Gedatolisib: First Approval.

Gedatolisib (REVTORPYK®) is a kinase inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms and mechanistic target of rapamycin (mTOR) complexes. It is being developed by Celcuity, under a license from Pfizer, for the treatment of various cancers. PIK3CA, which encodes the catalytic subunit of PI3K, is frequently mutated in a range of cancers, including breast cancer. Gedatolisib received its first approval in the USA on 14 July 2026 for use in combination with fulvestrant, with or without palbociclib, for the treatment of adult patients with hormone receptor positive (HR+), human epidermal growth factor receptor 2 negative (HER2-) locally advanced or metastatic breast cancer without a PIK3CA mutation detected following progression on or after treatment with at least one line of endocrine therapy in the metastatic setting. This article summarizes the milestones in the development of gedatolisib leading to this first approval for HR+/HER2- breast cancer.