Drug intelligence / Profile preview

niacin + omega-3 acid ethyl esters

Development stage
Unknown
Lead developer
University of South Dakota
Modality
Small Molecules
Administration
Oral
01

Overview

This combination therapy consists of extended-release niacin (Niaspan) and omega-3 acid ethyl esters (Lovaza/Omacor). It was evaluated in a Phase 4 clinical trial (NCT00286234) conducted by the University of South Dakota for the treatment of metabolic syndrome and hypertriglyceridemia. Niacin (nicotinic acid) primarily acts as an agonist of the hydroxycarboxylic acid receptor 1 (HCAR1) and inhibits hepatic diacylglycerol acyltransferase-2 (DGAT2), leading to reduced triglyceride synthesis and increased HDL cholesterol levels. Omega-3 fatty acids (EPA and DHA) primarily lower triglyceride levels by activating peroxisome proliferator-activated receptor alpha (PPAR-alpha) and inhibiting acyl-CoA:1,2-diacylglycerol acyltransferase, which promotes fatty acid oxidation and reduces hepatic VLDL production. The combination aims to provide synergistic lipid-lowering effects and improve insulin sensitivity in patients with metabolic syndrome without adversely affecting glucose levels.

Brand names
NiaspanLovazaOmacor
Other names
combined treatment-University of South Dakota-metabolic syndrome-hypertriglyceridemianiacin + omega-3 acid ethyl estersNiaspan + LovazaNiaspan + Omacorextended-release niacin + omega-3 acid ethyl esters
02

Targets

HCAR1 (Hydroxycarboxylic acid receptor 1)PPARA (Peroxisome proliferator-activated receptor alpha)DGAT2 (Hepatic diacylglycerol acyltransferase 2)HCAR3 (Hydroxycarboxylic acid receptor 3)

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