BG-7520

BG-7520 is an orally bioavailable, selective small molecule inhibitor of the histone lysine acetyltransferases KAT6A and KAT6B, currently under development by BeiGene. KAT6A is a member of the MYST family of acetyltransferases and is frequently amplified or overexpressed in various cancers, particularly hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer. By inhibiting KAT6A/B, BG-7520 aims to modulate chromatin structure and suppress the transcription of oncogenic drivers, including the estrogen receptor (ER) signaling pathway. It is currently being evaluated in Phase 1 clinical trials for the treatment of advanced solid tumors, with a focus on patients who have progressed on prior endocrine therapies and CDK4/6 inhibitors.