Drug intelligence / Profile preview

enlicitide

Development stage
Approved
Lead developer
Merck
Modality
Cyclic Peptides → Modified Peptides → Peptides, Small Molecules
Administration
Oral
01

Overview

Enlicitide (also known as MK-0616, enlicitide chloride, and enlicitide decanoate) is an investigational oral macrocyclic peptide drug developed to lower cholesterol levels, specifically targeting hypercholesterolemia and related cardiovascular risks. It acts as a PCSK9 inhibitor by binding to the proprotein convertase subtilisin/kexin type 9 (PCSK9) protein and blocking its interaction with the LDL receptor, thereby increasing LDL receptor availability on hepatocytes and enhancing clearance of low-density lipoprotein cholesterol (LDL-C) from the bloodstream. Enlicitide is notable for being orally administered—unlike most other PCSK9 inhibitors that require injection—and requires co-formulation with permeation enhancers due to its low intrinsic bioavailability. The drug is currently in phase 3 clinical trials for hypercholesterolemia, type IIa hyperlipoproteinemia, and high cardiovascular risk populations[1][3][4][6][7][8].

Brand names
Lipfendra
Other names
enlicitide chlorideenlicitide decanoate
02

Targets

PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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