Basis for targeting BTK

The CGI Pharmaceuticals Inc. unit of Gilead Sciences Inc. and Roche's Genentech Inc. unit have jointly identified a new inhibitor of the tyrosine kinase BTK andelucidated two BTK-mediated inflammatory pathways involved in arthritis.¹ The data give mechanistic validation to small molecule BTK inhibitors in clinical development from Avila Therapeutics Inc. and Pharmacyclics Inc. and also describe a distinct mode of inhibition that could be exploited in developing new compounds targeting the kinase.

Bruton's tyrosine kinase (BTK), a member of the Tec family of tyrosine kinases, is involved in both cancer and autoimmune diseases like rheumatoid arthritis (RA). Despite the links to multiple diseases, BTK's biological role is not well understood because a lack of highly selective BTK inhibitors has impeded efforts to tease out the kinase's function...