, Volume 42, Issue 1 Supplement, pp S31-S43

Clinical pharmacology of camptothecins

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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

Work presented at the 13th Bristol-Myers Squibb Nagoya International Cancer Treatment Symposium, “Strategic Cross Talk between Major Oncology Groups/Clinical Pharmacology in Cancer Chemotherapy,” 17–18 October 1997, Nagoya, Japan