Mocetinostat Explained

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]

Notes and References

1. Pharmion Corporation (PHRM) Release: Clinical Data On Oncology HDAC Inhibitor MGCD0103, Presented At The American Society of Clinical Oncology 42nd Annual Meeting . dead . June 6, 2006 . BioSpace . Colorado, United States . https://web.archive.org/web/20110716091432/http://www.biospace.com/news_story.aspx?NewsEntityId=20794 . July 16, 2011 .
2. 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 . Gelmon, K. . Tolcher, A. . Carducci, M. . Reid, G. K. . Li, Z. . Kalita, A. . Callejas, V. . Longstreth, J. . Besterman, J. M. . Siu, L. L. . 2005 ASCO Annual Meeting. . . 23 . 16S . 2005 . 3147 . https://archive.today/20120711180327/http://meeting.ascopubs.org/cgi/content/abstract/23/16_suppl/3147 . dead . 2012-07-11 .
3. 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)
4. News: METHYLGENE TO RESUME DEVELOPMENT OF ITS HDAC INHIBITOR, MGCD0103 (MOCETINOSTAT) . 21 Sep 2009 . 13 September 2010 . 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 . 29 February 2012 . dead .
5. News: Final Phase 2 Clinical Data for Mocetinostat (MGCD0103) in Relapsed/Refractory Hodgkin Lymphoma Patients . 6 Dec 2010 .
6. Specific NuRD components are required for fin regeneration in zebrafish . Catherine . Pfefferli . Fritz . Müller . Anna . Jaźwińska . Chantal . Wicky . . 10.1186/1741-7007-12-30 . 12 . 30 . 30 . 2014 . 24779377 . 4038851 . free .
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 . 10.1158/1535-7163.mct-07-2026 . 1535-7163. free . 18413790 .