Preexisting oncogenic events impact trastuzumab sensitivity in ERBB2-amplified gastroesophageal adenocarcinoma

J Clin Invest. 2014 Dec;124(12):5145-58. doi: 10.1172/JCI75200. Epub 2014 Nov 17.

Abstract

Patients with gastric and esophageal (GE) adenocarcinoma tumors in which the oncogene ERBB2 has been amplified are routinely treated with a combination of cytotoxic chemotherapy and the ERBB2-directed antibody trastuzumab; however, the addition of trastuzumab, even when tested in a selected biomarker-positive patient population, provides only modest survival gains. To investigate the potential reasons for the modest impact of ERBB2-directed therapies, we explored the hypothesis that secondary molecular features of ERBB2-amplified GE adenocarcinomas attenuate the impact of ERBB2 blockade. We analyzed genomic profiles of ERBB2-amplified GE adenocarcinomas and determined that the majority of ERBB2-amplified tumors harbor secondary oncogenic alterations that have the potential to be therapeutically targeted. These secondary events spanned genes involved in cell-cycle regulation as well as phosphatidylinositol-3 kinase and receptor tyrosine kinase signaling. Using ERBB2-amplified cell lines, we demonstrated that secondary oncogenic events could confer resistance to ERBB2-directed therapies. Moreover, this resistance could be overcome by targeting the secondary oncogene in conjunction with ERBB2-directed therapy. EGFR is commonly coamplified with ERBB2, and in the setting of ERBB2 amplification, higher EGFR expression appears to mark tumors with greater sensitivity to dual EGFR/ERBB2 kinase inhibitors. These data suggest that combination inhibitor strategies, guided by secondary events in ERBB2-amplified GE adenocarcinomas, should be evaluated in clinical trials.

Publication types

  • Clinical Trial
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma* / drug therapy
  • Adenocarcinoma* / enzymology
  • Adenocarcinoma* / genetics
  • Adenocarcinoma* / pathology
  • Antibodies, Monoclonal, Humanized / administration & dosage*
  • Antineoplastic Agents / administration & dosage*
  • Biomarkers, Tumor* / genetics
  • Biomarkers, Tumor* / metabolism
  • Drug Resistance, Neoplasm
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism
  • Esophageal Neoplasms* / diet therapy
  • Esophageal Neoplasms* / enzymology
  • Esophageal Neoplasms* / genetics
  • Esophageal Neoplasms* / pathology
  • Female
  • Gene Amplification* / drug effects
  • Gene Amplification* / genetics
  • Humans
  • Male
  • Phosphatidylinositol 3-Kinases / genetics
  • Phosphatidylinositol 3-Kinases / metabolism
  • Receptor, ErbB-2* / genetics
  • Receptor, ErbB-2* / metabolism
  • Stomach Neoplasms* / drug therapy
  • Stomach Neoplasms* / enzymology
  • Stomach Neoplasms* / genetics
  • Stomach Neoplasms* / pathology
  • Trastuzumab

Substances

  • Antibodies, Monoclonal, Humanized
  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Phosphatidylinositol 3-Kinases
  • EGFR protein, human
  • ERBB2 protein, human
  • ErbB Receptors
  • Receptor, ErbB-2
  • Trastuzumab