Mocetinostat

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]

Mocetinostat
Names
Preferred IUPAC name
N-(2-Aminophenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide
Identifiers
CAS Number
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
PubChem CID
UNII
InChI
  • 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
SMILES
  • C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
Properties
Chemical formula
 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).
N verify (what is YN ?)
Infobox references

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.
  7. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo


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