Drug intelligence / Profile preview

resolvin e1

Development stage
Phase 1
Lead developer
Thetis Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Topical, Ophthalmic, Oral, Rectal, Intravenous, Inhalation, Intranasal, Intraperitoneal
01

Overview

Resolvin E1 is an endogenous lipid mediator derived from the omega-3 fatty acid eicosapentaenoic acid (EPA). It is a specialized pro-resolving mediator (SPM) with potent anti-inflammatory and pro-resolving actions. Resolvin E1 acts by binding to specific G protein-coupled receptors such as ChemR23 (ERV1/ChemR23) on monocytes/macrophages and Leukotriene B4 receptor BLT1 on neutrophils. Its mechanism of action includes reducing neutrophil infiltration at sites of inflammation, promoting macrophage-mediated clearance of apoptotic cells and microorganisms, enhancing phagocytosis-induced neutrophil apoptosis via caspase activation pathways, and counter-regulating proinflammatory gene expression. Resolvin E1 has shown efficacy in preclinical models for conditions such as peritonitis, retinopathy, periodontitis, colitis/intestinal inflammation, acute lung injury/ALI and neuroinflammation. A phase I clinical trial in healthy volunteers has been completed[2][5][6][7][8].

Other names
5S,12R,18R-trihydroxy-6Z,8E,10E,14Z,16E-eicosapentaenoic acidresolvin E1
02

Targets

LTB4R (Leukotriene B4 Receptor 1)CMKLR1 (Chemokine-like receptor 1)

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