Targeting HER2-AXL heterodimerization to overcome resistance to HER2 blockade in breast cancer

Sci Adv. 2022 May 20;8(20):eabk2746. doi: 10.1126/sciadv.abk2746. Epub 2022 May 20.

Abstract

Anti-HER2 therapies have markedly improved prognosis of HER2-positive breast cancer. However, different mechanisms play a role in treatment resistance. Here, we identified AXL overexpression as an essential mechanism of trastuzumab resistance. AXL orchestrates epithelial-to-mesenchymal transition and heterodimerizes with HER2, leading to activation of PI3K/AKT and MAPK pathways in a ligand-independent manner. Genetic depletion and pharmacological inhibition of AXL restored trastuzumab response in vitro and in vivo. AXL inhibitor plus trastuzumab achieved complete regression in trastuzumab-resistant patient-derived xenograft models. Moreover, AXL expression in HER2-positive primary tumors was able to predict prognosis. Data from the PAMELA trial showed a change in AXL expression during neoadjuvant dual HER2 blockade, supporting its role in resistance. Therefore, our study highlights the importance of targeting AXL in combination with anti-HER2 drugs across HER2-amplified breast cancer patients with high AXL expression. Furthermore, it unveils the potential value of AXL as a druggable prognostic biomarker in HER2-positive breast cancer.

MeSH terms

  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / genetics
  • Breast Neoplasms* / pathology
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm / genetics
  • Female
  • Humans
  • Phosphatidylinositol 3-Kinases / metabolism
  • Receptor, ErbB-2 / genetics
  • Trastuzumab / pharmacology
  • Trastuzumab / therapeutic use

Substances

  • Receptor, ErbB-2
  • Trastuzumab