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CGI-1746 is a selective and potent inhibitor of Bruton's tyrosine kinase (BTK) with IC50 value of 1.9 nM [1][2].

Bruton's tyrosine kinase (BTK) is a member of the Tec tyrosine kinase family and plays an important role in differentiation, proliferation and development of B cells. It is an attractive target for the treatment of immunological disorders such as B-cell malignancies, rheumatoid arthritis (RA), multiple sclerosis (MS) and lupus [3].

CGI-1746 potently inhibits both auto- and transphosphorylation of BTK. It binds to un-phosphorylated BTK and stabilizes it in an inactive enzyme state. In cellular assays, CGI-1746 blocks BCR-mediated B-cell proliferation and suppresses the production of IL-6, IL-1βand TNF in macrophages [1].

In experimental mouse models, CGI-1746 shows a robust anti-arthritic activity [1]. In B10.RIII mice model, CGI1746 resulted in a significant inhibition (97%) of clinical arthritis scores, which were better than dexamethasone treatment (56% inhibition) [2].

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