Breast Cancer

, Volume 14, Issue 2, pp 156–162

Does lapatinib, a small-molecule tyrosine kinase inhibitor, constitute a breakthrough in the treatment of breast cancer?

  • Yoshinori Ito
  • Nahomi Tokudome
  • Tsutomu Sugihara
  • Shunji Takahashi
  • Kiyohiko Hatake
Review Article

DOI: 10.2325/jbcs.971

Cite this article as:
Ito, Y., Tokudome, N., Sugihara, T. et al. Breast Cancer (2007) 14: 156. doi:10.2325/jbcs.971


ErbB/HER receptor or its signal transduction pathway is an attractive therapeutic target for breast cancer. Lapatinib, an orally administered dual inhibitor of ErbB1 (EGFR) and ErbB2 (HER2) receptor tyrosine kinases has shown promising results for metastatic breast cancer (MBC). Lapatinib exhibited activity against trastuzumab-refractory MBC and showed an acceptable adverse event profile such as tran-sient mild rash, diarrhea and nausea. The addition of lapatinib to capecitabine resulted in significantly pro-longed time to progression. Large randomized trials using lapatinib following chemotherapy and surgery are ongoing for early stage HER2-overexpressing breast cancer. Various combinations with agents such as paclitaxel, aromatase inhibitors, or other molecular targeted agents are currently being investigated in clinical trials. If these approaches overcome the limitations of trastuzumab, lapatinib will become an effec-tive treatment option for breast cancer in the near future.


Breast cancerErbBHERLapatinib



Metastatic breast cancer


Epidermal growth factor receptor


Mitogen-activated protein kinase


Phatidylinositol 3 kinase


Insulin-like growth factor-l receptor


Cyclin-dependent kinase


Estrogen receptor


Aromatase inhibitor



Copyright information

© The Japanese Breast Cancer Society 2007

Authors and Affiliations

  • Yoshinori Ito
    • 1
  • Nahomi Tokudome
    • 1
  • Tsutomu Sugihara
    • 1
  • Shunji Takahashi
    • 1
  • Kiyohiko Hatake
    • 1
  1. 1.Department of Medical OncologyCancer Institute Hospital, Japanese Foundation for Cancer ResearchJapan
  2. 2.Department of Medical OncologyCancer Institute Hospital, Japanese Foundation for Cancer ResearchKoto-ku, TokyoJapan