PF-08032562

PF-08032562 is an orally bioavailable small molecule inhibitor of Lysine Acetyltransferase 6A (KAT6A) and 6B (KAT6B), developed by Pfizer. KAT6A and KAT6B are members of the MYST family of histone acetyltransferases that play critical roles in regulating gene expression and cell cycle progression. KAT6A is frequently amplified or overexpressed in several cancers, including hormone receptor-positive (HR+) breast cancer, where it acts as a co-activator for estrogen receptor-mediated transcription and promotes oncogenesis. By inhibiting KAT6A/B, PF-08032562 induces cellular senescence and inhibits tumor growth. It is currently being evaluated in Phase 1 clinical trials as a monotherapy and in combination with other agents, such as fulvestrant or cetuximab, for the treatment of advanced or metastatic solid tumors, specifically breast cancer and colorectal cancer.