
SAN ANTONIO, Texas-Irinotecan is metabolized via CYP3A4 to the less active oxidative metabolites APC and NPC and is bioactivated in the liver and intestine by human carboxylesterases (hCE) to the topoisomerase I inhibitor SN-38 (Figure 1). The pharmacology of irinotecan (Camptosar, CPT-11), a water-soluble, semisynthetic derivative of camptothecin, was reviewed at the Vanderbilt University Symposium by John G. Kuhn, PharmD, of the Departments of Medicine and Pharmacology, University of Texas Health Science Center, San Antonio, and College of Pharmacy, University of Texas.

