GenSci145

GenSci145 is a selective small molecule inhibitor of mutant PI3Kα (p110α), encoded by the PIK3CA gene, developed by Changchun GeneScience Pharmaceutical. It is designed for the treatment of locally advanced or metastatic solid tumors, particularly HR+/HER2- breast cancer, that harbor PIK3CA mutations. GenSci145 is engineered for high selectivity toward mutant isoforms over wild-type PI3Kα, which significantly reduces the risk of hyperglycemia, a common side effect of non-selective PI3K inhibitors. Furthermore, the molecule exhibits enhanced blood-brain barrier penetration, making it a potential therapeutic option for patients with brain metastases. It is currently undergoing Phase 1/2 clinical evaluation as a monotherapy and in combination with fulvestrant and/or palbociclib.