells (PBMCs) were ex vivo manipulated, using a technique involving membrane disruption to get the HPV16 E6 and E7 proteins into the cells; the resulting APCs present the antigens in a major histocompatibility type I (MHC-I) manner. Upon administration of the APCs-expressing HPV16 E6/E7 SQZ-PBMC-HPV, these cells activate the immune system to mount a cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing HPV16 E6 and E7. HPV16 E6 and E7 play an important role in the development of certain types of cancer.
  • 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 asp1951 - A human, high-affinity, tetravalent monospecific agonistic monoclonal antibody targeting glucocorticoid-induced tumor necrosis factor receptor (GITR; tumor necrosis factor superfamily member 18; TNFRSF18; CD357), with potential immune checkpoint modulating activity. Upon administration, anti-GITR agonistic monoclonal antibody ASP1951 binds to and activates GITR, which is expressed on the cell surface of multiple types of T-lymphocytes. This induces both the activation and proliferation of tumor antigen-specific T-effector cells (Teffs), and suppresses the function of activated T-regulatory cells (Tregs), which may promote the elimination of tumor cells. 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 agonistic monoclonal antibody bms-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-globo h/mmae antibody-drug conjugate obi 999 - An antibody-drug conjugate (ADC) composed of OBI-888 (OBI 888), a humanized monoclonal antibody directed against the tumor-associated antigen (TAA) globohexaosylceramide (globo H), covalently linked to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration of anti-globo H/MMAE ADC OBI 999, the antibody moiety of OBI 999, OBI 888, targets and binds to globo H on tumor cells and is rapidly internalized, thereby delivering MMAE intracellularly. Upon proteolytic cleavage, MMAE targets and binds to tubulin and inhibits its polymerization, resulting in G2/M checkpoint arrest and apoptosis in globo H-expressing tumor cells. Globo H, a hexasaccharide glycosphingolipid, is (over)expressed on the surface of many types of tumor cells. Globo H is minimally or not expressed on healthy, normal cells; its expression on cancer cells is associated with increased proliferation and poor prognosis.
  • Anti-glypican 3/cd3 bispecific antibody ery974 - An anti-glypican 3 (GPC3; GPC-3)/anti-CD3 bispecific monoclonal antibody, with potential immunostimulating and antineoplastic activities. Anti-GPC3/CD3 bispecific antibody ERY974 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 GPC3, a tumor-associated antigen (TAA) overexpressed on the surface of certain tumor cells. Upon administration of ERY974, this bispecific antibody simultaneously binds to both CD3-expressing and GPC3-expressing cells, thereby crosslinking GPC3-expressing tumor cells and cytotoxic T-lymphocytes (CTLs). This may result in potent CTL-mediated lysis of GPC3-expressing tumor cells. GPC3, a heparan sulfate proteoglycan and an oncofetal antigen protein, is overexpressed in a variety of cancers; it plays a role in cell division and growth regulation.
  • 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 cancers.
  • 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-gpc3-car t-lymphocytes tak-102 - A preparation of 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 T-lymphocytes TAK-102 specifically targets and binds 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 on normal, healthy cells; GPC3 plays an important role in cellular proliferation and differentiation.
  • Anti-gpr20/dxd antibody-drug conjugate ds-6157a - An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against the G protein-coupled receptor 20 (GPR20) conjugated to the cytotoxic DNA topoisomerase I inhibitor and exatecan derivative DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration of the anti-GPR20/DXd ADC DS-6157a, the anti-GPR20 antibody targets and binds to GPR20-expressing tumor cells. Upon cellular uptake, the DXd moiety 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 the proliferation of GPR20-expressing tumor cells. GPR20 is overexpressed on certain tumor cell types.
  • Anti-gremlin-1 monoclonal antibody ucb6114 - A monoclonal antibody directed against gremlin-1 (GREM1; Drm), with potential antineoplastic activity. Upon administration, anti-gremlin-1 antibody UCB6114 specifically targets and binds to gremlin-1, thereby neutralizing Gremlin-1. This may block the gremlin-1-mediated inhibition of bone morphogenetic protein (BMP) signaling pathways, and may lead to the inhibition of tumor cell growth and proliferation. Gremlin-1, a BMP antagonist that is overexpressed in a variety of cancer cell types, is involved in cancer cell growth and proliferation as well as tissue fibrosis.
  • 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-hepcidin monoclonal antibody ly2787106 - A humanized monoclonal antibody (MoAb) targeting the peptide hormone hepcidin, with potential anti-anemic activity. Upon intravenous administration, anti-hepcidin MoAb LY2787106 binds to hepcidin and prevents it from binding to the iron exporting protein ferroportin, which is expressed on both the basolateral surface of gastrointestinal (GI) enterocytes and the plasma membrane of macrophages. This prevents hepcidin-induced internalization and degradation of ferroportin and increases ferroportin-mediated iron export, thus increasing iron export from macrophages and iron absorption by enterocytes. This normalizes plasma iron levels, increases erythropoiesis and may inhibit anemia. Hepcidin, produced in hepatocytes, plays a key role in the homeostasis of systemic iron; it is upregulated during acute and chronic inflammation in response to cytokines and, in certain cancers, may contribute to cancer-associated anemia.
  • Anti-her2 antibody conjugated natural killer cells ace1702 - An off-the-shelf preparation of natural killer (NK) cells conjugated to a monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), with potential antineoplastic activity. Upon administration of anti-HER2 antibody conjugated natural killer cells ACE1702, the antibody moiety targets and binds to HER2 on tumor cells, which may lead to cell lysis of HER2-expressing tumor cells by the NK cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
  • 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 bat8001 - An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated via an uncleavable linker to an as of yet undisclosed maytansine derivative, with potential antineoplastic activity. Upon administration of the anti-HER2 ADC BAT8001, the anti-HER2 monoclonal antibody targets and binds to HER2 expressed on tumor cells. Upon cellular uptake, the cytotoxic maytansine derivative binds to tubulin, thereby affecting microtubule assembly and disassembly dynamics. This inhibits tumor cell proliferation and induces apoptosis in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
  • Anti-her2 antibody-drug conjugate dp303c - 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 DP303c, 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 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 ADC 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-her-2 bispecific antibody kn026 - An engineered Fc-based heterodimeric bispecific monoclonal antibody, derived from trastuzumab and pertuzumab, directed against two distinct epitopes of the extracellular dimerization domain of the tumor-associated antigen (TAA) human tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), with potential immunomodulating and antineoplastic activities. Upon administration, anti-HER-2 bispecific antibody KN026 simultaneously targets and binds to two separate, non-overlapping epitopes of HER-2, thereby inhibiting HER-2 heterodimerization and prevents the activation of HER-2 signaling pathways. By binding to HER-2, KN026 induces an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER-2. This results in tumor cell apoptosis and inhibits tumor cell proliferation of HER-2-overexpressing tumor cells. HER-2, overexpressed on a variety of tumor cell types, plays an important role in proliferation, differentiation and survival.
  • Anti-her2 bispecific antibody-drug conjugate zw49 - An antibody-drug conjugate (ADC) consisting of a bispecific monoclonal antibody (ZW25) directed against two different epitopes of the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (HER2, receptor tyrosine-protein kinase erbB-2) linked to an as of yet undisclosed cytotoxic payload, with potential antineoplastic activity. Upon intravenous administration, anti-HER2 bispecific ADC ZW49 targets and binds to HER2 expressed on tumor cells. Following receptor internalization, the cytotoxic payload is released and induces tumor cell death through an as of yet unknown mechanism of action. Additionally, binding of HER2 may inhibit HER2 activation, HER2 signaling and HER2-mediated tumor cell growth. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
  • Anti-her2 immune stimulator-antibody conjugate njh395 - An immune stimulator-antibody conjugate (ISAC) composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated to a not yet disclosed immune stimulator, with potential antineoplastic and immunostimulating activities. Upon administration of the anti-HER2 immune stimulator-antibody conjugate NJH395, the antibody moiety targets and binds to HER2 expressed on tumor cells. Upon antibody/antigen binding, the immune-stimulating moiety may, through an as of yet undisclosed mechanism, enhance the immune-mediated killing of HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed in many cancer types and plays a key role in tumor cell proliferation and tumor vascularization.
  • Anti-her2 monoclonal antibody b002 - A humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), with potential antineoplastic activity. Upon administration, anti-HER2 monoclonal antibody B002 targets and binds to HER2 on HER2-expressing tumor cells. This prevents HER2-mediated signaling and may lead to antitumor activity. 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 hlx22 - A humanized immunoglobulin (lg) G1 monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2), with potential immunomodulating and antineoplastic activity. Upon administration, anti-HER2 monoclonal antibody HLX22 targets and binds to HER2 on tumor cell surface. This may induce a cytotoxic T-lymphocyte (CTL) response 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/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/her3 dendritic cell vaccine - A dendritic cell (DC)-based cancer vaccine against the tumor-associated antigens (TAAs) human epidermal growth factor receptor 2 (HER2; EGFR2, ERBB2) and 3 (HER3; ErbB3), with potential immunomodulatory and antineoplastic activities. Upon administration of the anti-HER2/HER3 DC vaccine, the immune system gets exposed to HER2 and HER3, which may stimulate a potent cytotoxic T-lymphocyte (CTL) response against HER-2/3-positive tumor cells. This may result in tumor cell death and decreased tumor growth. HER-2/3, members of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, are overexpressed by a variety of cancers.
  • Anti-her2/mmae antibody-drug conjugate mrg002 - An antibody-drug conjugate (ADC) composed of a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Following administration, the antibody moiety of anti-HER2/MMAE ADC MRG002 targets and binds to HER2 on the surface of tumor cells. Following internalization of MRG002, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
  • 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-Her-2 (epidermal growth factor receptor 2) chimeric T cell receptor (CAR) gene with potential immunostimulatory and antineoplastic activities. Autologous CTLs from a patient with Her-2- and CMV-positive glioblastoma multiforme (GBM) are genetically modified to express CAR gene specific for Her-2 on their cell surfaces. After expansion in culture and reintroduction into the patient, the anti-HER2-CAR autologous CMV-specific CTLs bind to Her-2 antigen on tumor cell surfaces; subsequently, Her-2-positive tumor cells and stem cells may be lysed. Her-2 (ErbB-2), 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, which express 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 both tumor cell proliferation and tumor angiogenesis.
  • Anti-her2-dm1 adc b003 - An antibody-drug conjugate (ADC) consisting of a recombinant humanized anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody conjugated to the maytansinoid DM1 via a nonreducible thioether linkage (MCC), with potential antineoplastic activity. Upon administration of B003, the anti-HER2 monoclonal antibody moiety targets and binds to HER2 on tumor cell surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics, inhibiting cell division and the proliferation of cancer cells that overexpress HER2.
  • Anti-her2-dm1 antibody-drug conjugate gq1001 - An antibody-drug conjugate (ADC) composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) and conjugated, via a site-specific linker, to the cytotoxic maytansinoid mertansine (DM1), with potential antineoplastic activity. Upon administration of anti-HER2-DM1 ADC GQ1001, the antibody moiety targets and binds to HER2 on tumor cell surfaces. Upon cellular uptake and internalization, DM1 binds to tubulin and interferes with microtubule assembly and disassembly dynamics. This inhibits cell division and the proliferation of tumor cells that overexpress HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
  • 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 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-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-hiv-1 lentiviral vector-expressing sh5/c46 cal-1 - A gene transfer construct composed of a self-inactivating (SIN) lentiviral vector (LV) expressing a short hairpin RNA (shRNA) that targets the human C-C chemokine receptor type 5 (CCR5) mRNA (sh5) and expressing the HIV entry inhibitor C46, with potential anti-human immunodeficiency virus (HIV) type 1 (HIV-1) activity. Upon transduction of the anti-HIV-1 LVsh5/C46 Cal-1 in specified blood cell populations, such as peripheral blood mononuclear cells (PBMCs), hematopoietic stem/progenitor cells (HSPCs) and CD4+ T-lymphocytes, the cells express shCCR5 and C46. shCCR5 targets and binds to CCR5 mRNA, which inhibits the expression of CCR5 and prevents binding of the virus to the cellular CCR5 co-receptor. The cell surface expression of the cell membrane-anchored C46 peptide blocks HIV-1 fusion to the cellular membrane. The removal of CCR5 from and the production of C46 in the bone marrow and white blood cells, make the transduced cells resistant to and protect them from HIV-1 entry, infection and replication. HIV-resistant HSPCs could provide long-term protection against latent HIV infection and against HIV-associated cancers. C46 is a membrane-anchored 46-amino acid sequence found in HIV-1 gp41. CCR5 is a HIV-1 co-receptor that mediates HIV attachment and cell entry.
  • 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-hla-g antibody ttx-080 - An antibody targeting HLA-G histocompatibility antigen, class I, G (human leukocyte antigen G; HLA-G), with potential immune checkpoint inhibiting, immunomodulating and antineoplastic activities. Upon administration, the anti-HLA-G antibody TTX-080 targets and binds to HLA-G, thereby preventing the binding of HLA-G to its inhibitory receptors on a variety of immune cells, such as natural killer cells (NKs), T- and B-lymphocytes, and dendritic cells (DCs). This may prevent the HLA-G-mediated immune suppression, thereby activating both innate and adaptive immune responses. This may activate anti-tumor immune responses. HLA-G, an immune checkpoint normally expressed at the maternal-fetal interface, is expressed across multiple tumor types and plays a key role in cancer immune evasion.
  • Anti-human gitr monoclonal antibody amg 228 - An agonistic anti-human glucocorticoid-induced tumor necrosis factor receptor (tumor necrosis factor receptor superfamily, member 18; TNFRSF18; GITR; CD357) humanized monoclonal antibody, with potential immune checkpoint modulating activity. Anti-human GITR monoclonal antibody AMG 228 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 immune-mediated tumor cell eradication though a cytotoxic T-lymphocyte (CTL) response. 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-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-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 monoclonal antibody ky1044 - A human immunoglobulin G1 (IgG1) kappa monoclonal antibody that recognizes inducible T-cell co-stimulator (ICOS; CD278), with potential immunomodulating and antineoplastic activities. Upon administration, anti-ICOS monoclonal antibody selectively binds to dimeric ICOS expressed on certain 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. Additionally, KY1044 may eliminate ICOS-positive T-cells via 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-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-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 mabp1 - A human IgG1 monoclonal antibody directed against interleukin-1 alpha (IL1a) with potential 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-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 Hodgkin lymphoma 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-il-8 monoclonal antibody bms-986253 - A human monoclonal antibody against the pro-inflammatory mediator interleukin-8 (IL-8; CXCL8), with potential antineoplastic activities. Upon administration, BMS-986253 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, BMS-986253 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-ilt4 monoclonal antibody mk-4830 - A human monoclonal antibody directed against the inhibitory immune checkpoint receptor immunoglobulin-like transcript 4 (ILT4; leukocyte immunoglobulin-like receptor subfamily B member 2; LILRB2; lymphocyte immunoglobulin-like receptor 2; LIR2; monocyte/macrophage immunoglobulin-like receptor 10; MIR-10; CD85d), with potential immunomodulating and antineoplastic activities. Upon administration, anti-ILT4 monoclonal antibody MK-4830 targets and binds to ILT4. This prevents the binding of ILT4 ligands to their receptor and prevents ILT4-mediated signaling. This abrogates the immunosuppressive activities of ILT4 in the tumor microenvironment (TME), activates the expression of pro-inflammatory cytokines, including GM-CSF and tumor necrosis factor alpha (TNFalpha), and enhances a cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response. ILT4, plays a key role in tumor immune evasion. ILT4, a transmembrane protein and inhibitory member of the immunoglobulin-like transcript (ILT) family of proteins, is expressed primarily by myeloid cells, including monocytes, macrophages, dendritic cells (DCs) and granulocytes, and certain tumor cells.
  • Anti-integrin beta-6/mmae antibody-drug conjugate sgn-b6a - An antibody-drug conjugate (ADC) composed of a humanized antibody targeting integrin beta-6 and conjugated to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, the antibody moiety of anti-integrin beta-6/MMAE ADC SGN-B6A targets and binds to integrin beta-6 on the surface of tumor cells. Following internalization of SGN-B6A and release of MMAE, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in integrin beta-6-expressing tumor cells. Integrin beta-6 is a subunit of integrin alpha-V beta-6 (aVb6). Integrin aVb6, a cell adhesion and signaling receptor, is upregulated in certain cancer cell types and has been associated with increased proliferation, migration and invasion of tumor cells.
  • 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. Integrin-targeted 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-irf4 antisense oligonucleotide ion251 - An antisense oligonucleotide (ASO) targeting the interferon regulatory factor 4 (IRF4) mRNA, with potential immunomodulating and antineoplastic activities. Upon intravenous administration, anti-IRF4 ASO ION251 hybridizes with IRF4 mRNA, which blocks translation of the IRF4 protein. Reduction of IRF4 levels prevents the expression of IRF4-controlled tumor promoter genes, and may enhance tumor cell apoptosis and prevent T-cell exhaustion. IRF4, a transcription factor expressed in lymphocytes and essential for plasma cell differentiation, is involved in immune cell development and plays a key role in T-cell functions. It is overexpressed in certain tumor cell types and is a key regulator of multiple genes controlling tumor cell survival.
  • Anti-kir monoclonal antibody iph 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-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-ksp/anti-vegf sirnas aln-vsp02 - A lipid nanoparticle formulation containing two small interfering RNAs (siRNAs) for kinesin spindle protein (KSP) and vascular endothelial growth factor (VEGF) with potential antitumor activity. Upon intravenous administration, the siRNAs in KSP/VEGF siRNAs ALN-VSP02ALN bind to both KSP and VEGF messenger RNAs (mRNAs), preventing translation of KSP and VEGF proteins; this may result in growth inhibition of tumor cells that overexpress KSP and VEGF. VEGF and KSP are upregulated in many tumor cells and play an important role in tumor proliferation and survival.
  • Anti-lag-3 monoclonal antibody ibi-110 - A monoclonal antibody targeting the co-inhibitory receptor lymphocyte-activation gene 3 protein (LAG-3; LAG3; CD223), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-LAG-3 monoclonal antibody IBI110 targets and binds to LAG-3 expressed by tumor infiltrating lymphocytes (TILs) and blocks the interaction between LAG-3 and major histocompatibility complex class II (MHC II) 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-MHC II binding and enhances a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells, leading to a reduction in tumor growth. LAG-3, a member of the immunoglobulin superfamily (IgSF), negatively regulates both the proliferation and activation of T-cells. Its expression on TILs is associated with tumor-mediated immune suppression.
  • Anti-lag-3 monoclonal antibody incagn02385 - A Fc-engineered immunoglobulin G1-kappa (IgG1k) monoclonal antibody targeting the co-inhibitory receptor lymphocyte-activation gene 3 protein (LAG-3; LAG3), with potential immune checkpoint inhibitory and antineoplastic activities. Upon intravenous administration, monoclonal antibody INCAGN02385 targets and binds to human LAG-3 on tumor-infiltrating lymphocytes (TILs) and blocks the interaction between LAG-3 and major histocompatibility complex class II (MHC II) 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-MHC II binding and enhances a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells, which leads to a reduction in tumor growth. LAG-3, a member of the immunoglobulin superfamily (IgSF), 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 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-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-latent tgf-beta 1 monoclonal antibody srk-181 - A monoclonal antibody directed against latent human transforming growth factor (TGF)-beta 1 (TGFb1; TGF-b1), with potential antineoplastic activity. Upon administration, anti-latent TGFb1 monoclonal antibody SRK-181 specifically targets, binds to, and inhibits the activation of latent TGFb1 complexes, thereby preventing TGFb1-mediated signaling. This abrogates TGFb1-mediated immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFb1-dependent proliferation of cancer cells. The TGF-beta signaling pathway is often deregulated in tumors and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis. It plays a key role in immunosuppression in the TME. TGFb1 is the predominant isoform in many tumors.
  • Anti-lewis b/lewis y monoclonal antibody gnx102 - A humanized monoclonal antibody directed against human tumor-associated carbohydrate antigens (TACAs) Lewis B (LeB) and Lewis Y (LeY), with potential antineoplastic activity. Upon administration, anti-LeB/LeY monoclonal antibody GNX102 binds to branched LeB and LeY glycans, which may induce an antibody-dependent cellular cytotoxicity (ADCC) response against LeB- and LeY-expressing tumor cells. LeB and LeY antigens, tetrasaccharides with low to moderate expression in monomeric form in normal adult tissues, is overexpressed in branched form in multiple forms of cancers.
  • 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 LRG5-mediated signal transduction pathways. This prevents proliferation of LRG5-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-lilrb4 monoclonal antibody io-202 - A monoclonal antibody directed against the immune inhibitory receptor leukocyte immunoglobulin-like receptor B4 (LILRB4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-LILRB4 monoclonal antibody IO-202 targets, binds to and inhibits LILRB4 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, and inhibit tumor infiltration. LILRB4, an immune inhibitory receptor normally expressed on monocytic cells and highly expressed on monocytic acute myeloid leukemia (AML) cells, functions as an immune checkpoint that negatively regulates T-cell activation as its extracellular domain inhibits T-cell activity. It plays an important role in tumor infiltration in leukemias through multiple signaling pathways.
  • Anti-ly6e antibody-drug conjugate rg 7841 - 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 RG 7841 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-mage-a4 t-cell receptor/anti-cd3 scfv fusion protein imc-c103c - A T-cell re-directing bi-specific biologic composed of a modified form of human T-cell receptor (TCR) specific for the tumor-associated antigen (TAA) human melanoma-associated antigen A4 (MAGE-A4) and fused to an anti-CD3 single-chain variable fragment (scFv), with potential antineoplastic activity. Upon intravenous administration of IMC-C103C, the TCR moiety of this agent targets and binds to MAGE-A4 on tumor cells and the anti-CD3 scFv moiety binds to CD3- expressing T-lymphocytes. This selectively cross-links tumor cells and T-lymphocytes and results in a CTL-mediated death of MAGE-A4-expressing tumor cells. MAGE-A4 is overexpressed by a variety of cancer cell types.
  • Anti-melanin monoclonal antibody pti-6d2 - A monoclonal antibody (MoAb) against extracellular melanin with tumor targeting activity. Anti-melanin monoclonal antibody PTI-6D2 binds to extracellular melanin, a melanocyte pigment which is released during tumor cell turnover from dead melanoma tumor cells, while avoiding the binding of melanin in normal, healthy tissue because of melanin's normal intracellular location. Upon labeling with the beta-emitting radioisotope rhenium Re 188 (PTI-188), this MoAb may target multiple melanoma (MM) cells, thereby delivering a cytotoxic dose of radiation specifically to the targeted tumor cells.
  • 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 cancers, 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 cir mrna-electroporated autologous t cells - 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 CIR mRNA-electroporated autologous T cells 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 cancers.
  • 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 the administered 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/mmae antibody-drug conjugate dmot4039a - An antibody-drug conjugate (ADC) composed of MMOT0530A, a humanized immunoglobulin (Ig) G1 monoclonal antibody directed against the cell surface glycoprotein mesothelin (MSLN), and 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 DMOT4039A binds to MSLN-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. MSLN, a tumor-associated antigen (TAA), is overexpressed by all mesotheliomas and a variety of other cancers, while it is minimally expressed in normal tissue.
  • Anti-mesothelin/mmae antibody-drug conjugate rc88 - An antibody-drug conjugate (ADC) composed of an antibody directed against the human cell surface glycoprotein mesothelin and conjugated, via a cleavable linker, to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, the antibody moiety of anti-mesothelin/MMAE ADC RC88 targets and binds to the tumor associated antigen (TAA) mesothelin on the surface of tumor cells. Upon internalization and the release of MMAE, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in mesothelin-expressing tumor cells. Mesothelin is overexpressed by all mesotheliomas and a variety of other cancers, while it is minimally expressed in normal tissue.
  • Anti-mesothelin-pseudomonas exotoxin 24 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-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-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-muc1 monoclonal antibody bth1704 - A monoclonal antibody against the tumor associated antigen (TAA) mucin-1 (MUC1), with potential antineoplastic activity. Upon administration, anti-MUC1 monoclonal antibody BTH1704 targets and binds to MUC1 expressed on the surface of tumor cells, which can potentially activate the immune system to induce an antibody-dependent cellular cytotoxicity (ADCC) against MUC1-expressing tumor cells. MUC1, a glycoprotein overexpressed on the surface of a variety of cancer cells, plays a key role in tumor cell survival and proliferation.
  • Anti-muc16/cd3 bispecific antibody regn4018 - A bispecific, human monoclonal antibody with potential antineoplastic activity. REGN4018 contains two antigen-recognition sites: one for human CD3, a T cell surface antigen that is part of the T cell receptor complex, and one for human mucin 16 (MUC16, cancer antigen 125; CA125; FLJ14303), a member of the mucin family of glycoproteins that is overexpressed by several epithelial cancers, including ovarian cancer. Upon administration, REGN4018 binds to both T-cells and MUC16-expressing tumor cells, which cross-links the T-cells to the tumor cells, and may result in a potent cytotoxic T-lymphocyte (CTL) response against the MUC16-expressing tumor cells.
  • 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-muc17/cd3 bite antibody amg 199 - A half-life extended (HLE), 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 17 (MUC17), and one directed against human CD3, a T-cell surface antigen found on T-lymphocytes, with potential antineoplastic activity. Upon administration, anti-MUC17/CD3 BiTE antibody AMG 199 binds to both CD3 on T-cells and MUC17 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 MUC17-expressing tumor cells. MUC17, a member of the mucin family of glycoproteins, is overexpressed in a variety of tumor cells of epithelial origin and plays a key role in tumor cell dissemination.
  • Anti-napi2b antibody-drug conjugate xmt-1592 - An antibody-drug conjugate (ADC) composed of XMT-1535, a humanized monoclonal antibody against human sodium-dependent phosphate transport protein 2B (SLC34A2; NaPi2b), that is site-specifically bioconjugated to the cytotoxic aurastatin derivative auristatin F-HPA (AF-HPA; auristatin F-hydroxypropylamide), with potential antineoplastic activity. Upon administration of anti-NaPi2b ADC XMT-1592, the antibody moiety targets and binds to NaPi2b expressed on tumor cells. Following internalization of XMT-1592 and release of AF-HPA, 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.
  • Antineoplastic biological agent - Any agent that has a biological nature, such as agents containing living organisms, derived from living organisms, or comprised of ex vivo synthesized analogs of substances derived from living organisms, and that exerts antineoplastic activity.
  • Antineoplastic hormonal/endocrine agent - Any agent that affects hormone levels and exerts antineoplastic effects. Antineoplastic hormonal/endocrine agents treat either hormone-dependent or hormone-sensitive cancers by modulating hormone levels and manipulating the endocrine system.
  • Antineoplastic immunomodulating agent - Any agent that is capable of modulating the immune system in order to exert antineoplastic effects. Antineoplastic immunomodulating agents either activate the immune system, restore certain immune system activators or abrogate immunosuppression.
  • 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-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-nrp1 antibody asp1948 - A human immunoglobulin G4 (IgG4) monoclonal antibody directed against neuropilin-1 (NRP1; CD304; BDCA-4), with potential immunomodulatory and antineoplastic activities. Upon administration, anti-NRP1 antibody ASP1948 specifically targets and binds to NRP1. This prevents the binding of NRP1 to its ligand and may block the immune inhibitory actions of regulatory T-cells (Tregs) mediated by the interaction of NRP1 with its ligand. This may enhance the immune response against tumor cells. NRP1 is a transmembrane co-receptor protein expressed in Tregs; it plays an important role in maintaining the stability and function of Tregs.
  • 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-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-ofa immunotherapeutic bb-mpi-03 - A cancer vaccine composed of 3 different cytotoxic T-cell epitopes derived from the tumor-associated antigen oncofetal antigen (OFA), with potential immunostimulating and antineoplastic activities. Upon intradermal administration, anti-OFA immunotherapeutic vaccine BB-MPI-03 activates the immune system to elicit a specific cytotoxic T-lymphocyte (CTL) response against tumor cells expressing OFA. OFA, also called immature laminin receptor protein (iLRP), is expressed in fetal tissues and is overexpressed in various cancers; its expression is correlated with cancer cell survival.
  • Anti-ox40 agonist monoclonal antibody bgb-a445 - An agonistic monoclonal antibody targeting the co-stimulatory receptor OX40 (CD134; tumor necrosis factor receptor superfamily member 4; TNFRSF4), with potential immunostimulatory and antineoplastic activities. Upon administration, anti-OX40 agonist monoclonal antibody BGB-A445 selectively binds to OX40, thereby activating OX40. This induces the proliferation of memory and effector T-lymphocytes and results in a T-cell-mediated immune response against tumor cells, which leads to tumor cell lysis. OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T-lymphocytes and provides a co-stimulatory signal that promotes both the proliferation and survival of activated T-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 hexavalent agonist antibody inbrx-106 - An agonistic, recombinant, humanized, hexavalent immunoglobulin G (IgG) antibody targeting the co-stimulatory receptor OX40 (CD134; tumor necrosis factor receptor superfamily member 4; TNFRSF4), with potential immunostimulatory and antineoplastic activities. Upon administration, anti-OX40 hexavalent agonist antibody INBRX-106 selectively binds to six OX40 receptors per molecule, thereby clustering and activating OX40. This induces the proliferation of memory and effector T-lymphocytes and results in a T-cell-mediated immune response against tumor cells, which leads to tumor cell lysis. OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T-lymphocytes and provides a co-stimulatory signal that promotes both the proliferation and survival of activated T-cells. Utilizing a hexavalent OX40 antibody may improve receptor clustering and downstream signaling over tetravalent or bivalent OX40 antibodies.
  • 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 gsk3174998 - An agonistic humanized immunoglobulin G1 (IgG1) monoclonal antibody against the cell surface receptor OX40 (CD134; TNFRSF4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-OX40 monoclonal antibody GSK3174998 selectively binds to and activates OX40. Receptor activation induces proliferation of memory and effector T-lymphocytes and results in a T-cell-mediated immune response against tumor cells, which leads to tumor cell lysis. OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T-lymphocytes and provides a co-stimulatory signal that promotes both the proliferation and survival of activated T-cells.
  • Anti-ox40 monoclonal antibody ibi101 - An agonistic fully human anti-OX40 (tumor necrosis factor receptor superfamily member 4; TNFRSF4; CD134; OX40L receptor) with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-OX40 monoclonal antibody IBI101 selectively binds to and activates OX40. Receptor activation induces proliferation of memory and effector T-lymphocytes and results in a T-cell-mediated immune response against tumor cells, which leads to tumor cell lysis. OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T-lymphocytes and provides a co-stimulatory signal that promotes both 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 antibody-interleukin-21 mutein fusion protein amg 256 - An antibody directed against the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) fused to a mutein of the cytokine interleukin-21 (IL-21), with potential immune checkpoint inhibitory, immunomodulating and antineoplastic activities. Upon administration of anti-PD-1 antibody-IL-21 mutein fusion protein AMG 256, the antibody moiety specifically 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. The IL-21 mutein moiety binds to the IL-21 receptor and activates IL-21 cytokine signaling in PD-1-expressing cells. This may modulate the proliferation and/or differentiation, promote survival, and increase the cytolytic activity of PD-1-expressing T-cells, thereby enhancing 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; cluster of differentiation 274; CD274) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity. IL-21 plays an important role in the regulation of cellular immune responses.
  • 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-pd-1 monoclonal antibody 609a - A recombinant immunoglobulin G4 (IgG4) kappa 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 609A 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 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 amg 404 - A human 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 AMG 404 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; B7-H1; CD274) and 2 (PD-L2); it plays an important role in tumor evasion from host immunity.
  • Anti-pd-1 monoclonal antibody bat1306 - A recombinant, 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 BAT1306 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; cluster of differentiation 274; CD274) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.
  • Anti-pd-1 monoclonal antibody cs1003 - A humanized, 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 CS1003 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 f520 - A human immunoglobulin G1 (IgG1) 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 F520 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; B7-H1; CD274) and 2 (PD-L2); it plays an important role in tumor evasion from host immunity.
  • Anti-pd-1 monoclonal antibody gls-010 - 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 GLS-010 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; B7-H1; CD274) and 2 (PD-L2); it plays an important role in tumor evasion from host immunity.
  • Anti-pd-1 monoclonal antibody hx008 - A recombinant human 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 HX008 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 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 sct-i10a - A recombinant, 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 SCT-I10A targets, binds to, and inhibits PD-1 and its downstream signaling pathways. This may restore immune functions 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 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-pd1/anti-ctla4 antibody mixture psb205 - A mixture of two engineered monoclonal antibodies produced by a single cell line of which one is directed against the human negative immunoregulatory checkpoint receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) and the other one is directed against the cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD1/anti-CTLA4 antibody mixture PSB205 targets and binds to both PD-1 and CTLA4 expressed on tumor-infiltrating 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 enhances T-cell activation and proliferation more than the blockade of either immune checkpoint receptor alone.
  • Anti-pd-1/anti-ctla4 dart protein mgd019 - A hinge stabilized immunoglobulin G4 (IgG4) tetravalent bispecific antibody-like protein 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, the anti-PD-1/anti-CTLA4 dual-affinity re-targeting (DART) protein MGD019 specifically binds to both PD-1 and CTLA4 expressed on tumor-infiltrating lymphocytes (TILs) and inhibits the PD-1- and CTLA4-mediated downregulation of T-cell activation and proliferation. Dual blockade of PD1 and CTLA4 pathways provides enhanced activity against PD1+CTLA4+ double positive cells and may increase T-cell activation and proliferation compared to the blockade of either immune checkpoint alone.
  • Anti-pd-1/anti-her2 bispecific antibody ibi315 - A recombinant human immunoglobulin G1 (IgG1) bispecific antibody directed against the human epidermal growth factor receptor 2 (HER2) and 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, the anti-PD-1/anti-HER2 bispecific antibody IBI315 simultaneously targets, binds to and inhibits HER2 and PD-1 and their downstream signaling pathways, and bridges PD-1-expressing T-cells to HER2-expressing tumor cells. This may inhibit tumor cell proliferation of HER2-overexpressing cells. Inhibition of PD-1-mediated signaling may restore immune function through the activation of T-cells and T-cell-mediated immune responses against the HER2-expressing 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/anti-lag-3 bispecific antibody ro7247669 - A bispecific antibody directed against the human negative immunoregulatory checkpoint receptors programmed cell death protein 1 (PD-1; PD1; PDCD1; CD279; Programmed Death 1) and lymphocyte activation gene 3 protein (LAG-3; LAG3; CD223), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1/anti-LAG-3 bispecific antibody RO7247669 targets and binds to both PD-1 and LAG-3 expressed on T-cells and inhibits the PD-1- and LAG-3-mediated downregulation of T-cell activation and proliferation. This may lead to cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. PD-1 and LAG-3 play key roles in suppressing T-cell activation and proliferation.
  • 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/anti-pd-l1 bispecific antibody ibi318 - A recombinant immunoglobulin G1 (IgG1) bispecific antibody targeting both the human negative immunoregulatory checkpoint receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) and its ligand, human programmed death-ligand 1 (PD-L1; CD274), with potential checkpoint inhibitory, immunostimulating and antineoplastic activities. Upon administration, anti-PD-1/anti-PD-L1 bispecific antibody IBI318 simultaneously targets and binds to PD-1, which is expressed on a variety of leukocyte subsets including activated T-lymphocytes in the tumor microenvironment (TME), and PD-L1, which is expressed on tumor cells. This crosslinks PD-1-expressing T cells and PD-L1-expressing tumor cells. This prevents PD-L1 from binding to and activating its receptor PD-1 and inhibits the PD-L1/PD-1-mediated downregulation of T-cell activation and proliferation. 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. 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.
  • Anti-pd-1/anti-pd-l1 bispecific antibody ly3434172 - A bispecific antibody targeting both the human negative immunoregulatory checkpoint receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) and its ligand, human programmed death-ligand 1 (PD-L1; CD274), with potential checkpoint inhibitory, immunostimulating and antineoplastic activities. Upon administration, anti-PD-1/anti-PD-L1 bispecific antibody LY3434172 simultaneously targets and binds to PD-1, which is expressed on a variety of leukocyte subsets including activated T-lymphocytes in the tumor microenvironment (TME), and PD-L1 expressed on tumor cells. This prevents PD-L1 from binding to and activating its receptor PD-1 and inhibits the PD-L1/PD-1-mediated downregulation of T-cell activation and proliferation. 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. 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.
  • Anti-pd-1/cd47 infusion protein hx009 - A bispecific antibody fusion protein directed against the human negative immunoregulatory checkpoint receptors programmed cell death protein 1 (PD-1; PDCD1; CD279) and the human cell surface antigen CD47, with potential immunostimulating, phagocytosis-inducing and antineoplastic activities. Upon administration of anti-PD-1/CD47 infusion protein HX009, the agent simultaneously and selectively targets and binds to PD-1 expressed on T-lymphocytes and CD47 on tumor cells. The CD47 binding by HX009 blocks the interaction of CD47 with signal regulatory protein alpha (SIRPalpha), an inhibitory protein expressed on macrophages and dendritic cells (DCs), which prevents CD47/SIRPalpha-mediated signaling and abrogates the CD47/SIRPalpha-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, which results in macrophage activation and the specific phagocytosis of the CD47-expressing tumor cells. The binding of HX009 to PD-1 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 effector T-cell functions and may further activate cytotoxic T-lymphocyte (CTL)-mediated tumor cell killing. CD47, also called integrin-associated protein (IAP), is a tumor-associated antigen (TAA), widely expressed on normal, healthy cells, such as red blood cells and platelets, 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. By co-targeting CD47 and PD-1, HX009 has the potential to overcome the limitations of existing CD47-targeted therapies by possibly avoiding the side effects caused by binding to CD47 on healthy hematopoietic stem cells (HSCs), which causes unwanted macrophage-mediated phagocytosis. PD-1, an inhibitory receptor belonging to the immunoglobulin superfamily (IgSF), is expressed on activated T-lymphocytes; 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/ctla-4 bispecific antibody medi5752 - An engineered fragment crystallizable (Fc) domain bispecific human immunoglobulin G1 (IgG1) monoclonal 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 MEDI5752 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. In addition, MEDI5752 is internalized and is able to degrade PD-1. 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 PD1 and CTLA4 with MEDI5752 may enhance T-cell activation and proliferation more than the blockade of either immune checkpoint receptor alone. It may also decrease toxicity by avoiding the binding to CTLA-4-expressing T-cells that are devoid of PD-1. The engineered Fc domain may reduce Fc effector function.
  • 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-pd-1/tim-3 bispecific antibody ro7121661 - A bispecific antibody directed against both the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) and 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, anti-PD-1/TIM-3 bispecific antibody RO7121661 simultaneously targets and binds to both TIM-3 and PD-1 expressed on certain T-cells. This blocks the interaction of TIM-3 with some of its physiologic ligands and prevents the activation of PD-1 by its ligands, programmed cell death-1 ligand 1 (PD-L1) or 2 (PD-L2). 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. Dual checkpoint blockade of PD-1 and TIM-3 may enhance T-cell activation and proliferation more than the blockade of either immune checkpoint receptor alone.
  • Anti-pd-1/vegf bispecific antibody ak112 - A bispecific antibody directed against the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) and the human vascular endothelial growth factor (VEGF), with potential immune checkpoint inhibitory, anti-angiogenic and antineoplastic activities. Upon administration of anti-PD-1/VEGF bispecific antibody AK112, this agent simultaneously targets and binds to both PD-1 expressed on certain T-cells and VEGF. The binding of AK112 to PD-1 prevents the activation of PD-1 by its ligands, programmed cell death-1 ligand 1 (PD-L1) and/or 2 (PD-L2). This abrogates T-cell inhibition, activates antigen-specific T-lymphocytes and enhances cytotoxic T-lymphocyte (CTL)-mediated tumor cell lysis, which may lead to a reduction in tumor growth. The binding of AK112 to VEGF prevents binding of VEGF to its receptor VEGFR, abrogates VEGF/VEGFR-mediated signaling and may lead to the inhibition of vascular endothelial cell proliferation. The inhibition of tumor angiogenesis may further decrease tumor cell proliferation and prevent metastasis. 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 PD-L1/ or PD-L2; it plays an important role in tumor evasion from host immunity. VEGF is overexpressed in a variety of cancers and is associated with increased invasiveness and decreased survival.
  • Anti-pd-l1 monoclonal antibody a167 - A 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 A167 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed cell death 1 (PD-1; cluster of differentiation 279; CD279). 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 (IgSF) 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 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 gr1405 - 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 GR1405 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed cell death 1 (PD-1; cluster of differentiation 279; CD279). 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 (IgSF) 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 imc-001 - A 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 IMC-001 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed cell death 1 (PD-1; cluster of differentiation 279; CD279). 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. In addition, anti-PD-L1 monoclonal antibody IMC-001 also induces antibody-dependent cell-mediated cytotoxicity (ADCC). 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 (IgSF) 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 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 rc98 - 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 RC98 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed cell death 1 (PD-1; cluster of differentiation 279; CD279). 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 (IgSF) 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 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 monoclonal antibody tg-1501 - 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 TG-1501 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed cell death 1 (PD-1; cluster of differentiation 279; CD279). 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 (IgSF) 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 zkab001 - A 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 intravenous administration, anti-PD-L1 monoclonal antibody ZKAB001 specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed cell death 1 (PD-1; cluster of differentiation 279; CD279). 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 (IgSF) 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-l1/4-1bb bispecific antibody inbrx-105 - A recombinant, humanized, bispecific antibody targeting both the human programmed death-ligand 1 (PD-L1) and 4-1BB (CD137; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential checkpoint inhibitory, immunostimulating and antineoplastic activities. Upon administration, anti-PD-L1/4-1BB bispecific antibody INBRX-105 simultaneously targets and binds to 4-1BB, which is expressed on a variety of leukocyte subsets including activated T-lymphocytes, and PD-L1 expressed on tumor cells. Through 4-1BB binding, INBRX-105 acts as a conditional 4-1BB agonist, resulting in T-cell co-stimulation and enhanced anti-tumor activity. At the same time, INBRX-105 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. 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. 4-1BB, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity.
  • Anti-pd-l1/anti-4-1bb bispecific monoclonal antibody gen1046 - A recombinant, Fc-silenced immunoglobulin G1 (IgG1) bispecific antibody targeting both the human programmed death-ligand 1 (PD-L1) and 4-1BB (CD137; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential checkpoint inhibitory, immunostimulating and antineoplastic activities. Upon administration, anti-PD-L1/4-1BB bispecific antibody GEN1046 simultaneously targets and binds to 4-1BB, which is expressed on a variety of leukocyte subsets including activated T-lymphocytes, and PD-L1 expressed on tumor cells. Through 4-1BB binding, GEN1046 acts as a conditional 4-1BB agonist, resulting in T-cell co-stimulation and enhances T-lymphocyte-mediated anti-tumor activity. At the same time,GEN1046 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. 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. 4-1BB, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity.
  • Anti-pd-l1/cd137 bispecific antibody mcla-145 - A full-length, Fc-silenced immunoglobulin G1 (IgG1) bispecific antibody targeting both the human programmed death-ligand 1 (PD-L1) and CD137 (4-1BB; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential checkpoint inhibitory, immunostimulating and antineoplastic activities. Upon administration, anti-PD-L1/CD137 bispecific antibody MCLA-145 simultaneously targets and binds to CD137, which is expressed on a variety of leukocyte subsets including activated T-lymphocytes, and PD-L1 expressed on tumor cells, thereby crosslinking PD-L1-expressing tumor cells and T-lymphocytes. Through CD137 binding, MCLA-145 acts as a conditional CD137 agonist, resulting in T-cell co-stimulation and enhanced anti-tumor activity. At the same time, MCLA-145 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. 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. CD137, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity. Crosslinking of PD-L1-expressing tumor cells and activated T-lymphocytes may enhance T-lymphocyte-mediated lysis of PD-L1-expressing tumor 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/il-15 fusion protein kd033 - A fusion protein composed of a monoclonal antibody directed against the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274) fused to the immunostimulatory cytokine interleukin-15 (IL-15), with potential immunostimulatory and antineoplastic activities. Upon administration of the anti-PD-L1/IL-15 fusion protein KD033, the anti-PD-L1 antibody moiety specifically targets and binds to PD-L1 expressing cells in the tumor microenvironment (TME). In turn, IL-15 stimulates the proliferation of natural killer (NK) cells, cytotoxic T-lymphocytes (CTLs) and memory T-cells locally in the TME, which induces an anti-tumor immune response. This may increase tumor cell killing and decrease tumor cell proliferation. IL-15 regulates CD8+ T and NK cell development, activation and proliferation. PD-L1, a transmembrane protein, is expressed on the surface of antigen presenting cells (APCs) and on many cancer cell types. PD-L1 binding to PD-1, a negative regulator of the immune system on activated T-cells, limits the expansion and survival of CD8-positive T-cells, suppresses the immune system and results in immune evasion.
  • 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.
  • 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 cancers.
  • 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-prame immunotherapeutic gsk2302032a - An immunotherapeutic agent targeting the tumor-associated antigen (TAA), preferentially expressed antigen of melanoma (PRAME), with potential antineoplastic activity.
  • Anti-prame t-cell receptor/anti-cd3 scfv fusion protein imc-f106c - A T-cell re-directing bi-specific biologic composed of a modified form of human T-cell receptor (TCR) specific for the tumor-associated antigen (TAA) preferentially expressed antigen in melanoma (PRAME) and fused to an anti-CD3 single-chain variable fragment (scFv), with potential antineoplastic activity. Upon administration of IMC-F106C, the TCR moiety of this agent targets and binds to PRAME on tumor cells and the anti-CD3 scFv moiety binds to CD3- expressing T-lymphocytes. This selectively cross-links tumor cells and T-lymphocytes and results in a CTL-mediated death of PRAME-expressing tumor cells. The TAA PRAME is overexpressed by a variety of cancer cell types.
  • 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 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 MK4721 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 cancers 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 mln591-dm1 immunoconjugate mln2704 - An immunoconjugate that consists of a humanized monoclonal antibody (MLN591), directed against prostate-specific membrane antigen linked to a maytansinoid (DM1). The monoclonal antibody moiety of MLN2704 binds to tumor cells expressing prostate-specific membrane antigen; MLN274 is then internalized into the tumor cell where the DM1 maytansinoid moiety binds to tubulin and inhibits tubulin polymerization and microtubule assembly, resulting in a disruption of microtubule activity and cell division, and cell death.
  • 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/cd28 bispecific antibody regn5678 - A bispecific antibody directed against both the tumor-associated antigen (TAA) prostate-specific membrane antigen (PSMA) and the co-stimulatory T-cell-specific surface glycoprotein CD28, with potential immunostimulating and antineoplastic activities. Upon administration of anti-PSMA/CD28 bispecific antibody REGN5678, this bispecific antibody binds to both CD28 on cytotoxic T-lymphocytes (CTLs) and PSMA found on PSMA-expressing tumor cells. This activates and redirects CTLs to PSMA-expressing tumor cells, which may result in the CTL-mediated cell death of PSMA-expressing tumor cells. PSMA is overexpressed on the surface of metastatic and hormone-refractory prostate cancer cells.
  • Anti-psma/cd3 bispecific antibody ccw702 - A bispecific antibody that targets both the tumor-associated antigen (TAA) human prostate-specific membrane antigen (PSMA) and the CD3 antigen found on T-lymphocytes, with potential immunostimulatory and antineoplastic activities. Upon administration of anti-PSMA/CD3 bispecific antibody CCW702, 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 is overexpressed on the surface of metastatic and hormone-refractory prostate cancer cells.
  • Anti-psma/cd3 bispecific antibody jnj-63898081 - A bispecific 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 bispecific antibody JNJ-63898081, 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 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 cancers; its expression is associated with poor prognosis and metastasis.
  • 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-rankl monoclonal antibody gb-223 - A monoclonal antibody directed against the receptor activator of nuclear factor kappa beta ligand (RANKL) with potential antiosteoclast and antineoplastic activities. Upon administration, anti-RANKL monoclonal antibody GB-223 specifically binds to RANKL and blocks the interaction of RANKL with RANK, a receptor located on osteoclast cell surfaces. This results in the inhibition of osteoclast activity, a decrease in bone resorption, and a potential increase in bone mineral density. By blocking the activation of the RANK/RANKL-mediated signaling pathway, GB-223 may also reduce tumor-associated bone destruction and may result in tumor regression in bone tumors with high RANK and RANKL expressions. RANKL, a protein expressed by osteoblastic cells, plays an important role in osteoclastic differentiation and activation. Both RANKL and RANK are overexpressed in certain bone tumors, and the RANK/RANKL-mediated signaling pathway plays an important role in certain bone tumors.
  • Anti-rankl monoclonal antibody jmt103 - A recombinant, human, immunoglobulin G4 (IgG4) monoclonal antibody directed against the receptor activator of nuclear factor kappa beta ligand (RANKL), with potential antiosteoclast and bone-sparing activities. Upon administration, anti-RANKL monoclonal antibody JMT103 specifically binds to RANKL and blocks the interaction of RANKL with RANK, a receptor located on osteoclast cell surfaces. This may inhibit osteoclast activity, decrease bone resorption, increase bone mineral density, and may protect bones from tumor metastasis. This may abrogate hypercalcemia of malignancy and may correct serum calcium levels. RANKL, a protein expressed by osteoblastic cells, plays an important role in osteoclastic differentiation and activation. Both RANKL and RANK are overexpressed in certain bone tumors, and the RANK/RANKL-mediated signaling pathway plays an important role in certain bone tumors.
  • Anti-ribonucleoprotein antibody atrc-101 - An engineered, human immunoglobulin (Ig) G1 monoclonal antibody directed against a ribonucleoprotein (RNP) complex, with potential immunostimulating and antineoplastic activities. Upon administration, anti-RNP antibody ATRC-101 targets and binds to its RNP complex antigen on tumor cells. This may activate the innate immune system, change the local tumor microenvironment (TME) and promote T cell-mediated killing of tumor cells. The tumor-restricted RNP complex is expressed in a variety of tumor cells.
  • 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-ror1/pnu-159682 derivative antibody-drug conjugate nbe-002 - An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody against the tumor-associated antigen (TAA) receptor tyrosine kinase-like orphan receptor 1 (ROR1) site-specifically conjugated to a derivative of the highly potent anthracycline PNU-159682, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of NBE-002 targets and binds to ROR1 expressed on tumor cells. Upon binding and internalization, the anthracycline-based toxin intercalates into DNA and interacts with topoisomerase II. This leads to an inhibition of DNA replication and repair, and prevents RNA and protein synthesis. This kills the ROR1-expressing cancer cells. In addition, the PNU-159682 derivate may promote immunogenic cell death (ICD) and activate a cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response, thereby further killing the ROR1-expressing tumor cells. 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-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.
  • Antisecretory factor-enriched egg yolk powder supplement - A dietary supplement composed of dried egg yolk powder that is highly enriched in the protein anti-secretory factor (AF), with anti-inflammatory, anti-diarrheal, immunomodulating and chemo-adjuvant activities. Upon intratumoral administration of the AF-enriched egg yolk powder supplement, AF is able to normalize fluid flow by regulating the ion and fluid balance across the cell membranes, and decreases high interstitial fluid pressure (IFP). As elevated IFP presents a barrier to drug uptake and poor perfusion in solid tumors, reducing IFP levels allows for increased uptake and an enhanced effect of chemotherapeutic agents. In addition, AF may be able to modulate the immune system and may have immunomodulatory effects on myeloid cells. It may also modulate the secretion of immunomodulatory agents from tumor cells. In addition, AF may affect the secretion of various pro-inflammatory mediators such as interleukin-6 (IL-6), IL-8, monocyte chemotactic protein-1 (MCP-1; monocyte chemoattractant protein-1; C-C Motif Chemokine Ligand 2; CCL2), macrophage inflammatory protein-1alpha (MIP-1a), and macrophage inflammatory protein-1beta (MIP-1b). AF, a 41 kilodalton (kDa) endogenous and essential protein secreted in plasma and other tissue fluids in mammals, is increased after exposure to bacterial toxins and endogenous triggers of inflammation.
  • Antisense oligonucleotide gti-2040 - A 20-mer antisense oligonucleotide complementary to a coding region in the mRNA of the R2 small subunit component of human ribonucleotide reductase. GTI-2040 decreases mRNA and protein levels of R2 in vitro and may inhibit tumor cell proliferation in human tumors in vivo.
  • 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 cancers, including bladder cancer, some forms of lung cancer, breast cancer and glioblastoma.
  • Anti-tag-72 monoclonal antibody scfv cc-49/218 - An immunoglobulin derived from the single-chain antigen-binding domain (sFv) of the monoclonal antibody CC-49 with potential antineoplastic activity. The parent monoclonal antibody CC-49 binds to the tumor-associated glycoprotein TAG-72 with high affinity, recognizing many tumor cell types that express TAG-72. Because of its single-chain structure, CC-49/218 sFv may exhibit a longer half-life than the parent monoclonal antibody CC-49; 218 represents the linker sequence that helps reduce aggregation and proteolysis of this agent.
  • 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-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 ab154 - A humanized immunoglobulin G1 (IgG1) 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 AB154 targets and 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; PRR2; 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. This leads to CD226 dimerization and CD226-mediated signaling and activates the immune system to exert a T-cell-mediated immune response against cancer cells. TIGIT, a member of the Ig super family (IgSF) 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 bgb-a1217 - A humanized immunoglobulin G1 (IgG1) 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 BGB-A1217 targets and 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; PRR2; 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. This leads to CD226 dimerization and CD226-mediated signaling and activates the immune system to exert a T-cell-mediated immune response against cancer cells. TIGIT, a member of the Ig super family (IgSF) 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 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 com902 - A fully 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 COM902 targets and binds to TIGIT expressed on various immune cells, particularly on tumor-infiltrating lymphocytes (TILs), thereby preventing the interaction of TIGIT with its ligands CD112 (nectin-2; poliovirus receptor related-2; PRR2; 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. This leads to CD226 dimerization and CD226-mediated signaling and activates the immune system to exert a T-cell-mediated immune response against cancer cells. TIGIT, a member of the Ig super family (IgSF) 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 sgn-tgt - A nonfucosylated human immunoglobulin G1 (IgG1) 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 SGN-TGT targets and binds to TIGIT expressed on various immune cells, particularly on tumor-infiltrating T-lymphocytes (TILs). This prevents the interaction of TIGIT with its ligands CD112 (nectin-2; poliovirus receptor related-2; PRR2; PVRL2) and CD155 (poliovirus receptor; PVR; nectin-like protein 5; NECL-5), and 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. This enhances depletion of TIGIT-positive regulatory T-cells (Tregs) and activates the immune system to exert a T-cell-mediated immune response against cancer cells. TIGIT, a member of the Ig super family (IgSF) 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-tim-3 monoclonal antibody incagn02390 - A fully human Fc-engineered immunoglobulin G1 kappa (IgG1kappa) 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, INCAGN02390 forms a high-affinity interaction with TIM-3 expressed on certain T-cells, 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. Additionally, INCAGN02390 elicits TIM-3 receptor internalization, potentially preventing interactions with other ligands.TIM-3, a transmembrane protein and immune checkpoint receptor expressed on certain lymphocytes, including tumor infiltrating lymphocytes (TILs), 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-tim3 monoclonal antibody shr-1702 - 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, anti-TIM3 monoclonal antibody SHR-1702 targets and 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-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-trailr2/cdh17 tetravalent bispecific antibody bi 905711 - A tetravalent bispecific antibody targeting both the pro-apoptotic death receptor tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) receptor 2 (TRAILR2; death receptor 5; DR5) and cadherin-17 (CDH17), with potential pro-apoptotic and antineoplastic activities. Upon administration of anti-TRAILR2/CDH17 tetravalent bispecific antibody BI 905711, the antibody targets and binds to both TRAILR2 and CDH17, expressed on tumor cells. Receptor clustering and activation of TRAILR2 induces apoptosis in CDH17-positive cancer cells. Activation of TRAILR2 plays a key role in the induction of apoptosis. CDH17-dependent clustering of TRAILR2 allows BI 905711 to selectively induce apoptosis in CDH17-expressing tumor cells thereby increasing efficacy and decreasing liver toxicity. CDH17 is overexpressed in a variety of cancer cell types while its expression is restricted in normal liver tissue.
  • Anti-trop2 antibody-drug conjugate bat8003 - An antibody-drug conjugate (ADC) composed of a monoclonal antibody against tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1) conjugated via an uncleavable linker to an as of yet undisclosed maytansine derivative toxin, with potential antineoplastic activity. Upon administration of the anti-TROP2 ADC BAT8003, the anti-TROP2 antibody targets and binds to TROP2 expressed on tumor cells. Upon cellular uptake, the cytotoxic maytansine derivative binds to tubulin, thereby affecting microtubule assembly and disassembly dynamics. This inhibits tumor cell proliferation of TROP2-expressing tumor cells. TROP2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.
  • Anti-trop2 antibody-drug conjugate skb264 - An antibody-drug conjugate (ADC) composed of a monoclonal antibody against tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1) conjugated to an as of yet undisclosed toxin, with potential antineoplastic activity. Upon administration of the anti-TROP2 ADC SKB264, the anti-TROP2 antibody targets and binds to TROP2 expressed on tumor cells. Upon cellular uptake, the undisclosed toxin exerts, through an as of yet not disclosed mechanism of action, its cytotoxic effect. 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.
  • 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 cancers.
  • Anti-tweak monoclonal antibody rg7212 - A humanized monoclonal antibody directed against the apoptotic ligand TNF-like weak inducer of apoptosis (TWEAK) with potential antineoplastic activity. Anti-TWEAK monoclonal antibody RG7212 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.

Alphabetic list of antineoplastic agents - 0-9 - A1 - A2 - A3 - A4 - A5 -A6 - B - C - D - E - F - G - H - I - JK - L - M - NO - PQ - R - S - T - UVW - XYZ

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