Lapatinib: an oral dual tyrosine kinase inhibitor for HER-2-positive breast cancer

Womens Health (Lond). 2015 Jun;11(3):281-94. doi: 10.2217/whe.15.9.

Abstract

Breast cancer is the most common form of cancer and the second leading cause of cancer deaths among women in the USA. A quarter of all newly diagnosed cases are characterized by overexpression of HER-2 which is associated with poor prognosis. In March 2007, lapatinib, an oral dual-tyrosine kinase inhibitor was approved in combination with capecitabine for metastatic HER-2-positive breast cancer that has progressed on prior trastuzumab therapy, and in combination with letrozole for postmenopausal women with HER-2 and hormone receptor-positive advanced breast cancer. In the future, lapatinib may play an important role in dual HER-2 blockade with trastuzumab and other targeted agents for women with HER-2-overexpressing breast cancer.

Keywords: ERBB2; GW572016; HER-2; capecitabine; lapatinib; letrozole; metastatic breast cancer; trastuzumab.

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / genetics
  • Female
  • Humans
  • Lapatinib
  • Postmenopause
  • Protein Kinase Inhibitors / therapeutic use*
  • Quinazolines / therapeutic use*
  • Receptor, ErbB-2*
  • United States
  • Women's Health

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Quinazolines
  • Lapatinib
  • ERBB2 protein, human
  • Receptor, ErbB-2