Disease & Drug Info

Drug Dictionary

IAP inhibitor AT-406

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. Check for active clinical trials using this agent. (NCI Thesaurus)

IAP inhibitor HGS1029

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. Check for active clinical trials using this agent. (NCI Thesaurus)

iAPA-based dendritic cells/cytotoxic T lymphocytes

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. Check for active clinical trials using this agent. (NCI Thesaurus)

ibandronate sodium

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Ibrance

(Other name for: palbociclib)

ibritumomab tiuxetan

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. Check for active clinical trials using this agent. (NCI Thesaurus)

ibrutinib

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 trials using this agent. (NCI Thesaurus)

ibuprofen

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. Check for active clinical trials using this agent. (NCI Thesaurus)

ibuprofen intravenous

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. Check for active clinical trials using this agent. (NCI Thesaurus)

iC9-GD2-CD28-OX40-expressing T lymphocytes

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. Check for active clinical trials using this agent. (NCI Thesaurus)

ICE regimen

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

IC-GREEN

(Other name for: indocyanine green solution)

Iclusig

(Other name for: ponatinib hydrochloride)

icodextrin solution

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. Check for active clinical trials using this agent. (NCI Thesaurus)

icotinib hydrochloride

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. Check for active clinical trials using this agent.

icrucumab

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. Icrucumabspecifically 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. Check for active clinical trials using this agent. (NCI Thesaurus)

Idamycin

(Other name for: idarubicin hydrochloride)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

idarubicin-eluting beads

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. Check for active clinical trials using this agent. (NCI Thesaurus)

idasanutlin

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. Check for active clinical trials using this agent. (NCI Thesaurus)

idelalisib

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. Check for active clinical trials using this agent. (NCI Thesaurus)

IDH mutant inhibitor AG-881

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. Check for active clinical trials using this agent. (NCI Thesaurus)

IDH1 inhibitor AG-120

An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Upon administration, AG-120 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. Check for active clinical trials using this agent. (NCI Thesaurus)

IDH1(R132) inhibitor IDH305

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. Check for active clinical trials using this agent. (NCI Thesaurus)

IDH1R132H mutation-targeting IDH1 peptide vaccine

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). Check for active clinical trials using this agent. (NCI Thesaurus)

IDH1R132H-specific peptide vaccine PEPIDH1M

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). Check for active clinical trials using this agent. (NCI Thesaurus)

IDH2 inhibitor AG-221

An orally available inhibitor of isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. Upon administration, AG-221 specifically inhibits IDH2 in the mitochondria, which inhibits the formation of 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH2-expressing tumor cells. IDH2, an enzyme in the citric acid cycle, is mutated in a variety of cancers; It initiates and drives cancer growth by blocking differentiation and the production of the oncometabolite 2HG. Check for active clinical trials using this agent. (NCI Thesaurus)

idiotype-pulsed autologous dendritic cell vaccine APC8020

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. Check for active clinical trials using this agent. (NCI Thesaurus)

IDO inhibitor NLG919

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. Check for active clinical trials using this agent. (NCI Thesaurus)

idoxuridine

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. Check for active clinical trials using this agent. (NCI Thesaurus)

idronoxil

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Ifex

(Other name for: ifosfamide)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Ifosfamidum

(Other name for: ifosfamide)

IGF ligand neutralizing antibody BI 836845

A humanized IgG1 insulin-like growth factor (IGF) monoclonal antibody targeting the IGF ligands 1 (IGF-1) and 2 (IGF-2), with potential antineoplastic activity. Upon administration, IGF ligand neutralizing antibody BI 836845 binds to both IGF-1 and IGF-2 and inhibits the binding of these ligands to their receptor, IGF-1R. This blocks the insulin growth factor (IGF) signaling pathway, which is upregulated in a number of cancer cell types and plays a key role in cancer cell proliferation and chemoresistance. In addition, BI 836845 prevents the binding of IGF-2 to insulin receptor variant A (IR-A), preventing its activation. Check for active clinical trials using this agent. (NCI Thesaurus)

IGF-1R antagonist BMS-754807

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. Check for active clinical trials using this agent. (NCI Thesaurus)

IGF-1R antisense oligodeoxynucleotide-treated autologous glioma cells

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 patients 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 patients 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. Check for active clinical trials using this agent. (NCI Thesaurus)

IGF-1R inhibitor PL225B

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. Check for active clinical trials using this agent. (NCI Thesaurus)

IGF-1R/IR inhibitor KW-2450

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. Check for active clinical trials using this agent. (NCI Thesaurus)

IGF-methotrexate conjugate

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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