Cancer chemotherapy: a SN-38 (7-ethyl-10-hydroxycamptothecin) glucuronide prodrug for treatment by a PMT (Prodrug MonoTherapy) strategy

  • Bioorg Med Chem Lett. 2003 Mar 10;13(5):947-50. doi: 10.1016/s0960-894x(02)01080-6.
Stéphane Angenault  1 ,  Sylvie Thirot ,  Frédéric Schmidt ,  Claude Monneret ,  Bruno Pfeiffer ,  Pierre Renard
Affiliations
  • 1. UMR176 CNRS/Institut Curie, 26, rue d'Ulm, 75248 Paris Cedex 05, France.
PMID: 12617927 DOI: 10.1016/s0960-894x(02)01080-6
Abstract

A glucuronide-based prodrug of SN-38 (7-ethyl-10-hydroxycamptothecin) has been synthesized for use in a Prodrug MonoTherapy Strategy (PMT). Since this prodrug is significantly less cytotoxic than SN-38 itself and efficiently releases the drug in vitro in the presence of beta-D-glucuronidase, it can be considered as an appropriate candidate for Cancer treatment by a PMT strategy.