S016

S016 is a novel oral small-molecule proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor being developed by Chengdu Shibeikang Biomedical Technology and Chengdu Medical College for the treatment of hypercholesterolemia and atherosclerotic cardiovascular disease (ASCVD). S016 selectively binds to the functional domain of PCSK9, blocking its interaction with the low-density lipoprotein receptor (LDLR). This inhibition prevents LDLR degradation, thereby increasing LDLR density on hepatocytes and enhancing the clearance of low-density lipoprotein cholesterol (LDL-C) from the blood. In preclinical studies, S016 demonstrated potent, dose-dependent inhibition of PCSK9 secretion, rapid and sustained reduction of LDL-C levels in vivo, and a favorable cardiac safety profile with no significant hERG channel inhibition.