Bruton’s tyrosine kinase (Btk) plays a crucial role in B-cell development and activation through the B cell receptor signaling pathway. CC-292 [N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide] is a selective, Btk inhibitor and a sensitive and quantitative assay that determines whether CC-292-Btk engagement has been developed. Studies demonstrate that the quantity of Btk bound by CC-292 correlates with the efficacy of CC-292 in vitro and in collagen-induced arthritis model of autoimmune disease. Recently, CC-292 was incorporated into human clinical trials demonstrating that a single oral dose of 2 mg/kg CC-292 consistently had engaged in circulating Btk protein and provides the basis for rational dose selection in future clinical trials.
See article at J Pharmacol Exp Ther 2013, 346:219–228.
- Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics