Epothilones in development for non-small-cell lung cancer: Novel anti-tubulin agents with the potential to overcome taxane resistance

Martin J. Edelman, Marianna Shvartsbeyn

Research output: Contribution to journalReview articlepeer-review

23 Scopus citations

Abstract

Progress in the treatment of non-small-cell lung cancer (NSCLC) will require the introduction of new agents as well as better use of existing therapies. Targeted therapies are likely to have a profound effect on the treatment of NSCLC after identification of patients who are most likely to benefit. The epothilones are novel anti-tubulin agents derived from Sorangium cellulosum. β III tubulin overexpression has been implicated as a mechanism of anti-tubulin resistance that can be overcome by epothilones. Several epothilones have advanced to clinical trials; ixabepilone (BMS247550, aza-epothilone B, Bristol-Myers Squibb, New York, NY), patupilone (EPO906, Novartis, Basel, Switzerland) and sagopilone (ZK-EPO, ZK-219477, Schering AG, Berlin-Wedding, Germany) are currently in active development. Several of the epothilones, most notably ixabepilone, have demonstrated activity in lung cancer in phase I and II trials, including taxane-resistant patients. Although a phase II study failed to show superior outcome in patients with β III tubulin overexpression, other aspects of the epothilones argue for their continued development.

Original languageEnglish
Pages (from-to)171-180
Number of pages10
JournalClinical Lung Cancer
Volume13
Issue number3
DOIs
StatePublished - May 2012
Externally publishedYes

Keywords

  • Anti-tubulin agents
  • Epothilones
  • Lung cancer
  • Resistance
  • β-tubulin III

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