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.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology
  • Camptothecin / analogs & derivatives*
  • Camptothecin / pharmacokinetics
  • Camptothecin / pharmacology*
  • Glucuronidase / metabolism
  • Glucuronides / chemical synthesis*
  • Glucuronides / pharmacokinetics
  • Glucuronides / pharmacology*
  • HT29 Cells
  • Humans
  • Inhibitory Concentration 50
  • Irinotecan
  • Prodrugs / chemical synthesis*
  • Prodrugs / pharmacokinetics
  • Prodrugs / pharmacology*

Substances

  • Antineoplastic Agents
  • Glucuronides
  • Prodrugs
  • Irinotecan
  • Glucuronidase
  • Camptothecin