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Epigenetics


Current and future applications that are driving novel drug discovery

August 16th 2010

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Epigenetics is an active and exciting area of research that is being driven by the massive amounts of new information being generated by currently available research tools, the potential for effective new therapies in areas of unmet medical need and new diagnostic, screening or pharmacoepigenomic tests.

Significant investment is being made into basic research and will enable standardised, whole epigenome maps that will be freely available for additional research and analysis. This research will develop our understanding of the interplay between different epigenetic mechanisms, and has the potential to uncover new drug targets.

Commercially available products – current and near term
The development of new drugs and diagnostics based on our understanding of epigenetic mechanisms and the ways in which they cause changes in gene expression, is an area of research which has produced commercial products. Whilst four drugs have already been marketed in this area, these represent the tip of the iceberg. Scientists have now identified large numbers of individual enzymes responsible for making specific alterations to histones and these are the focus of drug discovery efforts. miRNA is also a growing field in terms of both therapeutic and diagnostic development.

In addition to the four currently marketed drugs for epigenetic targets, more than six additional drugs will reach the marketplace over the next decade. These first generation products will be replaced in the longer-term by more selective inhibitors of a wide range of novel epigenetic targets such as histone methylases and demethylases, histone acetylases, and readers (bromodomains and chromodomains).

Broadening the therapeutic horizon
Current pan- and class-selective histone deacetylase inhibitors will be improved upon by the next generation of selective inhibitors. These offer perhaps the greatest potential as they may be applicable outside the oncology arena where the burden of toxicity must be low. The development of this generation of targeted compounds will be undertaken alongside companion diagnostic tests, helping to generate the best outcomes for individual patients in the future.

Epigenetic Biomarkers
Over the next five years a number of new diagnostic tests will enter the market based on the identification of epigenetic biomarkers. These tests will focus on cancer and will progress from tissue or fine needle aspirate-based diagnostic tests, to far less invasive bodily fluid (blood, sputum, urine) based screening. Prognostic markers that will guide treatment decisions are also on the radar. Further into the future these tests will broaden into therapeutic areas other than cancer.

More Information...

Expert opinions from...

    • Professor Stephan Beck University College London Cancer Institute

    • Dr Chris Adams

      Senior R&D Manager/ Epigenetics, Life Technologies

    • Dr Bernd Hentsch
      Chief Development Officer,
      4SC AG

    • Dr David Simmons (CSO) &
      Dr Gitte Neubauer
      (VP Research Operations), Cellzome

    • Dr Robert Gould

      CEO, Epizyme Inc

    • Martin Bonde

      CEO, EpiTherapeutics

    • Dr Andreas Bader

      Associate Director of Research, Mirna Therapeutics, Inc.