2007•Birkhäuser Basel eBooksRequires access
Topoisomerase inhibitors
Hans Gelderblom, Alex Sparreboom
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Abstract
DNA topoisomerase inhibitors, known for their broad antitumour activity, represent one of the most widely used groups of anticancer agents. In spite of the early discovery and long-standing clinical use, the mechanism of action of these agents was not recognized until the 1980s [, , ].Currently agents available for clinical use include the topoisomerase I inhibitors of the camptothecin class (topotecan and irinotecan) and the topoisomerase II inhibitors in the class of epipodophyllotoxins (etoposide and teniposide). Many new formulations and structurally-related agents are currently undergoing clinical development. This chapter highlights the most important aspects of the past, current and future development of topoisomerase I and II inhibitors, and provides an overview of pharmacology and clinical data, with a focus on recent developments.