Drug intelligence / Profile preview

benzo-lipoxin A4 methyl ester

Development stage
Phase 2
Lead developer
Brigham and Women's Hospital
Modality
Small Molecules
Administration
Topical, Intravenous, Intraperitoneal
01

Overview

Benzo-lipoxin A4 methyl ester is a synthetic, metabolically stable analog of the endogenous specialized pro-resolving mediator (SPM) Lipoxin A4 (LXA4). Naturally occurring LXA4 is rapidly inactivated by 15-hydroxyprostaglandin dehydrogenase (15-PGDH); however, the benzo-analog incorporates a benzene ring into the carbon chain, which confers resistance to metabolic degradation while preserving biological potency. The molecule acts as a high-affinity agonist of the Formyl peptide receptor 2 (FPR2), also known as the ALX receptor. Its mechanism involves the active resolution of inflammation by inhibiting the recruitment and activation of neutrophils (PMNs) and promoting the non-phlogistic phagocytosis of apoptotic cells by macrophages. The methyl ester modification serves as a prodrug to enhance cellular permeability and bioavailability, which is subsequently hydrolyzed by intracellular esterases to the active acid form. It is primarily used as a research tool and has shown efficacy in preclinical models of inflammatory diseases such as periodontitis, asthma, and acute lung injury.

Brand names
ClinRinse-1ClinRinse1ClinRinse 1
Other names
benzo-lipoxin A4 methyl esterbenzo-LXA4 methyl esterbenzo-LXA-4 methyl esterbenzo-LXA 4 methyl esterbenzo-LXA4 methyl ester prodrugbenzo-LXA-4 methyl ester prodrugbenzo-LXA 4 methyl ester prodrug
02

Targets

FPR2 (Formyl peptide receptor type 2)

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