Mocetinostat: Difference between revisions
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'''Mocetinostat''' ('''MGCD0103''') is a [[benzamide]] [[histone deacetylase inhibitor]] undergoing [[clinical trial]]s for treatment of various cancers including [[follicular lymphoma]], [[Hodgkin's lymphoma]] and [[Acute myeloid leukemia|acute myelogenous leukemia]].<ref> |
'''Mocetinostat''' ('''MGCD0103''') is a [[benzamide]] [[histone deacetylase inhibitor]] undergoing [[clinical trial]]s for treatment of various cancers including [[follicular lymphoma]], [[Hodgkin's lymphoma]] and [[Acute myeloid leukemia|acute myelogenous leukemia]].<ref>{{cite press release | url=http://www.biospace.com/news_story.aspx?NewsEntityId=20794 | url-status=dead | title=Pharmion Corporation (PHRM) Release: Clinical Data On Oncology HDAC Inhibitor MGCD0103, Presented At The American Society of Clinical Oncology 42nd Annual Meeting | date=June 6, 2006 | publisher=BioSpace | location=Colorado, United States | archive-url=https://web.archive.org/web/20110716091432/http://www.biospace.com/news_story.aspx?NewsEntityId=20794 | archive-date=July 16, 2011 }}</ref><ref>{{cite conference | title=Phase I trials of the oral histone deacetylase (HDAC) inhibitor MGCD0103 given either daily or 3x weekly for 14 days every 3 weeks in patients (pts) with advanced solid tumors | author=Gelmon, K. | author2=Tolcher, A. | author3=Carducci, M. | author4=Reid, G. K. | author5=Li, Z. | author6=Kalita, A. | author7=Callejas, V. | author8=Longstreth, J. | author9=Besterman, J. M. | author10=Siu, L. L. | conference=2005 ASCO Annual Meeting. | journal=[[J. Clin. Oncol.]] | volume=23 | issue=16S | year=2005 | id=3147 | url=http://meeting.ascopubs.org/cgi/content/abstract/23/16_suppl/3147 | archive-url=https://archive.today/20120711180327/http://meeting.ascopubs.org/cgi/content/abstract/23/16_suppl/3147 | url-status=dead | archive-date=2012-07-11 }}</ref><ref>[http://www.earthtimes.org/articles/show/methylgene-to-resume-development-of-its-hdac-inhibitor-mgcd0103-mocetinostat,967740.shtml MethylGene to Resume Development of its HDAC Inhibitor, MGCD0103 (Mocetinostat)], Sept 2009</ref> |
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One clinical trial (for refractory [[follicular lymphoma]]) was temporarily put on hold due to cardiac problems but resumed recruiting in 2009.<ref>{{cite news |url=http://www.lifescience-online.com/METHYLGENE_TO_RESUME_DEVELOPMENT_OF_ITS_HDAC_INHIB,17766.html?portalPage=Lifescience+Today.News |
One clinical trial (for refractory [[follicular lymphoma]]) was temporarily put on hold due to cardiac problems but resumed recruiting in 2009.<ref>{{cite news |url=http://www.lifescience-online.com/METHYLGENE_TO_RESUME_DEVELOPMENT_OF_ITS_HDAC_INHIB,17766.html?portalPage=Lifescience+Today.News |title=METHYLGENE TO RESUME DEVELOPMENT OF ITS HDAC INHIBITOR, MGCD0103 (MOCETINOSTAT) |date=21 Sep 2009 |access-date=13 September 2010 |archive-url=https://web.archive.org/web/20120229053415/http://www.lifescience-online.com/METHYLGENE_TO_RESUME_DEVELOPMENT_OF_ITS_HDAC_INHIB,17766.html?portalPage=Lifescience+Today.News |archive-date=29 February 2012 |url-status=dead }}</ref> |
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In 2010 favourable results were announced from the phase II trial for [[Hodgkin's lymphoma]].<ref>{{cite news |url=http://www.sys-con.com/node/1637603 |title=Final Phase 2 Clinical Data for Mocetinostat (MGCD0103) in Relapsed/Refractory Hodgkin Lymphoma Patients |date=6 Dec 2010 }}</ref> |
In 2010 favourable results were announced from the phase II trial for [[Hodgkin's lymphoma]].<ref>{{cite news |url=http://www.sys-con.com/node/1637603 |title=Final Phase 2 Clinical Data for Mocetinostat (MGCD0103) in Relapsed/Refractory Hodgkin Lymphoma Patients |date=6 Dec 2010 }}</ref> |
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MGCD0103 has also been used as a research reagent where blockage of members of the HDAC-family of histone deacetylases is required.<ref name=pfefferli2014>{{cite journal | title=Specific NuRD components are required for fin regeneration in zebrafish | first1=Catherine | last1=Pfefferli | first2=Fritz | last2=Müller | first3=Anna | last3=Jaźwińska | first4=Chantal | last4=Wicky | journal=[[BMC Biol.]] | doi=10.1186/1741-7007-12-30 | volume=12 | issue=30 | pages=30 | year=2014 | pmid=24779377 | pmc=4038851 | doi-access=free }}{{open access}}</ref> |
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==Mechanism of action== |
==Mechanism of action== |
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It works by inhibiting mainly histone deacetylase 1 ([[HDAC1]]), but also [[HDAC2]], [[HDAC3]], and [[HDAC11]].<ref> |
It works by inhibiting mainly histone deacetylase 1 ([[HDAC1]]), but also [[HDAC2]], [[HDAC3]], and [[HDAC11]].<ref>{{Cite journal |last1=Fournel |first1=Marielle |last2=Bonfils |first2=Claire |last3=Hou |first3=Yu |last4=Yan |first4=Pu Theresa |last5=Trachy-Bourget |first5=Marie-Claude |last6=Kalita |first6=Ann |last7=Liu |first7=Jianhong |last8=Lu |first8=Ai-Hua |last9=Zhou |first9=Nancy Z. |last10=Robert |first10=Marie-France |last11=Gillespie |first11=Jeffrey |last12=Wang |first12=James J. |last13=Ste-Croix |first13=Hélène |last14=Rahil |first14=Jubrail |last15=Lefebvre |first15=Sylvain |date=2008-04-01 |title=MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity ''in vitro'' and ''in vivo'' |journal=Molecular Cancer Therapeutics |volume=7 |issue=4 |pages=759–768 |doi=10.1158/1535-7163.mct-07-2026 |issn=1535-7163|doi-access=free |pmid=18413790 }}</ref> |
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==References== |
==References== |
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{{ |
{{Reflist}} |
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{{HDAC inhibitors}} |
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[[Category:Pyrimidines]] |
[[Category:Pyrimidines]] |
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[[Category: |
[[Category:3-Pyridyl compounds]] |
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[[Category:Benzanilides]] |
[[Category:Benzanilides]] |
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[[Category:Histone deacetylase inhibitors]] |
[[Category:Histone deacetylase inhibitors]] |
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{{pharma-stub}} |
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[[de:Mocetinostat]] |