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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
BioMed Central
2013
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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. |
format | Online Article Text |
id | pubmed-3751776 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | BioMed Central |
record_format | MEDLINE/PubMed |
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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