A wealth of new epigenetic drugs

November 27, 2012

While there are only four FDA-approved drugs that target the epigenome, there are a large number in various stages of development, as explained by Dr. Peter Ordentlich at the Third World Epigenetics Summit held in Boston in July, 2012. Ordentlich, who is VP of Translational Medicine at Syndax Pharmaceuticals mentioned a number of molecules that are in various stages, ranging from preclinical development to phase III clinical trials.

Almost all of these compounds are in anti-cancer trials; their mode of action is most frequently through demethylation of controller elements next to tumor suppressor genes. This allows the tumor suppressors to become activated, blocking the growth and expansion of tumor cells.

There are seven DNA methyltransferase inhibitors, including two that have reached Phase II. Among 28 histone deacetylase inhibitors are 13 in Phase II, and two, panobinostat and belinostat that are in Phase III. There are two bromodomain inhibitors in in Phase II, and six in the discovery phase. There are 16 lysine methyl transferase and histone de-methylase inhibitors, all in preclinical discovery.

As this information was gathered several months ago, there are likely a number of others moving down the pipeline. These numbers bode well for the advancement of this therapeutic approach.

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