Drug intelligence / Profile preview

Elsibucol

Development stage
Unknown
Lead developer
AtheroGenics
Modality
Small Molecules
Administration
Oral
01

Overview

Elsibucol (AGI-1096) is a novel oral small molecule antioxidant and selective anti-inflammatory agent developed to address accelerated inflammation of grafted blood vessels, known as transplant arteritis, which is common in chronic organ transplant rejection. It is a phenolic intracellular antioxidant with anti-inflammatory and antiproliferative properties. Mechanistically, it inhibits the inducible expression of vascular cell adhesion molecule 1 (VCAM-1), E-selectin, and monocyte chemoattractant protein 1 (MCP-1) in endothelial cells; it also suppresses tumor necrosis factor alpha (TNF-alpha) and interleukin-1 beta secretion from LPS-stimulated peripheral blood mononuclear cells. Additionally, it inhibits serum-stimulated proliferation of aortic smooth-muscle cells. Preclinical studies demonstrated its efficacy in reducing transplant arteriosclerosis in animal models[1][2][3][4][5].

Other names
216167-95-2O7T92N1Y8TO-7T92N1Y8TO 7T92N1Y8T
02

Targets

VCAM1 (Vascular cell adhesion molecule 1)IL1B (Interleukin-1 beta)TNFA (Tumor necrosis factor alpha (soluble))SELE (E-selectin)

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