prifetrastat + fulvestrant

Prifetrastat (PF-07248144) in combination with fulvestrant is an investigational therapeutic regimen for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Prifetrastat is a first-in-class, oral small molecule inhibitor of the histone acetyltransferases KAT6A and KAT6B. These enzymes are epigenetic regulators that facilitate gene transcription by acetylating lysine 23 on histone H3 (H3K23); their inhibition leads to the downregulation of key oncogenic drivers, including the estrogen receptor. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to and promotes the degradation of the estrogen receptor, thereby blocking estrogen-mediated signaling. The combination is being evaluated in patients who have progressed on prior endocrine therapies and CDK4/6 inhibitors, aiming to overcome resistance mechanisms associated with epigenetic dysregulation. The Phase II UNLOCK-EPIBREAST study, sponsored by UNICANCER, specifically investigates this combination in pretreated HR+/HER2- metastatic breast cancer patients.

Other names

PF-07248144 plus fulvestrantPF07248144 plus fulvestrantPF 07248144 plus fulvestrant