Lapatinib: a review of its use in the treatment of HER2-overexpressing, trastuzumab-refractory, advanced or metastatic breast cancer

Drugs. 2009 Oct 22;69(15):2125-48. doi: 10.2165/11203240-000000000-00000.

Abstract

Lapatinib (Tyverb, Tykerb) is an orally active, small molecule, reversible, dual tyrosine kinase inhibitor of human epidermal growth factor receptor type 1 (HER1) and type 2 (HER2). In the EU, lapatinib in combination with capecitabine is indicated for the treatment of women with HER2-overexpressing, advanced or metastatic breast cancer that has progressed after treatment with regimens that include anthracyclines, taxanes and, in the metastatic setting, trastuzumab. The orally administered combination of lapatinib and capecitabine was a more effective treatment than capecitabine alone, and was a generally well tolerated, conveniently administered combination for women with trastuzumab-refractory, HER2-positive advanced or metastatic breast cancer in a clinical trial. Lapatinib combined with capecitabine provides an effective therapeutic option for a group of patients who currently have few treatment choices.

Publication types

  • Review

MeSH terms

  • Anthracyclines / therapeutic use
  • Antibodies, Monoclonal / adverse effects*
  • Antibodies, Monoclonal / therapeutic use
  • Antibodies, Monoclonal, Humanized
  • Antimetabolites, Antineoplastic / therapeutic use
  • Breast Neoplasms / drug therapy*
  • Capecitabine
  • Cell Line, Tumor
  • Deoxycytidine / analogs & derivatives
  • Deoxycytidine / pharmacology
  • Deoxycytidine / therapeutic use
  • Drug Resistance, Neoplasm*
  • ErbB Receptors / metabolism
  • Female
  • Fluorouracil / analogs & derivatives
  • Fluorouracil / pharmacology
  • Fluorouracil / therapeutic use
  • Gene Expression
  • Humans
  • Lapatinib
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinases / metabolism
  • Quinazolines / therapeutic use*
  • Randomized Controlled Trials as Topic
  • Receptor, ErbB-2 / genetics
  • Receptor, ErbB-2 / metabolism*
  • Taxoids / therapeutic use
  • Trastuzumab

Substances

  • Anthracyclines
  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Antimetabolites, Antineoplastic
  • Protein Kinase Inhibitors
  • Quinazolines
  • Taxoids
  • Lapatinib
  • Deoxycytidine
  • Capecitabine
  • Protein Kinases
  • ErbB Receptors
  • Receptor, ErbB-2
  • Trastuzumab
  • Fluorouracil