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Innovations Epigenetics: advances in technology, business Aarkstore Diagnostics and Therapeutics
DNA methylation Three main mechanisms – Modifications of histones and changes in noncoding RNA – have been elucidated in epigenetics. Each in its own way the industry can provide a greater understanding of the mechanism of an underlying disease, act as a potential source of biomarkers of disease and provide new targets for therapeutic intervention.
In addition to the tools of DNA from each day of analysis, epigenetics researchers have needed to adopt more complex technologies such as immunoprecipitation chromatin (chip) and DNA methylation methodologies and develop analytical tools to decipher the vast amount of epigenetic information. Advances in these technologies should allow investigation Epigenetics reduce costs and increase the samples to make it more commercially attractive in the industry to discover and validate novel targets epigenetic biomarkers for the development of diagnostics and drugs.
epigenetic drugs has arrived. The market is over 560 million dollars from the sale of three anticancer drugs that target the two epigenetic pathways – DNA methyltransferase (Dnmt) and histone deacteylase (HDAC) – Thirty epigenetic drugs are in development for more than a dozen biotechnology companies. These drugs are focused on cancer treatment neurodegenerative diseases and infectious diseases, although research is ongoing to explore the role of epigenetics in diseases of the cardiovascular parameters, metabolic, and others. Although this market is still in its infancy that KOL is on the verge of a revolution, one that could change the way patients are diagnosed and treated in the future.
The main features of this report
• Identify the leading companies in the vanguard of research in epigenetics, which lead the market to develop a new generation of epigenetic therapies and diagnostics.
• Provide case studies leading companies in the development of epigenetic therapies to treat cancer, neurodegenerative diseases and infectious diseases.
• Analyze the main trends and issues facing the development of epigenetic therapies.
• Review of alliances, mergers, acquisitions and corporate strategies adopted by biotechnology and pharmaceutical companies to take advantage of recent major advances in epigenetics.
Scope of this report
• Identify the leading companies in the area of epigenetic research in a range of therapeutic areas
• Strategies Company for review and development of epigenetic programs
• Learn about the latest advances in epigenetic research and how non-coding RNAs may open the Pandora's box of other epigenetic research.
• Identify and explore innovative pharmaceutical companies to adopt strategies to exploit both the potential epigenetic biomarkers of disease and targets for therapeutic intervention
Key Market Issues
• The productivity of industry in decline: It is well documented that productivity in the pharmaceutical industry has declined in the last 15 years. The process of identifying new biomarkers of disease could help the R & D and support the preclinical development and clinical therapy of small molecules.
• innovative new drugs classes: Identification of mechanisms underlying diseases may identify new targets
small molecule therapeutic intervention that can be used alone or in combination with traditional therapies
extend their use.
The main conclusions of this report
• The new epigenetic therapies came on the market. The first drugs were approved in 2006 for the treatment of cancer and a host of new therapies for small molecules are currently being developed that are more selective and target different classes of modifying enzymes chromatin to allow a more coordinated approach to treatment.
• The ability of companies to generate innovative intellectual property is a key factor for the sector in the market to be more competitive in this new field of science. The dismantling of the human epigenome is the first step in identifying new markers epigenetic biomarkers that have potential as an area of considerable interest to the pharmaceutical industry present.
Key questions answered
• Which companies are market leaders in the industry Epigenetics identified in therapeutic areas (cancer, infectious diseases, diseases neurodegenerative, metabolic, cardiovascular, ophthalmologic, other diseases) and recent alliances with pharmaceutical companies?
• What are the main products of these companies and how they illustrate the future direction of epigenetic therapy?
• How the pharmaceutical industry to address the need for new epigenetic therapies directed and what strategies are being?
Content:
Content
Innovations Epigenetics
Executive Summary 10
Introduction 10
Implementation in R & D and technological progress 10
Exploring new therapeutic targets 11
Epigenetics market, major pharmaceutical companies and strategies 12
The future of epigenetics 13
Chapter 1 Introduction 16
What is Epigenetics? 17
Epigenetics and 19 phenotypes
Epigenetic a new biological paradigm 19
Epigenetics, genetics, genomics, pharmacogenomics and 20
Epigenetic molecular mechanisms associated with 22
DNA methylation 22
23 histone modifications
Nucleosome remodeling 23
RNA 24 noncoding
X chromosome inactivation 24
Gene footprint 24
RNA Interference 24
epigenetic basis of disease 25
Epigenetics 25 syndromes
25 Angelmann syndrome
The Beckwith-Wiedemann syndrome 26
on 26 Prader-Willi
Why interest to epigenetic the pharmaceutical industry? 27
biomarker discovery and diagnosis 28
New therapeutic small molecule epigenetic 28
Novel 28 antisense therapeutic
Stem cells and regenerative medicine 29
Conclusions 29
Chapter 2 Implementation in R & D and technological progress 32
The application of epigenetics in drug R & D 33
DNA methylation biomarkers 34
histone modification biomarkers 35
Technological advances 35 in the epigenetic
36 Chromatin immunoprecipitation
38 DNA methylation technologies
No encryption technology NRA 43
Bioinformatics 43 models
Conclusions 44
Chapter 3 Exploring new therapeutic targets 48
Possible new therapeutic targets 49
The 50 epigenetics in cancer
DNA methyltransferase Dnmt inhibitors and 52
Case study of Vidaza (Celgene Corporation) and Dacogen (Eisai / J & J) 53
Case Study: 56 Zebularine search
Histone acetyltransferase (HAT) and histone deacetylase (HDAC) 59
Case Study: Zolinza (Merck & Co.) 61
Case study of MGCD0103 (MethylGene / Taiho Pharmaceutical) 62
Case study: PCI-24781 (Pharmacyclics / Servier) 63
Histone demethylases and methyltranserases 65 histone
Case study of PG11144 PG11047 & (Progen Pharmaceuticals) 66
Potential diagnosis based on epigenetic 67
The diagnosis of cancer of DNA methylation 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 (pharmaceuticals ENVIVO) 73
Epigenetics in infectious diseases 75
Case Study: MGCD290 (MethylGene) 75
Case Study: siRNA against HIV-1 (Kevin Morris, of Scripps, La Jolla) 76
Epigenetic disorders 78 metabolic
Epigenetics cardiovascular disease in 81
Epigenetics in ocular disorders 83
Case Study: kinase inhibitors (Otsuka Pharmaceutical / MethylGene) 84
Case Study: inhibitors of the kinase / S-adenosyl methionine (SAM) (Epizyme). 85
Conclusions 86
Chapter 4 Market epigenetic major pharmaceutical companies and strategies 90
91 Epigenetics Market
income epigenetic therapy: Present and future 92
93 leading companies epigenetic
4SC AG, Planegg-Martinsried, Germany 94
Celgene Corporation, Summit, New Jersey 95
Curis Inc., Cambridge, MA 96
Chroma Therapeutics Ltd., Oxon, United Kingdom 98
Constellation Pharmaceuticals, Cambridge, MA 99
ENVIVO Pharmaceuticals, Watertown, MA 100
EpiTherapeutics Apps, Copenhagen, Denmark 101
Epizyme, Cambridge, MA 101
Gloucester Pharmaceuticals, Cambridge, MA 103
MethylGene Inc. Montreal Quebec 104
Pharmacyclics, Sunnyvale, CA 106
Progen Pharmaceuticals, Brisbane, Australia 107
Repligen Corporation, Waltham, MA 108
SuperGen, Dublin, CA 109
Pharmaceuticals Syndax, Waltham, MA 112
TopoTarget, Copenhagen, Denmark 113
Summary of epigenetic-based companies 114
Recent alliances, mergers and acquisitions in epigenetic 115
118 epigenetic drug strategies
GlaxoSmithKline, Middlesex, United Kingdom 118
Novartis, Basel, Switzerland 119
Merck & Co., Whitehouse, NJ 121
Eisai Corporation of North America, 122 NJ
Takeda, Osaka, Japan 123
World Opinion 123
Chapter 5 The future 126 of epigenetics
The future of epigenetics 127
Epigenetic partnerships; unravel the human epigenome 128
NIH Roadmap Epigenomics Program Initiative 128
European Network of Excellence Epigenome 130
Human Epigenome Consortium 130
Epigenetic KOL 131
John Mattick, Institute for Molecular Biosciences University of Queensland,
Australia 132
Overview 132
Technology 133
133 Applications
Future 134
Kevin Morris of the Institute Scripps, La Jolla, CA 134
Overview 134
Technology 135
135 Applications
Future 136
Monika Lachner, Max-Planck Immunobiology Department
Epigenetics, Freiburg, Germany 136
Overview 136
Technology 136
137 Applications
Future 137
Whetstine Johnathan, Department of Medicine, Massachusetts General
Cancer Center Hospital 137
Overview 138
Technology 138
Applications 138
Future 139
Peter Fraser, Chief, Senior Fellow of the Medical Research Council UK
Babraham Institute, Cambridge 139
Information 139 general
Technology 140
140 Applications
Future 141
Summary of Comments KOL 141
142 Challenges
142 Basic Research
Technology requires 142
Financial constraints 143
IP 144
144 Opportunities
biomarker discovery and diagnosis 144
Therapeutic intervention 145
145 Regenerative Medicine
Conclusions 146
Chapter 6 Appendix 150
150 Glossary
Acknowledgements 156
157 Index
157 Index
Bibliography 159
165 Notes
LOF
Figure 1.1: Timeline of epigenetic study of 18
Figure 1.2: Diagram of the structure of chromatin 22
Figure 1.3: Overview of epigenetic mechanisms related to health and disease 23
Figure 1.4: epigenetic applications by the pharmaceutical industry 27
Figure 2.5: Epigenetics in the discovery process of drug development and 34
Figure 2.6: Schematic Key technologies used in the 36 epigenetic
Figure 2.7: Diagram of the 37-chip technology
Figure 2.8: Epigenomics AG methylation-specific PCR (MSP) methods 42
Figure 3.9: Objectives of 51 DNA methylation epigenetics of cancer treatments
Figure 3.10: Mechanism of action of HAT and HDAC 61
Figure 3.11: Broadband Test proColon Epi 70 colorectal epigenetic
Figure 3.12: Competitive rates of 71 Epi proColon
Figure 3.13: Cascade ENVIVO 74 HDAC detection
Figure 3.14: Agouti mice epigenetic manipulation 79
Figure 3.15: rational design of inhibitor molecules Epizyme 85 HMT small
Figure 4.16: epigenetic therapies: class products and stage of development 91
Figure 4.17: epigenetic therapy: focus on therapy and stage of development 92
Figure 4.18: CUDU-101 Structure and design: the combination of multiple pharmacophore 97
List of Tables
Table 2.1: DNA methylation PCR methods 40
Table 2.2: Techniques for analyzing DNA methylation 41
Table 3.3: Examples of Dnmt inhibitors: agents potential cancer targeting epigenetic pathways 54
Table 3.4: Examples of research tools 55 Dnmt inhibitor
HDAC Table 3.5: Potential agents targeted cancer epigenetic pathways 57
Table 3.6: Examples of HDAC research tools 59
Table 3.7: Modification of histones and their effect 60 gene expression
Table 3.8: Profile PCI Security rivals 24781-64
Table 3.9: DNA methylation sites associated with cancer 67
Table 3.10: hypothetical validated miRNA targets for diabetes and obesity 81
Table 4.11: epigenetic therapies Revenue ($ millions), 2009-2020 93
Table 4.12: Preliminary clinical data of 24,781 Pharmacyclics PCI-106
Table 4.13: Recent alliances, acquisitions and mergers in the field of epigenetics 117
Table 5.14: NIH Roadmap epigenetic – 129 projects funded by the epigenetic
Content
Innovations Epigenetics
Executive Summary 10
Introduction 10
Implementation in R & D and technological progress 10
The exploration of new therapeutic targets 11
Epigenetics market, major pharmaceutical companies and strategies 12
Future 13 of epigenetics
Chapter 1 Introduction 16
What is Epigenetics? 17
Epigenetics and phenotypic 19
Epigenetic a new biological paradigm 19
Epigenetics, genetics, genomics and pharmacogenomics 20
The molecular mechanisms involved in epigenetics 22
DNA methylation 22
23 histone modifications
The nucleosome remodeling 23
Noncoding RNA 24
X chromosome inactivation 24
Gene 24 print
RNA Interference 24
Epigenetic basis of the disease 25
Epigenetics syndromes 25
25 Angelmann syndrome
The Beckwith-Wiedemann syndrome 26
The Prader-Willi syndrome 26
Why Epigenetics of interest to the pharmaceutical industry? 27
biomarker discovery and diagnosis 28
New therapeutic small molecule epigenetic 28
new treatments antisense 28
Stem cells and regenerative medicine 29
Conclusions 29
Chapter 2 Implementation in R & D and 32 Technological advances
The application of epigenetics in drug R & D 33
DNA methylation biomarkers 34
biomarkers of change of histones 35
Technological advances in epigenetics 35
36 Chromatin immunoprecipitation
38 DNA methylation technologies
No encryption technology NRA 43
Bioinformatics modeling 43
Conclusions 44
Chapter 3 Exploring new therapeutic targets 48
Possible new therapeutic targets 49
Epigenetics in cancer 50
DNA methyltransferase Dnmt inhibitors and 52
Case study of Vidaza (Celgene Corporation) and Dacogen (Eisai / J & J) 53
Case Study 56 Zebularine search
Histone acetyltransferase (HAT) and histone deacetylase (HDAC) 59
Case Study: Zolinza (Merck & Co.) 61
Case study of MGCD0103 (MethylGene / Taiho Pharmaceutical) 62
Case study: PCI-24781 (Pharmacyclics / Servier) 63
Histone demethylases and histone methyltranserases 65
Case study of PG11144 PG11047 & (Progen Pharmaceuticals) 66
Based diagnostics 67 potential epigenetic
67 The diagnosis of cancer DNA methylation biomarkers
Case Study: proColon Epi (Epigenomics AG) 69
Next generation of epigenetic cancer biomarkers 71
72 neurological Epigenetics
Case Study: EVP-0334 (pharmaceuticals ENVIVO) 73
Epigenetics in infectious diseases 75
Case Study: MGCD290 (MethylGene) 75
Case Study: siRNA against HIV-1 (Kevin Morris, of Scripps, La Jolla) 76
Epigenetics in 78 metabolic disorders
Epigenetics in cardiovascular disease 81
Epigenetics in ocular disorders 83
Case Study: Kinase inhibitors (Otsuka Pharmaceutical / MethylGene) 84
Case Study: inhibitors of the kinase / S-adenosyl methionine (SAM) (Epizyme). 85
Conclusions 86
Chapter 4 Market epigenetics, the big pharmaceutical companies and strategies 90
91 Epigenetics Market
epigenetic therapy income: 92 present and future
93 leading companies epigenetic
4SC AG, Planegg-Martinsried, Germany 94
Celgene Corporation, Summit, New Jersey 95
Curis Inc. Cambridge, MA 96
Chroma Therapeutics Ltd., Oxon, United Kingdom 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, Quebec 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
Abstract 114 companies based epigenetic
Recent alliances, mergers and acquisitions in epigenetic 115
Pharmaceutical epigenetic 118 strategies
GlaxoSmithKline, Middlesex, United Kingdom 118
Novartis, Basel, Switzerland 119
Merck & Co., 121 NJ Whitehouse
Eisai Corporation of North America, 122 NJ
Takeda, Osaka, Japan 123
General conclusions 123
Chapter 5 The future 126 of epigenetics
The future of epigenetics 127
Epigenetic partnerships; unravel the human epigenome 128
NIH Roadmap Epigenomics Program Initiative 128
European Network of Excellence Epigenome 130
Human Epigenome Consortium 130
Epigenetic KOL 131
John Mattick, Institute of Molecular Biosciences University of Queensland,
Australia 132
Overview 132
Technology 133
133 Applications
Future 134
Kevin Morris of the Institute Scripps, La Jolla, CA 134
Overview 134
Technology 135
135 Applications
Future 136
Monika Lachner, Max Planck Institute for Immunobiology, Department
Epigenetics, Freiburg, Germany 136
Overview 136
Technology 136
137 Applications
Future 137
Whetstine Johnathan, Department of Medicine, Massachusetts General
137 Hospital Cancer Center
Overview 138
Technology 138
138 Applications
Future 139
Peter Fraser, Chief, Senior Fellow of the Medical Research Council, UK
Babraham Institute, Cambridge 139
Overview 139
Technology 140
140 Applications
Future 141
Summary KOL 141 comments
142 Challenges
142 Basic Research
Technology requires 142
Financial constraints 143
IP 144
144 Opportunities
diagnostic biomarker discovery and 144
Therapeutic intervention 145
145 Regenerative Medicine
Conclusions 146
Chapter 6 Appendix 150
150 Glossary
Acknowledgements 156
157 Index
Index 157
Bibliography 159
165 Notes
LOF
Figure 1.1: Timeline of study of epigenetics 18
Figure 1.2: Diagram of the structure Chromatin 22
Figure 1.3: Overview of epigenetic mechanisms related to health and illness 23
Figure 1.4: epigenetics industry applications 27 Pharmaceuticals
Figure 2.5: Epigenetics in the process of drug discovery and development 34
Figure 2.6: Diagram key technologies in the epigenetic 36
Figure 2.7: Diagram of 37-chip technology
Figure 2.8: Epigenomics AG methylation specific PCR (MSP) methods 42
Figure 3.9: Objectives DNA methylation for epigenetic cancer therapies 51
Figure 3.10: Mechanism of action of HAT and HDAC 61
Figure 3.11: Test band Epi colorectal wide epigenetic proColon 70
Figure 3.12: Competitive rates of 71 Epi proColon
Figure 3.13: Project HDAC detection cascade ENVIVO 74
Figure 3.14: Agouti mice and manipulations Epigenetic 79
Figure 3.15: Epizyme rational design of small molecule inhibitors of HMT 85
Figure 4.16: therapies epigenetic: class products and the stage of development 91
Figure 4.17: The epigenetic therapy: focus on therapy and stage of development 92
Figure 4.18 CUDU-101 Structure and design: combines several pharmacophore 97
List of Tables
Table 2.1: DNA methylation PCR methods 40
Table 2.2: Analysis 41-DNA methylation
Table 3.3: Examples of Dnmt inhibitors: potential anti-cancer agents targeting epigenetic pathways 54
Table 3.4: Examples of research tools 55 Dnmt inhibitor
HDAC Table 3.5: Potential anticancer drugs targeting epigenetic pathways 57
Table 3.6: Examples of HDAC research tools 59
Table 3.7: histone modification and its effect on gene expression 60
Table 3.8: Profile PCI Security rivals 24781-64
Table 3.9: DNA methylation sites associated with cancer 67
Table 3.10: hypothetical miRNA validated targets for diabetes and obesity 81
Table 4.11: Therapeutic epigenetic revenue ($ m), 2009-2020 93
Table 4.12: Preliminary clinical data of 24,781 Pharmacyclics PCI-106
Table 4.13: Alliances recent acquisitions and mergers in the field of epigenetics 117
Table 5.14: NIH Roadmap epigenetics – 12 projects funded epigenetics
For more information please contact:
About the Author
Minal H
SEO
vinod.minal@gmail.com
http://www.aarkstore.com
Time travel technology Disclosure (1/16) on Coast to Coast AM 01-31-10
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