Drug intelligence / Profile preview

Omega-3 carboxylic acids

Development stage
Phase 2
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Omega-3 carboxylic acids are a prescription lipid-regulating agent derived from fish oil, primarily containing the free fatty acid forms of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). Developed by AstraZeneca, this drug was approved by the FDA in 2014 as an adjunct to diet for reducing triglyceride levels in adults with severe hypertriglyceridemia. Unlike ethyl ester formulations, omega-3 carboxylic acids are absorbed directly without requiring pancreatic enzyme activity, resulting in enhanced bioavailability. The mechanism of action is not fully understood but is thought to involve inhibition of acyl-CoA:1,2-diacylglycerol acyltransferase, increased mitochondrial and peroxisomal beta-oxidation in the liver, decreased hepatic lipogenesis, increased plasma lipoprotein lipase activity, reduced synthesis of triglycerides due to EPA/DHA being poor substrates for TG synthesis enzymes, and inhibition of esterification of other fatty acids. Clinical studies have shown significant reductions in serum triglycerides as well as non-HDL cholesterol and VLDL-C[1][2][5][6][8].

Brand names
Epanova
Other names
omega-3-carboxylic acidsomega3-carboxylic acidsomega 3-carboxylic acidsfish oil-derived free fatty acidseicosapentaenoic acid and docosahexaenoic acid (EPA and DHA) mixture
02

Targets

DGAT1 (Diacylglycerol O-acyltransferase 1)LPL (Lipoprotein lipase)

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