Ibrutinib - Revision history

Michal Harel at 09:42, 17 January 2024

Michal Harel — Wed, 17 Jan 2024 09:42:07 GMT

←Older revision		Revision as of 09:42, 17 January 2024
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-	<StructureSection load='' size='340' side='right' caption='~~Caption for this structure~~' scene='99/997914/Cv/1'>	+	<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].

Alexander Berchansky at 13:21, 8 October 2023

Alexander Berchansky — Sun, 08 Oct 2023 13:21:41 GMT

←Older revision		Revision as of 13:21, 8 October 2023
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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 <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>	+	<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/>

Alexander Berchansky at 13:20, 8 October 2023

Alexander Berchansky — Sun, 08 Oct 2023 13:20:43 GMT

←Older revision		Revision as of 13:20, 8 October 2023
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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/>

Alexander Berchansky at 13:17, 8 October 2023

Alexander Berchansky — Sun, 08 Oct 2023 13:17:31 GMT

←Older revision		Revision as of 13:17, 8 October 2023
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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.[6]	+	<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>

	</StructureSection>		</StructureSection>
	== References ==		== References ==
	<references/>		<references/>

Alexander Berchansky at 13:16, 8 October 2023

Alexander Berchansky — Sun, 08 Oct 2023 13:16:35 GMT

←Older revision		Revision as of 13:16, 8 October 2023
Line 4:		Line 4:
	<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.	+	<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.[6]

	</StructureSection>		</StructureSection>
	== References ==		== References ==
	<references/>		<references/>

Alexander Berchansky at 14:36, 5 October 2023

Alexander Berchansky — Thu, 05 Oct 2023 14:36:46 GMT

←Older revision		Revision as of 14:36, 5 October 2023
Line 4:		Line 4:
	<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/2'>Ibrutinib binding site</scene>. Water molecules are shown as red spheres.	+	<scene name='99/997914/Binding_site/3'>Ibrutinib binding site</scene>. Water molecules are shown as red spheres.

	</StructureSection>		</StructureSection>
	== References ==		== References ==
	<references/>		<references/>

Alexander Berchansky at 14:34, 5 October 2023

Alexander Berchansky — Thu, 05 Oct 2023 14:34:54 GMT

←Older revision		Revision as of 14:34, 5 October 2023
Line 3:		Line 3:

	<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/2'>Ibrutinib binding site</scene>. Water molecules are shown as red spheres.

	</StructureSection>		</StructureSection>
	== References ==		== References ==
	<references/>		<references/>

Alexander Berchansky at 14:18, 5 October 2023

Alexander Berchansky — Thu, 05 Oct 2023 14:18:58 GMT

←Older revision		Revision as of 14:18, 5 October 2023
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	<StructureSection load='' size='340' side='right' caption='Caption for this structure' scene='99/997914/Cv/1'>		<StructureSection load='' size='340' side='right' caption='Caption for this structure' 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]]).

	</StructureSection>		</StructureSection>
	== References ==		== References ==
	<references/>		<references/>

Alexander Berchansky at 13:43, 5 October 2023

Alexander Berchansky — Thu, 05 Oct 2023 13:43:53 GMT

←Older revision		Revision as of 13:43, 5 October 2023
Line 1:		Line 1:
	<StructureSection load='' size='340' side='right' caption='Caption for this structure' scene='99/997914/Cv/1'>		<StructureSection load='' size='340' side='right' caption='Caption for this structure' 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].

	</StructureSection>		</StructureSection>
	== References ==		== References ==
	<references/>		<references/>

Alexander Berchansky at 13:35, 4 October 2023

Alexander Berchansky — Wed, 04 Oct 2023 13:35:39 GMT

←Older revision		Revision as of 13:35, 4 October 2023
Line 1:		Line 1:
	<StructureSection load='' size='340' side='right' caption='Caption for this structure' scene='99/997914/Cv/1'>		<StructureSection load='' size='340' side='right' caption='Caption for this structure' 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>	+	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].

	</StructureSection>		</StructureSection>
	== References ==		== References ==
	<references/>		<references/>