LOXO-783

LOXO-783 is an orally bioavailable, brain-penetrant, highly selective and irreversible small molecule inhibitor targeting the class I phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (PI3Kα; PIK3CA) with a specific focus on the H1047R mutation. This mutation occurs in a significant proportion of PIK3CA-mutant breast cancers and other solid tumors. LOXO-783 was developed to address limitations of existing PI3K inhibitors by providing greater selectivity for mutant PI3Kα over wild-type, aiming to reduce dose-limiting toxicities such as hyperglycemia and improve tolerability. Preclinical studies demonstrated antitumor activity in models of ER+/HER2– PI3Kα H1047R-mutant breast cancer without increasing plasma insulin or C-peptide levels. Clinical development included evaluation as monotherapy and in combination with endocrine therapies for advanced breast cancer and other solid tumors harboring PIK3CA mutations[1][2][5][6].

Other names

LY3849524LY-3849524LY 3849524LOXO-783LOXO783LOXO 783