Drug intelligence / Profile preview

statin + niacin + laropiprant

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

Overview

This combination therapy consists of a statin (HMG-CoA reductase inhibitor), extended-release niacin (nicotinic acid), and laropiprant. It was evaluated in a Phase 4 clinical trial by the University of Ioannina for the treatment of mixed hyperlipidemia. The statin component (which may include rosuvastatin or other existing statins) reduces LDL cholesterol by inhibiting HMG-CoA reductase. Niacin acts as an agonist at the GPR109A receptor, reducing triglycerides and VLDL while increasing HDL cholesterol. Laropiprant is a selective antagonist of the prostaglandin D2 receptor 1 (DP1), specifically included to mitigate the skin flushing commonly associated with niacin therapy. This triple combination aims to provide comprehensive lipid management in patients who do not reach their lipid targets with statin monotherapy. The niacin/laropiprant component was originally developed by Merck & Co. under the brand name Tredaptive.

Brand names
Tredaptive
Other names
statin + niacin ER/laropiprantstatin + ER-NA/LRPTstatin + extended-release niacin/laropiprant
02

Targets

HCAR2 (Hydroxycarboxylic acid receptor 2)PTGDR (Prostanoid DP1 receptor)

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