Annals of the New York Academy of Sciences
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CPT-11 is a derivative of camptothecin, which has a broad spectrum of antitumor activity, both in vitro and in vivo. Like camptothecin, CPT-11 is a selective inhibitor of the DNA enzyme topoisomerase I. Phase I trials were conducted in Europe with the aim of determining the recommended CPT-11 dose and schedule for evaluation in phase II trials. ⋯ To date, CPT-11 has showed remarkable efficacy in colorectal cancer, even in patients resistant to 5-FU. Interesting results have also been obtained in pancreatic, cervical and lung cancer. Future trials will make it possible to assess whether there is a place for CPT-11 in combination with other cytotoxic agents or radiotherapy.