NYX-PCSK9i

NYX-PCSK9i is an orally bioavailable small-molecule inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). It functions by disrupting the protein-protein interaction between PCSK9 and the low-density lipoprotein receptor (LDLR), thereby preventing the PCSK9-mediated degradation of LDLR and increasing hepatic LDLR protein levels to facilitate the clearance of LDL cholesterol from the blood. Developed as a structural analog of compound 3f, NYX-PCSK9i has demonstrated significant dose-dependent reductions in plasma total cholesterol and non-HDL cholesterol in murine models of hyperlipidemia, both as a monotherapy and in combination with statins like atorvastatin. It also appears to influence cholesterol metabolism through potential secondary mechanisms, such as the reduction of microsomal triglyceride transfer protein (Mttp) transcription and the promotion of trans-intestinal cholesterol excretion.

Other names

cardiovascular PCSK9 inhibitorPCSK9 inhibitorPCSK-9 inhibitorPCSK 9 inhibitor