Drug intelligence / Profile preview

plant sterol esters + eicosapentaenoic acid + docosahexaenoic acid

Development stage
Unknown
Lead developer
Cultech
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This combination therapy targets dyslipidemia by utilizing two distinct mechanisms. Plant sterol esters, which are structurally similar to cholesterol, competitively inhibit the absorption of dietary and biliary cholesterol in the small intestine by interacting with the Niemann-Pick C1-like 1 (NPC1L1) transporter, thereby reducing low-density lipoprotein (LDL) cholesterol levels. Eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are long-chain omega-3 fatty acids that primarily reduce serum triglyceride levels. They act as agonists for peroxisome proliferator-activated receptor alpha (PPAR-alpha) and inhibit diacylglycerol O-acyltransferase (DGAT), leading to decreased hepatic very-low-density lipoprotein (VLDL) synthesis and increased fatty acid oxidation. This combination is widely used in dietary supplements and functional foods to provide a synergistic approach to cardiovascular health by addressing both cholesterol and triglyceride levels.

Brand names
Swanson Omega-3 & Plant SterolsBlackmores Cholesterol HealthCardio-Sterol
Other names
phytosterol esters + EPA + DHAomega-3 fatty acids + plant sterolsplant sterols + fish oil
02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)PPARA (Peroxisome proliferator-activated receptor alpha)DGAT1 (Diacylglycerol O-acyltransferase 1)SREBP-1 / SREBF1 (SREBP-1)

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