BYL719

BYL719 is an orally bioavailable, next generation PI3K α- isoform specific inhibitor with potential antineoplastic activity. BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations. In vivo, BYL719 shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 has a low clearance, a half-life of 8.5 h in humans and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC. BYL719 is currently in phase II clinical trial in adult patients with selected advanced solid tumors.