Irinotecan (136572-09-3) is a semi-synthetic derivative of camptothecin (Cat.# 10-1041) that is an FDA approved anticancer drug. It is a prodrug that is converted by tissue esterases to 7-ethyl-10-hydroxycamptothecin (SN-38, Cat.# 10-2425), a potent inhibitor of DNA topoisomerase I.1,2 Although irinotecan is also a topoisomerase inhibitor, SN-38 is approximately 1000 times as potent in purified enzyme studies. In vitro cytotoxicity assays show much greater variability in potency between the two (2-2000 fold).3
Irinotecan Hydrochloride Trihydrate is a DNA topoisomerase inhibitor.
ChEBI: A hydrate that is the trihydrate form of irinotecan hydrochloride. Onivyde is used in combination with fluorouracil and leucovorin, for the treatment of patients with metastatic adenocarcinoma of the pancreas after disease progression following gemcitabine
based therapy. It is converted via hydrolysis of the carbamate linkage to its active metabolite, SN-38, which is ~1000 times more active.
Camptosar (Pharmacia &Upjohn)
.
Moderately toxic by ingestion.
1) Kunimoto et al. (1987) Antitumor activity of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxy-camptothecin, a novel water-soluble derivative of camptothecin against murine tumors; Cancer Res., 47 5944
2) Mathijssen et al., (2002) Pharmacology of topoisomerase I inhibitors irinotecan (CPT-11) and topotecan; Curr. Cancer Drug Targets, 253 5892
3) Pfizer drug insert
