tersolisib

**Tersolisib (STX-478)** is an orally bioavailable, brain-penetrant small molecule that acts as a selective allosteric inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (PI3Kα), specifically targeting the mutant H1047X form (including H1047R). Developed initially by Scorpion Therapeutics and now advanced by Eli Lilly following acquisition, it binds allosterically to prevent activation of the PI3K/Akt/mTOR pathway in mutant-expressing tumor cells, inducing apoptosis and growth inhibition while sparing wild-type PI3Kα to minimize toxicities like hyperglycemia seen with other inhibitors. It demonstrates robust antitumor activity in preclinical models of PIK3CA-mutant cancers including breast, colon, lung, and head and neck squamous cell carcinoma, outperforming or matching alpelisib in xenograft studies.[1][2][3][5][7][9]

Other names

LY4064809LY-4064809LY 4064809