Drug intelligence / Profile preview

laropiprant + niacin

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

Overview

Laropiprant + niacin is a fixed-dose combination drug that was developed for the treatment of dyslipidemia, particularly in patients with combined mixed dyslipidemia and primary hypercholesterolemia. Niacin (nicotinic acid) is a lipid-modifying agent that lowers LDL cholesterol and triglycerides while raising HDL cholesterol, but its use is limited by frequent flushing side effects. Laropiprant acts as a selective antagonist of the prostaglandin D2 receptor subtype DP1, reducing the incidence and intensity of niacin-induced flushing without affecting its lipid-lowering efficacy. The combination was intended to improve patient compliance with niacin therapy by mitigating this adverse effect. Despite initial approvals in Europe under brand names such as Tredaptive and Cordaptive, large clinical trials failed to demonstrate cardiovascular benefit and revealed increased adverse events, leading to global withdrawal of the product[1][2][5][7].

Brand names
Pelzont
Other names
laropiprant / niacinlaropiprant-niacin mixt.
02

Targets

TYMP (Thymidine phosphorylase)PTGDR (Prostanoid DP1 receptor)HCAR2 (Hydroxycarboxylic acid receptor 2)

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