Cancer Chemotherapy and Pharmacology

, Volume 42, Supplement 1, pp S31–S43

Clinical pharmacology of camptothecins



Camptothecins (CPTs) are a unique class of chemotherapeutic agent which inhibit DNA synthesis by inhibiting topoisomerase I activity. Structure-activity studies on the original CPT alkaloid led to the development of the new analogues irinotecan (CPT-11), topotecan, and 9-aminocamptothecin, which have improved water solubility and lower toxicity. CPT analogues exhibit interesting pharmacokinetic/pharmacodynamic and metabolic properties that are of major research and clinical interest. This review describes the clinical pharmacology of these 3 CPT analogues. Specific areas such as absorption after extra-vascular administration, pharmacokinetic/pharmacodynamic variability, metabolism, and administration in special populations are discussed. Key words Camptothecins • Irinotecan • Topotecan • 9-Aminocamptothecin • Clinical pharmacology

Copyright information

© Springer-Verlag 1998

Authors and Affiliations

  1. 1.Committee on Clinical PharmacologyUniversity of ChicagoChicagoUSA
  2. 2.Department of Medicine and Cancer Research CenterUniversity of ChicagoChicagoUSA
  3. 3.University of ChicagoChicagoUSA

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