Enlicitide decanoate

Enlicitide (MK-0616) decanoate is an orally active macrocyclic peptide PCSK9 inhibitor. Enlicitide decanoate binds to PCSK9, blocks its interaction with low-density lipoprotein receptor ( LDLR ), and enhances hepatic clearance of LDL-C. Enlicitide decanoate reduces atherogenic lipoproteins, including non-HDL cholesterol, apolipoprotein B, and lipoprotein (a). Enlicitide decanoate is applicable to research related to hypercholesterolemia, heterozygous familial hypercholesterolemia, and atherosclerotic cardiovascular disease ^{[1] [2]}.

In Vitro, Enlicitide decanoate specifically binds to the LDL receptor-binding domain of PCSK9, blocks the interaction between PCSK9 and LDL receptor, prevents PCSK9 from degrading LDL receptors on the surface of hepatocytes, thereby increasing the number of available LDL receptors on hepatocyte surface, enhancing the hepatic clearance efficiency of low-density lipoprotein cholesterol (LDL-C) in the blood, and achieving potent lipid-lowering effects^[1][2].

References:
[1]. Elbahloul MA, et al. The Oral PCSK9 inhibitor enlicitide for hypercholesterolemia. Eur J Intern Med. 2026 Mar 14:106835.
[2]. Merck. "Merck’s Enlicitide Decanoate, an Investigational Oral PCSK9 Inhibitor, Significantly Reduced LDL-C in Phase 3 CORALreef Lipids Trial." Merck, 8 Nov. 2025.