Ibrutinib: Difference between revisions
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<StructureSection load='' size='340' side='right' caption=' | <StructureSection load='' size='340' side='right' caption='Ibrutinib' scene='99/997914/Cv/1'> | ||
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.<ref name="a5">[https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0dfd0279-ff17-4ea9-89be-9803c71bab44 "Imbruvica- ibrutinib capsule Imbruvica- ibrutinib tablet, film coated".] DailyMed. 8 April 2020. Retrieved 21 April 2020.</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> See also [https://en.wikipedia.org/wiki/Ibrutinib Ibrutinib]. | 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.<ref name="a5">[https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0dfd0279-ff17-4ea9-89be-9803c71bab44 "Imbruvica- ibrutinib capsule Imbruvica- ibrutinib tablet, film coated".] DailyMed. 8 April 2020. Retrieved 21 April 2020.</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> See also [https://en.wikipedia.org/wiki/Ibrutinib Ibrutinib]. | ||
<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 <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 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/> | ||
Latest revision as of 12:42, 17 January 2024
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.[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.