OP-3136

OP-3136 is a novel, orally available small molecule that potently and selectively inhibits lysine acetyltransferase 6 (KAT6), specifically targeting both KAT6A and KAT6B. These enzymes are epigenetic regulators implicated in the proliferation of various cancers, including breast, ovarian, prostate, and non-small cell lung cancer. Preclinical studies have demonstrated that OP-3136 exhibits strong anti-proliferative activity in estrogen receptor-positive (ER+) breast cancer models as well as significant tumor growth inhibition and regression in ovarian, prostate, and lung cancer models. The compound has shown synergy with endocrine therapies such as palazestrant (OP-1250) and cyclin-dependent kinase 4/6 inhibitors. Currently, OP-3136 is being evaluated in a Phase 1 clinical trial for multiple solid tumor types[1][5][9][10].