astx528

ASTX528 is a novel small molecule inhibitor targeting the histone acetyltransferase (HAT) domain of CREB-binding protein (CBP) and its paralog p300. It was developed by Astex Pharmaceuticals using a proprietary fragment-based drug discovery approach. The drug aims to overcome dose-limiting tolerability issues seen with previous CBP/p300 bromodomain inhibitors by specifically inhibiting the HAT domain, which may improve the therapeutic window. Preclinical studies have demonstrated potent in vivo activity and a favorable safety profile in preclinical species, with promising preliminary toxicity evaluation and low predicted human dose. ASTX528 is being investigated for use in hormone-dependent cancers such as breast cancer and prostate cancer[1][3][5].