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Ibrutinib and novel BTK inhibitors in clinical development

Akintunde Akinleye1, Yamei Chen12, Nikhil Mukhi1, Yongping Song3 and Delong Liu13*

Author Affiliations

1 Division of Hematology/Oncology, Department of Medicine, New York Medical College, Valhalla, New York 10595, USA

2 Department of Hematology, Xiamen Zhongshan Hospital, Xiamen University, Xiamen, China

3 Institute of Hematology, Zhengzhou University Affiliated Tumor Hospital, Zhengzhou, China

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Journal of Hematology & Oncology 2013, 6:59  doi:10.1186/1756-8722-6-59

Published: 19 August 2013


Small molecule inhibitors targeting dysregulated pathways (RAS/RAF/MEK, PI3K/AKT/mTOR, JAK/STAT) have significantly improved clinical outcomes in cancer patients. Recently Bruton’s tyrosine kinase (BTK), a crucial terminal kinase enzyme in the B-cell antigen receptor (BCR) signaling pathway, has emerged as an attractive target for therapeutic intervention in human malignancies and autoimmune disorders. Ibrutinib, a novel first-in-human BTK-inhibitor, has demonstrated clinical effectiveness and tolerability in early clinical trials and has progressed into phase III trials. However, additional research is necessary to identify the optimal dosing schedule, as well as patients most likely to benefit from BTK inhibition. This review summarizes preclinical and clinical development of ibrutinib and other novel BTK inhibitors (GDC-0834, CGI-560, CGI-1746, HM-71224, CC-292, and ONO-4059, CNX-774, LFM-A13) in the treatment of B-cell malignancies and autoimmune disorders.