Enlicitide is an oral macrocyclic peptide PCSK9 inhibitor indicated as an adjunct to diet and exercise to reduce LDL-C in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia. PCSK9 binds low-density lipoprotein receptors (LDLR) on the surface of hepatocytes and promotes their degradation within the liver; by blocking this interaction, enlicitide increases the number of LDLRs available to clear low-density lipoprotein cholesterol (LDL-C),...
- Mechanism
- Curator reviewed · 3 references
Enlicitide is a macrocyclic peptide that binds to PCSK9. PCSK9 binds to low-density lipoprotein receptors (LDLR) on the surface of hepatocytes and promotes LDLR degradation within the liver. By inhibiting the binding of PCSK9 to LDLR, enlicitide increases the number of LDLRs available to clear LDL-C, which lowers LDL-C levels.
- Primary indication
- Enlicitide is indicated as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH).Curator reviewed · 2 structured indications
- First approval
- United States, 2026
Resolves to
What you can answer from here — as of November 02, 2026
Which drugs share a target with Enlicitide, and which of those have an active Phase 3 trial?
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