PI3KCA inhibitor

PI3KCA inhibitors are a class of targeted antineoplastic agents designed to selectively inhibit the alpha isoform of the catalytic subunit of phosphatidylinositol 3-kinase (PI3Kα), which is encoded by the PIK3CA gene. The PI3K/AKT/mTOR signaling pathway is frequently dysregulated in human cancers, often through gain-of-function mutations in PIK3CA, leading to uncontrolled cell proliferation and survival. In the clinical context of the PARAGON-II trial (NCT04449354), the term refers specifically to alpelisib (Piqray), a small molecule inhibitor developed by Novartis. Alpelisib is being investigated in combination with the aromatase inhibitor letrozole for the treatment of various hormone receptor-positive (HR+) gynecological malignancies, including endometrial cancer and platinum-resistant epithelial ovarian cancer. The trial evaluates the efficacy of this combination in both PIK3CA-mutated and wild-type tumors, comparing it against other targeted therapies like CDK4/6 inhibitors.

Other names

PI3KCA inhibitorPI-3KCA inhibitorPI 3KCA inhibitorPIK3CA inhibitorPIK-3CA inhibitorPIK 3CA inhibitorPI3K alpha inhibitorPI-3K alpha inhibitorPI 3K alpha inhibitor