PF-07248144 — Investigational Agent
Other · Phase 1/2 · Pfizer
Mechanism of Action
First-in-class selective catalytic inhibitor of the histone lysine acetyltransferases KAT6A and KAT6B (MYST family). Blocks acetylation of histone H3K23, downregulating ER-driven and cell-cycle transcriptional programs and inducing senescence; shows synergy with endocrine therapy and CDK4/6 inhibition in ER+ breast cancer.
Investigational Indications
- ER-positive/HER2-negative metastatic breast cancer
- Advanced or metastatic solid tumors
- Castration-resistant prostate cancer