BG-75202

**BG-75202** is an oral small molecule inhibitor targeting lysine acetyltransferase 6A and 6B (KAT6A/B), epigenetic enzymes implicated in oncogenesis, particularly in hormone receptor-positive breast cancer. Developed by BeOne Medicines (formerly BeiGene), it demonstrates preclinical efficacy superior to Pfizer's PF-07248144 with higher selectivity against KAT7. It is entering Phase 1 trials (NCT07222267) to assess safety, tolerability, PK/PD, and preliminary antitumor activity as monotherapy and in combinations with CDK4 inhibitors, estrogen receptor antagonists, or aromatase inhibitors in advanced solid tumors, focusing on breast cancer.[1][2][3][8][10]