jueves, 31 de mayo de 2018

NCI Drug Dictionary - National Cancer Institute | i/I/2

NCI Drug Dictionary - National Cancer Institute

National Cancer Institute

297 results found for: I
iodine I 124 iodo-azomycin galactopyranoside
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 124 iododeoxyuridine
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. (NCI Thesaurus)
iodine I 124 monoclonal antibody 3F8
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 124 monoclonal antibody 8H9
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 124 NM404
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.
iodine I 124 phospholipid ether analogue CLR1404
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 124 PU-AD
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 124-labeled anti-phosphatidylserine monoclonal antibody PGN650
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 124-labeled anti-PSCA A11 minibody
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 124-labeled HSP90 inhibitor PUH71
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 125
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 125 anti-EGFR-425 monoclonal antibody
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. (NCI Thesaurus)
iodine I 131
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 anti-fibronectin antibody fragment L19-SIP
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 chimeric monoclonal antibody G-250
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 ethiodized oil
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 iodocholesterol
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. Check for active clinical trials using this agent. (NCI Thesaurus)
Iodine I 131 Lipiodol
(Other name for: iodine I 131 ethiodized oil)
iodine I 131 MIP-1095
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 monoclonal antibody 3F8
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 monoclonal antibody 81C6
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. (NCI Thesaurus)
iodine I 131 monoclonal antibody 8H9
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 monoclonal antibody BC8
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 monoclonal antibody CC49-deltaCH2
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 monoclonal antibody F16SIP
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 monoclonal antibody TNT-1/B
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 NM404
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 rituximab
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 SGMIB-anti-HER2 VHH1
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 tenatumomab
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 TM-601
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131 tositumomab
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I 131-labeled anti-CEA/anti-HSG bispecific monoclonal antibody TF2
A tri-Fab bispecific monoclonal antibody (BiMoAb) divalent for the carcinoembryonic antigen (CEA) and monovalent for histamine-succinyl-glycine (HSG) peptide-hapten 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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine I-124 girentuximab
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodine-123 metaiodobenzylguanidine
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iodixanol
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. Check for active clinical trials using this agent. (NCI Thesaurus)
Iodotope
(Other name for: iodine I 131)
ioflubenzamide 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. Check for active clinical trials using this agent. (NCI Thesaurus)
iofolastat I123
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iohexol
An X-ray contrast medium containing iohexol in various concentrations, from 140 to 350 milligrams of iodine per milliliter. Check for active clinical trials using this agent. (NCI Thesaurus)
ionic silver-impregnated sodium carboxymethyl cellulose antimicrobial dressing
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iopamidol
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iopromide
A contrast medium. Check for active clinical trials using this agent. (NCI Thesaurus)
ipafricept
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ipamorelin
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ipatasertib
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ipilimumab
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. Check for active clinical trials using this agent. (NCI Thesaurus)
IPOL
(Other name for: inactivated poliovirus vaccine)
ipomeanol
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. (NCI Thesaurus)
iproplatin
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iratumumab
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. Check for active clinical trials using this agent. (NCI Thesaurus)
IRDye800CW-labeled heptapeptide KSP-910638G
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.
Iressa
(Other name for: gefitinib)
iriduim Ir 192
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. Check for active clinical trials using this agent. (NCI Thesaurus)
irinotecan hydrochloride
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. Check for active clinical trials using this agent. (NCI Thesaurus)
irinotecan hydrochloride liposome
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. Check for active clinical trials using this agent. (NCI Thesaurus)
irinotecan/P-glycoprotein inhibitor HM30181AK combination tablet
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. Check for active clinical trials using this agent. (NCI Thesaurus)
irinotecan-eluting beads
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. Check for active clinical trials using this agent. (NCI Thesaurus)
irofulven
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iron
An element with atomic symbol Fe, atomic number 26, and atomic weight 55.85. Check for active clinical trials using this agent. (NCI Thesaurus)
iron dextran complex
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. Check for active clinical trials using this agent. (NCI Thesaurus)
iron isomaltoside 1000
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. (NCI Thesaurus)
iron sucrose injection
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. Check for active clinical trials using this agent. (NCI Thesaurus)
IRX-2
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. Check for active clinical trials using this agent. (NCI Thesaurus)
isatuximab
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. Check for active clinical trials using this agent. (NCI Thesaurus)
isavuconazole
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. Check for active clinical trials using this agent. (NCI Thesaurus)
Iscar
(Other name for: mistletoe extract)
Iscomatrix
(Other name for: saponin-cholesterol-phospholipid adjuvant)
Isentress
(Other name for: raltegravir potassium)
ISIS 2503
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ISIS 3521
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ISIS 5132
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ISIS-STAT3rx
(Other name for: STAT3 antisense oligonucleotide ISIS 481464)
Isoflo
(Other name for: isoflurane)
iso-fludelone
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. Check for active clinical trials using this agent. (NCI Thesaurus)
isoflurane
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. Check for active clinical trials using this agent. (NCI Thesaurus)
isoniazid
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. Check for active clinical trials using this agent. (NCI Thesaurus)
isoquercetin
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. Check for active clinical trials using this agent. (NCI Thesaurus)
isosulfan blue
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. Check for active clinical trials using this agent. (NCI Thesaurus)
isotretinoin
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. Check for active clinical trials using this agent. (NCI Thesaurus)
Isovue
(Other name for: iopamidol)
ispinesib
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ISS 1018 CpG oligodeoxynucleotide
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. Check for active clinical trials using this agent. (NCI Thesaurus)
Istodax
(Other name for: romidepsin)
itacitinib
An orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity. Upon oral administration of itacitinib, this agent selectively inhibits the phosphorylation and activity of JAK1, which may result in inhibition of JAK1-mediated signaling, induction of apoptosis, and reduction of cell proliferation in JAK1-expressing tumor cells. JAK1 is overexpressed in a variety of tumor cell types and plays a key role in tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
itraconazole
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. Check for active clinical trials using this agent. (NCI Thesaurus)
itraconazole dispersion in polymer matrix
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ivabradine hydrochloride
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. Check for active clinical trials using this agent. (NCI Thesaurus)
IVAC mutanome vaccine
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. Check for active clinical trials using this agent. (NCI Thesaurus)
Iveegam EN
(Other name for: therapeutic immune globulin)
ivosidenib
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ixabepilone
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ixabepilone (oral)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ixazomib citrate
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. (NCI Thesaurus)
Ixempra
(Other name for: ixabepilone)
Ixoten
(Other name for: trofosfamide)

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