Second-generation inhibitors of Bruton tyrosine kinase

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. Re...

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Detalles Bibliográficos
Autores principales: Wu, Jingjing, Liu, Christina, Tsui, Stella T., Liu, Delong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2016
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5010774/
https://www.ncbi.nlm.nih.gov/pubmed/27590878
http://dx.doi.org/10.1186/s13045-016-0313-y
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author Wu, Jingjing
Liu, Christina
Tsui, Stella T.
Liu, Delong
author_facet Wu, Jingjing
Liu, Christina
Tsui, Stella T.
Liu, Delong
author_sort Wu, Jingjing
collection PubMed
description 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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spelling pubmed-50107742016-09-04 Second-generation inhibitors of Bruton tyrosine kinase Wu, Jingjing Liu, Christina Tsui, Stella T. Liu, Delong J Hematol Oncol Review 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. BioMed Central 2016-09-02 /pmc/articles/PMC5010774/ /pubmed/27590878 http://dx.doi.org/10.1186/s13045-016-0313-y Text en © The Author(s). 2016 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Review
Wu, Jingjing
Liu, Christina
Tsui, Stella T.
Liu, Delong
Second-generation inhibitors of Bruton tyrosine kinase
title Second-generation inhibitors of Bruton tyrosine kinase
title_full Second-generation inhibitors of Bruton tyrosine kinase
title_fullStr Second-generation inhibitors of Bruton tyrosine kinase
title_full_unstemmed Second-generation inhibitors of Bruton tyrosine kinase
title_short Second-generation inhibitors of Bruton tyrosine kinase
title_sort second-generation inhibitors of bruton tyrosine kinase
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5010774/
https://www.ncbi.nlm.nih.gov/pubmed/27590878
http://dx.doi.org/10.1186/s13045-016-0313-y
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