Trastuzumab emtansine: determining its role in management of HER2+ breast cancer

Future Oncol. 2018 Mar;14(7):589-602. doi: 10.2217/fon-2017-0477. Epub 2017 Dec 7.

Abstract

Trastuzumab emtansine is an antibody-drug conjugate comprised of the anti-HER2 monoclonal antibody trastuzumab linked to DM1 (emtansine), a potent cytotoxic maytansinoid derivative, by a stable linker. This structure results in improved tumor-directed cytotoxicity in HER2+ breast cancer with reduced systemic toxicities, particularly the cardiac toxicities associated with single agent trastuzumab. Phase III trials have demonstrated improved progression-free and overall survival in heavily pretreated patients with advanced HER2+ breast cancer, with an acceptable toxicity profile. However, its role in first-line treatment is less clear. Ongoing studies continue to evaluate its role in neoadjuvant and adjuvant management of HER2+ breast cancer.

Keywords: HER2; T-DM1; antibody–drug conjugate; breast cancer; lapatinib; pertuzumab; trastuzumab; trastuzumab emtansine.

MeSH terms

  • Ado-Trastuzumab Emtansine
  • Antibodies, Monoclonal, Humanized / chemistry
  • Antibodies, Monoclonal, Humanized / therapeutic use*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / pathology
  • Cell Proliferation / drug effects
  • Clinical Trials as Topic
  • Disease-Free Survival
  • Female
  • Humans
  • Immunoconjugates / chemistry
  • Immunoconjugates / therapeutic use*
  • Maytansine / analogs & derivatives*
  • Maytansine / chemistry
  • Maytansine / therapeutic use
  • Receptor, ErbB-2 / genetics
  • Trastuzumab / chemistry
  • Trastuzumab / therapeutic use*

Substances

  • Antibodies, Monoclonal, Humanized
  • Immunoconjugates
  • Maytansine
  • ERBB2 protein, human
  • Receptor, ErbB-2
  • Trastuzumab
  • Ado-Trastuzumab Emtansine