Lapatinib enhances herceptin-mediated antibody-dependent cellular cytotoxicity by up-regulation of cell surface HER2 expression

Anticancer Res. 2011 Sep;31(9):2999-3005.

Abstract

Background: Although it was previously reported that lapatinib combined with Herceptin improved the progression-free survival rate compared with lapatinib alone for patients with Herceptin-refractory HER2-positive metastatic breast cancer, the mechanism is purported to be an antiproliferative effect relating to the synergism of these two agents.

Materials and methods: We evaluated how lapatinib interacts with Herceptin in HER2-positive breast cancer, with a particular focus on Herceptin-mediated antibody-dependent cellular cytotoxicity (ADCC).

Results: In an in vitro assay, lapatinib induced HER2 expression at the cell surface of HER2-positive breast cancer cell lines, leading to the enhancement of Herceptin-mediated ADCC. Furthermore, we present a case report in which a second Herceptin treatment following lapatinib resulted in the marked shrinkage of multiple metastatic tumors in HER2-positive breast cancer.

Conclusion: Lapatinib may have the potential to convert Herceptin-refractory to Herceptin-sensitive tumors in HER2-positive breast cancer by up-regulation of the cell surface expression of HER2.

MeSH terms

  • Antibodies, Monoclonal / pharmacology*
  • Antibodies, Monoclonal, Humanized
  • Antibody-Dependent Cell Cytotoxicity / immunology*
  • Blotting, Western
  • Drug Synergism
  • Female
  • Flow Cytometry
  • Genes, erbB-2*
  • Humans
  • Lapatinib
  • Middle Aged
  • Quinazolines / pharmacology*
  • Trastuzumab
  • Up-Regulation*

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Quinazolines
  • Lapatinib
  • Trastuzumab