BMS-986142

Description: BMS-986142, a carbazole and tetrahydrocarbazole based compound, is a novel, potent and highly selective reversible Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 0.5 nM. Bruton's tyrosine kinase (BTK), a nonreceptor tyrosine kinase, is a member of the Tec family of kinases. BTK plays an essential role in B cell receptor (BCR)-mediated signaling as well as Fcgamma receptor signaling in monocytes and Fcepsilon receptor signaling in mast cells and basophils, all of which have been implicated in the pathophysiology of autoimmune disease. As a result, inhibition of BTK is anticipated to provide an effective strategy for the clinical treatment of autoimmune diseases such as lupus and rheumatoid arthritis. With significantly enhanced potency and selectivity, excellent in vivo properties and efficacy, and a very desirable tolerability and safety profile, BMS-986142 has been advanced into clinical studies.

References: PLoS One. 2017 Jul 24; 12(7):e0181782; J Med Chem. 2016 Oct 13; 59(19):9173-9200.