 | |
| Clinical data | |
|---|---|
| Other names | MK-0616 |
| Identifiers | |
| |
| CAS Number | |
| PubChemCID | |
| IUPHAR/BPS | |
| UNII | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C92H129FN14O17 |
| Molar mass | 1722.123 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Enlicitide decanoate (previously known asMK-0616[1]) is an orally availablemacrocyclic peptideinvestigational drug that is being evaluated for the treatment ofhypercholesterolaemia. It is aPCSK9 inhibitor.[2][3]
Enlicitide decanoate interacts with theLDL receptor binding domain of PCSK9 and inhibits its interaction with the receptor with anIC50 of 2.5 ±0.1 nM.[4]
A 2025 review paper of cholesterol-lowering drugs with PCSK9 and other biomolecules as a target, states that "[enlicitide] promises to be a blockbuster cholesterol-lowering drug as it exhibits a high degree of efficiency in clinical trials and of potential for applications in individuals wherestatins and dietary adjustments are not sufficient."[5] The drug is being developed byMerck, which expects to apply forFDA approval in early 2026.[6]
A double-blind, placebo-controlledPhase I clinical trial demonstrated that oral administration of the drug in 60 healthy males at doses of 10, 35, 100, 200, and 300 mg reduced free plasma levels of PCSK9 by more than 93%.[4] In a separate Phase I study with statin-treated participants, daily doses of 10 and 20 mg reducedLDL levels at 14 days by 58.2 and 60.5%, respectively.[4]
APhase IIB study of eight weeks evaluated efficacy and safety in patients with hypercholesterolemia. Daily oral doses of 6, 12, 18, or 30 mg reduced LDL by 41.2, 55.7, 59.1, and 60.9% at the end point. Essentially complete efficacy was reached after two weeks. Adverse events were comparable to placebo at all doses throughout the study period.[4]
On 10 August 2023 Merck launched the Phase III CORALreef Lipids clinical trial to evaluate the efficacy and safety of MK-0616 in adults with hypercholesterolemia.[7][8] The study included 2,912 participants and was completed on 28 July 2025 with results announced on 2 September 2025[9][6] and published on 4 February 2026.[10][11]