Mocetinostat

Last updated
Mocetinostat
Mocetinostat.png
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
PubChem CID
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) X mark.svgN
    Key: HRNLUBSXIHFDHP-UHFFFAOYSA-N X mark.svgN
  • 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 mass 396.454 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Mocetinostat (MGCD0103) is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers including follicular lymphoma, Hodgkin's lymphoma and acute myelogenous leukemia. [1] [2] [3]

One clinical trial (for refractory follicular 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 for Hodgkin'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

It works by inhibiting mainly histone deacetylase 1 (HDAC1), but also HDAC2, HDAC3, and HDAC11. [7]

References

  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 from the 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 from the 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 from the original on 29 February 2012. Retrieved 13 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 logo PLoS transparent.svg
  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 activity in vitro and in 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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