Histone deacetylase inhibitors: Moving from the bench to a promising companion for classic and targeted cancer therapies

The field of histone deacetylase inhibitors is moving into a new phase of development. The exponential growth in the level of research activity surrounding the histone deacetylases (HDACs) witnessed over the past decade has now started to produce success in the clinic, particularly in the field of oncology. Over the next few years experts believe that as first generation HDAC inhibitors produce clinical benefits and second generation inhibitors are rationally designed with improved specificity, this class will emerge as a new class of cancer treatment.

This report published in 2005 by the drug development analysts LeadDiscovery introduces the concept of histone plasticity and the molecular control of transcription by histone deacetylases. The report continues with an overview of the histone deacetylases and a discussion of the therapeutic effects of their inhibitors. The report provides an in depth profile of HDAC inhibitors in development and concludes with a detailed analysis of the benefits to be gained through HDAC inhibition and the hurdles that must be negotiated by drug development organizations while advancing this field. LeadDiscovery ’s primary conclusion is that HDAC inhibitors offer the potential to synergize with both classic and targeted cancer therapies. The most advanced therapeutic candidates such as SAHA and FK228 are already showing promising activity. This potential should be further realized as rationally designed inhibitors developed by companies such as MethyGene and TopoTarget emerge whose pharmacological profile targets those histone deacetylases key to cancer progression.

The authors of Histone deacetylase inhibitors: Moving from the bench to a promising candidate for classic and targeted cancer therapies set out to take the mystery out of molecular biology while at the sam e time analyzing the potential and the pitfalls in this exciting field. The report is targeted at all involved in drug development extending from preclinical drug discovery personnel to business development managers and strategists.

Publication date: May, 2005

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