Herceptin Research Today is a free monthly online journal that collates and summarizes the latest research about Herceptin, including details on side-effects, breast cancer, treatment, therapy.

Lapatinib: a tyrosine kinase inhibitor with a clinical role in breast cancer.

Mukherjee A, Dhadda AS, Shehata M, Chan S

Nottingham University Hospitals NHS Trust (City Hospital Campus), Department of Clinical Oncology, Nottingham, UK. steve.chan@nuh.nhs.uk

Lapatinib is a dual (ErbB-1 and ErB-2) receptor tyrosine kinase inhibitor (TKI) that was recently approved by the FDA for the treatment of advanced breast cancer. It shows synergy with trastuzumab, and has demonstrated clinical activity in trastuzumab-resistant tumour. This paper reviews the drug development of lapatinib from preclinical studies to the pivotal Phase III trial and ongoing clinical studies. Areas of interest include the advantages of small molecule TKIs versus antibodies in targeting HER receptors and the efficacy of lapatinib in the treatment of cerebral metastases. The surprisingly high response rate in inflammatory breast cancer raises the possibility of other novel predictive biomarkers. The potential for combination and sequencing with other biological and cytotoxic agents is both exciting and challenging.

Published 23 August 2007 in Expert Opin Pharmacother, 8(13): 2189-204.
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