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Mocetinostat

From Wikipedia, the free encyclopedia
Mocetinostat
Names
Preferred IUPAC name
N-(2-Aminophenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
KEGG
UNII
  • InChI=1S/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29) ☒N
    Key: HRNLUBSXIHFDHP-UHFFFAOYSA-N ☒N
  • InChI=1/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29)
    Key: HRNLUBSXIHFDHP-UHFFFAOYAW
  • C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
Properties
C23H20N6O
Molar mass396.454 g·mol−1
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is checkY☒N ?)
Chemical compound

Mocetinostat (MGCD0103) is abenzamidehistone deacetylase inhibitor undergoingclinical trials for treatment of various cancers includingfollicular lymphoma,Hodgkin's lymphoma andacute 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]
  1. ^"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 original on July 16, 2011.
  2. ^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 original on 2012-07-11.
  3. ^MethylGene to Resume Development of its HDAC Inhibitor, MGCD0103 (Mocetinostat), Sept 2009
  4. ^"METHYLGENE TO RESUME DEVELOPMENT OF ITS HDAC INHIBITOR, MGCD0103 (MOCETINOSTAT)". 21 Sep 2009. Archived fromthe original on 29 February 2012. Retrieved13 September 2010.
  5. ^"Final Phase 2 Clinical Data for Mocetinostat (MGCD0103) in Relapsed/Refractory Hodgkin Lymphoma Patients". 6 Dec 2010.
  6. ^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.PMC 4038851.PMID 24779377.Open access icon
  7. ^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 vitro andin vivo".Molecular Cancer Therapeutics.7 (4):759–768.doi:10.1158/1535-7163.mct-07-2026.ISSN 1535-7163.PMID 18413790.
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