Pharmacy World and Science

, Volume 20, Issue 4, pp 161–172 | Cite as

Clinical pharmacokinetics of camptothecin topoisomerase I inhibitors.

  • Virginie M.M. Herben
  • Jos H. Beijnen
  • Wim W. ten Bokkel Huinink
  • Jan H.M. Schellens


In this review the clinical pharmacokinetics of camptothecin topoisomerase I inhibitors, an important new class of anticancer drugs, is discussed. Two prototypes, topotecan and irinotecan, are currently marketed in many European countries and the USA for the treatment of patients with ovarian and colorectal cancer, respectively. Other camptothecin derivatives, including lurtotecan, 9‐aminocamptothecin (9‐AC) and 9‐nitrocamptothecin (9‐NC), are at different stages of clinical development. The common property of camptothecin analogues is their action against DNA topoisomerase I, but beyond this similarity the compounds differ widely in terms of antitumour efficacy, pharmacology, pharmacokinetics and metabolism. We review chemistry, mechanism of action, stability and bioanalysis of the camptothecins. Dosage and administration, status of clinical application, pharmacokinetics, pharmacodynamics and drug interactions are discussed.

Camptothecin Clinical pharmacokinetics Irinotecan Topoisomerase I inhibitors Topotecan 


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Copyright information

© Kluwer Academic Publishers 1998

Authors and Affiliations

  • Virginie M.M. Herben
    • 1
  • Jos H. Beijnen
    • 1
  • Wim W. ten Bokkel Huinink
    • 2
  • Jan H.M. Schellens
    • 2
  1. 1.Department of Pharmacy and PharmacologyThe Netherlands Cancer Institute/Slotervaart HospitalAmsterdamThe Netherlands
  2. 2.Department of Medical OncologyThe Netherlands Cancer Institute/Antoni van LeeuwenhoekhuisAmsterdamThe Netherlands

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