Irinotecan topoisomerase 1 inhibitor
Irinotecan is a topoisomerase inhibitor —it blocks the topoisomerase I enzyme, resulting in DNA damage and cell death. ... The molecular action of irinotecan occurs by trapping a subset of topoisomerase-1-DNA cleavage complexes, those with a guanine +1 in the DNA sequence. See more Irinotecan, sold under the brand name Camptosar among others, is a medication used to treat colon cancer, and small cell lung cancer. For colon cancer it is used either alone or with fluorouracil. For small cell lung cancer it is … See more Its main use is in colon cancer, in particular, in combination with other chemotherapy agents. This includes the regimen See more Camptothecin, one of the four major structural classifications of plant-derived anti-cancerous compounds, is a cytotoxic alkaloid which … See more Irinotecan is converted by an enzyme into its active metabolite SN-38, which is in turn inactivated by the enzyme UGT1A1 by glucuronidation. See more The most significant adverse effects of irinotecan include diarrhea, nausea and vomiting, neutropenia and fever, infections of blood or lungs (sepsis, pneumonia), shock, dehydration, kidney failure and thrombocytopenia (low levels of blood platelets). See more Administration Irinotecan can be administrated by 30- or 90-minute intravenous infusions of either 125 mg/m weekly for four of every six weeks or 350 mg/m … See more Irinotecan received accelerated approval from the U.S. Food and Drug Administration (FDA) in 1996, and full approval in 1998. Names See more WebAn anthracycline topoisomerase II inhibitor used as an adjuvant to treating axillary node metastases in patients who have undergone surgical resection of primary breast cancer. ... Irinotecan: DNA topoisomerase 1: target: Irinotecan: Cytochrome P450 3A4: enzyme: Irinotecan: Cytochrome P450 3A5: enzyme: Irinotecan: UDP-glucuronosyltransferase 1 ...
Irinotecan topoisomerase 1 inhibitor
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WebIrinotecan was applied every fourth week at a dose of 50 mg/m2 for four cycles followed by 100 mg/m2 for another eight cycles. Renal function and anti-double-stranded DNA antibodies as well as… Mehr anzeigen Objective: To evaluate the safety and effects of irinotecan, an inhibitor of topoisomerase I, on refractory lupus nephritis. WebIrinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. Features Irinotecan is a prodrug that …
WebNov 4, 2024 · Irinotecan is a topoisomerase I inhibitor used to treat several solid tumor types, especially in combination with other chemotherapeutic agents in the treatment of colorectal cancer. Irinotecan combined with 5-fluorouracil (5FU) is widely used in the treatment of colorectal cancer. [ 1] Inhibition of topoisomerase I by irinotecan and its … WebIrinotecan hydrochloride injection is an antineoplastic agent of the topoisomerase I inhibitor class. Irinotecan hydrochloride injection is supplied as a sterile, pale yellow, clear, aqueous solution. Each milliliter of solution contains 20 mg of irinotecan hydrochloride (on the basis of the trihydrate salt), 45 mg of sorbitol, NF, and 0.9 mg ...
WebThe anticancer agent, irinotecan, is a prodrug that is converted by tissue carboxylesterase to 7-ethyl-10-hydroxycamptothecin (SN-38), a potent inhibitor of DNA topoisomerase I. Its action is terminated by glucuronidation by UDP glucuronosyl transferase. Safety Information Pictograms GHS07 Signal Word Warning Hazard Statements H302 WebThis medication is classified as a "topoisomerase 1 inhibitor." (For more detail, see "How this drug works" section below). What Topotecan Is Used For: This medicine is used to treat cancer of the ovaries when other treatments have failed. Topotecan may also be used in certain types of lung cancer (small cell lung cancer). ...
WebIrinotecan is a water soluble topoisomerase I inhibitor with antitumor activity.In Vitro:Irinotecan is a topoisomerase I inhibitor. Irinotecan inhibits the growth of LoVo and HT-29 cells, with IC50s of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and induces similar amounts of cleavable complexes in both in LoVo and HT-29 cells [2].
WebAug 17, 2024 · BAY 1895344 Plus Topoisomerase-1 (Top1) Inhibitors in Patients With Advanced Solid Tumors, Phase I Studies With Expansion Cohorts in Small Cell Lung … toyota fyshwick service centreWebTopoisomerase I Inhibitors Name Topoisomerase I Inhibitors Accession Number DBCAT001116 Description Compounds that inhibit the activity of DNA TOPOISOMERASE I. Drugs Drugs & Drug Targets toyota g2 filterWebA. Alfirevic, M. Pirmohamed, in Medical and Health Genomics, 2016 Topoisomerase I Inhibitors. Irinotecan, used in colorectal cancer, is bioactivated into SN-38 by carboxyesterases 1 and 2 and then bioinactivated by glucuronidation via uridine diphosphate glucuronosyltransferase isoform 1A1 (UGT1A1).The variable number of tandem repeat … toyota g48 coolantWebJan 29, 2024 · Chemotherapy drugs, such as irinotecan liposome and topotecan, work in different ways to stop the growth of tumor cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading. ... (BAY 1895344) plus topoisomerase 1 (top1) inhibitor (liposomal irinotecan [irinotecan liposome] [nal-IRI] or topotecan ... toyota g57 transmissionWebMar 21, 2024 · Irinotecan, a prodrug of 7-ethyl 10-hydroxycamptothecin (SN38), is an antineoplastic agent of the topoisomerase (Top1) inhibitor class that is widely used to treat colorectal and other gastrointestinal cancers. The pharmacokinetics and metabolism of irinotecan and SN38 in humans are well described in the literature [ 1, 2, 3, 4, 5 ]. toyota g86 convertibleWebFeb 16, 2024 · Irinotecan liposome injection is a topoisomerase 1 inhibitor encapsulated in a lipid bilayer vesicle or liposome. Topoisomerase 1 relieves torsionalstrain in DNA by inducing single-strand breaks. … toyota g92c030020WebTopoisomerase inhibitors block the ligation step of the cell cycle, which generates DNA single- and double-strand breaks, leading to apoptotic cell death. Topoisomerase I … toyota g52 transmission parts diagram