title: Clinical pharmacology of camptothecins.
abstract: 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 extravascular administration, pharmacokinetic/pharmacodynamic variability, metabolism, and administration in special populations are discussed.
authors.affiliation: Committee on Clinical Pharmacology, University of Chicago, IL 60637, USA.
authors.forename: L
authors.initials: L
authors.lastname: Iyer
authors.forename: M J
authors.initials: MJ
authors.lastname: Ratain
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000493:pharmacokinetics / Q000494:pharmacology*; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002166:Camptothecin