Target intelligence / Profile preview

Eicosanoid system

Molecular classification
Enzyme, G protein-coupled receptor, Lipid signaling pathway
01

Overview

The eicosanoid system is a complex network of bioactive lipid mediators derived from 20-carbon fatty acids, primarily arachidonic acid [1]. These mediators, including prostaglandins, thromboxanes, and leukotrienes, function as autocrine and paracrine signaling molecules that regulate inflammation, vascular tone, and platelet aggregation [2]. The system is characterized by three major enzymatic pathways: the cyclooxygenase (COX) pathway, the lipoxygenase (LOX) pathway, and the cytochrome P450 pathway [3]. Dysregulation of these pathways is central to the pathogenesis of various inflammatory diseases, asthma, and cardiovascular conditions [4]. Pharmacological modulation of the eicosanoid system is a cornerstone of modern medicine, utilizing drugs like NSAIDs to block prostaglandin synthesis or leukotriene modifiers to treat respiratory ailments [5]. However, because these pathways are interconnected, inhibiting one branch can lead to the "biochemical shunting" of substrates into others, potentially causing adverse effects like aspirin-induced asthma [1].

Other names
Arachidonic acid cascadeEicosanoid signaling pathwayProstanoid and leukotriene systemsEicosanoid systems
02

Mechanism of action

Drugs targeting this system primarily function through the competitive or irreversible inhibition of biosynthetic enzymes (e.g., COX-1, COX-2, 5-LOX) or by acting as competitive antagonists at downstream G protein-coupled receptors (e.g., CysLT1, TP receptors) [1][4].

03

Biological functions

InflammationPlatelet aggregationSmooth muscle contractionPain signalingRenal blood flow regulationGastric mucosal protection
04

Disease associations

InflammationAsthmaCardiovascular diseaseRheumatoid arthritisColorectal cancerPain
05

Safety considerations

Gastrointestinal ulceration and perforationIncreased risk of thrombotic cardiovascular eventsRenal papillary necrosis and acute kidney injuryAspirin-exacerbated respiratory disease (AERD)Reye's syndrome in children
06

Interacting drugs

Aspirin

8 more in the full profile.

07

Biomarkers

Prostaglandin E2 (PGE2)Thromboxane B2 (TXB2)Leukotriene E4 (LTE4)11-dehydro-thromboxane B2

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