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A Fast and Clean BTK Inhibitor

Bruton’s tyrosine kinase (BTK) is a major drug target for B-cell related malignancies; however, existing BTK inhibitors approved for cancer treatment have significant off-targets that limit their use for autoimmune and inflammatory diseases. Remibrutinib (LOU064) is a novel covalent BTK inhibitor th...

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Detalles Bibliográficos
Autores principales: Gabizon, Ronen, London, Nir
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7304894/
https://www.ncbi.nlm.nih.gov/pubmed/32401033
http://dx.doi.org/10.1021/acs.jmedchem.0c00597
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author Gabizon, Ronen
London, Nir
author_facet Gabizon, Ronen
London, Nir
author_sort Gabizon, Ronen
collection PubMed
description Bruton’s tyrosine kinase (BTK) is a major drug target for B-cell related malignancies; however, existing BTK inhibitors approved for cancer treatment have significant off-targets that limit their use for autoimmune and inflammatory diseases. Remibrutinib (LOU064) is a novel covalent BTK inhibitor that binds an inactive BTK conformation, which affords it unprecedented selectivity. Its optimization led to rapid BTK engagement in vivo and fast clearance, further limiting systemic exposure. Remibrutinib is currently in phase 2 clinical trials for treatment of chronic urticaria and Sjoegren’s syndrome.
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spelling pubmed-73048942020-06-22 A Fast and Clean BTK Inhibitor Gabizon, Ronen London, Nir J Med Chem Bruton’s tyrosine kinase (BTK) is a major drug target for B-cell related malignancies; however, existing BTK inhibitors approved for cancer treatment have significant off-targets that limit their use for autoimmune and inflammatory diseases. Remibrutinib (LOU064) is a novel covalent BTK inhibitor that binds an inactive BTK conformation, which affords it unprecedented selectivity. Its optimization led to rapid BTK engagement in vivo and fast clearance, further limiting systemic exposure. Remibrutinib is currently in phase 2 clinical trials for treatment of chronic urticaria and Sjoegren’s syndrome. American Chemical Society 2020-05-13 2020-05-28 /pmc/articles/PMC7304894/ /pubmed/32401033 http://dx.doi.org/10.1021/acs.jmedchem.0c00597 Text en Copyright © 2020 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
spellingShingle Gabizon, Ronen
London, Nir
A Fast and Clean BTK Inhibitor
title A Fast and Clean BTK Inhibitor
title_full A Fast and Clean BTK Inhibitor
title_fullStr A Fast and Clean BTK Inhibitor
title_full_unstemmed A Fast and Clean BTK Inhibitor
title_short A Fast and Clean BTK Inhibitor
title_sort fast and clean btk inhibitor
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7304894/
https://www.ncbi.nlm.nih.gov/pubmed/32401033
http://dx.doi.org/10.1021/acs.jmedchem.0c00597
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