Irinotecan is a strong anticancer drug whose mechanism of action has been reported only for the inhibition of DNA topoisomerase I (Topo I) through its active metabolite SN-38. In this study, we present a new mechanism of Irinotecan which inhibits the activities of MDM2, an E3 ligase of ...
irinotecan is used adjunctively with other therapeutic agents against colorectal cancer as a first- or second-line treatment. This activity reviews the indications, action, and contraindications for irinotecan as a valuable
Based on animal data and the mechanism of action, can cause fetal harm when administered to pregnant women Advise women of reproductive potential to use effective contraception during treatment and for 1 month after the final dose Contraception Females: Advise women of reproductive potential to use e...
Based on its mechanism of action and findings in animals, Irinotecan Hydrochloride Injection, USP can cause fetal harm when administered to a pregnant woman. In animal studies, intravenous administration of irinotecan during the period of organogenesis resulted in embryofetal mortality and teratogenicity ...
Figure 1.Depicted are the steps involved in the activation and metabolism of irinotecan, as well as its mechanism of action. Numerals reflect areas in which enhancement (+) or interference (–) with irinotecan action and toxicity have been reported: 1, phenytoin and carbamazepine (–); 2, car...
Mechanism of Action Binds to topoisomerase I to produce double-strand breaks in DNA Pharmacokinetics Half-Life: 6-12 hr; SN-38 10-20 hr Pleak Plasma Concentration: 1660 ng/mL; SN-38 26.3 ng/mL Protein Bound: 30-68%; SN-38 95% ...
Irinotecan (Fig. 1), also known as CPT-11, is a semisynthetic derivative of 20(S)camptothecin ( 1 ), a pentacyclic alkaloid first identified in extracts of the Chinese shrub Camptotheca acuminata . The mechanism of action of camptothecin has been covered in other chapters of this book and ...
CPT-11 (irinotecan) in the treatment of colorectal cancer: a new mechanism of action for additional activity.Tumori. 1997 Jan-Feb;83(1 Suppl):S85-6. Reviewdoi:10.1177/03008916970831s137Harry Bleiberg... H Bleiberg - 《Tumori》 被引量: 1发表: 1997年 Irinotecan is an active agent in untrea...
Thus, any active agent with a new mechanism of action deserves further investigation. Irinotecan (CPT-11, Camptos) is an S-phase-specific, semisyn- thetic derivative of camptothecin which interferes with DNA replication and cell division through its potent interaction with the enzyme topoisomerase ...
CPT-11 (irinotecan) is a promising new agent for the treatment of colorectal cancer with a unique mechanism of action. CPT-11 is a DNA topoisomerase I inhibitor, which has not demonstrated susceptibility to the P-glycoprotein-mediated multidrug-resistant phenotype. Phase II studies with CPT-11 ...