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Autoimmune disease; inflammation; rheumatoid arthritis (RA)

CC chemokine receptor 1 (CCR1; CD191)

In vitro and mouse studies identified CCR1 antagonists that could help treat inflammation in RA and other diseases. Chemical synthesis, SAR and in vitro testing of 4-(4-chlorophenyl)piperidine analogs identified multiple compounds as selective nanomolar antagonists of CCR1. In a human monocyte chemotaxis assay, one of the lead compounds inhibited cell migration with a low nanomolar IC50 value. In mice, the compound showed good bioavailability and pharmacokinetics. Future studies could include testing the lead compound in animal models of RA.
CCX354, a small molecule CCR1 antagonist from ChemoCentryx Inc. and GlaxoSmithKline plc, has completed Phase II testing to treat RA.

SciBX 5(43); doi:10.1038/scibx.2012.1147
Published online Nov. 1, 2012

Patent and licensing status undisclosed

Cavallaro, C.L. et al. J. Med. Chem.; published online Oct. 17, 2012;
Contact: Cullen L. Cavallaro, Bristol-Myers Squibb Co., Princeton, N.J.