Showing posts with label Danirixin. Show all posts
Showing posts with label Danirixin. Show all posts

Sunday, October 30, 2016

Drugs in Clinical Pipeline: Danirixin | C-X-C Motif Chemokine Receptor 2 (CXCR2) Antagonist | CXCL8 (Interleukin-8) Antagonist | Management of Chronic Obstructive Pulmonary Disease (COPD)


Danirixin [(S)-1-(4-chloro-2-hydroxy-3-(piperidin-3-ylsulfonyl)phenyl)-3-(3-fluoro-2-methylphenyl)urea] is a small, selective and reversible antagonist for C-X-C motif chemokine receptor 2 (CXCR2, Interleukin 8 receptor, beta). It has high affinity for chemokine (C-X-C motif) ligand 8 (CXCL8) with nanomolar potency (IC50 for CXCL8 binding = 12.5 nM). The compound has demonstrated potent antagonism of CXCR2 activity in vitro and anti-inflammatory effects in various preclinical models [1, 2].



Structure of Danirixin. Intramolecular bond is predicted.
Danirixin: 2D and 3D Structure


The pharmacologic activity and duration of action following oral administration supports Danirixin’s potential use as an oral, anti-inflammatory agent in the treatment of disorders associated with the accumulation of neutrophils especially in development for treatment of chronic obstructive pulmonary disease (COPD).