Mocetinostat
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(Redirected fromMGCD0103)
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Preferred IUPAC name
N-(2-Aminophenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide | |
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Properties | |
C23H20N6O | |
Molar mass | 396.454g·mol−1 |
Except where otherwise noted, data are given for materials in theirstandard state(at 25 °C [77 °F], 100 kPa).
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Mocetinostat(MGCD0103) is abenzamidehistone deacetylase inhibitorundergoingclinical trialsfor treatment of various cancers includingfollicular lymphoma,Hodgkin's lymphomaandacute myelogenous leukemia.[1][2][3]
One clinical trial (for refractoryfollicular lymphoma) was temporarily put on hold due to cardiac problems but resumed recruiting in 2009.[4]
In 2010 favourable results were announced from the phase II trial forHodgkin's lymphoma.[5]
MGCD0103 has also been used as a research reagent where blockage of members of the HDAC-family of histone deacetylases is required.[6]
Mechanism of action
[edit]It works by inhibiting mainly histone deacetylase 1 (HDAC1), but alsoHDAC2,HDAC3,andHDAC11.[7]
References
[edit]- ^"Pharmion Corporation (PHRM) Release: Clinical Data On Oncology HDAC Inhibitor MGCD0103, Presented At The American Society of Clinical Oncology 42nd Annual Meeting"(Press release). Colorado, United States: BioSpace. June 6, 2006. Archived fromthe originalon July 16, 2011.
- ^Gelmon, K.; Tolcher, A.; Carducci, M.; Reid, G. K.; Li, Z.; Kalita, A.; Callejas, V.; Longstreth, J.; Besterman, J. M.; Siu, L. L. (2005).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.2005 ASCO Annual Meeting.J. Clin. Oncol.Vol. 23, no. 16S. 3147. Archived fromthe originalon 2012-07-11.
- ^MethylGene to Resume Development of its HDAC Inhibitor, MGCD0103 (Mocetinostat),Sept 2009
- ^"METHYLGENE TO RESUME DEVELOPMENT OF ITS HDAC INHIBITOR, MGCD0103 (MOCETINOSTAT)".21 Sep 2009. Archived fromthe originalon 29 February 2012.Retrieved13 September2010.
- ^"Final Phase 2 Clinical Data for Mocetinostat (MGCD0103) in Relapsed/Refractory Hodgkin Lymphoma Patients".6 Dec 2010.
- ^Pfefferli, Catherine; Müller, Fritz; Jaźwińska, Anna; Wicky, Chantal (2014)."Specific NuRD components are required for fin regeneration in zebrafish".BMC Biol.12(30): 30.doi:10.1186/1741-7007-12-30.PMC4038851.PMID24779377.
- ^Fournel, Marielle; Bonfils, Claire; Hou, Yu; Yan, Pu Theresa; Trachy-Bourget, Marie-Claude; Kalita, Ann; Liu, Jianhong; Lu, Ai-Hua; Zhou, Nancy Z.; Robert, Marie-France; Gillespie, Jeffrey; Wang, James J.; Ste-Croix, Hélène; Rahil, Jubrail; Lefebvre, Sylvain (2008-04-01)."MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activityin vitroandin vivo".Molecular Cancer Therapeutics.7(4): 759–768.doi:10.1158/1535-7163.mct-07-2026.ISSN1535-7163.PMID18413790.