Alpelisib. Phosphatidylinositol 3-kinase alpha (PI3K alpha) inhibitor Oncolytic

Phosphatidylinositol 4,5-bisphosphate 3-kinases (PI3Ks) play a central role in numerous biological processes (such as cell death and proliferation, cell migration, energetic metabolism, etc.), which indicates that they have specific involvement in many oncogenic processes. PI3Ks frequently mutate, and most mutations lead to overactivation of the corresponding protein. Based on these observations, pharmaceutical companies have developed various PI3K inhibitors: pan-PI3K, dual-PI3K/mTOR pathway and PI3K-specific inhibitors. There are three different subclasses of enzyme isoform for PI3Ks. The protein p110alpha (PIK3CA) is in class I, and is the flagship member of this family because of its very high mutation frequency in cancer. BYL-719 or alpelisib is an ATP-competitive p110alpha-specific inhibitor recently developed by Novartis and currently in clinical evaluation after positive preclinical investigations. The present paper is an overview of recent publications on progress made with PI3Ks, and how they are of interest in oncology, and on alpelisib and its clinical therapeutic prospects.