Target intelligence / Profile preview

Eicosapentaenoic acid (EPA)

Target
EPA
Molecular classification
Other (Omega-3 polyunsaturated fatty acid), Not classified as receptor/enzyme/transporter/etc.
01

Overview

Eicosapentaenoic acid (EPA) is an essential long-chain omega‑3 polyunsaturated fatty acid found primarily in cold-water fish oils. Chemically designated C20H30O2 with five cis double bonds along its carbon chain, it serves both structural and signaling roles within the body. As an integral component of cell membranes—especially within cardiovascular tissues—it acts as a precursor for anti-inflammatory eicosanoids including prostaglandin E₃ and thromboxane A₃. Clinically, purified ethyl esters of EPA are approved therapies for lowering elevated triglyceride levels and reducing residual cardiovascular risk among statin-treated patients with mixed dyslipidemia. Its mechanisms involve modulation of lipid metabolism pathways and reduction in inflammatory mediator synthesis via competition with arachidonic-acid-derived substrates. While widely available through diet or supplements—including prescription formulations like Vascepa—its use should be monitored due to potential interactions affecting coagulation parameters.

Other names
EPAIcosapentaenoic acidTimnodonic acidall cis-5,8,11,14,17-Eicosapentaenoic AcidOmega 3 eicosapentaenoic acid
02

Mechanism of action

Reduces hepatic production/secretion of very low-density lipoproteins/triglycerides. Alters cell membrane composition to favor anti-inflammatory eicosanoid production over pro-inflammatory ones. Inhibits cyclooxygenase and lipoxygenase pathways leading to less potent inflammatory mediators compared to arachidonic-acid-derived analogues. Reduces platelet aggregation by increasing prostaglandin I₃ synthesis.

03

Biological functions

Precursor for eicosanoids (prostaglandin 3-series, thromboxane 3-series, leukotriene 5-series)Component of cell membrane phospholipidsModulation of inflammation (anti-inflammatory effects)Regulation of blood lipid levels (triglycerides)Inhibition of platelet aggregation
04

Disease associations

Cardiovascular disease (prevention/reduction of risk factors such as hypertriglyceridemia)Inflammation-related diseases: Rheumatoid arthritisInflammation-related diseases: PsoriasisInflammation-related diseases: AsthmaInflammation-related diseases: Atherosclerosis/atherogenic dyslipidemiaCancer prevention/adjunctive therapy in some cancers [lung cancer/prostate cancer/supportive care during chemotherapy]
05

Safety considerations

Increased bleeding risk at high doses due to antiplatelet effectsPotential gastrointestinal side effectsRarely atrial fibrillation/flutter reported at high dosesMay affect LDL cholesterol slightly; monitoring recommended when treating hypertriglyceridemia patients on statins
06

Interacting drugs

Icosapent ethyl (Vascepa)

2 more in the full profile.

07

Biomarkers

EPA levels in plasma/red blood cellsOmega‑3 indexConsumption of salt-water fishTriglyceride levels (clinical endpoint)

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