Description
BYL-719 is an ATP-competitive oral PI3K inhibitor selective for the p110α isoform that is activated by a mutant PIK3CA gene in HER2+ breast cancers and gastric cancers. BYL-719 exhibits anticancer chemotherapeutic activity and inhibits proliferation in a variety of cell lines. IGF1 and neuregulin 1 activate mTOR, a downstream target of PI3K that mediates resistance to BYL-719 in some in vitro cancer models. This compound also decreases invasion and epithelial-to-mesenchymal transition (EMT) in cellular and animal models of squamous cell lung cancer.