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. Author manuscript; available in PMC: 2020 Jan 31.
Published in final edited form as: Curr Opin Hematol. 2019 Jan;26(1):28–33. doi: 10.1097/MOH.0000000000000476

Table 1.

Commonly used CXCR2 chemical antagonists

Name Structure Model Therapeutic use or clinical trial Reference
Danirixin 1-[4-chloro-2-hydroxy-3-[(3S)-piperidin-3-yl] sulfonylphenyl]-3-(3-fluoro-2-methylphenyl)urea Rat Phase II for COPD [41-43]
SCH527123 (MK-7123) 2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobuten-1-yl]amino]benzamide Mouse, rat Phase II for COPD, asthma, traumatic brain injury, breast cancer, pancreatic cancer, acute-on-chronic liver failure [44-46]
Reparixin (2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide Rat, mouse, and pig Phase II for kidney and lung transplantation, metastatic breast cancer;
Phase III for pancreatic islet transplantation in type 1 diabetes
[47-51]
AZD5069 N-(2-((2,3-difluorobenzyl)thio)-6-(((2R,3S)-3,4-dihydroxybutan-2-yl)oxy)pyrimidin-4-yl)azetidine-1-sulfonamide Monkey Phases Ib and II for head and neck cancer, metastatic castration-resistant prostate cancer;
Phase II for asthma, COPD, bronchiectasis, coronary artery disease
[39,52-55]
AZD8309 (R)-5-[[(2,3-difluorophenyl)methyl]thio]-7-[(2-hydroxy-1-methylethyl)amino]-thiazolo[4,5-d]pyrimidin-2(3H)-one Mouse Phase I for rheumatoid arthritis, COPD, pancreatitis [56,57]
G31P 6-Chloronicotinamide N-oxide 4a Mouse, rat, and guinea pig Aspiration pneumonia; ischemia and reperfusion injury; lung cancer; mastitis lesions; diabetic nephropathy; UAN kidneys; hepatocellular carcinoma; prostate cancer; ulcerative colitis [58-61]
Ladarixin (1,1-dioxo-1λ6-thiomorpholin-4-yl)-{6-[3-(4-fluoro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-pyridin-3-yl}-methanone Mouse Type 1 diabetes [62]

COPD, chronic obstructive pulmonary disease; UAN, uric acid nephropathy.