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Dictionary of drugs:I

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Dictionary of pharmaceutical drugs/medications sorted alphabetically

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Dictionary of drugs I

A radioimmunoconjugate of the humanized monoclonal antibody CC49 labeled with iodine I 131. Iodine I 131 monoclonal antibody CC49 delivers beta and gamma radiation-emitting I 131 radionuclide specifically to tumor cells that express tumor-associated glycoprotein (TAG)-72, allowing localization of TAG-72-expressing tumor cells with radioimaging devices in diagnostic applications or resulting in specific TAG-72-expressing tumor cell radiocytotoxicity in therapeutic applications. Monoclonal antibody CC49 binds to TAG-72, a pancarcinoma antigen, with high affinity.

An orally bioavailable inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins with potential apoptotic inducing and antineoplastic activity. IAP inhibitor AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP). This may restore and promote the induction of apoptosis through apoptotic signaling pathways. AT-406 may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their BIR (baculoviral lAP repeat) domains.

The hydrochloride salt of a small-molecule inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins with potential antineoplastic activity. IAP inhibitor HGS1029 selectively inhibits the biological activity of IAP proteins, which may restore apoptotic signaling pathways; this agent may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their BIR (baculoviral lAP repeat) domains.

A cell-based product composed of dendritic cells (DCs) pulsed with tumor-associated antigens (TAAs) and devoid of the inhibitory effect of antigen presentation attenuators (iAPA) combined with cytotoxic T-lymphocytes (CTLs) (iAPA-DC/CTL), with potential immunostimulating and antineoplastic activities. DCs are transduced with a viral vector containing small interfering RNAs (siRNAs) against APAs, which prevents the expression of APA genes and inhibits attenuation of antigen presentation. Upon administration of iAPA-DC/CTL, the DCs are able to efficiently present antigens to the immune system, stimulate the immune system against tumor-associated antigens (TAAs) and hyperactivate TAA-specific CTLs and T-helper cells. Also, the iAPA-based DCs inhibit the activity of the T-regulatory cells (Tregs), thereby abrogating their negative effect on CTL activation and preventing their immunosuppressive activity against TAAs. Altogether, this inhibits tumor cell proliferation. Additionally, the administered CTLs induce direct cancer cell lysis. APAs negatively regulate antigen presentation, activate Tregs and their immunosuppressive activity, affect inflammatory cytokine production by DCs, and negatively regulate the immunostimulatory activity of DCs; they have an overall inhibitory effect on the stimulation of the immune system.

The sodium salt of ibadronic acid, a synthetic nitrogen-containing bisphosphonate. Ibandronic acid inhibits farnesyl pyrophosphate synthase, resulting in a reduction in geranylgeranyl GTPase signaling proteins and apoptosis of osteoclasts. This agent increases bone mineral density, decreases bone remodeling, inhibits osteoclast-mediated bone resorption, and reduces metastases-related and corticosteroid-related bone pain.

Brand name for palbociclib

An immunoconjugate of the monoclonal antibody ibritumomab conjugated with the linker-chelator tiuxetan, a high affinity, conformationally restricted chelation site for radioisotopes. When bound to indium In 111 or yttrium Y 90, ibritumomab tiuxetan, targeting the CD20 antigen on B cell surfaces, specifically delivers a potentially cytotoxic dose of radiation to B lymphocytes. Ibritumomab is a murine IgG1 kappa monoclonal antibody directed against the CD20 antigen, which is found on the surface of normal and malignant B lymphocytes.

An orally bioavailable, small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon oral administration, ibrutinib binds to and irreversibly inhibits BTK activity, thereby preventing both B-cell activation and B-cell-mediated signaling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is required for B cell receptor signaling, plays a key role in B-cell maturation, and is overexpressed in a number of B-cell malignancies. The expression of BTK in tumor cells is also associated with increased proliferation and survival. Check for active clinical trialsusing this agent.

An orally bioavailable inhibitor of cyclic nucleotide phosphodiesterase (PDE), mainly PDE-3, -4, -10, and -11, with anti-(neuro)inflammatory, vasorelaxant, bronchodilator, analgesic, neuroprotective and potential anti-tumor activities. Ibudilast (IBD) is able to cross the blood-brain barrier (BBB). Upon administration, IBD exerts its potential anti-tumor activity against glioblastoma multiforme (GBM) cells by inhibiting PDE-4 and the pro-inflammatory cytokine macrophage migration inhibitory factor (MIF), which results in a decrease in MIF, its receptor CD74, and AKT expression, and attenuates the immunosuppressive properties of monocytic myeloid-derived suppressor cells (MDSCs) and reduces T-regulatory cells (Tregs). This causes GBM cell apoptosis and inhibits GBM cell proliferation. In addition, IBD reduces, through its inhibitory effect on various PDEs, the production of certain pro-inflammatory cytokines, such as interleukin-6 (IL-6), IL- 1beta, leukotriene B4, and tumor necrosis factor-alpha (TNF-a). IBD also upregulates the anti-inflammatory cytokine (IL-10), and promotes the production of neurotrophic factors, such as brain-derived neurotrophic factor (BDNF), nerve growth factor (NGF), and neurotrophin-4 (NT-4). It also blocks toll-like receptor-4 (TLR-4), inhibits nitric oxide (NO) synthesis and reduces the level of reactive oxygen species (ROS). It also prevents platelet aggregation, causes cerebral vasodilation, bronchial smooth muscle relaxation, and improves cerebral blood flow. In addition, IBD attenuates the PDE-mediated activation of glial cells and abrogates PDE-mediated neuroinflammation and neurodegeneration. MIF is secreted by cancer stem cells (CSCs) and is highly expressed within GBM and plays a key role in tumor cell proliferation. Co-expression of MIF and CD74 in GBM is associated with poor patient survival.

A propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. This leads to decreased prostaglandin synthesis, by prostaglandin synthase, the main physiologic effect of ibuprofen. Ibuprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation.

A formulation for intravenous injection containing ibuprofen, a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID), with anti-inflammatory, analgesic, and antipyretic activities. Upon intravenous injection, ibuprofen inhibits the activity of the enzymes cyclooxygenase I (COX-1) and II (COX-2), resulting in a decreased formation of precursors of prostaglandins and thromboxanes. Inhibition of COX-2 specifically blocks the conversion of arachidonic acid (AA) to prostaglandins, which mediate inflammation, fever and pain.

A preparation of autologous interleukin-15 (IL-15)-expressing natural killer T cells (NKT) transduced with a retroviral vector encoding a chimeric antigen receptor (CAR) derived from the antibody 14G2a that recognizes disialoganglioside GD2 (GD2-CAR) that is coupled to the co-stimulatory domains of CD28 and OX40 (CD134), and to the zeta chain of the TCR/CD3 complex (CD3-zeta), and linked to the suicide gene inducible caspase 9 (iCasp9 or iC9), with potential immunomodulating and antineoplastic activities. Upon transfusion, the iC9-GD2-CAR-CD28-OX40-expressing autologous NKT cells recognize, bind to and induce selective cytotoxicity in GD2-expressing tumor cells. The tumor-associated antigen (TAA) GD2 is overexpressed on the surface of neuroblastoma cells and by other neuroectoderm-derived neoplasms, while it is minimally expressed on normal, healthy cells. The iCasp9 safety switch consists of a full-length caspase 9, including its caspase recruitment domain, linked to a human FK506 drug-binding domain with an F36V mutation (FKBP12-F36V). If the administered NKT cells lead to unacceptable side effects, the chemical homodimerizer AP1903, which binds to the FKBP12-F36V drug-binding domain, activates caspase 9, and results in apoptosis of the administered NKT cells, can be administered.

Modified T-lymphocytes expressing a 3rd generation chimeric antigen receptor (CAR) specific for the disialoganglioside GD2, which contains the CD3zeta chain, the signaling domains of the co-stimulatory molecules CD28 and CD134 (OX-40) and the suicide gene inducible caspase 9 (iCasp9), with potential immunomodulating and antineoplastic activities. Upon administration, iC9-GD2-CD28-OX40-expressing T lymphocytes target the GD2 antigen on tumor cells, thereby providing selective toxicity towards GD2-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, the chemical homodimerizer AP1903 can be administered, which binds to the drug binding FKBP12-F36V domain and activates caspase 9, resulting in the apoptosis of the administered T-cells. The tumor-associated antigen GD2 is overexpressed on the surface of almost all tumors of neuroectodermal origin. OX40 and CD28, both T-cell surface-associated co-stimulatory molecules, are required for full T-cell activation.

A chemotherapy regimen consisting of ifosfamide, carboplatin and etoposide used in the treatment of relapsed and refractory non-Hodgkin and Hodgkin lymphomas.

Brand name for indocyanine green solution

Brand name for ponatinib hydrochloride

An isosmotic solution containing icodextrin, a starch-derived, water-soluble glucose polymer, used in peritoneal dialysis and for the prevention of adhesion after surgery. Due to its isoosmotic nature and inability to cross the peritoneal membrane, the icodextrin solution, upon administration into the peritoneal cavity, is able to exert osmotic pressure. This allows for the removal of excess fluids and waste products in dialysis patients. In addition, icodextrin can provide a barrier between tissue surfaces when administered during surgery. This physically separates tissues, prevents adhesion after surgery and promotes wound healing.

An orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Icotinib selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. This may lead to an inhibition of EGFR-mediated signal transduction and may inhibit cancer cell proliferation. EGFR, a receptor tyrosine kinase, is upregulated in a variety of cancer cell types.

A fully human IgG1 monoclonal antibody directed against human vascular endothelial growth factor receptor 1 (VEGFR-1/FLT-1) with potential antiangiogenesis and antineoplastic activities. Icrucumab specifically binds to and inhibits the activity of VEGFR-1, which may prevent the activation of downstream signaling pathways and so inhibit tumor angiogenesis; the subsequent reduction in tumor nutrient supply may inhibit tumor cell proliferation. Tumor cell overexpression of VEGFR-1 may be associated with tumor angiogenesis and tumor cell proliferation and invasion; VEGFR-1 may modulate VEGFR-2 signaling.

Brand name for idarubicin hydrochloride

The hydrochloride salt of the anthracycline antineoplastic antibiotic idarubicin. Idarubicin intercalates into DNA and inhibits topoisomerase II, thereby inhibiting DNA replication and ultimately, interfering with RNA and protein synthesis. Due to its high lipophilicity, idarubicin penetrates cell membranes more efficiently than other anthracycline antibiotic compounds.

A sustained-release drug delivery embolization system containing small polymeric beads impregnated with the anthracycline antibiotic idarubicin with potential antineoplastic activity. The beads consist of polyvinyl alcohol (PVA) microspheres modified with sulfonic acid groups and loaded with idarubicin. During transarterial chemoembolization (TACE) in the hepatic artery, idarubicin-eluting beads embolize to the tumor vasculature, occlude tumor blood vessels and induce ischemic necrosis of tumor tissue due to mechanical blockage of the tumor vasculature. Simultaneously, idarubicin-eluting beads release cytotoxic idarubicin locally and in a sustained manner. This may result in idarubicin-mediated inhibition of tumor cell proliferation.

An orally available, small molecule, antagonist of MDM2 (mouse double minute 2; Mdm2 p53 binding protein homolog), with potential antineoplastic activity. Idasanutlin binds to MDM2 blocking the interaction between the MDM2 protein and the transcriptional activation domain of the tumor suppressor protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded and the transcriptional activity of p53 is restored. This may lead to p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger nuclear phosphoprotein and negative regulator of the p53 pathway, is often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival.

An orally bioavailable, small molecule inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Idelalisib inhibits the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3), preventing the activation of the PI3K signaling pathway and inhibiting tumor cell proliferation, motility, and survival. Unlike other isoforms of PI3K, PI3K-delta is expressed primarily in hematopoietic lineages. The targeted inhibition of PI3K-delta is designed to preserve PI3K signaling in normal, non-neoplastic cells.

An orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP+], mitochondrial) in the mitochondria, with potential antineoplastic activity. Upon administration, pan-IDH mutant inhibitor AG-881 specifically inhibits mutant forms of IDH1 and IDH2, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH mutations. In addition, AG-881 is able to penetrate the blood-brain barrier (BBB). IDH1 and 2, metabolic enzymes that catalyze the conversion of isocitrate into a-KG, play key roles in energy production and are mutated in a variety of cancer cell types. In addition, mutant forms of IDH1 and 2 catalyze the formation of 2HG and drive cancer growth by blocking cellular differentiation and inducing cellular proliferation.

An inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity. Upon administration, IDH305 specifically inhibits IDH1(R132) mutant forms in the cytoplasm, which inhibits the formation of the oncometabolite 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1(R132)-expressing tumor cells. IDH1(R132) mutations are highly expressed in certain malignancies, including gliomas. They initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.

A peptide vaccine consisting of a 20-mer peptide derived from isocitrate dehydrogenase type 1 (IDH1) containing the point mutation R132H (IDH1R132H), with potential antineoplastic activity. Upon subcutaneous vaccination with the IDH1R132H mutation-targeting IDH1 peptide vaccine, the vaccine stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells that express the IDH1R132H protein. R132H is a point mutation, which contains an amino acid substitution where arginine is replaced by histidine at position 132 of IDH1, and is highly expressed in gliomas as well as other tumor types; this mutation is associated with increased production of the oncometabolite R-2-hydroxyglutarate (2HG).

A peptide vaccine consisting of a peptide derived from isocitrate dehydrogenase 1 (IDH1) containing the point mutation R132H (IDH1R132H), with potential antineoplastic activity. Intradermal vaccination with the IDH1R132H-specific peptide vaccine PEPIDH1M may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells that express the IDH1R132H protein. The IDH1 point mutation of amino acid residue 132 is highly expressed in gliomas and is associated with increased production of the oncometabolite R-2-hydroxyglutarate (2HG).

Brand name for enasidenib mesylate

A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with tumor-derived clonal immunoglobulin (Ig) with potential immunostimulatory and antineoplastic activities. Upon administration, idiotype-pulsed autologous dendritic cell vaccine APC8020, containing idiotype (Id) protein structures that can be recognized by antibodies and by CD41 T lymphocytes and CD81 T lymphocytes, may stimulate antitumoral cytotoxic T lymphocyte (CTL) and antibody responses against Id-expressing tumor cells. The Id represents the unique antigenic determinants in the variable regions of the clonal Ig.

An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, NLG919 targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the essential amino acid tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, this agent increases tryptophan levels, restores the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, T-lymphocytes, and causes a reduction in tumor-associated regulatory T-cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against the IDO1-expressing tumor cells. IDO1 is overexpressed by a variety of tumor cell types and plays an important role in immunosuppression. Tryptophan depletion is associated with immunosuppression caused by T-cell suppression.

An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1) and the kynurenine-producing hepatic enzyme tryptophan 2,3-dioxygenase (TDO), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1/TDO inhibitor HTI-1090 specifically targets and binds to both IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine, and TDO, a hepatic enzyme catalyzing the first step of tryptophan degradation. By inhibiting IDO1 and TDO, HTI-1090 decreases kynurenine levels in tumor cells, restores tryptophan and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells and T lymphocytes. This reduces the number of tumor-associated regulatory T cells (Tregs) and activates the immune system to induce a cytotoxic T-lymphocyte (CTL) response against the IDO1/TDO-expressing tumor cells, thereby inhibiting the growth of the tumor cells. IDO1 and TDO, both overexpressed by multiple tumor cell types, play important roles in immunosuppression and the promotion of tumor cell survival and proliferation. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.

An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1 inhibitor BMS-986205 specifically targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, BMS-986205 restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against the IDO1-expressing tumor cells, thereby inhibiting the growth of IDO1-expressing tumor cells. IDO1, overexpressed by multiple tumor cell types, plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system. Check for active clinical trialsusing this agent.

An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1 inhibitor KHK2455 targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, KHK2455 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes; KHK2455 also induces increased interferon (IFN) production, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1, a cytosolic enzyme responsible for tryptophan catabolism and the conversion of tryptophan into kynurenine, is overexpressed by a variety of tumor cell types and antigen presenting cells (APCs); it plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.

An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1 inhibitor LY3381916 specifically targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, LY3381916 restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against the IDO1-expressing tumor cells, thereby inhibiting the growth of IDO1-expressing tumor cells. IDO1, overexpressed by multiple tumor cell types, plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system. Check for active clinical trialsusing this agent.

An orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1 inhibitor PF-06840003 targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, PF-06840003 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes; PF-06840003 also induces increased interferon (IFN) production, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1, a cytosolic enzyme responsible for tryptophan catabolism and the conversion of tryptophan into kynurenine, is overexpressed by a variety of tumor cell types and antigen presenting cells (APCs); it plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.

An iodinated analogue of deoxyuridine, with antiviral activity against herpes simplex virus (HSV) and potential radiosensitizing activities. Upon ocular administration, idoxuridine (IUdR) is converted to its mono-, di-, and triphosphate forms, is incorporated into DNA and disrupts viral replication. Upon oral administration of the idoxuridine prodrug ropidoxuridine and hepatic conversion by aldehyde oxidase into idoxuridine, this agent incorporates into DNA and sensitizes cells to ionizing radiation by increasing DNA strand breaks.

A synthetic flavonoid derivative. Idronoxil activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis (XIAP), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex, thereby preventing DNA replication and resulting in tumor cell death.

A proprietary, suppository-based formulation composed of idronoxil, a synthetic flavonoid derivative, surrounded by a proprietary lipid that protects idronoxil from phase 2 degradation, with potential chemo- and radio-sensitizing activities. Upon administration, idronoxil blocks the activity of ecto-NOX disulfide-thiol exchanger 2 (ENOX2; tNOX), a tumor-specific external NADH oxidase that maintains the transmembrane electron potential across the plasma membrane and is overexpressed in certain cancer cell types while absent in normal, healthy cells. Loss of this potential directly inhibits certain pro-survival signal transduction pathways, such as the PARP1/PI3 kinase/Akt signaling pathway. The inhibition of these pathways prevents resistance to standard chemo- and radio-therapy and makes tumor cells more susceptible to the anti-tumor activity of conventional chemotherapeutic agents and radiotherapy. The formulation prevents detoxification of idronoxil to an inactive form by bypassing phase 2 metabolism; this increases idronoxil’s bioavailability as compared to idronoxil alone.

Brand name for ifosfamide

A synthetic analogue of the nitrogen mustard cyclophosphamide with antineoplastic activity. Ifosfamide alkylates and forms DNA crosslinks, thereby preventing DNA strand separation and DNA replication. This agent is a prodrug that must be activated through hydroxylation by hepatic microsomal enzymes.

An oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity. Dual IGF-IR/InsR inhibitor BMS-754807 binds reversibly to and inhibits the activities of IGF-1R and InsR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-1R and InsR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in mitogenesis, angiogenesis, and tumor cell survival.

Autologous glioma cells treated ex vivo with an 18-mer antisense oligodeoxynucleotide of insulin-like growth factor receptor 1 (IGF-1R/AS ODN), with potential antineoplastic activity. IGF-1R/AS ODN pre-treated glioma cells encapsulated in small Lucite diffusion chambers are implanted into a subcutaneous pocket in the patient’s abdominal rectus sheath. Within the diffusion chambers, IGF-1R/AS ODN binds to IGF-1R mRNA, and shuts down the translation of IGF-1R in the glioma cells. Downregulation of IGF-1R induces apoptosis and causes the release of exosomes, which contain tumor-associated antigens (TAAs). The diffusion of exosomes and IGF-1R/AS ODN from the Lucite chambers may active the patient’s immune system and mount a cytotoxic T-lymphocyte (CTL) response against cells expressing these TAAs. IGF-1R, a receptor tyrosine kinase, is overexpressed in a variety of tumor cell types and is essential for tumor cell growth, transformation and survival.

An orally bioavailable inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. IGF-1R inhibitor PL225B selectively binds to and inhibits the activities of IGF-1R, which may result in both the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis in IGF-1R-overexpressing tumor cells. IGF-1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a significant role in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

An orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

A conjugate containing the antimetabolite and antifolate agent methotrexate conjugated to insulin-like growth factor (IGF), with potential antineoplastic activity. After intravenous administration, the IGF moiety of the IGF-methotrexate conjugate binds to and is internalized by IGF receptors (IGFR) on the surface of tumor cells. Following cell entry, the methotrexate then binds to and inhibits the enzyme dihydrofolate reductase, which catalyzes the conversion of dihydrofolate to tetrahydrofolate. This results in both the inhibition of DNA and RNA synthesis and the induction of death in rapidly dividing cells. Binding to IGFR can localize the cytotoxic effect of methotrexate in tumor cells. This may increase its efficacy while decreasing its toxicity to normal, healthy cells. IGFR is overexpressed on many types of cancer cells and has been implicated in metastasis and resistance to apoptosis.

An immunoglobulin preparation consisting of immunoglobulin G (IgG) and immunoglobulin A (IgA), supplemented with immunoglobulin M (IgM), with potential antibacterial and immunomodulatory properties. Upon intravenous administration, IgM-enriched immunoglobulins may increase the elimination of infectious pathogens in comparison to immunoglobulin regimens lacking IgM. IgM is the major immunoglobulin secreted during the primary immune response and plays a significant role in compliment activation and in the neutralization of bacterial endo- and exotoxins.

An oligomeric proanthocyanidin extracted from grape seeds. IH636 grape seed proanthocyanidin extract exhibits dose-dependent free-radical scavenging and antioxidant properties.

An agent that downregulates the activity of the anti-inflammatory cytokine human interleukin-10 (IL-10), with potential immunomodulating and antineoplastic activities. Upon administration, IL-10 immunomodulator MK-1966 blocks the activity of IL-10 and may abrogate the IL-10-induced immunosuppressive tumor microenvironment. This activates cell-mediated immunity against cancer cells, increases cytokine production, including interferon-gamma (IFN-g), decreases T regulatory cell (Treg) activity, and induces a tumor-specific cytotoxic CD8+ T-cell-mediated immune response, which enhances tumor cell death.

Human mesenchymal stem cells (MSCs) transduced with a retroviral vector encoding a modified form of the cytokine interleukin-12 (IL-12), with potential immunomodulating and antineoplastic activities. Upon intratumoral administration, IL-12-expressing MSC vaccine GX-051 secretes IL-12. IL-12 activates the immune system by both promoting the secretion of interferon-gamma, which activates natural killer cells (NKs), and inducing cytotoxic T-cell responses, which may result in both decreased cell proliferation and increased cell death in tumor cells.

A preparation of ex vivo expanded, genetically modified autologous central memory-enriched T-cells (Tcm) transduced with a replication-incompetent, self-inactivating (SIN) lentiviral vector expressing a hinge-optimized, chimeric antigen receptor (CAR) specific for interleukin-13 receptor alpha 2 (IL13Ra2), and containing the cluster of differentiation 137 (CD137; 4-1BB) co-stimulatory signaling domain fused to the signaling domain of the T cell antigen receptor complex zeta chain (CD3-zeta), and a truncated form of human cluster of differentiation 19 (CD19t), with potential immunostimulating and antineoplastic activities. Upon intratumoral or intracavitary administration, IL13Ra2-specific, hinge-optimized, 41BB-co-stimulatory CAR/truncated CD19 expressing T-lymphocytes are directed to, and induce selective toxicity and cytolysis in IL13Ra2-expressing tumor cells. IL13Ra2, overexpressed by a variety of tumor cell types, is associated with increased tumor cell proliferation, migration and invasiveness. The costimulatory signaling domain enhances both proliferation of T cells and antitumor activity. Hinge optimization prevents the recognition and clearance of the CAR by endogenous Fc receptors (FcRs). CD19t is used as a surface marker to both quantify and track the gene-modified T cells in vivo.

A preparation of ex vivo expanded, genetically modified autologous naïve and memory T cells (TN/MEM) transduced with a replication incompetent, self-inactivating (SIN) lentiviral vector expressing a hinge-optimized, chimeric antigen receptor (CAR) specific for interleukin-13 receptor alpha 2 (IL13Ra2), and containing the cluster of differentiation 137 (CD137; 4-1BB) co-stimulatory signaling domain fused to the signaling domain of the T-cell antigen receptor complex zeta chain (CD3-zeta), and a truncated form of human cluster of differentiation 19 (CD19t), with potential immunostimulating and antineoplastic activities. Upon intratumoral or intracavitary administration, IL13Ra2-specific hinge-optimized 4-1BB-co-stimulatory CAR/truncated CD19-expressing autologous TN/MEM cells are directed to, and induce selective toxicity and cytolysis in, IL13Ra2-expressing tumor cells. IL13Ra2, overexpressed by a variety of tumor cell types, is associated with increased proliferation, migration and invasiveness of tumor cells. The co-stimulatory signaling domain enhances both proliferation of T cells and antitumor activity. Hinge optimization prevents the recognition and clearance of the CAR by endogenous Fc receptors (FcRs). CD19t is used as a surface marker to both track and quantify the modified T cells in vivo.

An immunotherapeutic agent consisting of a plasmid DNA encoding human Interleukin-2 (IL-2) complexed with a cationic lipid, 1,2-dimyristyloxypropyl-3-dimethyl-hydroxyethyl ammonium bromide/dioleyl-phosphatidyl-ethanolamine (DMRIE/DOPE), in a 5:1 ratio. Due to the lipophilic nature of this cation liposome complex, this gene transfer system may improve the efficiency of introducing the IL-2 gene into the cells, thereby increasing the production of IL-2 and inducing an immune response.

A recombinant protein consisting of the cytokine interleukin-2 (IL-2) fused to a humanized soluble T-cell receptor (TCR) directed against a tumor suppressor p53-derived antigen with potential immunopotentiating and antineoplastic activities. The TCR moiety of IL-2 recombinant fusion protein ALT-801 binds to tumor cells displaying p53 epitope/MHC complexes; subsequently, the tumor cell-localized IL-2 moiety may stimulate natural killer (NK) cell and T cell cytotoxic immune responses against p53-expressing tumor cells.

A pegylated peptide antagonist that binds to the common gamma chain (gc; IL2RG; CD132) of the signaling receptor for the pro-inflammatory cytokines interleukin (IL)-2, IL-9, and IL-15, with potential immunomodulating and antineoplastic activities. Upon administration, IL-2/9/15 gc receptor inhibitor BNZ-1 specifically targets and binds to the IL binding site on the gc receptor and blocks IL-2, IL-9 and IL-15 binding, thereby inhibiting IL-2-, IL-9-, and IL-15-mediated signaling and downstream pathways. This may inhibit proliferation of tumor cells that are dependent on IL-2/9/15 signaling for their growth. IL-2/9/15 are upregulated in certain tumor cell types and play a key role in tumor progression and survival.

A cancer vaccine consisting of allogeneic neuroblastoma tumor cells have been genetically modified to secrete the human cytokine interleukin-2 (IL-2) and the human chemokine lymphotactin (Lptn) with potential immunostimulating and antineoplastic activities. Upon administration, IL-2 and Lptn are secreted by the IL-2/Lptn gene-modified allogeneic neuroblastoma tumor cell vaccine, potentially enhancing the cytotoxic T lymphocyte (CTL) response elicited by vaccine neuroblastoma tumor-associated antigens (TAAs) against host neuroblastoma tumor cells. Produced by activated progenitor T cells, Lptn belongs to the C chemokine subfamily and is a potent chemotactic factor for lymphocytes; IL-2 stimulates natural killer (NK) cells and may enhance a vaccine-elicited CTL immune response against tumor cells.

A fusion protein consisting of the cytokine interleukin-4 (IL-4) linked to a truncated form of Pseudomonas exotoxin with potential antineoplastic activity. Upon specific, high-affinity binding to IL-4 receptors (IL-4Rs) located on the tumor cell surface., IL4-Pseudomonas exotoxin fusion protein MDNA55 is internalized; the exotoxin moiety then binds to translation elongation factor 2 (EF-2), which may result in ADP ribosylation, deactivation of EF-2, inhibition of protein synthesis, and tumor cell apoptosis. The Pseudomonas exotoxin moiety of this agent has been engineered to reduce non-specific binding to cells expressing its receptor, the multiligand cell surface receptor alpha 2-macroglobulin receptor/low-density lipoprotein receptor-related protein (alpha 2MR/LRP). IL-4R is a type I transmembrane protein that binds IL-4 and IL-13 and may be overexpressed by cancers such as renal cell carcinoma (RCC) and glioma.

A substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity. A weak base, ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.

Brand name for canakinumab

An off-the-shelf immune primer consisting of allogeneic monocyte-derived dendritic cells (MoDCs) that have been stimulated with a combination of activating factors to produce pro-inflammatory factors including tumor necrosis factor-alpha (TNF-alpha), interleukin-1 beta (IL-1 beta), interleukin-12, p70 (IL-12 p70), C-C motif chemokine 4 (CCL4; macrophage inflammatory protein 1-beta; MIP-1-beta), C-C motif chemokine 5 (CCL5; RANTES), and C-X-C motif chemokine 10 (CXCL10), with potential immunostimulating and antineoplastic activities. Upon intratumoral injection of ilixadencel, the dendritic cells (DCs) release type 1 T-helper cell (Th1)-associated chemokines, including CCL4, CCL5 and CXCL10, that may recruit natural killer (NK)-cells and pre-DCs into the tumor microenvironment (TME). The interaction between NK cells and ilixadencel DCs may induce NK-cell-mediated killing of tumor cells, resulting in release of tumor-associated-antigens (TAAs). The production of interferon-gamma (IFN-gamma) by activated NK-cells and TNF-alpha/beta released by ilixadencel DCs will induce maturation and promote cross-presentation of TAAs by recruited endogenous "bystander" DCs. Migration of these antigen-loaded and matured "bystander" DCs to the tumor-draining lymph node will lead to a Th1-polarized activation of tumor-specific T-cells.

Brand name for dexpanthenol cream

A prostacyclin analogue with potential chemopreventive activity. Iloprost binds to the prostacyclin receptor in various target cells, thereby causing vasodilation, inhibition of platelet aggregation, and decreased tumor cell adhesion to endothelium among other effects. Prostacyclin is a naturally occurring eicosanoid with anti-inflammatory, antineoplastic, and anti-metastatic properties.

An orally bioavailable, adenosine triphospate mimetic, and inhibitor of Aurora kinases, vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptor (PDGFRs), with potential antineoplastic activity. Upon administration, ilorasertib selectively binds to and inhibits Aurora kinases A, B and C, which may disrupt both the assembly of the mitotic spindle apparatus and chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells. In addition, ilorasertib selectively binds to and inhibits VEGFRs and PDGFRs, which may result in the inhibition of both angiogenesis and tumor cell proliferation in VEGFR/PDGFR-overexpressing tumor cells. This agent also inhibits the Src family of cytoplasmic tyrosine kinases. Aurora kinases A, B and C, are serine/threonine kinases that play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of tumor cell types. Both VEGFRs and PDGFRs are receptor tyrosine kinase families whose members may be upregulated in various tumor cell types.

Brand name for erythromycin

Brand name for [[perflubron) * imaging agent QRH-882260 heptapeptide An orally bioavailable fluorescent imaging agent composed of the near-infrared (NIR) fluorophore cyanine 5 (Cy5) linked to a seven-amino acid long peptide that specifically binds to the tumor-associated antigen (TAA) epithelial growth factor receptor (epidermal growth factor receptor; EGFR), that can potentially be used for the imaging of EGFR-expressing tumor cells. Upon oral administration of the fluorescent imaging agent QRH-882260 heptapeptide, the peptide moiety selectively binds to EGFR expressed on tumor cells in the gastrointestinal (GI) tract. Upon fluorescence imaging, EGFR-expressing tumor cells can be visualized. EGFR, a member of the epidermal growth factor receptor family, is overexpressed on the surfaces of various tumors cells.

A human, recombinant monoclonal antibody (MoAb) against macrophage migration inhibitory factor (MIF), with potential immunomodulating, anti-inflammatory and antineoplastic activities. Upon intravenous administration, imalumab binds to MIF, blocking its activity and preventing the MIF-mediated secretion of certain cytokines, including interleukin-1 beta and tumor necrosis factor-alpha. This may lead to an inhibition of cancer cell proliferation in MIF-overexpressing tumor cells. MIF, a pro-inflammatory cytokine overexpressed in some cancers, plays a key role in inflammation, immune responses and cancer cell proliferation.

The mesylate salt of imatinib, a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Inhibition of the bcr-abl TK results in decreased proliferation and enhanced apoptosis in malignant cells of Philadelphia-positive (Ph+) hematological malignancies such as CML and ALL; effects on c-kit TK activity inhibit mast-cell and cellular proliferation in those diseases overexpressing c-kit, such as mastocytosis and gastrointestinal stromal tumor (GIST).

Brand name for ibrutinib

The sodium salt of imetelstat, a synthetic lipid-conjugated, 13-mer oligonucleotide N3' P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase RNA (hTR), imetelstat acts as a competitive enzyme inhibitor that binds and blocks the active site of the enzyme (a "telomerase template antagonist"), a mechanism of action which differs from that for the antisense oligonucleotide-mediated inhibition of telomerase activity through telomerase mRNA binding. Inhibition of telomerase activity in tumor cells by imetelstat results in telomere shortening, which leads to cell cycle arrest or apoptosis.

A 2-cyanoaziridine derivative with antitumor activity in multiple myeloma. Although its mechanism of action is not clearly known, imexon may induce apoptosis via a pathway involving cleaved caspase-3, caspase-9, and/or caspase-8. Other cytotoxic mechanisms of action of this agent may involve thiol depletion, generation of reactive oxygen species (ROS), and decreases in the mitochondrial membrane potential.

Brand name for durvalumab

A synthetic derivative of imidazole with potent antineoplastic properties. Imidazole mustard alkylates DNA, preferentially at guanine residues, resulting in DNA interstrand crosslinks and inhibition of DNA replication and RNA and protein synthesis.

An orally bioavailable small molecule, with potential hematopoiesis inducing and antiviral activities. Upon oral administration, myelo001 stimulates the differentiation of bone marrow cells of the leukocytic, lymphocytic, and erythrocytic lineages, and prevents apoptosis of hematopoietic cells. This prevents chemotherapy-induced neutropenia (CIN), inhibits the risk of infections, increases tolerance and allows for the continuation of the neutropenia-inducing chemotherapeutic agent. In addition, myelo 001 has antiviral properties.

A broad-spectrum, semi-synthetic beta-lactam carbapenem derived from thienamycin, produced by Streptomyces cattleya. Imipenem binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes that are involved in the last stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. This inactivation results in the weakening of the bacterial cell wall and eventually causes cell lysis. Imipenem has the greatest affinity for PBP 1A, 1B, and 2, and its lethal effect is related to binding to PBP 2 and 1B. This antibiotic is active against a wide range of gram-positive and gram-negative organisms and is stable in the presence of beta-lactamases.

A synthetic tricyclic derivative, antidepressant Imipramine enhances monoamine neurotransmission in certain areas of the brain. It also induces sedation through histamine 1 receptor blockage; hypotension through beta-adrenergic blockage; and diverse parasympatholytic effects. Imipramine has less sedative effect than other members of its therapeutic family. It is used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders.

A synthetic agent with immune response modifying activity. As an immune response modifier (IRM), imiquimod stimulates cytokine production, especially interferon production, and exhibits antitumor activity, particularly against cutaneous cancers. Imiquimod's proapoptotic activity appears to be related to Bcl-2 overexpression in susceptible tumor cells.

A manganese-based non-peptidyl mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD), with potential antioxidant and chemo/radioprotective activities. Upon administration, imisopasem manganese mimics the activity of MnSOD and scavenges reactive oxygen species (ROS), such as superoxide anion, which prevents oxygen free radical damage to macromolecules such as DNA. This reduces ROS-mediated lipid peroxidation, prevents apoptosis and protects against oxygen free radical-induced toxicity in normal tissues.

Brand name for sumatriptan succinate

Brand name for talimogene laherparepvec

An immediate-release (IR) tablet formulation containing afuresertib, an inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Upon oral administration of the IR formulation, afuresertib binds to and inhibits the activity of Akt, which may result in the inhibition of PI3K/Akt signaling pathway, decreased tumor cell proliferation and the induction of tumor cell apoptosis in Akt-expressing tumor cells. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

An immediate-release (IR) formulation of onapristone, an orally bioavailable progesterone receptor (PR) antagonist, with antineoplastic activity. Onapristone binds to the PR and inhibits both PR activation and the associated expression of PR-responsive genes. This may inhibit PR-mediated proliferative effects in cancer cells overexpressing PR. PR is expressed in certain cancer cell types and plays a key role in proliferation and survival.

Brand name for disaccharide tripeptide glycerol dipalmitoyl

Brand name for beta-glucan

Brand name for arginine/omega-3 fatty acids/nucleotides oral supplement

An immune checkpoint inhibitor with potential immunomodulating and antineoplastic activities. Although the exact target is undisclosed, ASP8374 inhibits the activity of an immune checkpoint protein, which ultimately leads to the activation of a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells.

A synthetic saponin, chemically identical to the natural saponin QS-21, with immunoadjuvant activity. When co-administered with vaccine antigens, immunoadjuvant QS-DG may increase total antitumoral vaccine-specific antibody responses and cytotoxic T-lymphocyte (CTL) responses.

Brand name for whey protein isolate

An immunoconjugate containing a glycoengineered, humanized monoclonal antibody directed against the human epidermal growth factor receptor HER3 (ErbB3), with potential antineoplastic activity. Upon administration, RO5479599 binds to the extracellular domain of HER3 and inhibits HER3 dimerization; thereby, preventing EGFR-dependent signaling. In addition, RO5479599 stimulates the immune system to exert antibody-dependent cellular cytotoxicity (ADCC). This may decrease proliferation of HER3-overexpressing tumor cells. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors; it has no active kinase domain but is activated through heterodimerization with other members of the EGFR receptor family, such as HER2.

A fusion protein consisting of the heavy-chains of the human antibody NHS76, raised against DNA released by necrotic tumor cells, and fused to two molecules of a genetically modified human interleukin-12 (IL-12) with potential immunostimulating and antineoplastic activities. Upon administration, the antibody moiety of immunocytokine NHS-IL12 binds to DNA released from necrotic tumor cells located primarily at the core of necrotic solid tumors, thereby delivering the IL-12 moiety. In turn, the IL-12 moiety of this agent stimulates the host immune system to mount an immune response against tumor cells, thereby inhibiting tumor growth. IL-12 is a proinflammatory cytokine with numerous immunoregulatory functions and may augment host immune responses to tumor cells. By targeting tumor cells, NHS-IL-12 may reduce the toxicity associated with systemic administration of recombinant human IL-12.

A fusion protein consisting of a mouse-human chimeric antibody directed against DNA released by necrotic tumor cells fused to two molecules of a genetically modified human interleukin-2 (IL-2) with potential antineoplastic activity. Upon administration, the antibody moiety of immunocytokine NHS-IL2-LT binds to DNA released by necrotic tumor cells located primarily at the core of necrotic solid tumors, delivering the IL-2 moiety. In turn, the IL-2 moiety of this agent activates the immune system to mount a cytotoxic T lymphocyte response against nearby tumor cells.

A purified, natural saponin isolated from the soapbark tree Quillaja saponaria Molina with potential immunoadjuvant activity. When co-administered with vaccine peptides, OPT-821 may increase the antibody and cytotoxic T-cell responses against the targeted antigen(s).

An orally bioavailable immunomodulating agent with potential antineoplastic activity

A peptide-nucleic acid immunomodulator with proinflammatory, broad-spectrum antiviral, and potential antineoplastic activities. Immunomodulator OHR/AVR118 stimulates the peripheral blood mononuclear cell (PBMC) production of the proinflammatory cytokines IFN-y, IL-1b, IL-6 and TNF-a. This agent may reduce HIV-1 p24 antigen; viral reverse transcriptase activity; syncitial cell formation; and viral mRNA in infected PBMCs and human CD4+ lymphocyte H9 cells, and may decrease viral loads and increase CD4+ and CD8+ T-cell counts in HIV patients. In vitro, immunomodulator OHR/AVR118 has been shown to induce the maturation of HL60 leukemic cells and to inhibit the invasive and metastatic properties of a highly malignant breast cancer cell line.

A proprietary, orally available, small molecule and thalidomide analog, with potential immunomodulating and antineoplastic activity. CC-11006 appears to have a similar mechanism to thalidomide and may modulate the expression of proinflammatory and regulatory cytokines.

An immunotherapeutic combination product composed of LV305, an engineered lentiviral vector that both targets dendritic cells (DCs) and contains nucleic acids encoding the human tumor-associated cancer-testis antigen NY-ESO-1 (CTAG1), and G305, a cancer vaccine comprised of an NY-ESO-1 recombinant protein and glucopyranosyl lipid adjuvant (GLA)-stable emulsion (GLA-SE), with potential synergistic immunostimulatory and antineoplastic activities. Upon intradermal administration of LV305, the DC-targeting lentiviral vector targets and binds to dermal DCs via the DC-specific intercellular adhesion molecule-3-grabbing non-integrin (DC-SIGN) receptor. Upon internalization of the vector, the NY-ESO-1 protein is expressed, which stimulates DC maturation, and activates the immune system to mount a cytotoxic T-lymphocyte (CTL) response against NY-ESO-1-expressing cells; this may result in tumor cell lysis. Upon the sequential intramuscular injection of G305, the adjuvant portion of G305 binds to toll-like receptor 4 (TLR-4) expressed on various immune cells, including DCs, monocytes, macrophages and B-cells. The activated DCs present the NY-ESO-1 antigen to CD4-positive Th1 T-lymphocytes. The induction of antigen-specific CD4-positive T-lymphocytes further induces a CTL response against NY-ESO-1-expressing tumor cells. In addition, G305 induces an NY-ESO-1-specific antibody response. NY-ESO-1, expressed in normal testes and on the surfaces of various tumor cells, plays a key role in tumor cell proliferation and survival.

An immunotherapeutic containing a proprietary adjuvant system combined with a melanoma-associated antigen peptide MAGE-A3 epitope with potential immunomodulating and antineoplastic activities. Intramuscular administration with GSK1572932A may stimulate the immune system to exert both humoral and cellular immune responses against MAGE-A3-expressing tumor cells. MAGE-A3, a tumor associated antigen (TAA), is overexpressed in a variety of tumor cell types, including non-small cell lung cancer (NSCLC), melanoma, head and neck cancer, and bladder cancer.

An immunotherapy regimen containing three components: a plasmid encoding portions of the two melanoma-associated antigens Melan A (also called MART-1) and tyrosinase and two synthetic analogs of Melan-A and tyrosinase antigen epitopes with potential immunostimulating and antitumor activities. First, the plasmid is injected directly into lymph nodes in order to sensitize or prime antigen-presenting cells (APCs) and central memory T cells in lymph nodes to plasmid-expressed Melan A and tyrosinase. After several priming injections with plasmids, the Melan A and tyrosinase synthetic epitope analogs are injected directly into lymph nodes; upon binding to major histocompatibility complex (MHC) molecules on APC cell surfaces, these synthetic epitope analogs may stimulate a "primed" cytotoxic T lymphocyte (CTL) response against melanoma tumor cells, resulting in tumor cell lysis. Melan-A and tyrosinase are overexpressed by melanoma tumor cells.

A humanized immunotoxin directed against the Lewis Y antigen conjugated with calicheamicin, a hydrophobic enediyne antibiotic, with potential antineoplastic activity. CMD193 binds to the Lewis Y antigen, a tetrasaccharide expressed on the cell surfaces of many tumor cell types. Upon binding, CMD-193 is internalized, thereby delivering the attached calicheamicin to Lewis Y antigen-expressing tumor cells. Calicheamicin binds non-covalently to the minor groove of DNA and prompts conformational changes and DNA oxidation, thereby inhibiting DNA synthesis and inducing apoptosis.

A recombinant immunotoxin fusion protein consisting of single-chain variable-region antibody fragments (scFvs), which contain disulfide stabilized heavy- (Vh) and light- (Vl) chain variable regions of the monoclonal antibody D2C7 (D2C7-scdsFv), targeting both the wild-type form (EGFRwt) and the in-frame deletion mutant form (EGFRvIII) of epidermal growth factor receptor (EGFR), and fused, via a 15-amino acid peptide linker to domains II and III of the Pseudomonas exotoxin A (PE38KDEL) (D2C7-(scdsFv)-PE38KDEL), with potential antineoplastic activity. Upon intratumoral administration by convection-enhanced delivery, the scFv moiety of immunotoxin anti-EGFR scFv monoclonal antibody fragment immunotoxin D2C7-(scdsFv)-PE38KDEL targets and binds to a specific amino acid epitope present in the extracellular domain of both the EGFRwt and EGFRvIII proteins. This binding facilitates the internalization of the immunotoxin by tumor cells. Inside the cells, the exotoxin portion of the fusion protein binds to translation elongation factor 2 (EF-2), and deactivates EF-2 through ADP ribosylation. This results in the inhibition of protein synthesis, the induction of apoptosis and a reduction in cell proliferation of EGFRwt/EGFRvIII-expressing tumor cells. Compared to intact IgG antibodies and single-chain antibodies, scFvs are smaller with increased tumor-penetrating capacity which may enhance therapeutic efficacy. The EGFR gene, a transmembrane receptor tyrosine kinase, and its mutant form, EGFRvIII, which contains a deletion of exons 2–7 of the EGFR gene, are frequently amplified and overexpressed in a variety of cancers. KDEL increases the toxin’s intracellular retention, thereby enhancing its cytotoxicity. Check for active clinical trialsusing this agent.

Brand name for thymopentin

Brand name for loperamide hydrochloride

A T-cell immunostimulatory factor derived from the soluble form of lymphocyte-activation gene 3 (LAG-3) protein with potential antineoplastic activity. Upon administration, alone or in combination with tumor antigens, IMP321 binds, with high affinity, to MHC class II molecules expressed by dendritic cells (DC), which may result in DC maturation, DC migration to lymph nodes, enhanced DC cross-presentation of antigens to T cells, and antitumor cytotoxic T cell responses.

Brand name for arginine/omega-3 fatty acids/nucleotides oral supplement

Brand name for PGG beta-glucan

A multi-peptide cancer vaccine with potential immunostimulating and antineoplastic activities. IMT-1012 immunotherapeutic vaccine contains twelve different synthetic peptides or tumor associated antigens (TAAs), including cyclin I (CCNI), cyclin-dependent kinase CDC2, EDDRI and TACE/ADAM17, each of which is involved in a different pathway associated with tumor growth, survival, and metastasis. Each antigen in the vaccine elicits a specific cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing that antigen. This multi-antigen/multi-pathway targeting strategy provides broad immunotherapeutic coverage with respect to tumor complexity and heterogeneity and may result in enhanced vaccine efficacy.

Brand name for azathioprine sodium

A vaccine consisting of inactivated poliovirus (IPV) types 1,2 and 3, with active immunizing activity against poliomyelitis. Upon intramuscular vaccination, inactivated poliovirus vaccine (IPV) activates the immune system to develop antibodies against polioviruses.

A cancer vaccine comprised of a recombinant vaccinia viral vector encoding the carcinoembryonic antigen (CEA), MUC-1 (mucin-1), a transmembrane glycoprotein secreted by glandular tissues, and TRICOM, comprised of the three co-stimulatory molecule transgenes B7-1, ICAM-1 and LFA-3. Upon administration, inalimarev may enhance CEA and MUC-1 presentation to antigen presenting cells (APC) and may activate a cytotoxic T lymphocyte (CTL) response against CEA- and MUC-1-expressing tumor cells.

Brand name for droperidol

Brand name for biricodar dicitrate

Brand name for telaprevir

A water-in-oil emulsion that stimulates the T-cell immune response to antigens and may be used in various types of cancer vaccines.

A chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis.

Brand name for propranolol hydrochloride

A synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines.

A natural pyrrolizidine alkaloid with antineoplastic properties. Indicine-N-oxide alkylates and crosslinks DNA.

A synthetic antiviral agent. Indinavir selectively binds to the active site of human immunodeficiency virus (HIV) protease and inhibits its activity, preventing the protease-mediated cleavage of gag-pol viral polyproteins; as a result immature, noninfectious virions are produced.

Brand name for indium In 111 capromab pendetide

A radioimmunoconjugate containing the murine IgG1 anti-CD45 monoclonal antibody (MoAb) BC8 labeled with the gamma-emitting isotope indium 111 (In 111), with potential radioimaging application. Upon administration, indium In 111 anti-CD45 monoclonal antibody BC8 binds to CD45 antigen, a receptor protein tyrosine phosphatase expressed on the surface of most of the normal and malignant hematopoietic cells. After binding and internalization by CD45-expressing tumor cells, radioactive In 111 allows for the detection of BC8 distribution and tumor localization using gamma scintigraphy.

A radioimmunoconjugate composed of a humanized monoclonal antibody IgG1 directed against the epidermal growth factor receptor (EGFR) and labeled with the radioisotope indium In 111, with potential radioimaging activity. Indium In 111 anti-EGFR monoclonal antibody ABT-806 binds to a specific epitope of either wild-type or EGFR variant III mutant on tumor cells, thereby allowing imaging of EGFR-expressing tumor cells using gamma scintigraphy. ABT-806 is the humanized version derived from the predecessor chimeric monoclonal antibody 806. EGFR, a receptor tyrosine kinase overexpressed on the cell surfaces of many tumor cell types, plays a key role in tumor cell proliferation.

A radioimmunoconjugate comprised of the recombinant humanized monoclonal antibody bevacizumab conjugated with the gamma-emitting radioisotope indium In 111. Indium I 111 bevacizumab binds to vascular endothelial growth factor (VEGF), allowing the detection of VEGF distribution using gamma scintigraphy. Check for active clinical trialsusing this agent.

A radioimmunoconjugate consisting of the murine IgG1 kappa monoclonal antibody capromab (7E11-C5.3), conjugated to the linker-chelator glycyl-tyrosyl-(N,-diethylenetriaminepentaacetic acid)-lysine hydrochloride (GYK-DTPA-HCl) and labeled with radioisotope indium In 111, with ligand-binding and gamma-emitting activities. Upon intravenous administration, indium In 111-capromab pendetide binds to a cytoplasmic epitope of human prostate specific membrane antigen (PSMA) expressed on prostate tumor cell surfaces via its capromab moiety and, upon internalization, allows radioimmunolocalization with gamma scintigraphy. PSMA is a cell surface glycoprotein abundantly expressed by prostate epithelium and is typically overexpressed by prostate cancer cells.

A recombinant chimeric, mouse-human monoclonal antibody IgG1, directed against the epidermal growth factor receptor (EGFR) and labeled with the radioisotope indium-111, with potential radioimaging activity. Indium 111 chimeric monoclonal antibody 806 binds to a specific epitope on EGFR-expressing tumor cells, allowing imaging of EGFR-expressing tumor cells using gamma scintigraphy. EGFR is a receptor tyrosine kinase that is involved in the regulation of cell growth and is found to be overexpressed on the cell surfaces of many tumor cell types.

An indium I 111-labeled trastuzumab with potential use as an imaging agent. Indium In 111 CHX-A DTPA trastuzumab is chemically conjugated via a bifunctional metal chelator molecule, 2-(p-isothiocyanatobenzyl)-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-A DTPA), a backbone-substituted derivative of DTPA. This agent may allow radioimmunolocalization of HER2-positive cells. Trastuzumab, a recombinant humanized monoclonal antibody that selectively binds with high affinity to the extracellular domain of human epidermal growth factor receptor 2 (HER2), may elicit an antibody-dependent cellular cytotoxicity (ADCC) against tumor cells that overexpress HER2.

A targeted radioimmunoconjugate composed of a murine monoclonal anti-CD20 antibody (ibritumomab) linked by a chelator (tiuxetan) to the imaging radioisotope indium-111. This radioimmunoconjugate binds to CD20-positive cells, permitting radioimmuno-localization of CD20-positive cell biodistribution.

A radioconjugate consisting of the minigastrin analog, CP04, labeled with the gamma-emitting radioisotope indium-111, with radioimaging potential. Upon intravenous administration, 111In-CP04 binds to and is subsequently internalized by cells expressing cholecystokinin receptor subtype 2 (CCK2R), which is overexpressed in certain tumor types. 111In-CP04 emits gamma radiation and X-ray photons that allow detection of tumor localization and distribution using gamma scintigraphy.

A humanized monoclonal antibody conjugated to the imaging radioisotope (indium-111). This radioimmunoconjugate binds to the breast epithelial mucin antigen, which is found primarily on breast cancer cells, permitting radioimmmuno-localization of mucin-positive tumor cells and an estimate of radiation dosimetry prior to administration of cytotoxic radiotherapy.

A radioimmunoconjugate containing the recombinant humanized monoclonal antibody J591 directed against the extracellular domain of prostate-specific membrane antigen (PSMA) and labeled with the gamma-emitting isotope indium 111 (In 111; 111In), with potential radioimaging application. Upon administration, indium In 111 monoclonal antibody J591 targets and binds to PSMA expressed on tumor cells. The use of gamma scintigraphy allows for the detection and imaging of the radioactive In 111, which can be used to determine the distribution and tumor localization of PSMA. PSMA is a transmembrane peptidase that is highly expressed on prostate tumor cells.

The humanized monoclonal antibody huPAM4, directed against the pancreatic cancer antigen MUC-1 and radiolabled with the gamma-emitting radioisotope indium I 111, with radioisotopic and antibody activities. Upon administration, indium In 111 monoclonal antibody huPAM4 may bind to MUC-1-positive tumor cells, allowing radioimmunolocalization with gamma scintigraphy. Overexpressed by many tumor cell types, MUC-1 antigen, a mammary-type apomucin, is a high-molecular-weight transmembrane glycoprotein.

A sterile, non-pyrogenic, isotonic solution of radioactive indium In 111 diethylenetriamine pentaacetate (DTPA). When administered intrathecally, indium In 111 pentetate percolates up the spinal canal with the cerebrospinal fluid (CSF) to the basal cisterns of the posterior and middle cranial fossas. This agent is used in radionuclide cisternography to image the flow of CSF, for the identification of abnormalities in CSF circulation, for location of sites of CSF leakage, and for evaluation of CSF shunt patency. Normally, this agent does not penetrate into the brain ventricles.

An indium 111 radioconjugate of pentetreotide, the diethylenetriaminopentaacetic (DTPA) conjugate of the human hormone somatostatin peptide analogue (octreotide), used for radioimaging neuroendocrine tumor cells. The pentetreotide moiety of indium In 111 pentetreotide binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells. Upon binding and internalization, this radioconjugate allows for specific imaging of neuroendocrine tumors that overexpress somatostatin using scintigraphic imaging techniques. In addition, high dose indium In 111 pentetreotide may specifically deliver a cytotoxic dose of gamma radiation to SSTR-positive cells thereby killing SSTR-expressing tumor cells.

A radioimmunoconjugate composed of a humanized recombinant monoclonal antibody directed against the extracellular dimerization domain of the tyrosine kinase receptor human epidermal growth factor-2 (HER-2) and linked to the gamma-emitting radioisotope indium In 111, with potential use in radioimaging. Upon administration, indium In 111 pertuzumab binds to HER-2. After binding and internalization into HER-2-expressing tumor cells, radioactive In 111 facilitates the detection of HER-2-expressing tumor cells using single photon emission computed tomography (SPECT). This may predict or evaluate the tumor's response to certain HER-2-targeting chemotherapeutics.

A radiolabeled antibody-targeted antineoplastic antibiotic consisting of the enediyne antibiotic calicheamicin conjugated with anti-Lewis Y antibody and labeled with indium In 111. In 111 CMD-193 binds to Lewis Y antigen-expressing tumor cells via its antibody moiety and is internalized; subsequently, the calicheamicin moiety binds to the minor groove of tumor cell DNA, causing double-strand DNA breaks, the inhibition of DNA synthesis, and apoptosis. The indium In 111 radiolabel allows the detection of CMD-193 distribution and tumor localization using gamma scintigraphy.

A radioimmunoconjugate of biotin conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and labeled with indium 111 (In-111). Biotin is a water-soluble B-complex vitamin, present in minute amounts in every living cell, while its level in cancerous tissue is higher than that of normal tissue. In 111-DOTA-Biotin could be used in 3-step pre-targeting radioimmunotherapy that employs tumor targeting antibody conjugated with streptavidin, the natural ligand of biotin.

A radiopharmaceutical composed of the glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 linked by the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the positron-emitting radionuclide indium In 111, with potential use in diagnostic imaging upon positron emission tomography (PET). Upon administration of indium In 111-DOTA-exendin-4, the exendin-4 moiety binds to GLP-1R and is subsequently internalized. The radionuclide moiety can be detected using PET and GLP-1R-expressing tumors can be localized. GLP-1R, located on beta cells, is overexpressed on insulinomas, which are insulin-secreting neuroendocrine tumors.

A radioimmunoconjugate comprised of the chimeric monoclonal antibody girentuximab conjugated with the gamma-emitting radioisotope indium In 111. Indium In 111-DOTA-girentuximab binds to G250, allowing the localization of G250-expressing tumor cells using gamma scintigraphy. Found in the majority of renal cell carcinomas (RCCs), G250 or carbonic anhydrase isozyme IX (CA IX) is a cell surface tumor-associated antigen (TAA).

A radioimmunoconjugate composed of FPI-1175 (AVE1642), a humanized monoclonal antibody against insulin-like growth factor-1 receptor (IGF-1R) linked, via the bifunctional chelate FPI-1397, to the radioisotope indium-111 (111In or In-111), with potential imaging activity upon single photon emission computed tomography (SPECT). Upon administration of indium In 111-FPI-1547, the FPI-1547 moiety targets and binds to IGF-1R expressed on tumor cells. Upon uptake and imaging, IGF-1R-expressing tumor cells can be visualized. This allows assessment of IGF-1R expression on tumor cells as well as tumor uptake of the agent. The linker promotes increased clearance of the radioisotope. * indium In 111-labeled autologous peripheral blood mononuclear cells A preparation of autologous peripheral blood mononuclear cells (PBMCs) radiolabeled with indium In 111 with radioisoptoic activity. Autologous PBMCs are isolated, expanded ex vivo, radiolabeled with indium In 111, and then infused back into the patient. Gamma scintigraphy may then be used to image gamma ray-emitting indium In 111 PBMCs localized in lymhoma tissue.

A preparation of autologous peripheral polymorphonuclear (PMNLs) radiolabeled with indium In 111 with radioisoptic activity. Autologous PMNLs are isolated, expanded ex vivo, radiolabeled with indium In 111, and then infused back into the patient. Gamma scintigraphy may then be used to image gamma ray-emitting indium In 111 PMNLs localized in lymphoma tissue.

A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptide linked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide indium (In) 111. After pretargeting with a bispecific monoclonal antibody (BiMoAB) directed against both a tumor associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of administered indium-In-labeled di-HSG-DOTA peptide IMP-288 binds the anti-HSG portion of the BiMoAB; In-111 radioisotopic activity localized to tumor cells bearing the TAA can then be visualized scintigraphically. Check for active clinical trialsusing this agent. * Indocin Brand name for [[indomethacin) * indocyanine green solution A sterile solution of a nontoxic tricarbocyanine dye with a peak spectral absorption at 790 nm, used for determining cardiac output, hepatic function, and liver blood flow, as well as for ophthalmic angiography. Designed to be administered intravenously, indocyanine green solution (ICG) contains less than 5% sodium iodide. Upon intravenous injection, ICG rapidly binds to its principle carrier, plasma protein, and is thereby confined to the vascular space. This agent, with a half-life of 150 to 180 seconds, is removed exclusively by the liver from circulation to bile juice. Furthermore, due to poor uptake, ICG is not suitable for angiography or functional output analysis of kidney, lung, cerebro-spinal, or peripheral tissues.

A solution containing a non-toxic, fluorescent tricarbocyanine dye with a peak spectral absorption at 790 nm bound to the plasma protein albumin, that may be used in sentinel node mapping using a near infrared (NIR) imaging system. Upon injection of the indocyanine green (ICG)/albumin solution around the tumor, the ICG/albumin complex, travels though the vascular system. Using a NIR imaging system, the ICG, which emits light in the NIR range, permits the visualization of sentinel nodes and may help in cancer staging. * indocyanine green-labeled polymeric micelles ONM-100 A micellar polymer tracer labeled with the near-infrared (NIR) fluorescent imaging dye indocyanine green (ICG), with potential fluorescent imaging activity. Upon administration, the ICG-labeled polymeric micelles ONM-100 accumulate in tumor tissue. The micelles dissociate and subsequently fluoresce upon exposure to the acidic conditions of the tumor microenvironment (TME), allowing the visualization of tumors using infrared-based cameras. * indole-3-carbinol A naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, a natural compound present in a wide variety of plant food substances including members of the family Cruciferae with antioxidant and potential chemopreventive properties. Indole-3-carbinol scavenges free radicals and induces various hepatic cytochrome P450 monooxygenases. Specifically, this agent induces the hepatic monooxygenase cytochrome P4501A1 (CYP1A1), resulting in increased 2-hydroxylation of estrogens and increased production of the chemoprotective estrogen 2-hydroxyestrone.

An orally available capsule-based nutritional supplement containing indole-3-carbinol, calcium-D-glucarate, Schizandra, vitamin D3, milk thistle, stinging nettle and hydroxymatairesinol (HMR) lignans, with potential estrogen modulating, antiproliferative and antioxidant activity. Indole-3-carbinol, found in vegetables of the Cruciferae family, may inhibit mammary cell growth and exerts antiestrogenic activity; Milk thistle (Silybum marianum) and Schizandra chinensis may enhance some of the phase II detoxification enzymes; calcium-D-glucarate and vitamin D3 may inhibit mammary cell growth; stinging nettle may exert its effect through its aromatase inhibiting activity; HMR lignans may have a beneficial effect on estrogen balance and levels. Therefore, ingredients in indole-3-carbinol/calcium/Schizandra/vitamin D3/milk thistle/stinging nettle/lignan-based nutritional capsule may alter estrogen balance and may protect against mammary carcinogenesis.

A peptide vaccine against the immunomodulatory enzyme indoleamine 2,3-dioxygenase (IDO), with potential immunomodulating and antineoplastic activities. Vaccination with indoleamine 2,3-dioxygenase peptide vaccine may activate the immune system to induce an immune response against IDO-expressing cells. This may increase and restore the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T-lymphocytes, and may eradicate IDO-expressing tumor cells. IDO, a cytosolic enzyme responsible for tryptophan catabolism and conversion of tryptophan into kynurenine, is overexpressed by a variety of tumor cell types and antigen presenting cells (APCs) and plays an important role in immunosuppression; tryptophan depletion inhibits T-lymphocyte proliferation and activation, and suppresses the immune system.

A synthetic nonsteroidal indole derivative with anti-inflammatory activity and chemopreventive properties. As a nonsteroidal anti-inflammatory drug (NSAID), indomethacin inhibits the enzyme cyclooxygenase, thereby preventing cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines. This agent also may inhibit the expression of multidrug-resistant protein type 1, resulting in increased efficacies of some antineoplastic agents in treating multi-drug resistant tumors. In addition, indomethacin activates phosphatases that inhibit the migration and proliferation of cancer cells and downregulates survivin, which may result in tumor cell apoptosis.

A methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2,3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy.

An orally bioavailable prodrug of indoximod, a methylated tryptophan, with immune checkpoint inhibitory and antineoplastic activities. Upon oral administration, the indoximod prodrug NLG802 is converted to indoximod. Indoximod targets, binds to and inhibits the enzyme indoleamine 2,3-dioxygenase (IDO; IDO1), which converts the essential amino acid tryptophan into the immunosuppressive metabolite kynurenine. By increasing tryptophan levels and decreasing kynurenine levels, indoximod restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against IDO1-expressing tumor cells, thereby inhibiting their growth. IDO1, overexpressed by multiple tumor cell types, plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system. NLG802 elicits increased plasma concentrations of indoximod and improves its efficacy, compared to the direct administration of indoximod.

Inducible regulatory T-lymphocytes that express CD4, CD25 (the alpha chain of the interleukin 2 receptor) and forkhead box P3 (FOXP3), with potential immunomodulating activity. Inducible CD4+CD25+ T regulatory cells (iTregs) are a subset of CD4+ T lymphocytes that are induced from CD25- precursors in peripheral lymphoid organs with interleukin-2 and transforming growth factor-beta. These regulatory T cells are essential in maintaining immunologic homeostasis. They may also prevent autoimmunity by suppressing self-reactive T cells, and may induce tolerance to allogeneic organ transplants such as in hematopoietic stem cell transplants.

An analog of calcitriol and a vitamin D3 receptor (VDR) agonist, with potential antineoplastic activity. Upon administration, inecalcitol targets and binds to VDR. This activates VDR and VDR-mediated signal transduction pathways. This modulates the VDR-mediated expression of certain genes, including the expression of anti-cancer genes, enhances cellular differentiation, induces tumor cell apoptosis and inhibits tumor cell growth. VDR plays a central role in calcium homeostasis and in the growth of certain cancer cells.

Brand name for [[diphtheria toxoid/tetanus toxoid/acellular pertussis vaccine adsorbed) * Infasurf Intratracheal Suspension Brand name for [[calfactant) * Infergen Brand name for [[interferon alfacon-1) * infigratinib An orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. Infigratinib selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. FGFRs are a family of receptor tyrosine kinases which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival.

A recombinant chimeric, mouse-human monoclonal antibody directed against tumor necrosis factor alpha (TNF-alpha), a protein involved in inflammation, cell survival, and apoptosis. Infliximab may be pro- apoptotic or anti-apoptotic, depending on cell type.

Brand name for morphine sulfate

A topical, aqueous gel formulation containing a derivative of ingenol, a selective small-molecule activator of protein kinase C (PKC) that is isolated from the sap of Euphorbia species, with the potential to treat preneoplastic skin lesions. Upon topical application of the ingenol derivative LEO 43204 gel, the agent presumably activates various PKC isoforms, which may induce apoptosis in abnormal cells found in severely sun-damaged skin with multiple actinic keratoses. This may decrease the number of actinic keratoses and prevent the development of skin neoplasms. The PKC family consists of signaling isoenzymes that regulate many cell processes, including proliferation, differentiation, and apoptosis.

A selective small-molecule activator of protein kinase C (PKC) isolated from the plant Euphorbia peplus with potential antineoplastic activity. Ingenol mebutate (I3A) activates various protein kinase C (PKC) isoforms, thereby inducing apoptosis in some tumor cells, including myeloid leukemia cells, melanoma cells, and basal cell carcinoma cells. The PKC family consists of signaling isoenzymes that regulate many cell processes including proliferation, differentiation, and apoptosis.

A topical, aqueous gel formulation containing the mebutate salt form of ingenol, a selective small-molecule activator of protein kinase C (PKC) that is isolated from the sap of Euphorbia species, with potential antineoplastic activity. Upon topical application of the ingenol mebutate gel, ingenol activates various PKC isoforms, which induces apoptosis in certain tumor cells, including myeloid leukemia cells, melanoma cells, and basal cell carcinoma cells. The PKC family consists of signaling isoenzymes that regulate many cell processes, including proliferation, differentiation, and apoptosis.

A small molecule iodobenzamide with potential cytotoxic and antineoplastic activities. Although the mechanism of action is unknown, iniparib appears to be cytotoxic in cells with DNA alterations or DNA damage, like that found in tumor cells with mutations in the ataxia telangiectasia mutated (ATM) gene. ATM encodes a serine/threonine protein kinase and mutations of the gene are associated with ataxia telangiectasia and contribute to certain cancers such as T-cell acute lymphoblastic leukemia, B-cell chronic lymphocytic leukemia and B-cell non-Hodgkin lymphomas.

An injectable form of a polysaccharide isolated from the radix of Astragalus membranaceus (PG2), used in traditional Chinese medicine, with potential hematopoiesis inducing and immunomodulating activities. Upon injection, APS may be able to relieve certain chemotherapy-induced side effects, including myelosuppression, fatigue, mucositis, pain, nausea and vomiting, as well as loss of appetite and body weight. Also, APS may exert immunostimulatory activities by stimulating B-lymphocytes, activating T-lymphocytes, inducing cytokine production, and activating macrophages and natural killer cells through as of yet unidentified mechanism(s). APS may improve compliance of radiotherapy and/or chemotherapy.

An injectable, sphingomyelin/cholesterol liposome-encapsulated formulation of the semisynthetic vinca alkaloid vinorelbine with antineoplastic activity. Vinorelbine binds to tubulin and prevents formation of the mitotic spindle, resulting in cell cycle arrest in metaphase. Like other vinca alkaloids, vinorelbine may also interfere with the metabolism of nucleic acids, lipids, amino acids, cAMP, and glutathione, as well as other biological processes including calmodulin-dependent Ca2+-transport, ATPase activity, or cellular respiration. Liposomal delivery of vinorelbine may improve drug penetration into tumors and decreases drug clearance, increasing the duration of therapeutic effects while lowering the toxicity profile.

Brand name for ferric carboxymaltose solution

Brand name for axitinib

A synthetic, 5-amino acid peptide and innate defense regulator (IDR), with immunomodulating, anti-inflammatory, anti-infective and anti-mucositis activities. Upon intravenous administration, SGX942 binds to the ZZ domain of sequestosome-1, also called p62, and activates regulatory signaling transduction pathways involved in the modulation of the innate immune system, such as those mediated by mitogen-activated protein kinase (MAPK) p38 and CCAAT-enhancer-binding protein. This agent promotes monocyte and macrophage recruitment to, and accelerates healing in damaged and infected tissue; it suppresses inflammation through the regulation of the expression of multiple cytokines. This agent may prevent or decrease chemo- or radiotherapy-induced mucositis as well as other types of infection. p62, an intracellular adaptor protein that functions downstream of certain signaling receptors, plays a key role in the activation of the innate immune system.

A recombinant 19 kDa protein derived from the Apicomplexa protozoan Eimeria with potential immunostimulating and antitumor activities. Upon administration, innate immunostimulator rBBX-01 activates dendritic cells (DCs), stimulates the Toll-like receptor 11 (TLR-11)-mediated release of interleukin-12 (Il-12) from DCs, and induces a T-helper 1 (Th1) type immune response, which may induce an immune response against tumor cells. Infection with Eimeria, a coccidian commonly infecting the intestine, may be negatively correlated with tumorigenesis.

Brand name for tinzaparin sodium

A isoindolinone derivative and potent inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with chemosensitization and radiosensitization properties. INO-1001 inhibits PARP, which may result in inhibition of tumor cell DNA repair mechanisms and, so, tumor cell resistance to chemotherapy and radiation therapy. PARP enzymes are activated by DNA breaks and have been implicated in the repair of DNA single-strand breaks (SSB).

A recombinant DNA plasmid carrying the gene for diphtheria toxin-A (dT-A) chain under the regulation of the H19 promoter, with potential antineoplastic activity. Upon intravesical administration, dT-A chain expression is triggered by the presence of H19 transcription factors that are upregulated in tumor cells. The dT-A chain binds to nicotinamide adenine dinucleotide (NAD) and inactivates the ADP-ribosylation of elongation factor 2 (EF2), resulting in the inhibition of protein synthesis and cell death leading to tumor cell destruction. Inodiftagene Vixteplasmid does not carry the gene for the diphtheria toxin-B (dT-B) chain, thereby preventing the transfer of the toxic dT-A chain between cells. H19, a paternally imprinted, oncofetal gene, is highly expressed in embryonic and certain malignant tissues, but minimally expressed in normal, adult tissues.

An orally bioavailable inhibitor of inosine 5'- monophosphate dehydrogenase (IMPDH), with potential antineoplastic activity. Upon administration, IMPDH inhibitor FF-10501-01 competitively inhibits the enzyme IMPDH, thereby preventing the conversion of inosine monophosphate to xanthosine monophosphate. This inhibits the synthesis of guanine nucleotides, deprives cancer cells of guanosine triphosphate (GTP), disrupts DNA and RNA synthesis, and decreases tumor cell proliferation. Tumor cells are highly susceptible to IMPDH inhibition because they are rapidly dividing cells that are dependent on rapid DNA synthesis, which requires a high concentration of nucleotides. IMPDH, an enzyme that catalyzes the rate-limiting step in the synthesis of guanosine triphosphate (GTP), is overexpressed in numerous tumor cell types.

A toxic purine analogue. Inosine dialdehyde inhibits ribonucleotide reductase, resulting in decreased synthesis of DNA, RNA, and proteins, and G2/M-phase cell cycle arrest. This agent also forms stable covalent crosslinks in proteins, thereby inhibiting the activity of enzymes involved in nucleic acid synthesis.

A natural sugar found in cell membrane phospholipids, plasma lipoproteins, and (as the phosphate form) in the nucleus with potential chemopreventive properties. As one of a number of intracellular phosphate compounds, inositol is involved in cell signaling and may stimulate tumor cell differentiation.

A CD22-targeted cytotoxic immunoconjugate composed of a humanized IgG4 anti-CD22 antibody covalently linked to N-acetyl-gamma-calicheamicin dimethyl hydrazide (CalichDMH) with potential antineoplastic activity. Inotuzumab ozogamicin is rapidly internalized upon binding of the antibody moiety to B cell-specific CD22 receptors, delivering the conjugated CalichDMH intracellularly; the CalichDMH moiety binds to the minor groove of DNA in a sequence-specific manner, resulting in double-strand DNA breaks and apoptosis. CalichDMH is a derivative of gamma calicheamicin, a cytotoxic antibiotic produced by the bacterium Micromonospora echinospora.

Brand name for gastrin immunotoxin

Brand name for eplerenone

A recombinant therapeutic agent which is chemically identical to or similar to endogenous human insulin. In lispro insulin, the amino acid proline at B-28 and the amino acid lysine at B-29 are reversed, resulting in the rapid dissolution of this insulin to a monomer that is absorbed rapidly after subcutaneous administration. Lispro insulin is equipotent to human insulin on a molar basis but its effects are faster and of shorter duration. Endogenous insulin, a pancreatic hormone composed of two polypeptide chains, is important in the normal metabolism of carbohydrates, proteins and fats, promoting glucose utilization and protein synthesis; it has anabolic effects on many types of tissues.

An intermediate-acting insulin used in the treatment of diabetes mellitus. Administered once or twice daily, NPH (neutral protamine hagedorn) insulin lowers blood glucose within 1 to 2 hours after administration and exerts a peak effect at 6 to 10 hours. Endogenous insulin, a pancreatic hormone composed of two polypeptide chains, is important in the normal metabolism of carbohydrates, proteins and fats, promoting glucose utilization and protein synthesis; it has anabolic effects on many types of tissues.

A recombinant form of the naturally occurring human pancreatic hormone insulin. Upon administration, regular insulin mimics the action of endogenous human insulin and binds to insulin receptors located on muscle and fat cells. This both facilitates the cellular uptake of glucose and lowers blood glucose levels. In addition, insulin inhibits the liver's conversion of stored glycogen into glucose, which also decreases blood glucose levels. Insulin also inhibits lipolysis in adipose tissue, inhibits proteolysis, and enhances protein synthesis.

A small molecule integrin receptor antagonist (IRA) with potential antineoplastic activity. Upon administration, GLPG0187 binds to and blocks the activity of 5 RGD-integrin receptor subtypes, including alphavbeta1, alphavbeta3, alphavbeta5, alphavbeta6 and alpha5beta1. This may result in the inhibition of endothelial cell-cell interactions and endothelial cell-matrix interactions, and the prevention of angiogenesis and metastasis in tumor cells expressing these integrin receptors. Integrin receptors are transmembrane glycoproteins expressed on the surface of tumor vessel endothelial cells and some types of cancer cells, and play a crucial role in endothelial cell adhesion and migration.

Brand name for absorbable adhesion barrier gel

An analogue of consensus interferon which contains an additional methionyl amino acid residue. Consensus interferon (also known as interferon alfacon-1, rCon-IFN, and CIFN) is a genetically engineered synthetic interferon created from the most common amino acid sequences from the naturally occurring alpha interferons. Alpha interferons bind to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune-modulating effects.

Human autologous mesenchymal stem cells (MSCs) harvested from the bone marrow of healthy individuals and transduced with a retroviral vector encoding the human cytokine interferon beta (IFNb), with potential immunomodulating and antineoplastic activities. Upon administration of IFNb-secreting MSCs, the cells are attracted and specifically migrate to tumor sites and become part of the tumor microenvironment. Since the MSCs express IFNb, these cells selectively deliver high levels of IFNb to the tumor site. In turn, IFNb binds to IFN-specific cell surface receptors and modulates the transcription and translation of certain genes whose protein products are involved in tumor cell proliferation. This decreases tumor cell growth.

A recombinant form of the endogenous cytokine interferon-gamma (IFN-gamma; IFNg), with a peptide length of 140 amino acids and modified with an N-terminal methionyl group, with potential immunomodulating and antineoplastic activities. Upon administration, IFNg-1b binds to IFNg cell surface receptors (IFNGRs), activates IFNg-stimulated signaling pathways, including the JAK-STAT pathway, and leads to the transcription of multiple IFNg-controlled genes, the expression of which may activate certain components of the immune system. IFNg activates natural killer (NK) cells, macrophages, and cytotoxic T lymphocytes (CTLs), stimulates antibody-dependent cellular cytotoxicity (ADCC) and induces the expression of major histocompatibility complex (MHC) molecules, which leads to an increase in antigen presentation, including tumor-associated antigens (TAAs), to the immune system, and modulates the expression of certain pro-inflammatory cytokines by antigen-presenting cells (APCs). Altogether, this increases tumor cell killing. IFNg-1b, a cell-signaling protein, plays a key role in the regulation and activation of the immune system.

A replication-defective adenoviral serotype 5 vector encoding a recombinant form of the human cytokine interferon-gamma (IFN-g), with potential antineoplastic and immunoregulatory activities. Upon intratumoral administration, the sustained expression of IFN-g by IFN-g-expressing adenovirus vaccine ASN-002 promotes a T-helper type 1 (Th1) immune response and inhibits the Th2-mediated cytokine production observed in many cutaneous lymphomas. IFN-g also mediates interleukin-12 (IL-12) production by antigen-presenting cells (APCs); activates macrophages, cytotoxic T-cells, and natural killer (NK) cells; upregulates major histocompatibility complex (MHC) molecules; and stimulates antibody-dependent cellular cytotoxicity (ADCC). Altogether, these IFN-g-mediated effects may result in both an inhibition of tumor cell proliferation and tumor cell death. Compared to IFN-g injections, the prolonged local production of IFN-g at the tumor site allows for higher efficacy and a reduction of systemic toxicity.

The DNA sequence that encodes the protein cytokine interleukin-12 (IL-12). When introduced as the complementary DNA (cDNA) form into tumor cells by, for example, a genetically engineered adenovirus vector, the transfected IL-12 cDNA expresses IL-12 which activates antitumoral natural killer (NK) cells and CD8+ T-cells and stimulates the secretion of interferon-gamma (IFN-gamma), potentially inhibiting tumor cell metastasis. This gene therapy may also result in IL-12-mediated inhibition of vascular endothelial growth factor (VEGF) and enhancement of matrix metalloproteinases (MMPs).

The DNA sequence that encodes the protein cytokine interleukin-2 (IL-2). When introduced as the complementary DNA (cDNA) form into tumor cells by, for example, a genetically engineered adenovirus vector, the transfected IL-2 cDNA expresses IL-2 which may activate antitumoral natural killer cells and elicit an antitumoral cytotoxic T-cell response, resulting in an inhibition of tumor progression.

A selective effector cell activator protein and agonist of the intermediate-affinity interleukin-2 (IL-2) receptor with potential immunostimulating and antineoplastic activity. Upon administration, intermediate-affinity interleukin-2 receptor agonist ALKS 4230 binds to and signals through the intermediate-affinity IL-2 receptor complex; this may selectively stimulate and activate natural killer (NK) cells and memory CD8 T cells, leading to tumor cell elimination, while circumventing the activation of immunosuppressive cells that may prevent the anti-tumor response. IL-2 is a cytokine signaling molecule that plays a critical role in the immune response.

A pan alpha-v human monoclonal antibody that recognizes alpha-v beta-1, alpha-v beta-3, alpha-v beta-5, and alpha-v beta-6 integrins with antiangiogenic and antitumor activities. Intetumumab competitively binds to and blocks both alpha-v beta-3 and alpha-v beta-5 integrins, resulting in inhibition of integrin-mediated tumor angiogenesis and tumor growth. Integrins facilitate the adhesion of stimulated endothelial cells to the extracellular matrix (ECM); trigger the secretion of ECM-rearranging proteases; and propagate signaling events that promote the survival and differentiation of cells in newly formed vasculature.

Brand name for cisplatin-e therapeutic implant

Brand name for fat emulsion

An intranasal formualtion of the synthetic cyclohexanone ketamine with analgesic and anesthetic activities. Although its mechanism of action is not well understood, ketamine appears to non-competitively block N-methyl-D-aspartate (NMDA) receptors and agonistically bind to and activate opiod mu and sigma receptors, thereby reducing pain perception, inducing sedation, and producing dissociative anesthesia.

Brand name for recombinant interferon alfa-2b

Brand name for ilixadencel

A naturally occurring, indigestible and non-absorbable oligosaccharide produced by certain plants with prebiotic and potential anticancer activity. Inulin stimulates the growth of beneficial bacteria in the colon, including Bifidobacteria and Lactobacilli, thereby modulating the composition of microflora. This creates an environment that protects against pathogens, toxins and carcinogens, which can cause inflammation and cancer. In addition, fermentation of inulin leads to an increase in short-chain fatty acids and lactic acid production, thereby reducing colonic pH, which may further control pathogenic bacteria growth and may contribute to inulin's cancer protective properties.

Brand name for ertapenem sodium

Brand name for saquinavir mesylate

Brand name for IL4-Pseudomonas exotoxin fusion protein MDNA55

An I 131 radioiodinated synthetic analogue of the neurotransmitter norepinephrine. Iobenguane localizes to adrenergic tissue and, in radioiodinated forms, may be used to image or eradicate tumor cells that take up and metabolize norepinephrine.

A water-soluble, tri-iodinated, non-ionic monomeric benzoate derivative and contrast medium used in diagnostic radiography. Upon administration, iobitridol is distributed through the vascular system and interstitial space. Like other organic iodine compounds, this agent blocks x-rays and appears opaque on x-ray film thus, enhancing the visibility of body parts containing this agent. Iobitridol is rapidly removed by the kidneys in an unchanged form, and in cases of renal failure, heterotropic excretion occurs via the biliary route. * iodinated contrast dye A contrast agent containing an iodine-based dye used in many diagnostic imaging examinations, including computed tomography, angiography, and myelography.

A radiopaque hydrogel containing cross-linked, iodinated polyethylene glycol (PEG) particles in a viscous carrier, with potential use as a contrast agent to enhance marking of soft tissue during a surgical procedure and concomitant radiotherapy upon computed tomography (CT), magnetic resonance (MR) and ultrasound imaging. Upon intratumoral injection, iodinated PEG-based hydrogel tissue marker localizes to and is maintained in soft tissue. Upon MR, ultrasound and/or CT imaging, the visualization of the tumor tissue is enhanced, which can facilitate tumor removal and image-guided radiotherapeutic treatment. The hydrogel particles are stable and visible through 3 months, after which they liquefy, and are absorbed by the body and cleared in the urine.

A radioiodine-labeled cholesterol analogue with radioisotopic activity. Iodine 131-l-6-beta-iodomethyl-19-norcholesterol accumulates in tissues where steroid hormones are produced, including the adrenal cortex and, to a lesser extent, the ovaries and the testes. After binding to low-density lipoprotein (LDL) receptors in the adrenal cortex, this agent is internalized, permitting scintigraphic localization of areas of adrenocortical glucocorticoid, mineralocorticoid and androgen secretion, and the scintigraphic assessment of adrenocortical function.

A radioactive isotope of iodine, a nonmetallic element of the halogen group with an atomic mass of 123 and a half-life of 13.2 hours with radioisotopic activity. Selectively accumulating in the thyroid tissue, iodine I 123 emits gamma rays that can be detected with gamma scintigraphy, allowing localization of thyroid tissue. This agent may be used as a tracer in whole body scintigraphy (WBS) to localize thyroid carcinoma metastases.

A radiopharmaceutical containing the serotonin transporter (SERT) ligand ADAM [2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine] labeled with the radioisotope iodine I 123, with SERT-binding and radioisotope activities. Upon administration, iodine I 123 ADAM selectively binds to SERT-expressing cells; subsequently, SERT-expressing tissues may be visualized using single photon emission computed tomography (SPECT). SERT is a monamine transporter protein found in the membranes of neurons and platelets; in neurons it transports the neurotransmitter serotonin from synaptic spaces into presynaptic neurons, terminating serotonin's function.

A radioimmunoconjugate comprised of a recombinant scFv dimer diabody of a monoclonal antibody against human carcinoembryonic antigen (CEA) labeled with iodine I 123 (I-123) with potential radioimmunolocalization applications. The antibody moiety of iodine I 123 anti-CEA recombinant diabody T84.66 binds to cells expressing CEA, selectively delivering I-123 upon cellular internalization and allowing the scintigraphic imaging of CEA-expressing tumor cells. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers. Compared to whole monoclonal antibodies, diabody fragments offer the advantages of rapid tumor targeting, rapid blood clearance, more uniform tumor distribution, and a lower potential for eliciting an immune response.

A radiopharmaceutical containing the dopamine D2/D3 receptor agonist iodobenzamide (IBZM) labeled with the radionuclide iodine I 123 with dopamine receptor-binding and radioisotopic activities. Upon administration, iodine I 123 iodobenzamide binds to dopamine D2/D3 receptors; subsequently, tissues expressing these receptors can be visualized using single photon emission computed tomography (SPECT). Dopamine receptors are a class of metabotropic G protein-coupled receptors found in the central nervous system (CNS) and neuroendocrine tumors such as pheochromocytoma and paraganglioma.

An iodine I-123 conjugate of metomidate (MTO) with potential application in adrenal imaging. Metomidate is a potent and selective inhibitor of the cytochrome P-450 enzymes, especially CYP11B1 (11 beta-hydroxylase) and CYP11B2 (aldosterone synthase). Because both CYP11B1 and CYP11B2 are expressed exclusively in the adrenal cortex, I-123 iodometomidate can be used as a radiotracer for adrenal scintigraphy.

A radioactive isotope of iodine, a nonmetallic element of the halogen group, with an atomic mass of 124 and a half-life of 4.18 days with radioisotopic activity. Selectively accumulating in thyroid tissue, iodine I 124 emits positrons that can be detected by positron emission tomography (PET), allowing localization of thyroid tissue. This radiosiotope also emits gamma rays.

A radioconjugate composed of the insulin-like growth factor 1 receptor (IGF-1R) binding agent CPD-1028 and conjugated to the radionuclide iodine I 124, with potential tumor imaging properties upon positron emission tomography/computed tomography (PET/CT). Upon administration, iodine I 124 CPD-1028 targets and binds to IGF-1R-expressing tumor cells. Upon PET/CT imaging, the iodine I 124 moiety can be visualized and the quantity of IGF-1R-expressing tumor cells can be assessed. IGF-1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a significant role in the stimulation of cellular proliferation, oncogenic transformation, and the suppression of apoptosis.

A radioconjugate containing the nucleoside analog 2'-fluoro-2'-deoxy-1beta-D-arabinofuranosyl-5-iodouracil (FIAU) labeled with the radioisotope iodine I 124 with positron-emitting activity. Chemotherapeutic agents such as bortezomib may induce viral thymidine kinase expression in EBV- and Kaposi's sarcoma herpesvirus (KSHV)-associated tumors. Subsequent to chemotherapy induction of viral TK in these tumors, administered iodine I 124 FIAU is phosphorylated by expressed viral TK, becoming selectively trapped within TK-expressing tumor cells; these cells can then be visualized with positron emission tomography (PET). Viral TK is either not expressed or is expressed at very low levels in EBV- and Kaposi's sarcoma herpesvirus (KSHV)-associated tumors and may be activated by certain chemotherapeutic agents.

A radioconjugate composed of the positron-emitting radioisotope iodine I 124 labeled to iobenguane, the synthetic aralkylguanidine analogue of the neurotransmitter norepinephrine (NE), with potential diagnostic imaging applications upon positron emitting tomography (PET) or computed tomography (CT). Upon administration, iodine I 124 iobenguane is taken up and accumulates in the granules of adrenal medullary chromaffin cells and in the pre-synaptic granules of adrenergic neurons in a manner almost identical with that of NE. In turn, tumor cells can be imaged upon PET or CT.

A diagnostic radiopharmaceutical comprised of iodo-azomycin galactopyranoside (IAZGP) labeled with the positron-emitting radioisotope iodine I 124 and used as an imaging agent. Iodine I 124 iodo-azomycin galactopyranoside (I-124 IAZGP) is reduced under hypoxic conditions, covalently binding to macromolecules in hypoxic cells. After incorporation into hypoxic tumor cell DNA, I-124 IAZGP can be localized and quantified using positron emission tomography (PET), allowing a quantitative assessment of hypoxic tumor burden. IAZGP appears to have a higher water solubility and faster clearance from normal tissue than traditional imidazole tracers.

A radiopharmaceutical comprised of the thymidine analog, 5-iodo-2-deoxyuridine (idoxuridine), labeled with the positron emitter iodine I 124. After incorporation into tumor cell DNA, positron emission tomography (PET) is used to image iodine I 124 localized to tumor cells for determining and monitoring tumor burden. Check for active clinical trialsusing this agent.

A radioimmunoconjugate consisting of 3F8, a murine anti-GD2 ganglioside monoclonal antibody labeled with iodine I 124 (I-124), with radioimaging activity using positron emission tomography (PET). Upon intravenous administration of iodine I 124 monoclonal antibody 3F8, the 3F8 moiety binds to GD2 expressed on tumor cells. This binding enables both PET imaging via iodine I 124 and the visualization of GD2-expressing tumor cells. GD2 is a ganglioside overexpressed in a variety of cancer cells, including neuroblastoma cells.

A radioimmunoconjugate consisting of the iodine I 124-radiolabeled murine IgG1 monoclonal antibody (MoAb) 8H9 directed against the cell surface glycoprotein CD276 (4Ig-B7-H3) with potential for radioimaging using positron emission tomography (PET). Through convection enhanced delivery, iodine I 124 monoclonal antibody 8H9 binds to the 4Ig domain of CD276, in turn CD276 expressing tumor cells may be visualized upon PET imaging of the iodine I 124 moiety. CD276, a tumor associated antigen and member of the B7 family of co-stimulatory proteins, suppresses natural killer (NK) cell and cytotoxic T-lymhocyte activation; it is expressed on the cell membranes of a wide variety of tumors of neuroectodermal, mesenchymal and epithelial origin and its expression is associated with increased aggressiveness, poor prognosis and resistance. * iodine I 124 monoclonal antibody A33 A radioimmunoconjugate of a humanized monoclonal antibody (MoAb) A33 labelled with iodine 124 (I-124). MoAb A33 recognizes A33 antigen, a 43 KDa transmembrane glycoprotein of the immunoglobulin superfamily, highly and homogenously expressed in 95% of colorectal cancer metastases, with only restricted expression in normal colonic mucosa. I-124 MoAb A33 delivers beta particle emitting I-124 nuclide directly to metastatic colorectal tissues, thereby this agent could be used in kinetics studies or radioimmunotherapy.

A radioimmunoconjugate comprised of M5A, a humanized monoclonal antibody directed against carcinoembryonic antigen-related cell adhesion molecule 5 (CEA or CEACAM5), labeled with iodine I 124 (I-124) with potential radiolocalization applications. Upon administration, the antibody moiety of iodine I 124 monoclonal antibody M5A specifically binds to cells expressing CEA. Upon binding, the radioisotope moiety can be detected using positron-emission tomography (PET), thereby allowing the imaging and quantification of CEA-expressing tumor cells. CEA, a tumor associated antigen and a member of the CEA family of proteins, plays a key role in cell migration, cell invasion, and cell adhesion and is overexpressed by a variety of cancer types.

A phospholipid ether analog labeled with iodine I 124, with a potential imaging property upon positron emission tomography (PET). Upon administration, iodine I 124 NM404 selectively accumulates in and is retained within tumor cells for a prolonged period of time due to the decreased activity of a phospholipase D (PLD), most likely isoform 1 of PLD, in tumor cells compared to normal cells. As tumor cells are unable to metabolize and eliminate MN404, tumor cells can be visualized upon PET imaging. In addition, iodine I 124 NM404 may provide a more accurate image of the tumor than imaging with the current standard. PLD is an enzyme found in the cell membrane of normal cells that degrades phospholipids.

A small molecule radiopharmaceutical composed of the radioisotope iodine I 124 covalently attached to a proprietary alkylphospholipid ether (PLE) analogue, with potential imaging activity upon positron emission tomography (PET). Iodine I 124 phospholipid ether analogue CLR1404 is selectively taken up by tumor cells via membrane lipid rafts and accumulates in tumor cells. The accummulation of this agent is due to a decreased ability of tumor cells to metabolize PLEs because certain tumor cells have lower levels of the enzyme phospholipase-D, in comparison to normal cells. This facilitates imaging of cancer cells by PET. Lipid rafts, specialized microdomains of plasma membrane, are overexpressed in cancer cells compared to normal cells. In addition, the radioiodine moiety of this agent is resistant to de-iodination.

A radioconjugate composed of PU-AD, a synthetic purine-scaffold inhibitor of the molecular chaperone heat shock protein 90 (Hsp90), conjugated to the radioisotope iodine I 124, with potential imaging activity upon positron emission tomography (PET). Upon administration of iodine I 124 PU-AD, the PU-AD moiety selectively binds to cancer cells expressing stress-induced Hsp90 (stress Hsp90). Upon PET, Hsp90-overexpressing cancer cells can be visualized and patients who may benefit from PU-AD therapy can be identified. This radioconjugate may also be used to determine the pharmacokinetics of the therapeutic agent PU-AD. PU-AD is able to cross the blood-brain-barrier (BBB) and specifically targets stress Hsp90, as seen in certain conditions, such as cancer and neurodegenerative diseases, while normal housekeeping Hsp90 complexes are not targeted by PU-AD at dose levels administered for imaging. Additionally, housekeeping Hsp90 complexes are only targeted at doses that are much larger than that are needed to exert an anticancer effect.

A radioimmunoconjugate composed of the F(ab')2 fragment of human monoclonal antibody PGN650 against phosphatidylserine (PS) labeled with the radioisotope iodine I 124, with potential imaging activity upon positron-emission tomography (PET). Upon administration, the MoAb moiety of PGN650 binds to exposed PS on tumor cells, thereby allowing for the visualization of tumors upon PET. This may facilitate the assessment of the effectiveness of antitumor agents. The phospholipid PS is normally located on the inner leaflet of the plasma membrane of healthy cells but is flipped to the outer leaflet in the endothelial lining of the tumor vasculature and other tumor cells in response to chemo- or radio- treatments in addition to oxidative stress.

A radioconjugate composed of an affinity-matured antibody fragment, the A11 minibody, directed against human prostate stem cell antigen (PSCA), and conjugated with the radioisotope iodine I 124, that can potentially be used as an imaging agent for positron emission tomography (PET)/computed tomography (CT). The minibody moiety of iodine I 124-labeled anti-PSCA A11 minibody selectively targets and binds to PSCA. The PSCA-expressing tumor cells can then be visualized using PET/CT. PSCA, a cell surface antigen expressed in normal human prostate and bladder, is overexpressed in a variety of cancers, including bladder, pancreatic, and prostate cancer. The A11 minibody is formed by the fusion of a single chain Fv fragment with the immunoglobulin G1 CH3 domain.

A radioconjugate containing the purine scaffold heat shock protein 90 (Hsp90) inhibitor PUH71 labeled with the radioisotope iodine I 124, with positron emitting activity. Hsp90 inhibitor PUH71 is thought to bind to cytosolic Hsp90 and the endoplasmic reticulum paralogue gp96 (HSP90B1), thereby inhibiting its molecular chaperone function and promoting the degradation of the oncogenic signaling proteins. This induces caspase-dependent apoptosis. The iodine I 124 moiety can be visualized using positron emission tomography (PET) imaging, thereby allowing an assessment of the accumulation of PUH71 in vivo, particularly in tumors. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.

A radioactive isotope of iodine, a nonmetallic element of the halogen group. With a half-life of 60 days, iodine 125 occurs naturally and can be produced artificially. This agent has both therapeutic and diagnostic uses, particularly in thyroid disease.

A radioimmunoconjugate consisting of a murine IgG2a monoclonal antibody directed against the human epidermal growth factor receptor (EGFR) labeled with iodine I 125 with potential antineoplastic activity. Iodine I 125 anti-EGFR-425 monoclonal antibody binds specifically to the epidermal growth factor receptor (EGFR). Upon binding to EGFR-expressing tumor cells, this agent is internalized, selectively delivering a potentially cytotoxic dose of gamma radiation. EGFR is a receptor tyrosine kinase that may be overexpressed on the cell surfaces of various solid tumors. Check for active clinical trialsusing this agent.

A radioactive isotope of iodine with an atomic mass of 131, a half life of eight days, and potential antineoplastic activity. Selectively accumulating in the thyroid gland, iodine I 131 emits beta and gamma particles, thereby killing thyroid cells and decreasing thyroid hormone production.

An iodine 131 radioimmunoconjugate of a small immunoprotein (SIP), derived from the variable region fragment of human monoclonal antibody L19, that is directed against the extra-domain B (ED-B) of fibronectin, with potential radioimmunotherapeutic activity. The SIP moiety of iodine I 131 anti-fibronectin antibody fragment L19-SIP binds to the ED-B domain of fibronectin on tumor cells in the tumor neovasculature. Upon internalization, the I 131 radionuclide may selectively detect or deliver cytotoxic radiation to fibronectin-expressing tumor cells. ED-B of fibronectin, a naturally occurring marker of tissue remodeling and angiogenesis, is expressed in the majority of aggressive solid human tumors, whereas it is not detectable in normal vessels and tissues.

A radioimmunoconjugate comprised of the chimeric monoclonal antibody G-250 conjugated with iodine I 131 with potential antineoplastic activity. The antibody moiety of iodine I 131 chimeric monoclonal antibody G-250 binds to G-250, a renal-cell carcinoma-associated antigen, delivering cytotoxic iodine I 131 specifically to renal cell carcinoma cells that express G-250.

A cytotoxic radioconjugate consisting of ethiodized oil, an iodinated ethyl ester derived from poppy seed oil, labeled with iodine 131 (I-131). Iodine I 131 ethiodized oil accumulates in hepatocellular carcinoma and hepatoblastoma tumor cells, resulting in targeted cytotoxicity to tumor cells while sparing surrounding normal cells and tissues.

A radioiodine-labeled cholesterol analogue with diagnostic imaging activity upon scintigraphy. Upon administration, iodine I 131 iodocholesterol accumulates in tissues where steroid hormones are produced, including the adrenal glands and, to a lesser extent, the ovaries and the testes. After binding to low-density lipoprotein (LDL) receptors on adrenocortical cells, this agent is internalized. As cholesterol is the precursor for all adrenocortical steroid hormones, areas of hormonal hypersecretion, can be visualized using scintigraphy and the adrenocortical function can be assessed.

Brand name for iodine I 131 ethiodized oil

A radioconjugate composed of MIP-1095, a urea-based ligand for the tumor-associated antigen (TAA) prostate-specific membrane antigen (PSMA), radiolabeled with iodine I 131 (I131), with potential antineoplastic activity. Upon administration of iodine I 131 MIP-1095, the MIP-1095 moiety selectively targets and binds to the extracellular domain of PSMA, thereby delivering cytotoxic iodine I 131 specifically to PSMA-expressing cancer cells. PSMA is a transmembrane glycoprotein that is highly expressed by malignant prostate epithelial cells and certain other tumor cells.

A radioimmunoconjugate consisting of 3F8, a murine anti-GD2 ganglioside monoclonal antibody labeled with iodine 131 (I-131), with radioimaging and radioimmunotherapeutic properties. Using monoclonal antibody 3F8 as a carrier for I-131 results in the targeted imaging and/or destruction of cells expressing GD2. GD2 is a ganglioside which is overexpressed in malignant melanoma, neuroblastoma, and small cell carcinoma of the lung.

A radioimmunoconjugate consisting of 81C6, a murine IgG2 anti-tenascin monoclonal antibody labeled with iodine 131 (I-131), with radioimaging and radioimmunotherapeutic activities. Using monoclonal antibody 81C6 as a carrier for I-131 results in the targeted imaging and/or destruction of cells expressing tenascin. Tenascin is an extracellular matrix protein which is overexpressed in gliomas and other cancers. Check for active clinical trialsusing this agent.

A radioimmunoconjugate consisting of the iodine 131-radiolabeled murine IgG1 monoclonal antibody 8H9 directed against the surface immunomodulatory glycoprotein 4Ig-B7-H3 with potential radioimaging and radioimmunotherapeutic uses. Iodine I 131 monoclonal antibody 8H9 binds to 4Ig-B7-H3 (human B7-H3 with 4 Ig-like domains) and may be used to radioimage and/or destroy tumor cells that express tenascin. 4Ig-B7-H3 inhibits T-cell activation and the production of effector cytokines such as interferon-gamma and interleukin-4; it is expressed on the cell membranes of a wide variety of tumors of neuroectodermal, mesenchymal and epithelial origin and is highly expressed on monocyte-derived dendritic cells (mdDCs). In vitro, it has been shown that monoclonal antibody-mediated masking of 4Ig-B7-H3 on neuroblastoma cells resulted in the enhancement of natural killer (NK)-mediated lysis of target cells.

A radioimmunoconjugate consisting of BC8, a murine IgG1 anti-CD45 monoclonal antibody labeled with iodine 131 (I-131), with radioimmunotherapeutic properties. Using monoclonal antibody BC8 as a carrier for I-131 results in the targeted destruction of cells expressing CD45. CD45 is tyrosine phosphatase expressed on virtually all leukocytes, including myeloid and lymphoid precursors in bone marrow and mature lymphocytes in lymph nodes; it is also expressed on most myeloid and lymphoid leukemic cells, but not on mature erythrocytes or platelets.

A radioimmunoconjugate consisting of the humanized CH2 domain-deleted monoclonal antibody CC49 and iodine I 131 with antineoplastic activity. Monoclonal antibody CC49-deltaCH2 targets the tumor-associated glycoprotein 72 (TAG-72) that is expressed by a wide range of human neoplasms including colorectal, gastric, pancreatic, ovarian, endometrial, breast, non-small cell lung, and prostate cancers. Iodine I 131 monoclonal antibody CC49-deltaCH2 binds to tumor cells expressing TAG-72, selectively delivering a cytotoxic dose of beta and gamma radiation.

A fully human monoclonal antibody (MoAb) against human A1 domain of tenascin-C, in small immunoprotein (SIP) format conjugated with iodine 131 with potential antineoplastic activity. Iodine I 131 MoAb F16SIP binds to tenascin-C on the vascular tissues and delivers cytotoxic radiation to the tumors, thereby minimizing systemic radiotoxicity. Tenascin-C is a glycoprotein of the extracellular matrix, and the large isoform of this matrix protein is expressed and restricted around vascular structures in the tumor stroma of a variety of different tumors.

An iodine 131 labeled radioimmunoconjugate of monoclonal antibody (MOAB) TNT-1/B with radioimaging and antineoplastic properties. MOAB TNT-1/B was developed for radioimmunotherapy of solid tumors, designated as Tumor Necrosis Treatment (TNT). TNT exploits the presence of degenerating and necrotic cells within tumors by utilizing MOAbs directed against universal, intracellular nucleosomal determinants consisting of histone H1 and DNA. This MOAB was conjugated with biotin (B) molecules, which increase pharmacokinetic performance of the monoclonal antibody. MOAB TNT-1/B delivers I 131 to tumor cells and results in the targeted imaging and/or destruction of cells with exposed necrotic antigens.

A phospholipid ether analog labeled with iodine I 131, with potential radiotherapeutic and radioimaging potential upon positron emission tomography (PET). Upon administration, iodine I 131 NM404 selectively accumulates in and is retained within tumor cells for a prolonged period of time due to the decreased activity of a phospholipase D (PLD), most likely isoform 1 of PLD, in tumor cells compared to normal cells. As tumor cells are unable to metabolize and eliminate MN404, tumor cells can be visualized upon PET imaging. In addition, iodine I 131 NM404 selectively delivers a cytotoxic dose of iodine I 131 to the tumor cells. PLD is an enzyme found in the cell membrane of normal cells that degrades phospholipids.

A radioimmunoconjugate comprised of rituximab, a recombinant chimeric monoclonal antibody directed against the CD20 antigen, and labeled with iodine I 131 with potential antineoplastic activity. The antibody moiety of iodine I 131 rituximab binds to the CD20 antigen thereby delivering cytotoxic iodine I 131 specifically to cancer cells expressing CD20. The CD20 antigen, a hydrophobic transmembrane protein, is expressed on normal pre-B and mature B lymphocytes.

A monoclonal antibody (MoAb) directed against the human epidermal growth factor receptor 2 (HER2; ERBB2) labeled with iodine I 131 using the residualizing radio-iodinating reagent N-succinimidyl 4-guanidinomethyl 3-iodobenzoate (SGMIB), with potential radiotherapeutic and radioimaging activities upon positron emission tomography (PET). Upon administration of iodine I 131 SGMIB-anti-HER2 VHH1, the HER2 MoAb moiety selectively targets and binds to HER2-expressing tumor cells. Upon PET imaging, tumor cells can be visualized. In addition, the iodine I 131 moiety of VHH1 selectively delivers a cytotoxic dose of iodine I 131 to the tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. SGMIB improves tumor retention of radioactivity and decreases exocytosis.

A radioimmunoconjugate of tenatumomab, a murine monoclonal antibody targeting the tumor-associated antigen (TAA) tenascin-C (TNC), labeled with iodine I 131, with potential antineoplastic activity. The antibody moiety of iodine I 131 tenatumomab binds to TNC, thereby delivering a cytotoxic dose of iodine I 131 specifically to tumors expressing TNC. TNC, an extracellular matrix protein, is upregulated in a variety of tumor cell types; it plays a key role in invasion, tumor cell proliferation and immune evasion.

An iodine 131 (I 131) radioconjugate of the synthetic chlorotoxin (CTX) TM-601 with potential antiangiogenic and antineoplastic activities. CTX is a 36 amino acid neurotoxin found in the venom of the giant yellow scorpion Leiurus quinquestriatus that preferentially binds malignant cells of neuroectodermal origin. The recombinant version of this peptide, TM-601, is expressed in and purified from E. coli and then covalently linked to I 131 to produce 131I-TM-601. 131I-TM-601 binds to tumor cells of neuroectodermal origin and is internalized; administered once, it may be used as a radioimaging agent; repeated administration may result in a tumor-specific, cumulative radiocytotoxic dose of I 131. In addition, TM-601 alone, similar to native CTX, may inhibit angiogenesis due to its ability to bind to and inhibit matrix metalloproteinase 2 (MMP-2), an endopeptidase involved in tissue remodeling processes such as angiogenesis.

A monoclonal antibody directed against the CD20 protein expressed on the surface of B-lymphocytes and radiolabeled with the radioisotope iodine I 131 with potential antineoplastic activity. Iodine I 131 tositumomab binds to and selectively delivers cyctotoxic radiation to CD20-expressing B-lymphocytes, thereby minimizing systemic radiotoxicity.

A tri-Fab bispecific monoclonal antibody (BiMoAb) divalent for the carcinoembryonic antigen (CEA) and monovalent for histamine-succinyl-glycine (HSG) peptide-hapten radiolabeled with iodine I 131 (I131) with antigen-binding and radioisotopic activities. Iodine I 131-labeled anti-CEA/anti-HSG bispecific monoclonal antibody TF2 binds to the tumor-associated antigen (TAA) CEA on CEA-expressing tumor cells; these cells may then be radioimaged scintigraphically.

A radioimmunoconjugate comprised of the chimeric monoclonal antibody G250 conjugated with the positron emitter iodine I 124. The antibody moiety of iodine I 124 girentuximab may bind to renal cell carcinoma (RCC) cells that express the RCC-associated antigen G250, allowing detection of tumor-localized iodine I 124 with positron emission tomography (PET). G250 is a cell surface tumor-associated antigen (TAA) that is found in the majority of renal cell carcinomas.

The neurotransmitter analogue 3-nitrobenzylguanidine conjugated to iodine I 123 and used as a gamma-emitting imaging agent. The adrenergic tissue uptake and storage of I-123 metaiodobenzylguanidine (I-123 MIBG) mimics that of norepinephrine (NE). The distribution of this agent enables the scintigraphic imaging of neural crest tumors, such as neuroblastoma and pheochromocytoma.

A dimeric iso-osmolar, non-ionic, hydrophilic iodinated radiocontrast agent used in diagnostic imaging. Upon intravascular administration and during computed tomography (CT) imaging, iodixanol blocks x-rays and appears opaque on x-ray images. This allows body structures that absorb iodine to be visualized. The degree of opacity produced by iodixanol is directly proportional to the total amount of the iodinated contrast agent in the path of the x-rays. The visualization of body structures is dependent upon the distribution and elimination of iodixanol. Compared to other iodinated contrast agents, iodixanol appears to exhibit less nephrotoxicity.

Brand name for iodine I 131

An iodine 131-radiolabeled small-molecule benzamide compound with potential antineoplastic activity. The benzamide moiety of ioflubenzamide I-131 binds to melanin, selectively delivering a cyotoxic dose of gamma and beta radiation to melanin-expressing tumor cells. Melanin pigments, polymer derivatives of the amino acid tyrosine, are over-expressed in approximately 40% of melanomas.

An iodine 123-radiolabled small molecule that exhibits high affinity for prostate-specific membrane antigen (PSMA) with potential use in molecular imaging. Iofolastat I123, a radiolabeled glutamate-urea-lysine analogue, selectively binds PSMA, which allows imaging of PSMA-expressing prostate cancer cells with gamma scintigraph. PSMA is a transmembrane glycoprotein highly expressed by malignant prostate epithelial cells and vascular endothelial cells of various solid tumors.

An X-ray contrast medium containing iohexol in various concentrations, from 140 to 350 milligrams of iodine per milliliter.

A textile fiber dressing composed of ionic silver-impregnated sodium carboxymethylcellulose with potential wound-healing and antimicrobial activities. Ionic silver-impregnated sodium carboxymethylcellulose antimicrobial dressing inhibits microbial growth and promotes wound healing while protecting the wound site from external factors that may cause pain, promote infection, or slow the natural wound healing process. Ionic silver has a high affinity for negatively charged side groups on microbial cell proteins. Upon binding, ionic silver alters the molecular structure of proteins with a role in normal microbial cell functions thereby interfering with cell wall synthesis, transcription, translation, electron transport across membranes and protein folding, resulting in microbial cell death.

An organic iodine compound and used as a non-ionic water soluble radiographic contrast medium. Iopamidol blocks x-rays as they pass through the body, thereby allowing body structures not containing iodine to be visualized. The degree of opacity produced by iopamidol is directly proportional to the total amount of the iodinated contrast agent in the path of the x-rays. The visualization of body structures is dependent upon the distribution and elimination of iopamidol.

A contrast medium.

A sterile, nonpyrogenic, aqueous solution intended for intravascular administration as a diagnostic radiocontrast agent. Ioversol is available in various concentrations, ranging from 240 to 350 milligrams of iodine per milliliter.

A proprietary fusion protein comprised of the cysteine-rich domain of frizzled family receptor 8 (Fzd8) fused to the human immunoglobulin Fc domain with potential antineoplastic activity. Upon intravenous administration, ipafricept competes with the membrane-bound Fzd8 receptor for its ligand, Wnt proteins, thereby antagonizing Wnt signaling. This may result in the inhibition of Wnt-driven tumor growth. Fzd8, a member of the Frizzled family of G protein-coupled receptors, is one of the components in the Wnt/beta-catenin signaling pathway that plays key roles in embryogenesis and cancer growth.

A pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) and a ghrelin mimetic with growth hormone (GH) releasing activity. Ipamorelin mimics ghrelin and binds to the ghrelin receptor (or GH secretagogue receptor, GHSR) in the brain, thereby selectively stimulating the release of GH from the pituitary gland. This results in increased plasma GH levels, which would affect many biological processes. Besides its presence in the brain, GHSR can also be found in the gastrointestinal tract, heart, lung, liver, kidney, pancreas, adipose tissue and immune cells. Unlike other GH releasing peptides, ipamorelin only stimulates GH release in a manner very similar to that of growth hormone releasing hormone.

An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Ipatasertib binds to and inhibits the activity of Akt in a non-ATP-competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

A recombinant human immunoglobulin (Ig) G1 monoclonal antibody directed against the human T-cell receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4), with immune checkpoint inhibitory and antineoplastic activities. Ipilimumab binds to CTLA4 expressed on T-cells and inhibits the CTLA4-mediated downregulation of T-cell activation. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells. CTLA4, an inhibitory receptor and member of the immunoglobulin superfamily, plays a key role in the downregulation of the immune system.

Brand name for inactivated poliovirus vaccine

A natural toxic furan isolated from a fungus-infected sweet potato (Ipomoea batatas) with potential antineoplastic activity. Ipomeanol is activated by mixed function oxidases in vivo to its epoxide form, an alkylating agent that covalently binds cell macromolecules. This agent causes cell death by a p53-independent mechanism. Check for active clinical trialsusing this agent.

A synthetic second-generation platinum-containing compound related to cisplatin. Iproplatin binds to and forms DNA crosslinks and platinum-DNA adducts, resulting in DNA replication failure and cell death. Although less prone to glutathione inactivation compared to cisplatin, resistance to this agent has been observed in vitro due to repair of platination damage by tumor cells.

An orally bioavailable, reversible inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), with potential antineoplastic, immunomodulating and anti-inflammatory activities. Upon oral administration, CA-4948 targets, binds to, and blocks the kinase activity of IRAK4. This inhibits IRAK4-mediated signaling, prevents the activation of IRAK4-mediated nuclear factor-kappa B (NF-kB) signaling and decreases the expression of inflammatory cytokines and certain pro-survival factors. This inhibits proliferation of IRAK4-overactivated tumor cells, which are found in cells harboring MYD88 activating mutations or those with overactivated toll-like receptor (TLR) pathways. In addition, CA-4948 may inhibit inflammation and immune-mediated cell destruction in inflammatory and auto-immune diseases where TLR or interleukin 1 receptor (IL-1R) signaling is overactivated and MYD88 is dysregulated. IRAK4, a serine/threonine-protein kinase that plays a key role in both the TLR and IL-1R signaling pathways, is activated though the adaptor protein MYD88 and links the TLR and IL-1R signaling pathway to the NF-kB pathway. Check for active clinical trialsusing this agent.

A fully human monoclonal antibody with potential antineoplastic activity. MDX-060 is a fully humanized antibody that targets CD30, a member of the tumor necrosis factor receptor superfamily found on activated lymphocytes. CD30 is over-expressed in various lymphoproliferative disorders, Hodgkin disease and other lymphomas, and other cancers.

An imaging agent composed of a heptapeptide targeting human epithelial growth factor receptor type 2 (EGFR2; HER2; ErbB2) conjugated, via a five-amino acid linker, to the near-infrared (NIR) fluorescent dye IRDye800CW, that can potentially be used for the imaging of HER2-expressing tumors. Upon oral administration of the IRDye800CW-labeled heptapeptide KSP-910638G, the peptide moiety targets and binds to HER2 expressed on tumor cells in the gastrointestinal (GI) tract. Upon fluorescence imaging of the fluorophore IRDye800CW, the tumor cells can be detected.

Brand name for gefitinib

A radioactive isotope of iridium. Iridium-192 emits gamma rays and has a half-life of 74 days. A high dose rate of this radioisotope can be used in brachytherapy to treat tumors by selectively delivering a cytotoxic dose of radiation to the tumor site.

The hydrochloride salt of a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

A liposomal formulation of the hydrochloride salt of the semisynthetic camptothecin analogue irinotecan with potential antineoplastic activity. During the S phase of the cell cycle, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell.

An orally bioavailable combination tablet containing the semisynthetic camptothecin derivative irinotecan and the multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp) inhibitor HM30181AK, with potential antineoplastic activity. HM30181A binds to P-gp and prevents the P-gp-mediated efflux of irinotecan from tumor cells, which may result in greater intracellular concentrations of irinotecan and enhanced cytotoxicity. Retained intracellularly, the prodrug irinotecan is converted, by a carboxylesterase-converting enzyme, to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38). SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. P-gp, encoded by the MDR-1 gene, is a member of the ATP-binding cassette (ABC) superfamily of transmembrane transporters and is overexpressed by some MDR tumors, preventing the intracellular accumulation of various cytotoxic agents.

Microporous hydrospheres of polyvinylalcohol (PVA) impregnated with irinotecan with potential antineoplastic activity. In transarterial chemoembolization (TACE), irinotecan-eluting beads are administered into blood vessels that feed the tumor, occluding tumor blood vessels and inducing ischemic tumor necrosis while simultaneously delivering high-dose chemotherapy locally. Irinotecan, a semisynthetic derivative of camptothecin, inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death.

A semisynthetic sesquiterpene derivative of illudin S, a natural toxin isolated from the fungus Omphalotus illudens. Irofulven alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle. This agent requires NADPH-dependent metabolism by alkenal/one oxidoreductase for activity. Irofulven is more active in vitro against tumor cells of epithelial origin and is more resistant to deactivation by p53 loss and MDR1 than other alkylating agents.

An element with atomic symbol Fe, atomic number 26, and atomic weight 55.85.

A colloidal solution containing ferric oxyhydroxide complexed with polymerized dextran, used as a form of parenteral iron-replacement therapy. Upon administration and absorption, the iron dextran complex is removed from plasma by the reticuloendothelial system which cleaves it into the components iron and dextran; ferric iron subsequently binds to transferrin or is stored as hemosiderin or ferritin. Transferrin-bound iron is transported in the plasma to the liver, spleen and bone marrow, where is it is incorporated into hemoglobin (Hgb) and to muscle where it is incorporated into myoglobin (Mb). Use of this agent circumvents the gastrointestinal adverse effects commonly encountered with the use of orally administered iron salt preparations. Because of cross-reactivity with antibodies targeted against polysaccharides similar to dextran, anaphylactic reactions may occur with this type of iron formulation.

An intravenous colloidal solution containing trivalent iron (Fe3+) chelated to isomaltosides, used as iron replacement. The iron in iron isomaltoside 1000 is strongly bound to the carbohydrate particles; each particle contains a trivalent iron core and a carbohydrate shell of isomaltosides which protects and stabilizes the iron core. This results in low levels of free iron and decreases inorganic, unbound iron-related toxicities thereby allowing for administration of higher doses of iron as compared to other iron-containing formulations. Upon parenteral administration and degradation of the carbohydrate shell, the iron in iron isomaltoside 1000 is released and replenishes iron stores. Check for active clinical trialsusing this agent.

A sterile aqueous complex of polynuclear iron (III)-hydroxide in sucrose for intravenous use. Following intravenous administration, iron sucrose is dissociated by the reticuloendothelial system into iron and sucrose; the sucrose component is eliminated mainly by urinary excretion. Iron sucrose can be administered with or without erythropoietin to raise hemoglobin levels and may be used in cases of oral iron therapy intolerance or ineffectiveness. Hypersensitivity reactions are less common with iron sucrose compared to other parenteral iron products, such as iron dextran.

A cell-free mixture comprised of a variety of naturally-derived cytokines obtained from normal, unrelated donor lymphocytes with potential immunostimulatory activity. The cytokines in IRX-2, including interleukin (IL)-1, -2, -6, -8, -10, -12, tumor necrosis factor alpha (TNF-a), interferon-gamma (IFN-g) and colony stimulating factors (CSFs), play vital roles in regulating cellular immunity and may synergistically stimulate a cellular immune response against tumor cells.

A humanized IgG1 monoclonal antibody directed against the cell surface glycoprotein CD-38 with potential antineoplastic activity. Isatuximab specifically binds to CD38 on CD38-positive tumor cells. This may trigger antitumoral antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC) and apoptosis eventually leading to cell lysis in CD38-expressing tumor cells. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies, and its expression has been correlated with poor prognosis.

A water-soluble triazole prodrug with broad-spectrum antifungal activity. Administered intravenously or orally with high oral bioavailability, isavuconazole is hydrolyzed to the active moiety BAL4815 by plasma esterases. BAL4815 inhibits fungal cytochrome P450 lanosterol 14-alpha-demethylase (CYP51), which catalyzes the conversion of lanosterol to ergosterol, an important component of the fungal cell membrane. CYP51 inhibition by this agent leads to a decrease in ergosterol pool, thus disturbing synthesis of the fungal cell membrane; increasing fungal cell membrane permeability; promoting the loss of essential intracellular elements; and resulting in fungal cell lysis and death.

The sulfate ester form of isavuconazonium, a prodrug of the triazole antifungal agent isavuconazole, with broad-spectrum antifungal activity. Upon administration, isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. Isavuconazole binds to and inhibits the fungal cytochrome P450 family enzyme lanosterol 14-alpha-demethylase (CYP51), which catalyzes the demethylation of lanosterol to yield ergosterol, an important component of the fungal cell membrane. Inhibition of CYP51 leads to a decrease in fungal ergosterol production and disrupts synthesis of the fungal cell membrane, which decreases membrane integrity, increases cell membrane permeability and promotes the loss of essential intracellular elements. This results in fungal cell lysis and death.

Brand name for mistletoe extract

Brand name for saponin-cholesterol-phospholipid adjuvant

Brand name for raltegravir potassium

A synthetic oligodeoxynucleotide. Functioning as an anti-sense agent, it hybridizes to the translation initiation region of the human mRNA for the oncogene H-Ras. ISIS 2503 selectively inhibits the expression of H-Ras, and may inhibit the growth of some Ras-dependent tumor cells.

A synthetic phosphorothioate oligodeoxynucleotide. As an antisense molecule, ISIS 3521 hybridizes to the 3-untranslated region of the human protein kinase C (PKC-alpha) mRNA, thereby inhibiting PKC-alpha expression and growth of PKC-alpha-dependent tumor cells.

A synthetic, 20-base antisense oligodeoxynucleotide that hybridizes to c-raf kinase messenger RNA. ISIS 5132 has been shown to specifically suppress Raf-1 expression both in vitro and in vivo. Raf-1 serine/threonine kinase functions as a critical effector of Ras-mediated signal transduction; constitutive activation of this pathway directly contributes to malignant transformation.

Brand name for danvatirsen

Brand name for isoflurane

A third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as well as reduced toxicity. In addition, this agent is a not a substrate of the P-glycoprotein (P-gp), a multidrug resistance pump often overexpressed in cancer cells.

A fluorinated ether with general anesthetic and muscle relaxant activities. Although the exact mechanism of action has not been established, inhaled isoflurane, appears to act on the lipid matrix of the neuronal cell membrane, which results in disruption of neuronal transmission. This agent enhances the release of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), thereby increasing the activity of the inhibitory neurotransmitter on synaptic transmission. Isoflurane may inhibit glutamatergic excitatory transmission by increasing glutamate re-uptake and it may potentiate glycine receptor activity, which decreases motor function. In addition, isoflurane may alter certain pro- and anti-inflammatory cytokines, including interleukin-6 and -10 (IL-6, IL-10), possibly through the activation of the nuclear factor kappa B (NF-KB) pathway, which may affect immune responses during surgery.

A synthetic derivative of nicotinic acid with anti-mycobacterial properties. Although its mechanism of action is still unclear, isoniazid appears to block the synthesis of mycolic acids, major components of the mycobacterial cell wall. This agent is only active against actively growing mycobacteria because, as a pro-drug, it requires activation in susceptible mycobacterial species. Isoniazid also interferes with mycobacterial metabolism of vitamin B6. Resistance occurs due to decreased bacterial wall penetration.

An orally bioavailable, glucoside derivative of the flavonoid quercetin and protein disulfide isomerase (PDI) inhibitor, with antioxidant and potential antithrombotic activity. As an antioxidant, isoquercetin scavenges free radicals and inhibits oxidative damage to cells. As a PDI inhibitor, this agent blocks PDI-mediated platelet activation, and fibrin generation, which prevents thrombus formation after vascular injury. In addition, isoquercetin is an alpha-glucosidase inhibitor. PDI, an oxidoreductase secreted by activated endothelial cells and platelets, plays a key role in the initiation of the coagulation cascade. Cancer, in addition to other thrombotic disorders, increases the risk of thrombus formation.

A synthetic visual lymphatic imaging agent. Injected into the periphery of the tumor site, isosulfan blue localizes to the lymphatic system and aids in the surgical identification of tumor sentinel nodes which stain blue.

A naturally-occurring retinoic acid with potential antineoplastic activity. Isotretinoin binds to and activates nuclear retinoic acid receptors (RARs); activated RARs serve as transcription factors that promote cell differentiation and apoptosis. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.

Brand name for iopamidol

A synthetic small molecule, derived from quinazolinone, with antineoplastic properties. Ispinesib selectively inhibits the mitotic motor protein, kinesin spindle protein (KSP), resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase, and cell death in tumor cells that are actively dividing. Because KSP is not involved in nonmitotic processes, such as neuronal transport, ispinesib may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents.

A short, synthetic, unmethylated CpG motif-based oligodeoxynucleotide (CpG ODN) with immunostimulatory activity. As an immunostimulatory sequence (ISS) that signals through Toll-like receptor 9 (TLR9), ISS 1018 CpG ODN induces the production of immunoglobulin by B cells and interferon (IFN) -alpha, IFN-beta, interleukin (IL) -12, and tumor necrosis factor (TNF) -alpha by plasmacytoid dendritic cells (pDC). In turn, pDC, through cell-cell contact and secretion of and IFN-alpha and -beta induce natural killer (NK) cell proliferation, NK cell production of IFN-gamma, and NK cell-mediated cytotoxicity; secreted IFNs also stimulate bystander T cell activation and differentiation of naive CD4+ T cells into T-helper 1 cells on specific antigen challenge. In addition, ISS 1018 CpG ODN promotes antigen presentation and co-stimulatory molecule expression. Unmethylated CpG motifs are regions of genomic DNA containing the cytosine-guanine dinucleotide in which cytosine remains unmethylated, especially in prokaryotic DNA.

Brand name for romidepsin

The adipate salt form of itacitinib, an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic and immunomodulating activities. Upon oral administration, itacitinib selectively inhibits JAK-1, thereby inhibiting the phosphorylation of signal transducer and activator of transcription (STAT) proteins and the production of proinflammatory factors induced by other cytokines, including interleukin-23 (IL-23) and interleukin-6 (IL-6). The JAK-STAT pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.

A synthetic triazole agent with antimycotic properties. Formulated for both topical and systemic use, itraconazole preferentially inhibits fugal cytochrome P450 enzymes, resulting in a decrease in fungal ergosterol synthesis. Because of its low toxicity profile, this agent can be used for long-term maintenance treatment of chronic fungal infections.

A proprietary oral formulation composed of the poorly soluble, synthetic triazole agent, itraconazole, dispersed in a polymer matrix, with antifungal and potential anti-angiogenic activities. Upon oral administration, itraconazole inhibits the enzyme cytochrome P450 lanosterol 14 alpha-demethylase, resulting in a decrease in fungal ergosterol synthesis. Although the exact mechanism through which itraconazole inhibits angiogenesis has yet to be fully elucidated, this agent appears to inhibit the Hedgehog (Hh) signaling pathway, cholesterol synthesis and mammalian target of rapamycin (mTOR) signaling in endothelial cells. This agent may also prevent the activation of and signaling by various angiogenic growth factors. By decreasing the tumor vasculature and nutrient supply, itraconazole ultimately inhibits tumor cell growth. The solid dispersion of itraconazole in the polymer matrix enhances dissolution of itraconazole in the gastrointestinal tract and increases its bioavailability; this allows for the administration of a much lower dose compared to itraconazole alone.

The hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization. This decreases heart rate, reduces myocardial oxygen demand and allows more time for blood to flow to the myocardium without affecting cardiac contractility. HCN channels, mixed sodium (Na+) and potassium (K+) channels that carry the inward If current, play a key role in the regulation of pacemaker firing rate in the SA node. The If pacemaker current, the inward flow of positively charged Na+-K+ ions, initiates the spontaneous diastolic depolarization phase and modulating heart rate.

An individualized, poly-neo-epitopic encoding, ribonucleic acid (RNA)-based cancer vaccine that targets a variety of patient-specific, immunogenic mutant epitopes, with potential immunostimulatory and antineoplastic activities. Upon intranodal administration, the RNA in the individualized mutanome vaccine is 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 patient-specific neoantigens.

Brand name for therapeutic immune globulin

An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Upon administration, ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells. IDH1, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.

An orally bioavailable semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. This agent demonstrates antineoplastic activity against taxane-resistant cell lines.

An enteric-coated formulation of ixabepilone, a semisynthetic analogue of epothilone B and a non-taxane tubulin inhibitor, with antineoplastic activity. Ixabepilone binds to and stabilizes tubulin molecules, thereby interfering with the dynamics of microtubule assembly/disassembly. This results in cell cycle arrest at the G2-M phase and leads to apoptosis within fast growing tumor cells. This agent demonstrates antineoplastic activity against taxane-resistant cell lines. Compared to intravenously administered ixabepilone, the oral formulation provides a more manageable way to administer this agent.

An orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. Ixazomib inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome, which results in an accumulation of unwanted or misfolded proteins; disruption of various cell signaling pathways may follow, resulting in the induction of apoptosis. Compared to first generation PIs, second generation PIs may have an improved pharmacokinetic profile with increased potency and less toxicity. Proteasomes are large protease complexes that degrade unneeded or damaged proteins that have been ubiquinated. Check for active clinical trialsusing this agent.

Brand name for ixabepilone

Brand name for trofosfamide

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