Vimnerixin (AZD4721) is an orally administered CXCR2 antagonist for inflammation studies.

Vimnerixin (RIST4721) inhibited KC-stimulated chemotaxis in a dose-dependent manner. Vimnerixin at 10 nM and 100 nM significantly suppressed chemotaxis, while the inhibitory effect at 1 nM was not evident. Vimnerixin at 1 μM completely blocked KC-induced chemotaxis.

In preclinical studies, Vimnerixin underwent systematic pharmacokinetic evaluation in male Sprague-Dawley (SD) rats and beagle dogs via intravenous injection (1 mg/kg) and oral administration, with bile duct cannulation (BDC) experiments conducted to assess its excretion pathways. The results demonstrated that Vimnerixin exhibited low clearance rates (2.4 ml/min/kg in rats, 0.5 ml/min/kg in dogs), low volume of distribution (0.15–0.19 L/kg), and prolonged half-life (3.7 hours for intravenous administration in dogs, extending to 8.4 hours for oral administration). The plasma concentration-time curves were highly consistent between bile-duct-cannulated and non-cannulated groups, indicating minimal influence from enterohepatic circulation.