Drug intelligence / Profile preview

mk-0524a + simvastatin

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-0524A + simvastatin refers to the co-administration of MK-0524A (a tablet containing extended-release niacin and laropiprant) with simvastatin. Niacin is an agent that reduces LDL cholesterol and triglycerides, and increases HDL cholesterol, while laropiprant is a selective prostaglandin D2 receptor antagonist designed to reduce flushing associated with niacin therapy. Simvastatin is an HMG-CoA reductase inhibitor (statin) that lowers LDL cholesterol. The combination was developed as adjunctive therapy to diet for the treatment of mixed dyslipidemia and primary hypercholesterolemia, aiming to maximize lipid modification while minimizing niacin-induced flushing. MK-0524A was developed by Merck Sharp & Dohme and intended for co-administration with simvastatin; it was never approved by the FDA for marketing due to safety, efficacy, or regulatory concerns[4][5]. The combination has been evaluated in clinical trials for lipid-lowering effect and safety[1][3][2].

Brand names
cordaptivetredaptive
Other names
extended-release niacin + laropiprant + simvastatiner niacin + laropiprant + simvastatin
02

Targets

HCAR3 (Hydroxycarboxylic acid receptor 3)PTGDR (Prostanoid DP1 receptor)HCAR2 (Hydroxycarboxylic acid receptor 2)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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