Foretinib (GSK1363089, XL880)

Foretinib (GSK1363089, XL880) is an inhibitor of MET and VEGFR2, which are believed to play cooperative roles in promoting tumor growth and angiogenesis. MET is thought to be mutationally activated in hereditary papillary renal cell carcinoma and in some head and neck cancers, may beactivated or overexpressed in glioblastomas, breast carcinomas, non-small cell lung cancers, and other solid tumors, and could be amplified in a subset of gastric and lung cancers. Exelixis discovered Foretinib internally and out-licensed the compound to GlaxoSmithKline. It is currently in an ongoing phase 1b/2 trial in triple negative metastatic breast cancer, and phase 1b/2 combination trials with lapatinib in HER2 positive breast cancer, and with erlotinib in NSCLC.