Drug intelligence / Profile preview

MK0524 + placebo

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

Overview

MK0524 (also known as Laropiprant) is a potent and selective antagonist of the prostaglandin D2 receptor DP1. It was developed to block prostaglandin D2-mediated effects such as vasodilation and flushing. The drug has been studied primarily for its ability to reduce niacin-induced flushing in patients treated for dyslipidemia and hypercholesterolemia. In clinical studies, MK0524 significantly reduced the severity of flushing associated with extended-release niacin therapy without affecting lipid-lowering efficacy[1][8]. Mechanistically, it acts as an inverse agonist at DP1 receptors and also displays pharmacochaperone activity[10]. "Placebo" in this context refers to an inactive comparator used in clinical trials.

Brand names
CordaptiveTredaptiveCardaptive
Other names
niacin ER/laropiprantPelzont571170-77-9
02

Targets

PTGDR (Prostanoid DP1 receptor)

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