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Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist. 2011
Chu-Biao Xue, and
Hao Feng, and
Ganfeng Cao, and
Taisheng Huang, and
Joseph Glenn, and
Rajan Anand, and
David Meloni, and
Ke Zhang, and
Lingquan Kong, and
Anlai Wang, and
Yingxin Zhang, and
Changsheng Zheng, and
Michael Xia, and
Lihua Chen, and
Hiroyuki Tanaka, and
Qi Han, and
D J Robinson, and
Dilip Modi, and
Lou Storace, and
Lixin Shao, and
Vaqar Sharief, and
Mei Li, and
Laurine G Galya, and
Maryanne Covington, and
Peggy Scherle, and
Sharon Diamond, and
Tom Emm, and
Swamy Yeleswaram, and
Nancy Contel, and
Kris Vaddi, and
Robert Newton, and
Greg Hollis, and
Steven Friedman, and
Brian Metcalf
Incyte Corporation , Experimental Station E336, Wilmington, Delaware 19880, United States.
We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors, and acceptable oral bioavailability in rodents and primates. In human clinical trials, INCB3284 exhibited a pharmacokinetic profile suitable for once-a-day dosing (T 1/2 = 15 h).
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