Drug intelligence / Profile preview

lipoxin A4

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intrathecal, Ophthalmic, Topical, Inhalation, Intravenous, Intraperitoneal
01

Overview

Lipoxin A4 is an endogenous lipid mediator derived from arachidonic acid metabolism. It is a trihydroxy eicosatetraenoic acid with potent anti-inflammatory and pro-resolving properties. Lipoxin A4 acts by modulating leukocyte activity—reducing neutrophil recruitment and activation while promoting the resolution of inflammation. It also inhibits natural killer cell cytotoxicity and can activate protein kinase C. At higher concentrations it binds to the aryl hydrocarbon receptor (AHR) and estrogen receptor alpha (ERα), influencing gene transcription related to xenobiotic metabolism and inflammatory responses[2][3][5]. Lipoxin A4 has shown potential therapeutic effects in conditions such as radicular pain[1], diabetic retinopathy[4], gingivitis (as analogs)[7], airway hyper-responsiveness[3], and other inflammatory diseases.

Other names
lipoxin A4LXA4LXA-4LXA 4Lipoxin A5S,6R-LipoxinA489663-86-5 (CAS)15-epi-lipoxin A4 (for the epimer)5(S),6(R)-Lipoxin A4
02

Targets

FPR2 (Formyl peptide receptor type 2)AHR (Aryl hydrocarbon receptor)ESR1 (ERα)

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