Enlicitide Decanoate (MK0616)

China [CN]

Enlicitide Decanoate (MK-0616) Key Information

Generic Name: Enlicitide Decanoate  Development Code: MK-0616, MK0616  Alias: Enlicitide Chloride CAS Number: 2407527-16-4 Molecular Formula: C₈₂H₁₁₀ClFN₁₄O₁₅ Molecular Weight: ~1580 Da Drug Type: Oral Macrocyclic Peptide PCSK9 Inhibitor (First-in-class) Originator: Merck Sharp & Dohme

Mechanism of Action

Core Target: PCSK9 (Proprotein Convertase Subtilisin/Kexin Type 9)

Mechanism: High-affinity binding to PCSK9 (Ki=5 pM), blocking its interaction with hepatic LDL receptors (LDL-R)

Lipid-lowering Principle: Prevents PCSK9-mediated LDL-R degradation, increasing the number of LDL-R on the surface of hepatocytes, significantly accelerating the clearance of LDL-C (bad cholesterol) from the blood

Oral Advantage: Optimized macrocyclic peptide structure, high oral bioavailability, no injection required, no absorption enhancers needed

Core Clinical Applications (2026)

1. Indications (Phase III completed, application pending)

Hypercholesterolemia (including heterozygous familial hypercholesterolemia HeFH)

**Atherosclerotic cardiovascular disease (ASCVD)** high-risk individuals

Patients intolerant to statins / patients who have not achieved target levels with statin therapy

2. Dosing Regimen

20 mg, oral, once daily (fixed dose, no titration required)

3. Key Phase III Data (CORALreef series)

CORALreef Lipids (ASCVD / Hypercholesterolemia):

Week 24: LDL-C reduced by 55.8% from baseline (primary analysis) / 59.7% (post-hoc analysis), vs. placebo (+3.0%)

**Non-HDL-C, ApoB, Lipoprotein (a)** also significantly decreased

CORALreef HeFH (Familial Hypercholesterolemia):

Week 24: LDL-C reduced by 58.2%, efficacy sustained and stable at 52 weeks

Safety: Comparable to placebo, mainly mild to moderate gastrointestinal reactions, compliance > 97%

4. Market Launch Progress (2026)

Global Filing: FDA NDA, EMA MAA, and NMPA marketing applications to be completed by the end of 2025

Expected Approval: Second half of 2026 (globally simultaneous)

Patents: Core compound and formulation patents protected until after 2040

Physicochemical and Supply Chain Highlights

Appearance: White to off-white solid (API)

Solubility: Water-soluble (oral tablets)

Stability: Store sealed at **2–30℃**, protected from moisture

Product Type: Active Pharmaceutical Ingredient (API), Reference Standard, Intermediate

Purity: Pharmaceutical grade ≥ 98% (HPLC)

HS Code: 2937190090 (Peptides)