Pharmacology of intraperitoneal CPT-11.

CPT-11 is clearly one of the most important new anticancer drugs developed in the last few decades, and CPT-11 combined with 5-fluorouracil (5-FU) and leucovorin is considered as reference first-line chemotherapy in the treatment of metastatic colorectal cancer. CPT-11 has a complex pharmacologic profile in vivo, and it needs caboxylesterase-mediated biotransformation to SN-38 before production of its cytotoxic effect. Intraperitoneal administration of CPT-11 has been studied recently in murine models and presented some potential advantage over the intravenous (i.