Ibrutinib: Difference between revisions
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<scene name='99/997914/Overall/1'>Tyrosine-protein kinase BTK with Ibrutinib</scene> ([[5p9j]]). | <scene name='99/997914/Overall/1'>Tyrosine-protein kinase BTK with Ibrutinib</scene> ([[5p9j]]). | ||
<scene name='99/997914/Binding_site/3'>Ibrutinib binding site</scene>. Water molecules are shown as red spheres. brutinib is a potent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK). The acrylamide group of ibrutinib forms a covalent bond with the cysteine residue C481 in the BTK active site, leading to sustained inhibition of BTK enzymatic activity. BTK is an important signalling molecule of the B-cell antigen receptor (BCR) pathway, which is plays a role in the pathogenesis of several B-cell malignancies including mantle cell lymphoma (MCL), diffuse large B-cell lymphoma (DLBCL), follicular lymphoma, and chronic lymphocytic leukemia (CLL). Preclinical studies have shown that ibrutinib effectively inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.</ref><ref name="a6">[https://www.ema.europa.eu/en/medicines/human/EPAR/imbruvica "Imbruvica EPAR".] European Medicines Agency (EMA). 8 July 2021. Retrieved 14 July 2021.</ref> | <scene name='99/997914/Binding_site/3'>Ibrutinib binding site</scene>. Water molecules are shown as red spheres. brutinib is a potent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK). The <scene name='99/997914/Covalent/1'>acrylamide group of ibrutinib forms a covalent bond with the cysteine residue C481 in the BTK active site</scene>, leading to sustained inhibition of BTK enzymatic activity. BTK is an important signalling molecule of the B-cell antigen receptor (BCR) pathway, which is plays a role in the pathogenesis of several B-cell malignancies including mantle cell lymphoma (MCL), diffuse large B-cell lymphoma (DLBCL), follicular lymphoma, and chronic lymphocytic leukemia (CLL). Preclinical studies have shown that ibrutinib effectively inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.</ref><ref name="a6">[https://www.ema.europa.eu/en/medicines/human/EPAR/imbruvica "Imbruvica EPAR".] European Medicines Agency (EMA). 8 July 2021. Retrieved 14 July 2021.</ref> | ||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 16:20, 8 October 2023
Ibrutinib, sold under the brand name Imbruvica among others, is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly binding the protein Bruton's tyrosine kinase (BTK). Blocking BTK inhibits the B-cell receptor pathway, which is often aberrantly active in B cell cancers. Ibrutinib is therefore used to treat such cancers, including mantle cell lymphoma, chronic lymphocytic leukemia, and Waldenström's macroglobulinemia.[1][2] See also Ibrutinib. (5p9j). . Water molecules are shown as red spheres. brutinib is a potent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK). The , leading to sustained inhibition of BTK enzymatic activity. BTK is an important signalling molecule of the B-cell antigen receptor (BCR) pathway, which is plays a role in the pathogenesis of several B-cell malignancies including mantle cell lymphoma (MCL), diffuse large B-cell lymphoma (DLBCL), follicular lymphoma, and chronic lymphocytic leukemia (CLL). Preclinical studies have shown that ibrutinib effectively inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.</ref>[2]
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ReferencesReferences
- ↑ "Imbruvica- ibrutinib capsule Imbruvica- ibrutinib tablet, film coated". DailyMed. 8 April 2020. Retrieved 21 April 2020.
- ↑ 2.0 2.1 "Imbruvica EPAR". European Medicines Agency (EMA). 8 July 2021. Retrieved 14 July 2021.