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Novel tubulin-targeting agents: anticancer activity and pharmacologic profile of epothilones and related analogues

P Fumoleau1, B Coudert, N Isambert

  • 1Medical Oncology Department, Centre Georges-François Leclerc, Dijon, France. pfumoleau@dijon.fnclcc.fr

Annals of Oncology : Official Journal of the European Society for Medical Oncology
|October 13, 2007
PubMed
Abstract

Insights

Epothilones show potent anticancer activity against drug-resistant tumors. These macrolides are well-tolerated and effective in various cancers, offering a promising alternative to taxanes.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Epothilones are macrolide compounds with antimicrotubule activity.
  • They exhibit potent antiproliferative effects against multidrug-resistant and paclitaxel-resistant cancer cell lines.

Purpose of the Study:

  • To review preclinical and clinical data on epothilone derivatives.
  • To evaluate their efficacy and toxicity in cancer treatment.

Main Methods:

  • Searched PubMed and ASCO proceedings (2000-2006) for studies on epothilone B, D, and their derivatives.
  • Focused on preclinical and Phase I clinical trial data.

Main Results:

  • Epothilones have linear pharmacokinetics, are well-tolerated, and show antitumor activity.
  • Toxicity profiles vary: diarrhea for patupilone, neurotoxicity/neutropenia for others.
  • Partial responses seen in taxane-pretreated breast cancer patients with patupilone and ixabepilone.

Conclusions:

  • Epothilones demonstrate significant antitumor activity in taxane-sensitive and -refractory tumors.
  • They offer a favorable side-effect profile at effective doses and schedules.

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