Irinotecan, a derivative of the alkaloid camptothecin (Cay-11694), functions as a prodrug that is converted by tissue carboxylesterase to 7-ethyl-10-hydroxycamptothecin, a potent inhibitor of DNA topoisomerase I. Its action is terminated by glucuronidation by UDP glucuronosyl transferase 1A1. Irinotecan demonstrates...

Soluble in DMSO at 100 mg/mL, very poorly soluble in ethanol, soluble in water at 25 mg/mL, buffers, serum or other additives may increase or decrease the aqueous solubility

Inhibitor of the nuclear enzyme topoisomerase I, which is involved in cellular DNA replication and transcription. During replication Topoisomerase I mediates the relaxation of super coiled DNA, and it's inhibition results in breakage of the DNA chain and likely induce apoptosis. Irinotecan is therefore an attractive...

Irinotecan (CPT-11) is a topoisomerase I inhibitor. It is a semisynthetic analog of the natural alkaloid camptothecin and has an active metabolite SN-38 (7-Ethyl-10-hydroxycamptothecin). During the S phase of the cell cycle, camptothecins selectively bind to and stabilize topoisomerase I-DNA complexes, inhibiting...