Drug intelligence / Profile preview

MK-0616A

Development stage
Unknown
Lead developer
Merck
Modality
Peptides, Small Molecules
Administration
Oral
01

Overview

**MK-0616A** is Merck's investigational oral fixed-dose combination tablet containing the macrocyclic peptide PCSK9 inhibitor **enlicitide decanoate** and the statin **rosuvastatin**. Enlicitide binds the LDL receptor-binding region of proprotein convertase subtilisin/kexin type 9, preventing PCSK9-mediated degradation of LDL receptors and thereby increasing hepatic LDL-cholesterol clearance. Rosuvastatin inhibits 3-hydroxy-3-methylglutaryl-coenzyme A reductase to reduce hepatic cholesterol synthesis and increase LDL-receptor expression. MK-0616A is being evaluated as a single-tablet lipid-lowering therapy for hypercholesterolemia; a Phase 1 study compared the relative bioavailability of the fixed-dose tablet with coadministration of its individual components in healthy adults.

Other names
enlicitide + rosuvastatinenlicitide decanoate + rosuvastatinenlicitide/rosuvastatin calciumenlicitide/rosuvastatin fixed-dose combination
02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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