Epigenetics: Current and future applications that are driving novel drug discovery

Published Date: 16/08/2010
Category: Drug Discovery & Development

Research Report Decription

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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.

Key Questions Answered:

With this report you can...

• Understand the current thinking in respect to epigenetic mechanisms: DNA methylation, Chromatin remodelling/histone modifications and Non-coding RNABe up-to-date with the technical challenges facing epigenetic research
• Evaluate the developments and impact on epigenetics of the latest generation sequencing technology
• Review the companies and projects that are targeting all three epigenetic mechanisms
• Easily assess the use of epigenetics in the development of clinical diagnostics
• Review the players, alliances and acquisitions in this fast growing area.
• Who’s developing what in key areas and what approaches are they taking?
• Assess the future development of epigenetic research with an evaluation of potential applications in disease areas other than cancer.
• Consider the scope and range of epigenetic research in 5 years time

Companies Mentioned:

4SC AG, Asuragen, Acetylon Pharmaceuticals, Celgene Corporation, Celleron Therapeutics, Cellzome, Chroma Therapeutics, Constellation Pharmaceuticals, Curis, EnVivo Pharmaceuticals, EpiTherapeutics Aps, Epizyme, Epigenomics AG, Exiqon, MethylGene, Mirna Therapeutics, miRagen Therapeutics, OncoMethylome Sciences, Orion Genomics, Pharmacyclics, Planegg-Martinsried, Progen Pharmaceuticals, Regulus Therapeutics, Repligen Corporation, Rosetta Genomics, Santaris Pharma A/S, SuperGen, Syndax Pharmaceuticals, TopoTarget

Paper Highlights:

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.