Drug intelligence / Profile preview

laropiprant

Development stage
Phase 4
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Laropiprant is a small molecule drug that acts as a selective antagonist of the prostaglandin D2 receptor subtype DP1. It was developed to reduce flushing associated with nicotinic acid (niacin) therapy for dyslipidemia and hypercholesterolemia. Flushing is caused by niacin-induced release of prostaglandin D2, which dilates blood vessels via activation of DP1 receptors in the skin. By blocking these receptors, laropiprant inhibits vasodilation and reduces flushing symptoms without affecting lipid levels or interfering with niacin’s lipid-modifying effects. Laropiprant was primarily used in fixed-dose combination products with extended-release niacin (e.g., Tredaptive, Cordaptive), but these products were withdrawn from the market after studies showed no additional cardiovascular benefit and increased adverse effects compared to placebo[2][3][5][6][7].

Brand names
CordaptiveTredaptiveTrevaclyn
Other names
laropiprant
02

Targets

PTGDR (Prostanoid DP1 receptor)TYMP (Thymidine phosphorylase)

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