A pharmacokinetic evaluation of topotecan as a cervical cancer therapy

Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):215-24. doi: 10.1517/17425255.2013.758249.

Abstract

Introduction: Topotecan was initially approved for the treatment of recurrent ovarian cancer. In cervical cancer, it has been investigated for its potential as part of systemic therapy for advanced and/or recurrent disease and in combination with cisplatin and radiation as a first-line treatment for advanced disease. As a topoisomerase I (topo I) inhibitor, its activity is predicted to be schedule-dependent and potentiated in a schedule-dependent manner by its interaction with DNA damaging agents.

Areas covered: The cytotoxicity of topotecan is believed to be due to double-stranded DNA damage produced when the DNA replication 'fork' on the opposing DNA strand is interrupted by the ternary complex formed by topotecan, topoisomerase I and DNA. This review focuses on: i) combination studies of cisplatin + topotecan both as neoadjuvant and with concomitant radiation; ii) adding this drug as a radiosensitizer in pilot studies for locally advanced disease and iii) topotecan as part of non-cisplatin combinations in metastatic disease.

Expert opinion: Cervical cancer continues to claim many victims among parts of the world where early detection and/or vaccination programs are not systemically applied. Topotecan is an attractive building block for improving therapy against advanced disease.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic / methods
  • Clinical Trials as Topic / trends
  • Drug Evaluation, Preclinical / methods
  • Drug Evaluation, Preclinical / trends
  • Female
  • Humans
  • Topoisomerase I Inhibitors / pharmacokinetics*
  • Topoisomerase I Inhibitors / therapeutic use
  • Topotecan / pharmacokinetics*
  • Topotecan / therapeutic use
  • Uterine Cervical Neoplasms / drug therapy*
  • Uterine Cervical Neoplasms / metabolism*

Substances

  • Topoisomerase I Inhibitors
  • Topotecan