Drug intelligence / Profile preview

etofibrate

Development stage
Phase 3
Lead developer
Merz Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

**Etofibrate** is an oral, small-molecule lipid-modifying fibrate used for hyperlipidemia, particularly mixed hyperlipidemia and hypertriglyceridemia. It is a single covalent ethylene-glycol diester combining a clofibrate-derived moiety with nicotinic acid, designed to undergo hydrolysis and gradually provide fibrate and niacin pharmacology. Its principal lipid-lowering activity is attributed to fibrate-mediated activation of peroxisome proliferator-activated receptor alpha, with niacin-related hydroxycarboxylic acid receptor 2 signaling also contributing to effects on lipid metabolism. Clinical studies reported reductions in triglycerides, total cholesterol, LDL cholesterol, and lipoprotein(a), with increased HDL cholesterol; it was also investigated in diabetic retinopathy. It has been marketed as Lipo-Merz and Tricerol. ([pubchem.ncbi.nlm.nih.gov](https://pubchem.ncbi.nlm.nih.gov/compound/Etofibrate))

Brand names
Lipo-MerzLipo-Merz RetardTricerolTricerol A.P.
Other names
ethofibrateetofibratoetofibratum2-[2-(4-chlorophenoxy)-2-methylpropanoyloxy]ethyl nicotinate
02

Targets

HCAR2 (Hydroxycarboxylic acid receptor 2)PPARA (Peroxisome proliferator-activated receptor alpha)

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