Drug intelligence / Profile preview

omega-3-acid ethyl esters + HMG-CoA reductase inhibitor

Development stage
Unknown
Lead developer
Hanmi Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

A combination therapy consisting of **omega-3-acid ethyl esters** (mainly ethyl esters of eicosapentaenoic acid [EPA] and docosahexaenoic acid [DHA]) and an **HMG-CoA reductase inhibitor** (statin; e.g., simvastatin, atorvastatin, or rosuvastatin). Administered together, this combination is used primarily for adults with hypertriglyceridemia who have persistently elevated triglyceride levels despite statin therapy. **Omega-3-acid ethyl esters** work mainly by reducing hepatic triglyceride synthesis and increasing triglyceride clearance, through inhibition of acyl-CoA:1,2-diacylglycerol acyltransferase, increased β-oxidation, and upregulation of lipoprotein lipase activity. **HMG-CoA reductase inhibitors** lower cholesterol by competitively inhibiting the enzyme HMG-CoA reductase, which is the rate-limiting step in cholesterol biosynthesis. The combination demonstrates additive effects in lowering triglycerides and non-HDL cholesterol, with statins as the primary lipid-lowering backbone and omega-3-acid ethyl esters as adjunct therapy to further reduce triglycerides in patients with high cardiovascular risk.

02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)DGAT1 (Diacylglycerol O-acyltransferase 1)SLC7A1 (Cationic amino acid transporter 1)LPL (Lipoprotein lipase)CRAT (Carnitine O-acetyltransferase)

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