CGT6297

CGT6297 is a potent, orally bioavailable allosteric inhibitor of phosphoinositide 3-kinase alpha (PI3Kα), developed by Cogent Biosciences. It is designed to selectively target the H1047R mutant form of PI3Kα with 25-fold selectivity over wild-type PI3Kα. Preclinical studies have demonstrated that CGT6297 provides robust inhibition of downstream signaling and efficacy in animal models, with high oral bioavailability and low clearance across species. In comparative mouse tumor models, it showed superior efficacy versus a currently approved therapy without increasing insulin levels. The drug is currently in preclinical development for cancer indications[1][2][5][6][8].