• PDF: Delivered by email usually within 4 to 8 UK business hours.

Epigenetics
Current and future applications that are driving novel drug discovery

  • Publication Date:August 2010
  • Publisher:Espicom
  • Product Type: Report
  • Pages:80
  • ISBN:978-1-85822-394-0

Epigenetics Current and future applications that are driving novel drug discovery

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.

With this report you can...

  • Understand the current thinking in respect to epigenetic mechanisms: DNA methylation, Chromatin remodelling/histone modifications and Non-coding RNA
  • Be 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

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.
  • Chapter 1 - Epigenetics Defined
    • Executive Summary
    • Epigenetics defined
    • Epigenetics defined
    • Epigenetic mechanisms
    • DNA methylation
    • Chromatin remodelling and histone modifications
    • Non-coding RNA
    • Unravelling the power of epigenetics
    • EXPERT COMMENTARY: Professor Stephan Beck, University College London Cancer Institute
    • Consortia for the study of epigenomics
    • Which epigenomes and what to study?
    • Applications of epigenomic data
    • New opportunities for biomarker discovery and drug targeting
    • Conclusion and report outline
  • Chapter 2 - Technical Challenges in Epigenetic R&D
    • Executive Summary
    • Technical challenges in epigenetic R&D
    • EXPERT COMMENTARY: Dr Chris Adams, Senior R&D Manager/Epigenetics, Life Technologies
    • next generation sequencing
    • DNA methylation
    • Chromatin structure and histone modifications
    • microRNA
    • Conclusion
  • Chapter 3 - Epigenetics in Drug Discovery & Development
    • Executive Summary
    • Epigenetics in drug discovery & development
    • Introduction
    • Epigenetics in cancer
    • Epigenetic drug targets in cancer: DNA methyltransferases
    • Epigenetic drug targets in cancer: HDAC inhibitors
    • Non-selective HDAC inhibitors
    • EXPERT COMMENTARY: Dr Bernd Hentsch, Chief Development Officer, 4SC AG
    • Selective HDAC inhibitors
    • EXPERT COMMENTARY: Dr David Simmons (CSO) & Dr Gitte Neubauer (VP Research Operations), Cellzome
    • beyond DNMT and HDAC inhibition: New targets
    • EXPERT COMMENTARY: Dr Robert Gould, CEO, Epizyme Inc
    • EXPERT COMMENTARY: Martin Bonde, CEO, EpiTherapeutics
    • Cancer the first frontier, where next?
    • Non-coding RNAs
    • EXPERT COMMENTARY: Dr. Andreas G. Bader, Associate Director of Research, Mirna Therapeutics, Inc.37
    • The future
  • Chapter 4 - Epigenetics in Clinical Diagnostics
    • Executive Summary
    • Epigenetics in clinical diagnostics
    • Introduction
    • DNA methylation patterns
    • Epigenomics AG
    • OncoMethylome Sciences
    • Orion Genomics
    • Histone modifications
    • miRNAs
    • Rosetta Genomics
    • Asuragen Diagnostics
    • Exiqon A/S
    • Biomarkers and personalised medicine
    • Outlook
  • Chapter 5 - Players, Alliances & Acquisitions
    • Executive Summary
    • Players, alliances & acquisitions
    • Company activities at a glance - Therapeutics
    • 4SC AG, Planegg-Martinsried, Germany
    • Acetylon Pharmaceuticals Inc, Boston, MA
    • Celgene Corporation, Summit, NJ
    • Celleron Therapeutics, Oxon, UK
    • Cellzome, Cambridge, UK, and Heidelberg, Germany
    • Curis Inc, Cambridge MA
    • Chroma Therapeutics Ltd, Oxon, UK
    • Constellation Pharmaceuticals, Cambridge, MA
    • EnVivo Pharmaceuticals, Watertown, MA
    • EpiTherapeutics Aps, Copenhagen, Denmark
    • Epizyme, Cambridge, MA
    • MethylGene, Inc. Montreal, Québec
    • Mirna Therapeutics, Austin, TX
    • miRagen Therapeutics, Boulder, CO
    • Pharmacyclics, Sunnyvale, CA
    • Progen Pharmaceuticals, Brisbane, Australia
    • Regulus Therapeutics, Torrey Pines, CA
    • Repligen Corporation, Waltham, MA
    • Santaris Pharma A/S, Denmark
    • SuperGen, Dublin, CA
    • Syndax Pharmaceuticals, Waltham, MA
    • TopoTarget, Copenhagen, Denmark
    • Alliances with market leaders - Therapeutics
    • Asuragen Inc, Austin, TX
    • Epigenomics AG, Berlin, Germany
    • Exiqon, Copenhagen, Denmark
    • OncoMethylome Sciences, Durham, NC
    • Orion Genomics, Saint Louis, MO
    • Rosetta Genomics, Rehovot, Israel
    • Alliances with market leaders - Diagnostics
    • Conclusion
  • Chapter 6 - Outlook & Future of Epigenetic Research
    • Executive Summary
    • Outlook & future of epigenetic research
    • Epigenetics research now
    • Therapeutic launches and new indications over the next 5 years
    • New combinations and a changing therapeutic paradigm in cancer
    • New diagnostic products
    • next generation sequencing
    • Epigenetics research in 5 to 10 years time
    • Therapeutic launches
    • Therapeutics and companion diagnostics for novel epigenetic targets
    • Epigenetics research more than 10 years from now
    • Conclusions
    • Glossary
    • Biography of the author
    • References
    • Endnotes
  • List of Tables
    • Table 1: Platforms for next generation sequencing
    • Table 2: Third generation sequencing platforms
    • Table 3: Methods for studying DNA methylation and their limitations
    • Table 4: Suppliers of research tools for the study of DNA methylation
    • Table 5: Suppliers of research tools for the study of histone and chromatin modifications
    • Table 6: Suppliers of research tools for the study of miRNA
    • Table 7: Approved drugs targeting DNMTs
    • Table 8: Pan-HDAC inhibitors in clinical development
    • Table 9: Selective HDAC inhibitors
    • Table 10: Companies developing drugs for novel epigenetic targets
    • Table 11: Companies developing therapeutics for epigenetic mechanisms in diseases other than cancer
    • Table 12: Companies developing therapeutic strategies related to miRNAs
    • Table 13: Therapeutic areas for miRNA-based therapeutic discovery
    • Table 14: Companies developing diagnostics to detect aberrant DNA methylation patterns
    • Table 15: Approved and developmental diagnostic products from Rosetta Genomics
    • Table 16: Exiqon's miRNA-based diagnostic pipeline
    • Table 17: Diagnostic/pharma partnerships for epigenetic biomarker discovery
    • Table 18: Areas of focus for companies developing drugs for epigenetic targets
    • Table 19: Alliances, acquisitions and mergers in the field of epigenetics since 2007
    • Table 20: Areas of focus for companies developing diagnostic tests based on epigenetics
    • Table 21: Revenues generated by Vidaza, Dacogen and Zolinza in 2009
    • Table 22: Examples of clinical trials of combinations of DNMTi, HDACi and chemotherapy
    • Table 23: Examples of clinical trials of drug combinations including panobinostat
    • Table 24: New diagnostic products identifying epigenetic biomarkers that will be launched to the market over the next few years69
  • List of Figures
    • Figure 1: Schematic showing the epigenetic mechanisms of DNA methylation and histone modification
    • Figure 2: Examples of covalent histone post-translational modifications
    • Figure 3: miRNA processing pathway
    • Figure 4: Schematic of a chromatin immunoprecipitation experiment
    • Figure 5: Proteins involved in the modification of histones
    • Figure 6: Number of drugs targeting epigenetic mechanisms by mechanism and stage of development
    • Figure 7: Epigenomics' development programme
    • Figure 8: OncoMethylome Sciences' development programme
    • Figure 9: Orion Genomics' product development pipeline
    • Figure 10: Progress in epigenetics related therapeutics and diagnostics over the next 5 years
    • Figure 11: Progress in epigenetics related therapeutics and diagnostics over the next 5 to 10 years
    • Figure 12: Progress in epigenetics-related therapeutics and diagnostics 10 years +
+44 20 8816 8548

Ask a question about Epigenetics

Enter the characters you see in the picture below
Captcha