CIENCIASMEDICASNEWS: NCI Drug Dictionary - National Cancer Institute

NCI Drug Dictionary - National Cancer Institute

259 results found for: E

ethinyl estradiol: A semisynthetic estrogen. Ethinyl estradiol binds to the estrogen receptor complex and enters the nucleus, activating DNA transcription of genes involved in estrogenic cellular responses. This agent also inhibits 5-alpha reductase in epididymal tissue, which lowers testosterone levels and may delay progression of prostatic cancer. In addition to its antineoplastic effects, ethinyl estradiol protects against osteoporosis. In animal models, short-term therapy with this agent has been shown to provide long-term protection against breast cancer, mimicking the antitumor effects of pregnancy. Check for active clinical trials using this agent. (NCI Thesaurus)
ethinyl estradiol/levonorgestrel: A combination of two steroid sex hormones, an estrogen and a progestin, used for contraceptive purposes. Estradiol, the endogenous counterpart of ethinyl estradiol (EE), is the principal, most potent estrogen hormone produced by the ovaries and is vital to the maintenance of fertility and secondary sexual characteristics in females. Levonorgestrel is a synthetic progestogen. This drug combination prevents or delays ovulation and causes a variety of hormonal changes. Ethinyl estradiol inhibits the release of follicle stimulating hormone (FSH), thus suppressing the development of ovarian follicle; levonorgestrel inhibits the release of luteinizing hormone (LH), thus preventing ovulation. This combination of agents alters the endometrium in such a way as to discourage implantation. Check for active clinical trials using this agent. (NCI Thesaurus)
ethinyl estradiol/norethindrone: An oral contraceptive formulation containing the semisynthetic estrogen, ethinyl estradiol, combined with the synthetic progestin, norethindrone, with estrogenic and progestogenic activities, respectively. Ethinyl estradiol binds to and activates intracellular estrogen receptors found in the reproductive tract and other estrogen-responsive tissues. The activated complex enters the nucleus, binds to the estrogen response elements on DNA, activates the transcription of genes involved in the maintenance of the female reproductive system, inhibits the release of follicle stimulating hormone (FSH) from the anterior pituitary, and suppresses the development of the ovarian follicle. Norethindrone binds to intracellular progesterone receptors in progesterone-responsive tissues, such as the pituitary and those found in the reproductive system, and the activated ligand/receptor complex interacts with specific progesterone response elements on DNA, which results in the alteration in protein synthesis, the inhibition of ovulation, an increase in cervical mucus production, the induction of the secretory phase of the endometrial cycle, and the inhibition of luteinizing hormone (LH) release. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system and alters the structure of the endometrium to discourage implantation. Check for active clinical trials using this agent.
ethiodized oil: A synthetic iodine addition product of the ethyl ester of the fatty acids of poppyseed oil. Ethiodized oil contains 37% organically bound iodine and is used as a diagnostic radiopaque medium or, labeled with I-131, as an antineoplastic agent. Selectively retained in tumor vessels for long periods, ethiodized oil is used for imaging organs such as liver, lung, stomach, and thyroid. Labeled with I-131 or other beta emitters (Y-90 or P-32), ethiodol can deliver a high internal radiation dose to certain tumors with minimal effect on healthy tissues. Check for active clinical trials using this agent. (NCI Thesaurus)
ethosuximide: A succinimide with anticonvulsant activity. The exact mechanism of action is not entirely understood, but most likely ethosuximide exerts its effects by partial antagonism of T-type calcium channels of the thalamic neurons. This leads to a decrease in burst firing of thalamocortical neurons, which stabilizes the nerve activity in the brain and prevents seizures. Check for active clinical trials using this agent. (NCI Thesaurus)
ethyl alcohol mouthwash: A mouthwash containing ethyl alcohol, with topical antibacterial activity. Upon rinsing the oral cavity with the ethyl alcohol mouthwash, ethyl alcohol denatures bacterial proteins, and dissolves and disrupts the bacterial lipid membrane, thereby killing the bacteria. This reduces oral colonization with harmful bacteria and may prevent oral mucositis. Check for active clinical trials using this agent. (NCI Thesaurus)
ethyl icosapentate: A highly purified omega-3 fatty acid that can decrease serum triglyceride levels. Ethyl icosapentate reduces serum triglycerides without an increase in LDL cholesterol, but increases the cholesterol and triglyceride content in skeletal muscle. Check for active clinical trials using this agent. (NCI Thesaurus)
ethylene-vinyl alcohol copolymer-based embolic agent: A non-adhesive, non-absorbable, permanent liquid embolic agent comprised of ethylene vinyl alcohol (EVOH) copolymer dissolved in dimethyl sulfoxide (DMSO), and of micronized tantalum powder that can be used to occlude blood vessels. Upon administration of the EVOH-based embolic agent, contact with fluids, such as blood, induces the solidification of EVOH into a sponge-like material. This causes occlusion of blood vessels and prevents blood flow to the treated area. Check for active clinical trials using this agent. (NCI Thesaurus)
Ethyol: (Other name for: amifostine)
etidronate-cytarabine conjugate MBC-11: A synthetic conjugate composed of the bisphosphonate etidronate linked to the cytostatic agent and antimetabolite cytarabine, with potential antineoplastic and antiresorptive activities. Upon intravenous administration of the etidronate-cytarabine conjugate MBC-11, the etidronate moiety targets bone and the two moieties are released upon hydrolysis of the phospho-ester bond locally. Etidronate binds to hydroxyapatite crystals in bone tissues and prevents its resorption. This prevents bone destruction and induces bone cell mineralization. In addition, the bone-targeting nature of this agent allows for the accumulation of cytarabine in bone tissue, where it is able to exert its antitumor effect locally by competing with cytidine for incorporation into DNA, thereby inhibiting DNA synthesis, while reducing systemic exposure. This leads to a destruction of bone-associated tumor cells, an inhibition of tumor cell proliferation and bone metastasis, and prevents tumor-mediated bone destruction. Check for active clinical trials using this agent.
Etilamide: (Other name for: buserelin)
etirinotecan pegol: An extended-release (ER) formulation composed of irinotecan, which is a semisynthetic derivative of camptothecin and a topoisomerase I-inhibitor prodrug, that is conjugated, via a proprietary biodegradable ester-based linker, to polyethylene glycol (PEG), with antineoplastic activity. Upon administration of etirinotecan pegol (EP), the agent penetrates into the leaky tumor vasculature and accumulates in the tumor. The linker slowly hydrolyzes and releases irinotecan, which leads to sustained exposure of the tumor to irinotecan. In turn, irinotecan is converted to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN38) by a carboxylesterase. SN38 inhibits topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and DNA; this results in DNA breaks that inhibit DNA replication and trigger apoptosis. Pegylation provides improved systemic exposure, increases drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic effects while lowering the toxicity profile. Check for active clinical trials using this agent. (NCI Thesaurus)
etodolac: A pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. Etodolac inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2. Check for active clinical trials using this agent. (NCI Thesaurus)
Etopophos: (Other name for: etoposide phosphate)
etoposide: A semisynthetic derivative of podophyllotoxin, a substance extracted from the mandrake root Podophyllum peltatum. Possessing potent antineoplastic properties, etoposide binds to and inhibits topoisomerase II and its function in ligating cleaved DNA molecules, resulting in the accumulation of single- or double-strand DNA breaks, the inhibition of DNA replication and transcription, and apoptotic cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle. Check for active clinical trials using this agent. (NCI Thesaurus)
etoposide phosphate: A phosphate salt of a semisynthetic derivative of podophyllotoxin. Etoposide binds to the enzyme topoisomerase II, inducing double-strand DNA breaks, inhibiting DNA repair, and resulting in decreased DNA synthesis and tumor cell proliferation. Cells in the S and G2 phases of the cell cycle are most sensitive to this agent. Check for active clinical trials using this agent. (NCI Thesaurus)
etoposide prodrug CAP7.1: A prodrug of etoposide, a semisynthetic derivative of podophyllotoxin extracted from the mandrake root Podophyllum peltatum, with potential antineoplastic activity. Upon intravenous administration of the etoposide prodrug CAP7.1, etoposide is released after enzymatic cleavage of CAP7.1 by specific carboxylesterases (CE) 1 and 2, which are upregulated in certain tumor cell types. Etoposide acts primarily in the G2 and S phases of the cell cycle. This drug binds to and inhibits topoisomerase II, an enzyme elevated in tumor cells. This results in the accumulation of double-strand DNA breaks, the inhibition of DNA replication and transcription and the induction of apoptotic cell death. The tumor-specific activation of etoposide increases its efficacy while lowering its systemic toxicity. Check for active clinical trials using this agent. (NCI Thesaurus)
etoricoxib: A synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic ,and potential antineoplastic properties. Etoricoxib specifically binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
Etrenol: (Other name for: hycanthone)
Etretin: (Other name for: acitretin)
Ets-family transcription factor inhibitor TK216: A proprietary biologic that inhibits the transcriptional-promoting activity of E26 transformation-specific (Ets, E-twenty-six) family transcription factors, with potential antineoplastic activity. Although the exact mechanism(s) of action through which this agent exerts its effect has yet to be fully elucidated, upon administration, Ets-family transcription factor inhibitor TK216 inhibits transcriptional activation mediated by Ets family proteins, including the oncogenic Ewing sarcoma breakpoint region 1/Friend leukemia virus integration 1 (EWSR1/FLI1; EWS/FLI1) fusion protein. This agent may both inhibit the malignant downstream effects mediated by genomic rearrangements that result in the overexpression of Ets family transcription factors and decrease tumor cell growth and proliferation. A chromosomal translocation t(11;22)(q24;q12) fuses the EWSR1 gene and the FLI1 gene and encodes the EWSR1/FLI1 fusion protein, which is an oncoprotein expressed by peripheral primitive neuroectodermal (pPNET) tumors. Check for active clinical trials using this agent. (NCI Thesaurus)
Eucerin: (Other name for: therapeutic lotion)
Evacet: (Other name for: pegylated liposomal doxorubicin hydrochloride)
Evaux spring water-based cream: A cream containing Evaux thermal spring water, with potential moisturizing and skin protecting activities. Upon application to the skin, Evaux spring water-based cream forms a protective barrier, which prevents water loss, provides moisture to the skin, protects the skin from damage, and soothes irritated skin. The Evaux thermal spring water contains the trace elements lithium and manganese which may help heal the skin. Check for active clinical trials using this agent. (NCI Thesaurus)
Evaux spring water-based topical spray: A skin spray composed of Evaux thermal spring water, the emulsifier polysorbate 20, the preservatives phenoxyethanol and chlorphenesin, zinc gluconate, and the moisturizer caprylyl glycol with prophylactic and calming activity. Evaux thermal spring water is rich in mineral elements particularly of lithium, strontium and manganese. When sprayed directly onto the skin or scalp, this topical spray may have a calming, moisturizing, healing and nurturing effect. This agent may prevent or decrease skin rashes associated with the administration of EGFR inhibitors or with radiochemotherapy-induced skin reactions. Check for active clinical trials using this agent.
Evaux thermal spring water-based solution: A topical solution containing Evaux thermal spring water, with potential moisturizing and skin protecting activities. Upon application to the nails and surrounding skin, Evaux spring water-based solution forms a film on the nails that serves as a protective barrier. This prevents water loss from, provides moisture to, and strengthens the nails, and protects them from damage. The solution also relieves pain caused by cracked, peeled, thinning or soft nails. Evaux thermal spring water contains the elements lithium, manganese and strontium which may help heal the nails and prevent onycholysis. It also contains chlorphenesin and piroctone olamine, both of which have antifungal activity. Some chemotherapy and/or radiation therapy can induce damage to the nails. Check for active clinical trials using this agent. (NCI Thesaurus)
everolimus: A derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties. In cells, everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production. Check for active clinical trials using this agent. (NCI Thesaurus)
everolimus tablets for oral suspension: Tablets for oral suspension containing everolimus, a derivative of the natural macrocyclic lactone sirolimus, with immunosuppressive and antineoplastic activities. After suspension of the everolimus tablets in water and oral administration, this agent inhibits the activation of the serine/threonine kinase mammalian target of rapamycin (mTOR) by binding to mTOR's cytosolic receptor immunophilin FK Binding Protein-12 (FKBP-12). Inhibition of the mTOR complex may result in the inhibition of the phosphatidylinositol 3 kinase/Akt/mTOR pathway and an inhibition in the expression of vascular endothelial cell growth factor (VEGF) and hypoxia-inducible factor. Ultimately, this may result in decreased tumor cell proliferation and tumor angiogenesis. This pediatric formulation can dissolve easily in a small volume of water making it easier to swallow and is available in smaller dose increments thereby allowing for greater dosing flexibility. Check for active clinical trials using this agent. (NCI Thesaurus)
Evista: (Other name for: raloxifene hydrochloride)
evofosfamide: A hypoxia-activated prodrug consisting of a 2-nitroimidazole phosphoramidate conjugate with potential antineoplastic activity. The 2-nitroimidazole moiety of evofosfamide acts as a hypoxic trigger, releasing the DNA-alkylating dibromo isophosphoramide mustard moiety within hypoxic regions of tumors. Normoxic tissues may be spared due to the hypoxia-specific activity of this agent, potentially reducing systemic toxicity. Check for active clinical trials using this agent. (NCI Thesaurus)
Evomela: (Other name for: melphalan hydrochloride)
EvoNail: (Other name for: Evaux thermal spring water-based solution)
Evoskin cream: (Other name for: Evaux spring water-based cream)
Evoxac: (Other name for: cevimeline hydrochloride)
ex vivo-activated autologous lymph node lymphocytes: Autologous human lymph node T-lymphocytes, with potential immunostimulatory and antineoplastic activity. Upon collection of immune cells from the tumor-draining lymph node, the human lymph node lymphocytes are activated with anti-CD3/anti-CD28 microbeads, cultured with recombinant, human interleukin-2 (IL-2), expanded and isolated ex vivo. Upon reintroduction into the patient, the ex vivo-activated autologous lymph node lymphocytes recognize and lyse the tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
ex vivo-expanded autologous T cells IMA101: A preparation of autologous cytotoxic T lymphocytes, specifically recognizing certain tumor-associated antigens (TAAs), with potential antineoplastic activity. The endogenous T cells are isolated, expanded ex vivo, and reintroduced back into the patient. Upon administration, the ex vivo-expanded autologous T cells IMA101 target and kill tumor cells. The T cells are analyzed beforehand for their ability to specifically recognize certain TAAs, based on a proprietary antigen warehouse. Check for active clinical trials using this agent. (NCI Thesaurus)
ex vivo-expanded HER2-specific T cells: T cells specific for the human epidermal growth factor receptor 2 (HER2) with potential immunopotentiating activity. T cells directed against HER2, overexpressed on many tumor cells, are collected from HER2-expressing tumor tissue, expanded ex vivo and, then re-introduced in the patient. Re-introduction of ex vivo-expanded HER2-specific T cells may enhance the cytotoxic T cell response against tumor cells overexpressing HER2, resulting in inhibition of tumor growth. Check for active clinical trials using this agent. (NCI Thesaurus)
exatecan mesylate: A semisynthetic, water-soluble derivative of camptothecin with antineoplastic activity. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogues. Check for active clinical trials using this agent. (NCI Thesaurus)
Exelon: (Other name for: rivastigmine tartrate)
exemestane: A synthetic androgen analogue. Exemestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. Check for active clinical trials using this agent. (NCI Thesaurus)
exenatide: A 39 amino acid peptide and synthetic version of exendin-4, a hormone found in the saliva of the venomous lizard Gila monster, with insulin secretagogue and antihyperglycemic activity. Exenatide is administered subcutaneously and mimics human glucagon-like peptide-1 (GLP-1). Compared to GLP-1, exenatide has a longer half-life of 2.4 hours. Check for active clinical trials using this agent. (NCI Thesaurus)
exendin 9-39: A truncated form of the glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 peptide, with GLP-1 receptor (GLP-1R) antagonistic and GLP-1R-mediated signaling inhibiting activities. Upon administration, exendin 9-39 competitively binds to and inhibits the activity of GLP-1R, thereby inhibiting GLP-1/GLP-1R-mediated signaling. This antagonizes the glucagonostatic and the insulinotropic effects of GLP-1. By abrogating GLP-1-mediated simulation of insulin release and reduction of glucagon secretion after food intake, exendin 9-39 may be used to help study the potential effects of overproduction of GLP-1 on food intake, weight loss and glucose levels. GLP-1R, located on pancreatic beta cells, is overexpressed on certain tumor cell types. GLP-1 is a gastrointestinal (GI) and insulinotropic hormone that is released after a meal and plays a key role in the regulation of blood glucose levels. Check for active clinical trials using this agent. (NCI Thesaurus)
Exherin: (Other name for: ADH-1)
exisulind: An inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac. After oral administration, sulindac undergoes extensive biotransformation including irreversible oxidation to sulindac sulfone. Approximately, one half of an administered dose of sulindac is eliminated through the urine, mostly as the conjugated sulfone metabolite. Check for active clinical trials using this agent. (NCI Thesaurus)
Exjade: (Other name for: deferasirox)
expanded umbilical cord blood product HSC835: An umbilical cord blood product that has been expanded ex vivo and can be used during single umbilical cord blood transplantation. Check for active clinical trials using this agent. (NCI Thesaurus)
Exparel: (Other name for: bupivacaine hydrochloride liposome injectable suspension)
extended release bupivacaine hydrochloride resorbable matrix formulation: An extended release (ER) injectable formulation composed of the hydrochloride salt form of bupivacaine, an amide-type, long-acting local anesthetic, in a resorbable sucrose acetate isobutyrate-based matrix, with analgesic activity. Following administration in or around a specific site, ER bupivacaine is released from the matrix over an extended period of time. Upon release, bupivacaine reversibly binds to specific voltage-gated sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions, membrane destabilization, and depolarization inhibition thus disrupting nerve impulse conduction. This eventually leads to a reversible loss of sensation. This formulation may provide pain relief up to 72 hours. Check for active clinical trials using this agent. (NCI Thesaurus)
extended-release flucytosine: An extended release (ER) oral tablet that contains flucytosine (5-FC), a fluorinated cytosine analog, with antifungal activity and potential anti-cancer activity. Following oral administration of ER 5-FC, the 5-FC is deaminated to its active metabolite 5-fluorouracil (5-FU). 5-FU replaces uracil during RNA synthesis, which consequently inhibits downstream protein synthesis. In addition, 5-FU is metabolized further to 5-fluorodeoxyuridylic acid monophosphate, which inhibits thymidylate synthetase. Inhibition of this enzyme interrupts nucleotide synthesis, DNA replication and cell proliferation. Negative regulation of protein synthesis, DNA replication and cell proliferation can lead to cell death. Following ingestion of ER 5-FC, intravenous injection of a retroviral vector encoding cytosine deaminase (TC 511) at a tumor site may result in higher local concentrations of 5-FU and its metabolites, and increased tumor cell death than other 5-FU treatment regimens. Check for active clinical trials using this agent. (NCI Thesaurus)
extended-release granisetron polymer formulation: An extended-release (ER), polymer-based injectable formulation containing the indazole derivative granisetron, a selective serotonin (5-hydroxytryptamine; 5-HT) receptor type 3 (5-HT3) antagonist, with anti-emetic activity. Upon subcutaneous administration, granisetron is released from the polymer in a sustained manner, which is based upon the controlled hydrolysis of the polymers, and selectively binds to and inhibits the activity of the 5-HT3 receptors located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema. By preventing stimulation of 5-HT3 receptors, granisetron is able to suppress chemotherapy-induced nausea and vomiting (CINV). Compared to the injection of granisetron alone, injection of the polymer-based formulation allows for therapeutic levels of granisetron over an extended period of time. Check for active clinical trials using this agent.
extended-release onapristone: An extended-release (ER) 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 on certain cancer cell types and plays a key role in proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)
Extren: (Other name for: acetylsalicylic acid)
E-Z Prep: (Other name for: povidone-iodine solution)
E-Z Scrub: (Other name for: povidone-iodine solution)
ezatiostat hydrochloride: The hydrochloride salt of a liposomal small-molecule glutathione analog inhibitor of glutathione S-transferase (GST) P1-1 with hematopoiesis-stimulating activity. After intracellular de-esterification, the active form of ezatiostat binds to and inhibits GST P1-1, thereby restoring Jun kinase and MAPK pathway activities and promoting MAPK-mediated cellular proliferation and differentiation pathways. This agent promotes the proliferation and maturation of hematopoietic precursor cells, granulocytes, monocytes, erythrocytes and platelets. Check for active clinical trials using this agent. (NCI Thesaurus)
ezetimibe: An azetidinone derivative and a cholesterol absorption inhibitor with lipid-lowering activity. Ezetimibe appears to interact physically with cholesterol transporters at the brush border of the small intestine and inhibits the intestinal absorption of cholesterol and related phytosterols. As a result, ezetimibe causes a decrease in the level of blood cholesterol or an increase in the clearance of cholesterol from the bloodstream. Overall, the following effects observed are a reduction of hepatic cholesterol stores and a reduction of total cholesterol, LDL cholesterol, and other triglycerides in the blood. Check for active clinical trials using this agent. (NCI Thesaurus)
ezetimibe/simvastatin: An orally bioavailable combination agent containing the cholesterol absorption inhibitor ezetimibe and the hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase inhibitor simvastatin, with lipid-lowering activity. Upon oral administration, ezetimibe binds to the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1) at the brush border of the small intestine and inhibits the intestinal absorption of biliary and dietary cholesterol and related phytosterols. This decreases blood cholesterol levels, decreases the delivery of intestinal cholesterol to the liver, reduces hepatic cholesterol stores and enhances the clearance of cholesterol from the bloodstream. Upon administration of simvastatin and subsequent hydrolyzation to its active beta-hydroxyacid form, this statin competitively inhibits HMG-CoA reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, which is an essential step in cholesterol synthesis. Ezetimibe and simvastatin together reduce blood levels of total cholesterol, low-density lipoprotein cholesterol (LDL-C), triglycerides (TGs), very-low-density lipoproteins (VLDL), and apolipoprotein B (Apo B), and increase the plasma concentration of high-density lipoprotein cholesterol (HDL-C). Higher cholesterol blood levels appear to be associated with an increased risk in the proliferation of certain cancer cells, such as prostate cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)
EZH1/2 inhibitor DS-3201: An orally available selective inhibitor of the histone lysine methyltransferases enhancer of zeste homolog 1 (EZH1) and 2 (EZH2), with potential antineoplastic activity. Upon oral administration, DS-3201 selectively inhibits the activity of both wild-type and mutated forms of EZH1 and EZH2. Inhibition of EZH1/2 specifically prevents the methylation of lysine 27 on histone H3 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways, enhances transcription of certain target genes, and results in decreased proliferation of EZH1/2-expressing cancer cells. EZH1/2, histone lysine methyltransferase (HMT) class enzymes and catalytic subunits of the polycomb repressive complex 2 (PRC2), are overexpressed or mutated in a variety of cancer cells and play key roles in tumor cell proliferation, progression, stem cell self-renewal and migration. Check for active clinical trials using this agent. (NCI Thesaurus)
EZH2 inhibitor CPI-1205: An orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity. Upon oral administration, CPI-1205 selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells. EZH2, a histone lysine methyltransferase (HMT) class enzyme and the catalytic subunit of the polycomb repressive complex 2 (PRC2), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation; its expression is correlated with tumor initiation, progression, stem cell self-renewal, migration and angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)