Lapatinib

Pharmacogenomic Information in the Context of the FDA-Approved Drug Label*

Excerpt from the lapatinib drug label:

"TYKERB, a kinase inhibitor, is indicated in combination with:
-capecitabine, for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 and who have received prior therapy including an anthracycline, a taxane, and trastuzumab.
-letrozole for the treatment of postmenopausal women with hormone receptor positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated."

"The recommended dose of TYKERB for hormone receptor positive, HER2 positive metastatic breast cancer is 1500 mg (6 tablets) given orally once daily continuously in combination with letrozole. When TYKERB is coadministered with letrozole, the recommended dose of letrozole is 2.5 mg once daily."

"Lapatinib is a 4-anilinoquinazoline kinase inhibitor of the intracellular tyrosine kinase domains of both Epidermal Growth Factor Receptor (EGFR (ErbB1)) and of Human Epidermal Receptor Type 2 (HER2 (ErbB2)) receptors (estimated Kiapp values of 3nM and 13nM, respectively) with a dissociation half-life of >=300 minutes. Lapatinib inhibits ErbB-driven tumor cell growth in vitro and in various animal models."

(For the complete drug label text with sections containing pharmacogenetic information highlighted, see the Lapatinib drug label PDF.)