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Ibrutinib and novel BTK inhibitors in clinical development

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 eme...

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Autores principales: Akinleye, Akintunde, Chen, Yamei, Mukhi, Nikhil, Song, Yongping, Liu, Delong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3751776/
https://www.ncbi.nlm.nih.gov/pubmed/23958373
http://dx.doi.org/10.1186/1756-8722-6-59
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author Akinleye, Akintunde
Chen, Yamei
Mukhi, Nikhil
Song, Yongping
Liu, Delong
author_facet Akinleye, Akintunde
Chen, Yamei
Mukhi, Nikhil
Song, Yongping
Liu, Delong
author_sort Akinleye, Akintunde
collection PubMed
description 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.
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spelling pubmed-37517762013-08-24 Ibrutinib and novel BTK inhibitors in clinical development Akinleye, Akintunde Chen, Yamei Mukhi, Nikhil Song, Yongping Liu, Delong J Hematol Oncol Review 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. BioMed Central 2013-08-19 /pmc/articles/PMC3751776/ /pubmed/23958373 http://dx.doi.org/10.1186/1756-8722-6-59 Text en Copyright © 2013 Akinleye et al.; licensee BioMed Central Ltd. http://creativecommons.org/licenses/by/2.0 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review
Akinleye, Akintunde
Chen, Yamei
Mukhi, Nikhil
Song, Yongping
Liu, Delong
Ibrutinib and novel BTK inhibitors in clinical development
title Ibrutinib and novel BTK inhibitors in clinical development
title_full Ibrutinib and novel BTK inhibitors in clinical development
title_fullStr Ibrutinib and novel BTK inhibitors in clinical development
title_full_unstemmed Ibrutinib and novel BTK inhibitors in clinical development
title_short Ibrutinib and novel BTK inhibitors in clinical development
title_sort ibrutinib and novel btk inhibitors in clinical development
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3751776/
https://www.ncbi.nlm.nih.gov/pubmed/23958373
http://dx.doi.org/10.1186/1756-8722-6-59
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