lapatinib

Lapatinib is an orally active small molecule antineoplastic agent and dual tyrosine kinase inhibitor developed by GlaxoSmithKline for the treatment of solid tumors, primarily advanced or metastatic HER2-positive breast cancer. It works by inhibiting the intracellular tyrosine kinase domains of both human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (EGFR/HER1/ERBB1), thereby blocking receptor autophosphorylation and downstream signaling that promotes tumor cell proliferation. Lapatinib is used in combination with capecitabine for patients who have received prior chemotherapy, or with letrozole in postmenopausal women with hormone-receptor positive, HER2-positive metastatic breast cancer. It was approved by the FDA in 2007.

Brand names

TykerbTyverb

Other names

lapatinib ditosylate