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Camptothecins in Cancer Therapy pp 127–151Cite as

Preclinical Models for Evaluating Topoisomerase I-Targeted Drugs

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Part of the book series: Cancer Drug Discovery and Development ((CDD&D))

Abstract

Type I and II DNA topoisomerases are the targets for numerous clinically efficacious antitumor agents. Over the last decade, considerable effort has been expended in developing camptothecin (CPT) derivatives that selectively target DNA topoisomerase I (TOP-I) (1). The prodrug irinotecan (CPT-11) is approved for treatment of colon carcinoma and has demonstrated significant activity against numerous other cancers in adults and children. Topotecan is approved for treatment of platinum- or taxane-resistant ovarian carcinoma and has demonstrated broad-spectrum activity (2). Other analogs are in clinical development, such as D5198f and the homocamptothecins and liposomal formulations of CPT derivatives, and offer the potential for prolonged plasma exposures.

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Author information

Authors and Affiliations

  1. Department of Molecular Pharmacology, St. Jude Children’s Research Hospital, Memphis, TN

    Aarti S. Juvekar PhD & Peter J. Houghton PhD

  2. Cancer Research Institute, Parel, Bombay, India

    Aarti S. Juvekar PhD

  3. Department of Hematology/Oncology, St. Jude Children’s Research Hospital, Memphis, TN

    Joyce Thompson MD

  4. Department of Pharmaceutical Sciences, St. Jude Children’s Research Hospital, Memphis, TN

    Clinton F. Stewart PharmD

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  1. Aarti S. Juvekar PhD
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  2. Joyce Thompson MD
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  3. Clinton F. Stewart PharmD
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  4. Peter J. Houghton PhD
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Editor information

Editors and Affiliations

  1. Department of Pharmacy Practice and Science, College of Pharmacy, University of Kentucky, Lexington, KY

    Val R. Adams PharmD

  2. Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY

    Thomas G. Burke PhD

  3. Experimental Therapeutics Program, Lucille P. Markey Cancer Center, University of Kentucky Medical Center, University of Kentucky, Lexington, KY

    Thomas G. Burke PhD

  4. Tigen Pharmaceuticals Inc., Lexington, KY

    Thomas G. Burke PhD

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Juvekar, A.S., Thompson, J., Stewart, C.F., Houghton, P.J. (2005). Preclinical Models for Evaluating Topoisomerase I-Targeted Drugs. In: Adams, V.R., Burke, T.G. (eds) Camptothecins in Cancer Therapy. Cancer Drug Discovery and Development. Humana Press. https://doi.org/10.1385/1-59259-866-8:127

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  • DOI: https://doi.org/10.1385/1-59259-866-8:127

  • Publisher Name: Humana Press

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