Purpose. The primary objective of this article is to discuss the pharmacology, pharmacokinetics, clin ical use, and adverse effects of the approved topoisomerase I inhibitors. This is the first in a series of two articles and will focus on topotecan.
Data Sources. We reviewed the literature through a MEDLINE search of English language articles from 1985 through 1997. 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, topotecan, topo isomerase I, Hycamtin, SKF 104864.
Data Extraction. We reviewed the current literature in order to discuss the pharmacology, pharmacokinetics, clinical use, toxicity, drug inter actions, indications, formulation, dosage and ad ministration, and pharmaceutical issues surround ing the use of topotecan.
Data Synthesis. The topoisomerase I inhibi tors are new antineoplastic agents with a unique mechanism of action. Promising areas of applica tion include ovarian cancer, lung cancer, radiation sensitization, and refractory leukemias. Clinical tri als detailing its activity in these areas are pre sented.
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