- 産業: Government; Health care
- Number of terms: 6957
- Number of blossaries: 0
- Company Profile:
The National Cancer Institute (NCI) is part of the National Institutes of Health (NIH), which is one of 11 agencies that compose the Department of Health and Human Services (HHS). The NCI, established under the National Cancer Institute Act of 1937, is the Federal Government's principal agency for ...
The sodium salt of imetelstat, a synthetic lipid-conjugated, 13-mer oligonucleotide N3' P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase RNA (hTR), imetelstat acts as a competitive enzyme inhibitor that binds and blocks the active site of the enzyme (a "telomerase template antagonist"), a mechanism of action which differs from that for the antisense oligonucleotide-mediated inhibition of telomerase activity through telomerase mRNA binding. Inhibition of telomerase activity in tumor cells by imetelstat results in telomere shortening, which leads to cell cycle arrest or apoptosis.
Industry:Pharmaceutical
The sodium salt of glycididazole with potential radiosensitizing activity. Due to its low redox potential, glycididazole is selectively activated via bioreduction in hypoxic tumor cells and may sensitize hypoxic tumor cells to the cytotoxic effects of ionizing radiation.
Industry:Pharmaceutical
The sodium salt of dichloroacetic acid with potential antineoplastic activity. Dichloroacetate ion inhibits pyruvate dehydrogenase kinase, resulting in the inhibition of glycolysis and a decrease in lactate production. This agent may stimulate apoptosis in cancer cells by restoring normal mitochondrial-induced apoptotic signaling.
Industry:Pharmaceutical
The sodium salt of bemiparin, a second generation, synthetic, low-molecular-weight heparin (LMWH) with anticoagulant activity. Derived, after depolymerisation and fractionation, from medical-grade porcine unfractionated heparin (UFH), bemiparin has an average molecular weight of 3,600 daltons and has a higher anti-factor Xa/anti-factor IIa ratio (8:1) than first-generation LMWHs. This anticoagulant binds to antithrombin III, thereby enhancing the inactivation of activated Factor X (Factor Xa) and, to a lesser extent, activated factor II (Factor IIa). Compared to unfractionated heparins, the use of bemiparin is associated with lower incidences of major bleeding, osteoporosis, and heparin-induced thrombocytopenia. Bemiparin also promotes a greater release of tissue factor pathway inhibitor than UFH or dalteparin.
Industry:Pharmaceutical
The sodium salt form of tasisulam, an acyl-sulfonamide compound with potential antiproliferative activity. Tasisulam activates, through an as of yet not fully elucidated mechanism, the intrinsic mitochondrial-mediated cell death pathway as manifested by decreased adenosine triphosphate (ATP), cytochrome C release, activation of caspases, loss of mitochondrial membrane potential, production of reactive oxygen species (ROS) and eventually apoptosis.
Industry:Pharmaceutical
The sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+/K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.
Industry:Pharmaceutical
The R-isomer of a synthetic quinoxaline phenoxypropionic acid derivative with proapoptotic and antiproliferative activities. R(+)XK469 selectively inhibits topoisomerase II-beta, blocks activation of MEK/MAPK signaling kinases, stimulates caspases, and upregulates p53-dependent proteins, including cyclins A and B1, thereby arresting cancer cells in the G2/M phase of the cell cycle. Both R(+) and S(-) isomers of this agent are cytotoxic, although the R-isomer is more potent.
Industry:Pharmaceutical
The R-enantiomer of the calcium channel blocker verapamil. Dexverapamil competitively inhibits the multidrug resistance efflux pump P-glycoprotein (MDR-1), thereby potentially increasing the effectiveness of a wide range of antineoplastic drugs which are inactivated by MDR-1 mechanisms. This agent exhibits decreased calcium antagonistic activity and toxicity compared to racemic verapamil.
Industry:Pharmaceutical
The recombinant form of human antihemophilic factor (AH) (Factor VIII) with coagulation promoting activity. Antihemophilic factor binds to factor IXa in the coagulation cascade along with calcium and phospholipid. This complex converts factor X to the activated form, factor Xa. In turn, factor Xa/Va complex activates thrombin, which cleaves fibrinogen into fibrin, eventually resulting in blood clot formation.
Industry:Pharmaceutical
The racemic form of a synthetic quinoxaline phenoxypropionic acid derivative with antineoplastic properties. XK469R selectively inhibits topoisomerase II by stabilizing the enzyme-DNA intermediates in which topoisomerase subunits are covalently linked to DNA through 5-phosphotyrosyl linkages, thereby interfering with DNA repair and replication, RNA and protein synthesis. This agent possesses unusual solid tumor selectivity and activity against multidrug-resistant cancer cells. XK469R is more water soluble and active than the pure isomers, R(+)XK469 and S(-)XK469.
Industry:Pharmaceutical
