CAS No.: 1415472-28-4 | Molecular Formula: Undisclosed | Molecular Weight: Undisclosed
Dosage Form: Oral Tablet | Manufacturer: Daewoong Pharmaceutical (South Korea), Co-developed with GC Pharma
Product Overview
Product Name: Enlicitide Chloride (Formerly MK-0616 Chloride)
Brand Name: Undisclosed (Late Phase Ⅲ Clinical Stage)
CAS No.: 2407527-16-4 | Molecular Formula: C₈₂H₁₁₀ClFN₁₄O₁₅ | Molecular Weight: 1586.29
Dosage Form: Oral Tablet | Manufacturer: Merck Sharp & Dohme Corp. (MSD)
Product Overview
Enlicitide Chloride is an orally active macrocyclic peptide PCSK9 inhibitor, initially developed by Merck (formerly known as MK-0616), currently in late Phase Ⅲ clinical trials globally. It is the first oral PCSK9 inhibitor to demonstrate statistically significant LDL-C reduction in Phase 3 trials, focusing on the treatment of hypercholesterolemia and related cardiovascular diseases.
Mechanism of Action
• Specifically inhibits PCSK9 activity, blocking the interaction between PCSK9 and LDL receptors (LDL-R), preventing LDL-R degradation and increasing the number of LDL-R on hepatocyte surfaces.
• Effectively promotes liver uptake and clearance of LDL-C, with an IC₅₀ of 2.5 nm, and can simultaneously reduce ApoB and Lp(a) levels, while improving lipid metabolism balance.
• Does not affect the absorption of triglycerides or fat-soluble vitamins, and has a favorable safety profile comparable to placebo.
Indications