Pharmacokinetics of irinotecan and its metabolites in human blood, bile, and urine

Cancer Chemother Pharmacol. 1995;36(1):79-82. doi: 10.1007/BF00685737.


Two patients were treated with CPT-11 for colorectal cancer and had a percutaneous biliary catheter for extrahepatic biliary obstruction. The first patient was treated with CPT-11 according to the 100-mg/m2 weekly therapeutic schedule, and the second patient was treated every 3 weeks, with a dose of 350 mg/m2 being given at the first course, after which it was decreased to 300 mg/m2 for the following courses. In plasma, the active identified metabolite of CPT-11, SN-38, occurred mainly in the form of a glucuronide conjugate. CPT-11 was mainly excreted in bile and urine as CPT-11. The cumulative biliary and urinary excretion of CPT-11 and its metabolites (SN-38 and SN-38 glucuronide conjugate) over a period of up to 48 h ranged from 25% (100 mg/m2 weekly) to 50% (300 mg/m2 every 3 weeks). This means that CPT-11 can be excreted under other, not yet identified metabolite forms.

MeSH terms

  • Antineoplastic Agents, Phytogenic / metabolism
  • Antineoplastic Agents, Phytogenic / pharmacokinetics*
  • Bile / chemistry
  • Camptothecin / analogs & derivatives*
  • Camptothecin / blood
  • Camptothecin / metabolism
  • Camptothecin / pharmacokinetics
  • Camptothecin / urine
  • Chromatography, High Pressure Liquid
  • Colorectal Neoplasms / metabolism
  • Female
  • Half-Life
  • Humans
  • Infusions, Intravenous
  • Irinotecan
  • Male
  • Middle Aged


  • Antineoplastic Agents, Phytogenic
  • Irinotecan
  • Camptothecin