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Prodrugs pp 1269-1279 | Cite as

Case Study: Irinotecan (CPT-11), A Water-soluble Prodrug of SN-38

  • M. J. Hageman
  • W. Morozowich
Part of the Biotechnology: Pharmaceutical Aspects book series (PHARMASP, volume V)

Abstract

Irinotecan (CPT-11) is a potent anticancer agent approved for use in the treatment of advanced colorectal cancer, as either a first-line therapy in combination with 5-fluorouracil or in the treatment of 5-flurouracil refractory cases (Sawada et al., 1995; Saltz, 1997). Irinotecan is a prodrug designed to deliver the poorly soluble parent molecule SN-38, an analog of a highly potent plant alkaloid camptothecin (CPT). Camptothecin and its analogs inhibit the nuclear enzyme topoisomerase I, inhibiting replication and demonstrating antitumor activity as an S-phase-specific drug (Garcia-Carbonero and Supko, 2002). The structure and enzymatic bioconversion of CPT-11 to SN-38 is shown in Scheme 1.

Keywords

Lactone Form Carboxylate Form Camptothecin Derivative Limited Sampling Model Irinotecan Hydrochloride 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  • M. J. Hageman
    • 1
  • W. Morozowich
    • 1
  1. 1.Pfizer Inc.Kalamazoo

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