Purpose. The primary objective of this article is to discuss the pharmacology, pharmacokinetics, clinical use, and adverse effects of the approved topoisomer ase I inhibitors. This is the second in a series of two articles and will focus on irinotecan.
Data Sources. We reviewed the literature through a MEDLINE search of English language arti cles from 1985 through 1998. Relevant articles cited in the titles obtained from the MEDLINE search were also used. The following terms were used for purpose of conducting the MEDLINE search: topoisomerase inhibitors, irinotecan, topoisomerase I, camptosar, and CPT-11.
Data Extraction. We have reviewed the current literature to discuss the pharmacology, pharmacokinet ics, clinical use, toxicity, drug interactions, indications, formulation, dosage and administration, and pharmaceu tical issues surrounding the use of irinotecan.
Data Synthesis. The topoisomerase I inhibitors are new antineoplastic agents with a unique mechanism of action. Promising areas of application include colo rectal cancer, non-small-cell lung cancer, small-cell lung cancer, cervical cancer, and lymphomas. Clinical trials detailing the activity of topoisomerase I inhibitors in these areas are presented.
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