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Camptothecins

A Review of Their Chemotherapeutic Potential

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Abstract

Camptothecin analogues and derivatives appear to exert their antitumour activity by binding to topoisomerase I and have shown significant activity against a broad range of tumours. In general, camptothecins are not substrates for either the multidrug-resistance P-glycoprotein or the multidrug-resistance-associated protein (MRP). Because of manageable toxicity and encouraging activity against solid tumours, camptothecins offer promise in the clinical management of human tumours. This review illustrates the proposed mechanism(s) of action of camptothecins and presents a concise overview of current camptothecin therapy, including irinotecan and topotecan, and novel analogues undergoing clinical trails, such as exatecan (DX-8951f), IDEC-132 (9-aminocamptothecin), rubitecan (9-nitrocamptothecin), lurtotecan (GI-147211C), and the recently developed homocamptothecins diflomotecan (BN-80915) and BN-80927.

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Acknowledgements

This work was funded, in part, by grants from the Pharmacia-Upjohn Ohio State University Research Collaboration Program to PWS, and the Ohio State University Comprehensive Cancer Center grant (CA16058). The authors have no conflicts of interest that are directly relevant to the content of this manuscript.

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  1. Division of Pharmaceutics, College of Pharmacy, The Ohio State University, 238 Parks Hall, 500 West 12th Avenue, Columbus, Ohio, 43210-1291, USA

    Hulya Ulukan &  Peter W. Swaan

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  1. Hulya Ulukan
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Ulukan, H., Swaan, P.W. Camptothecins. Drugs 62, 2039–2057 (2002). https://doi.org/10.2165/00003495-200262140-00004

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