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Journal of Hematology & Oncology
Published in: Journal of Hematology & Oncology 1/2016

Open Access 01-12-2016 | Review

Second-generation inhibitors of Bruton tyrosine kinase

Authors: Jingjing Wu, Christina Liu, Stella T. Tsui, Delong Liu

Published in: Journal of Hematology & Oncology | Issue 1/2016

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Abstract

Bruton tyrosine kinase (BTK) is a critical effector molecule for B cell development and plays a major role in lymphoma genesis. Ibrutinib is the first-generation BTK inhibitor. Ibrutinib has off-target effects on EGFR, ITK, and Tec family kinases, which explains the untoward effects of ibrutinib. Resistance to ibrutinib was also reported. The C481S mutation in the BTK kinase domain was reported to be a major mechanism of resistance to ibrutinib. This review summarizes the clinical development of novel BTK inhibitors, ACP-196 (acalabrutinib), ONO/GS-4059, and BGB-3111.
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Metadata
Title
Second-generation inhibitors of Bruton tyrosine kinase
Authors
Jingjing Wu
Christina Liu
Stella T. Tsui
Delong Liu
Publication date
01-12-2016
Publisher
BioMed Central
Published in
Journal of Hematology & Oncology / Issue 1/2016
Electronic ISSN: 1756-8722
DOI
https://doi.org/10.1186/s13045-016-0313-y

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