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SNV-002 is a novel, proprietary, and mutant-selective small molecule inhibitor of phosphatidylinositol 3-kinase alpha (PI3Kα), initially developed by Sinovant Sciences and currently under development by Synnovation Therapeutics. It is designed to selectively target oncogenic hotspot mutations of PI3Kα, such as H1047R, E545K, and E542K, while sparing wild-type PI3Kα. This selectivity aims to avoid the on-target toxicities, such as hyperglycemia, skin rash, and gastrointestinal issues, that limit the clinical utility of first-generation, non-selective PI3Kα inhibitors like alpelisib. Preclinical studies have demonstrated that SNV-002 potently suppresses the PI3K-AKT-mTOR pathway and inhibits tumor growth in mutant-bearing models with favorable pharmacokinetic properties, supporting its potential development for PI3Kα mutation-driven malignancies, including hormone receptor-positive, HER2-negative (HR+/HER2-) breast cancer.
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