Reportlinker Adds Innovations In Epigenetics: Advances in Technologies, Diagnostics & Therapeutics

Jan 19, 2010, 08:13 ET from Reportlinker

NEW YORK, Jan. 19 /PRNewswire/ -- announces that a new market research report is available in its catalogue:

Innovations In Epigenetics: Advances in Technologies, Diagnostics & Therapeutics

The study of epigenetics - changes in gene expression that occur without a change in a cell's DNA code – is becoming increasingly important as scientists explore how internal and external factors trigger cellular dysfunction and influence disease progression. Three main mechanisms - DNA methylation, histone modifications and changes in non-coding RNA - have been elucidated in epigenetics. Each in its own way may provide the industry with a greater understanding into the underlying mechanism of diseases, act as a potential source for biomarkers of disease and provide new targets for therapeutic intervention.

Besides everyday DNA analytical tools, epigenetic researchers have needed to adopt more complex technologies such as chromatin immunoprecipitation (ChIP) and DNA methylation methodologies as well as develop analytical tools to decipher the vast amount of epigenetic information. Advances in these technologies should enable epigenetic research to reduce cost and increase sample throughput making it more commercially attractive in the industry to discover biomarkers and validate novel epigenetic targets for diagnostic and pharmacological development.

Epigenetic medicine has arrived. The market is worth over $560 million derived from the sale of three anticancer products which target two epigenetic pathways - DNA methyltransferase (DNMT) and histone deacteylase (HDAC) – and around thirty epigenetic drugs are under development from more than a dozen biotechnology companies. These drugs focus mainly on the treatment of cancer, neurodegenerative and infectious diseases although research is underway to explore the role for epigenetics in cardiovascular, metabolic, ocular and other diseases. Whilst this market is still in its infancy KOLs believe it is on the cusp of a revolution, one which could change how patients are diagnosed and treated in the future.

Key features of this report

  • Identify leading companies at the forefront of epigenetic research who will drive the market to develop a new generation of epigenetic therapies and diagnostics.
  • Provide case studies of these leading companies developing epigenetic therapies to treat cancer, neurodegenerative and infectious diseases.
  • Analyze the key trends and issues confronting the development of epigenetic therapies.
  • Review the alliances, mergers, acquisitions and business strategies adopted by biotechs and big pharma to capitalize on the latest epigenetic developments.

Scope of this report

  • Identify the companies leading the field in epigenetic research across a range of therapeutic areas
  • Review their business strategies and the development of their epigenetic programs
  • Learn more about the latest developments in epigenetic research and how non-coding RNAs may open up another Pandora's box for epigenetic research.
  • Identify innovative pharmaceutical companies and discover the strategies they are adopting to tap into the epigenetic potential both as biomarkers of disease and targets for therapeutic intervention

Key Market Issues

  • Declining industry productivity: It is a well documented fact that productivity in the pharma industry has declined during the past 15 years. The identification of new biomarkers of disease could aide the R&D process and support the preclinical and clinical development of small molecule therapeutics.
  • Innovative new drug classes: The identification of underlying mechanisms of diseases could identify new target for small molecule therapeutic intervention that may be used alone or in combination with traditional therapies to extend their usage.

Key findings from this report

  • New epigenetic therapies have entered the market. The first medicines were approved in 2006 for the treatment of cancer and a host of new small molecule therapies are now under development which are more selective and target different classes of chromatin modifying enzymes enabling a more targeted approach to treatment.
  • The ability of innovative companies to generate intellectual property is a key driver for the sector as the market become more competitive in this new area of science. The unraveling of the human epigenome will be the first step in identifying new epigenetic markers which may have potential as biomarkers an area of considerable interest for the pharmaceutical industry at the present time.

Key questions answered

  • Which companies are the market leaders in the epigenetics industry, identified through therapeutic areas (cancer, infectious diseases, neurodegenerative diseases, metabolic, cardiovascular, ophthalmic, other diseases) and recent alliances with the pharmaceutical companies?
  • What are the key products of these companies and how do they exemplify the future direction of the epigenetic therapies?
  • How is the pharmaceutical industry approaching the need for new targeted epigenetic therapies and what strategies are they taking?

Table of Contents

Innovations in Epigenetics

Executive summary 10

Introduction 10

Application in R&D & technological advances 10

Exploring new therapeutic targets 11

Epigenetic market, leading companies & pharmaceutical strategies 12

The future of epigenetics 13

Chapter 1 Introduction 16

What is epigenetics? 17

Epigenetics and phenotypes 19

Epigenetics a new biological paradigm 19

Epigenetics, genetics, genomics & pharmacogenomics 20

Molecular mechanisms associated with epigenetics 22

DNA methylation 22

Histone modifications 23

Nucleosome remodeling 23

Non-coding RNA 24

X chromosome inactivation 24

Gene imprinting 24

RNA interference 24

Epigenetic basis of disease 25

Epigenetic syndromes 25

Angelmann syndrome 25

Beckwith-Wiedemann syndrome 26

Prader-Willi syndrome 26

Why is epigenetics of interest to the pharmaceutical industry? 27

Biomarker discovery & diagnostics 28

Novel small molecule epigenetic therapeutics 28

Novel antisense therapeutics 28

Stem cells & regenerative medicines 29

Conclusions 29

Chapter 2 Application in R&D & technological advances 32

The application of epigenetics in drug R&D 33

DNA methylation biomarkers 34

Histone modification biomarkers 35

Technological advances in epigenetics 35

Chromatin immunoprecipitation 36

DNA methylation technologies 38

Non-coding RNA technologies 43

Bioinformatic modeling 43

Conclusions 44

Chapter 3 Exploring new therapeutic targets 48

Potential new therapeutic targets 49

Epigenetics in cancer 50

DNA methyltransferase & DNMT inhibitors 52

Case study: Vidaza (Celgene Corporation) & Dacogen (Eisai /J&J) 53

Case study: Zebularine a research tool 56

Histone acetylase (HAT) and histone deacetylase (HDAC) 59

Case study: Zolinza (Merck & Co.) 61

Case study: MGCD0103 (MethylGene/Taiho Pharmaceutical) 62

Case study: PCI-24781 (Pharmacyclics/Servier) 63

Histone demethylases and histone methyltranserases 65

Case study: PG11144 & PG11047 (Progen Pharmaceuticals) 66

Potential epigenetic based diagnostics 67

Diagnostic DNA methylation cancer biomarkers 67

Case study: Epi proColon (Epigenomics AG) 69

The next generation of epigenetic cancer biomarkers 71

Epigenetics in neurological disorders 72

Case study: EVP-0334 (EnVivo Pharmaceuticals) 73

Epigenetics in infectious diseases 75

Case study: MGCD290 (MethylGene) 75

Case study: siRNA targeting HIV-1 (Kevin Morris, Scripps, La Jolla) 76

Epigenetics in metabolic disorders 78

Epigenetics in cardiovascular disease 81

Epigenetics in ocular disorders 83

Case study: Kinase inhibitors (Otsuka Pharmaceutical/MethylGene) 84

Case study: Kinase inhibitors/S-adenosyl methionine (SAM) (Epizyme). 85

Conclusions 86

Chapter 4 Epigenetic market, leading companies & pharmaceutical strategies 90

Epigenetic market 91

Epigenetic therapeutic revenues: Now and the future 92

Leading epigenetic companies 93

4SC AG, Planegg-Martinsried, Germany 94

Celgene Corporation, Summit, New Jersey 95

Curis Inc, Cambridge, MA 96

Chroma Therapeutics Ltd, Oxon, UK 98

Constellation Pharmaceuticals, Cambridge, MA 99

EnVivo Pharmaceuticals, Watertown, MA 100

EpiTherapeutics Aps, Copenhagen, Denmark 101

Epizyme, Cambridge, MA 101

Gloucester Pharmaceuticals, Cambridge, MA 103

MethylGene, Inc. Montreal, Québec 104

Pharmacyclics, Sunnyvale, CA 106

Progen Pharmaceuticals, Brisbane, Australia 107

Repligen Corporation, Waltham, MA 108

SuperGen, Dublin, CA 109

Syndax Pharmaceuticals, Waltham, MA 112

TopoTarget, Copenhagen, Denmark 113

Summary of epigenetic-based companies 114

Recent alliances, mergers & acquisitions in epigenetics 115

Pharmaceutical strategies in epigenetics 118

GlaxoSmithKline, Middlesex, UK 118

Novartis, Basel, Switzerland 119

Merck & Co., Whitehouse, NJ 121

Eisai Corporation of North America, NJ 122

Takeda, Osaka, Japan 123

Overall conclusions 123

Chapter 5 The future of epigenetics 126

The future of epigenetics 127

Epigenetic consortia; unraveling the human epigenome 128

NIH's Roadmap Epigenomics Program initiative 128

European Epigenome Network of Excellence 130

Human Epigenome Consortium 130

KOLs in epigenetics 131

John Mattick, Institute for Molecular Bioscience, University of Queensland,

Australia 132

Overview 132

Technology 133

Applications 133

Future 134

Kevin Morris, Scripps Institute, La Jolla, CA 134

Overview 134

Technology 135

Applications 135

Future 136

Monika Lachner, Max-Planck Institute of Immunobiology, Department of

Epigenetics, Freiburg, Germany 136

Overview 136

Technology 136

Applications 137

Future 137

Johnathan Whetstine, Department of Medicine, Massachusetts General

Hospital Cancer Center 137

Overview 138

Technology 138

Applications 138

Future 139

Peter Fraser, Head, Senior Fellow of the Medical Research Council, UK, The

Babraham Institute, Cambridge 139

Overview 139

Technology 140

Applications 140

Future 141

Summary of KOLs commentary 141

Challenges 142

Fundamental research 142

Technological demands 142

Financial constraints 143

Intellectual property 144

Opportunities 144

Biomarker discovery & diagnostics 144

Therapeutic intervention 145

Regenerative medicines 145

Conclusions 146

Chapter 6 Appendices 150

Glossary 150

Acknowledgements 156

Index 157

Index 157

Bibliography 159

Endnotes 165

List of Figures

Figure 1.1: Timeline of epigenetics study 18

Figure 1.2: Schematic of chromatin structure 22

Figure 1.3: Schematic of epigenetic mechanisms associated with health and disease 23

Figure 1.4: Epigenetic applications by the pharma industry 27

Figure 2.5: Epigenetics in the drug discovery & development process 34

Figure 2.6: Schematic of key technologies used in epigenetics 36

Figure 2.7: Schematic of ChIP technology 37

Figure 2.8: Epigenomics AG methylation specific PCR (MSP) methods 42

Figure 3.9: DNA methylation targets for epigenetic cancer therapies 51

Figure 3.10: Mechanism of action of HAT and HDAC 61

Figure 3.11: Epi proColon high throughput colorectal epigenetic test 70

Figure 3.12: Competitive pricing of Epi proColon 71

Figure 3.13: EnVivo's HDAC project screening cascade 74

Figure 3.14: Agouti mice and epigenetic manipulation 79

Figure 3.15: Epizyme's rational design of small molecule HMT inhibitors 85

Figure 4.16: Epigenetic therapies: product class and developmental phase 91

Figure 4.17: Epigenetic therapies: therapy target and developmental phase 92

Figure 4.18: CUDU-101 structure & design: combining multiple pharmacophores 97

List of Tables

Table 2.1: DNA methylation PCR methods 40

Table 2.2: Techniques to analyze DNA methylation 41

Table 3.3: Examples of DNMT inhibitors: potential anticancer agents targeting epigenetic pathways 54

Table 3.4: Examples of DNMT inhibitor research tools 55

Table 3.5: HDAC inhibitors: potential anticancer agents targeting epigenetic pathways 57

Table 3.6: Examples of HDAC inhibitor research tools 59

Table 3.7: Histone modification and their effect on gene expression 60

Table 3.8: Safety profiles of PCI-24781 rivals 64

Table 3.9: DNA methylation sites associated with cancers 67

Table 3.10: Validated and hypothetic miRNA targets for diabetes & obesity 81

Table 4.11: Epigenetic therapeutic revenues ($m), 2009-2020 93

Table 4.12: Preliminary clinical data for Pharmacyclics PCI-24781 106

Table 4.13: Recent alliances, acquisitions and mergers in the epigenetic arena 117

Table 5.14: NIH Epigenetic Roadmap – funded epigenetic projects 129

To order this report:

Genomics Industry: Innovations In Epigenetics: Advances in Technologies, Diagnostics & Therapeutics

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