lrinotecan hydrochloride, a semi-synthetic, water soluble derivative of the potent anticancer agent camptothecin, was launched in Japan for the treatment of lung, ovarian, and cervical cancers. lrinotecan exerts its antitumor activity via inhibition of topoisomerase I, a cellular enzyme that is involved in maintaining the topographic structure of DNA during the process of translation, transcription, and mitosis. lrinotecan undergoes de-esterification in vivo to yield an active metabolite, SN-38, which is 1000-fold more potent than the parent. Although being much less toxic than camptothecin, a significant number of patients in clinical trials exhibited side effects of leukopenia, diarrhea, nauseahromiting, and alopecia. Combination therapy of irinotecan with another widely used anticancer agent, cisplatin, has been reported to be superior to either agent alone. lrinotecan is in clinical trials for gastrointestinal, breast, skin, colorectal, pancreatic cancers, mesothelioma and non-Hodgkin’s lymphoma.

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