Publications

Bruton’s tyrosine kinase (BTK) is a part of the cytokine signalling pathways involved in malignancies and autoimmune disorders.. Akinleye et al. provide a review of all the current BTK inhibitors in preclinical and clinical trials for B-cell malignancies and autoimmune disorders, including rheumatoid arthritis. Particular focus is placed on ibrutinib, a novel human BTK-inhibitor, currently in phase III clinical trials. The authors also discuss four new compounds with potential indications in rheumatoid arthritis; GDC-0834, a reversible BTK inhibitor with nanomolar activity; RN-486, another small molecule with reversible inhibitory properties and subnanomolar activities; CGI-1746, a unique BTK inhibitor that inhibits both auto- and trans-phosphorylation of BTK and ONO-4059, an orally available BTK inhibitor which has shown a high level of potency.