Pertuzumab protects the achilles' heel of trastuzumab--emtansine

Clin Cancer Res. 2014 Jan 15;20(2):278-80. doi: 10.1158/1078-0432.CCR-13-2626. Epub 2013 Nov 15.

Abstract

Trastuzumab emtansine (T-DM1) represents a significant advancement in the treatment of HER2(+) breast cancers. Its clinical efficacy however will be limited by the development of therapeutic resistance. In this report, the HER3 ligand neuregulin is shown to mediate T-DM1 resistance, which was overcome by administration of pertuzumab, a steric inhibitor of HER2 dimerization.

Publication types

  • Research Support, Non-U.S. Gov't
  • Comment

MeSH terms

  • Animals
  • Antibodies, Monoclonal, Humanized / therapeutic use*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism*
  • Female
  • Humans
  • Neuregulins / antagonists & inhibitors*
  • Receptor, ErbB-2 / antagonists & inhibitors*
  • Trastuzumab

Substances

  • Antibodies, Monoclonal, Humanized
  • Neuregulins
  • Receptor, ErbB-2
  • pertuzumab
  • Trastuzumab