AS03157

AS03157 is a novel, orally active small molecule antagonist of inhibitor of apoptosis proteins (IAPs), specifically designed to target and degrade cellular inhibitor of apoptosis protein 1 (cIAP1) and X-linked inhibitor of apoptosis protein (XIAP). Overexpression of these antiapoptotic proteins is common in various hematologic and solid cancers, contributing to drug resistance and poor prognosis. By binding with high affinity to cIAP1 and XIAP, AS03157 efficiently induces degradation of cIAP1, disrupts pro-survival signaling pathways, activates caspases, promotes apoptosis in cancer cells, and demonstrates potent antiproliferative activity with IC50 values below 30 nM in preclinical models. The compound has shown promising efficacy and an acceptable safety profile in preclinical studies. It was discovered by Ascentage Pharma as part of their pipeline focused on targeting key regulators within the apoptotic pathway for cancer therapy[2][3][4][5].