irinotecan

Irinotecan is a water-soluble analogue of camptothecin and functions as a topoisomerase I inhibitor used primarily in chemotherapy. It is indicated for the treatment of metastatic carcinoma of the colon or rectum and pancreatic adenocarcinoma, and is also sometimes used for small cell lung cancer. Irinotecan acts as a prodrug that is converted in the liver to its active metabolite SN-38 by carboxylesterase enzymes. Both irinotecan and SN-38 inhibit DNA topoisomerase I by stabilizing the complex between topoisomerase I and DNA, preventing religation of single-strand breaks during DNA replication. This leads to replication arrest, double-stranded DNA breaks, and ultimately apoptosis in rapidly dividing cells. The drug was first approved in Japan in 1994 and by the FDA in 1996[1][2][5][6]. **Developers:** Yakult Honsha **Manufacturers:** Pfizer, Ipsen Biopharm

Brand names

CamptosarOnivyde

Other names

irinotecan hydrochlorideCPT-11CPT11CPT 11