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GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing
Date:10/25/2011

NEW YORK, Oct. 25, 2011 /PRNewswire/ -- Reportlinker.com announces that a new market research report is available in its catalogue:

GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing

http://www.reportlinker.com/p0660755/GPCRs-in-Drug-Discovery---Efforts-to-De-Orphanize-Novel-GPCR-Targets-are-Increasing.html#utm_source=prnewswire&utm_medium=pr&utm_campaign=In_Vitro_Diagnostic

GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing

Summary

GBI Research, the leading business intelligence provider, has released its latest research "GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing" which provides insights in to the technical and commercial importance of G protein coupled receptors, which are the most important category of receptors in the human body. The report provides a scientific understanding of GPCRs and details the novel research methods being employed in the research of new targets and molecules that can be more effective in treating many indications. A special note on Orphan GPCRs and ways to de-orphanize them is followed by a detailed pipeline analysis to understand the therapeutic classes and indications that are being targeted through GPCRs. The report provides an in-depth analysis of the competitive landscape, including the profiling of top companies and licensing agreements involving GPCR molecules and platform technologies.

Scope

The scope of this report includes -

- Detailed technical understanding of G protein coupled receptors

- Dedicated sections on Novel research methods being used to improve the GPCR targeted drug discovery and development process

- Understanding of Orphan GPCRs, its importance and novel methods to locate ligands and de-orphanize these receptors

- Pipeline analysis of products at various stages of development targeting receptors classified as GPCRs, including identification of major therapeutic areas and indications

- Analysis and review of important strategic partnerships and licensing agreements in the area of GPCR drug discovery and development

- The report also covers information on the leading market players and the competitive landscape, including specialist companies which have proprietary GPCR platform technology as well as major companies with molecules in not only the NDA Filed stage but also in Phase III

Reasons to buy

The report will enhance your decision making capability. It will allow you to -

- Develop business strategies by understanding the trends shaping and driving research in the field of GPCRs

- Understand the potential areas of application for GPCR therapies.

- Identify key molecules targeting GPCRs in development based on the therapy.

- Identify the key players investing in GPCR platform technologies

- Optimize your R&D pipeline through identification of novel technologies being used in GPCR research to improve the drug discovery process

- Identify emerging players with a potentially strong product portfolio of molecules targeting GPCRs and create effective counter-strategies to gain a competitive advantage.

- What's the next big thing in GPCR research? – Identify, understand and capitalize.

1 Table of Contents

1 Table of Contents 4

1.1 List of Tables 8

1.2 List of Figures 10

2 GPCRs in Drug Discovery – Introduction 12

2.1 GBI Research Report Guidance 12

3 GPCRs in Drug Discovery – Overview 13

3.1 Introduction 13

3.2 GPCR in the Human Genome 14

3.2.1 Introduction 14

3.2.2 The Traditional Classification System 14

3.2.3 The GRAFS Classification System 15

3.3 Structure of GPCRs 17

3.3.1 General Structure 17

3.3.2 Importance of the 7TM 17

3.4 Structure of G-proteins 18

3.5 Coupling to G-proteins 19

3.5.1 Introduction 19

3.5.2 The Signal Transduction Pathways Involving GPCR 19

3.6 Second Messengers in the GPCR System 22

3.6.1 Introduction to Second Messengers 22

3.6.2 Cyclic Adenosine Monophosphate (cAMP) 22

3.6.3 Cyclic Guanosine Monophosphate (cGMP) 23

3.6.4 Diacylglycerol (DAG) 23

3.6.5 Inositol 1, 4, 5-triphosphate (IP3) 24

3.6.6 Calcium Ions (Ca2+ ) 24

3.7 Post-Translational Modifications 25

3.7.1 Glycosylation, Palmitoylation and Phosphorylation 25

3.7.2 GPCR Desensitization 25

4 GPCRs in Drug Discovery – Novel Research Methods in GPCR Drug Discovery 26

4.1 Introduction 26

4.2 Structure-Based Research in GPCR 26

4.2.1 Introduction 26

4.2.2 New Avenues 26

4.2.3 Case Studies 27

4.3 Fragment-Based Drug Discovery 28

4.3.1 Introduction 28

4.3.2 New Avenues 28

4.3.3 Case Study 28

4.4 Ligand-Induced Selective Signaling (LiSS) 28

4.4.1 Introduction 28

4.4.2 New Avenues 29

4.4.3 Case Study 29

4.5 Allosterism and GPCRs 29

4.5.1 Introduction 29

4.5.2 New Avenues 30

4.5.3 Case Studies 31

4.6 GPCR Dimerization 32

4.6.1 Introduction 32

4.6.2 Need to Form Dimers 32

4.6.3 New Avenues 32

4.6.4 Case Studies 33

4.7 GPCR Oligomerization 34

4.7.1 Introduction 34

4.7.2 Classification of Oligomers 34

4.7.3 New Avenues 35

4.7.4 Case Studies 35

5 GPCRs in Drug Discovery – Orphan GPCRs 36

5.1 Introduction 36

5.1.1 Orphan GPCRs in the GRAFS Classification System 36

5.1.2 Orphan GPCRs in the Traditional Classification System 37

5.2 Current Methods Used in De-orphanization 38

5.2.1 Introduction 38

5.2.2 Reverse Pharmacology 39

5.2.3 Orphan Receptor Strategy 40

5.2.4 Phylogenetic Analysis and Chemogenomics 40

5.3 Functional Assays for De-orphanization 40

5.3.1 Introduction 40

5.3.2 G protein-dependent Assays 40

5.3.3 Recent G protein-independent Assays 41

6 GPCRs in Drug Discovery – Pipeline Analysis by Therapeutic Class 42

6.1 Central Nervous System 46

6.1.1 Introduction 46

6.1.2 Pipeline Profile 46

6.1.3 Major Indications 47

6.2 Oncology 52

6.2.1 Introduction 52

6.2.2 Pipeline Profile 52

6.2.3 Major Indications 53

6.3 Cardiovascular System 56

6.3.1 Introduction 56

6.3.2 Pipeline Profile 56

6.3.3 Major Indications 57

6.4 Metabolic Disorders 60

6.4.1 Introduction 60

6.4.2 Pipeline Profile 60

6.4.3 Major Indications 61

6.5 Gastrointestinal Disorders 64

6.5.1 Introduction 64

6.5.2 Pipeline Profile 64

6.5.3 Major Indications 65

6.6 Respiratory Diseases 67

6.6.1 Introduction 67

6.6.2 Pipeline Profile 67

6.6.3 Major Indications 68

6.7 Immunology 71

6.7.1 Introduction 71

6.7.2 Pipeline Profile 71

6.7.3 Major Indications 72

6.8 Women's Health 74

6.8.1 Introduction 74

6.8.2 Pipeline Profile 74

6.8.3 Major Indications 75

6.9 Ophthalmology 78

6.9.1 Introduction 78

6.9.2 Pipeline Profile 78

6.9.3 Major Indications 79

6.10 Genito-Urinary System and Sex Hormones 82

6.10.1 Introduction 82

6.10.2 Pipeline Profile 82

6.10.3 Major Indications 83

7 GPRCs in Drug Discovery – Pipeline Analysis by Indications 85

7.1 Diabetes 88

7.1.1 Introduction 88

7.1.2 Pipeline Profile 88

7.1.3 Analysis of Major Targets 89

7.2 Parkinson's Disease 91

7.2.1 Introduction 91

7.2.2 Pipeline Profile 91

7.2.3 Analysis of Major Targets 92

7.3 Pain 94

7.3.1 Introduction 94

7.3.2 Pipeline Profile 94

7.3.3 Analysis of Major Targets 95

7.4 Schizophrenia 97

7.4.1 Introduction 97

7.4.2 Pipeline Profile 97

7.4.3 Analysis of Major Targets 98

7.5 Obesity 100

7.5.1 Introduction 100

7.5.2 Pipeline Profile 100

7.5.3 Analysis of Major Targets 101

7.6 Hypertension 103

7.6.1 Introduction 103

7.6.2 Pipeline Profile 103

7.6.3 Analysis of Major Targets 104

7.7 Asthma 106

7.7.1 Introduction 106

7.7.2 Pipeline Profile 106

7.7.3 Analysis of Major Targets 107

7.8 Prostate Cancer 109

7.8.1 Introduction 109

7.8.2 Pipeline Profile 109

7.8.3 Analysis of Major Targets 110

7.9 Chronic Obstructive Pulmonary Disease (COPD) 112

7.9.1 Introduction 112

7.9.2 Pipeline Profile 112

7.9.3 Analysis of Major Targets 113

7.10 Glaucoma 115

7.10.1 Introduction 115

7.10.2 Pipeline Profile 115

7.10.3 Analysis of Top Targets 116

8 GPCRs in Drug Discovery – Competitive Landscape 118

8.1 GPCRs in Drug Discovery – Major Companies With GPCR Platform Technology 118

8.1.1 Heptares Therapeutics Ltd. 118

8.1.2 Receptos Inc. 118

8.1.3 7TM Pharma A/S 119

8.1.4 Dimerix Biosciences Pvt. Ltd. 119

8.1.5 Trevena, Inc. 119

8.1.6 Cara Therapeutics, Inc. 120

8.1.7 Addex Pharmaceuticals 120

8.1.8 Anchor Therapeutics 121

8.1.9 Domain Therapeutics 121

8.1.10 Euroscreen S.A. 122

8.1.11 Omeros Corporation 122

8.1.12 Arena Pharmaceuticals 123

8.1.13 Compugen, Ltd. 123

8.1.14 Tranzyme Pharma, Inc. 124

8.1.15 Oxagen Limited 125

8.1.16 Prosarix Ltd. 125

8.1.17 Acadia Pharmaceuticals Inc. 126

8.1.18 Actelion Ltd. 127

8.1.19 AcurePharma AB 127

8.1.20 DiscoveRx 127

8.2 GPCRs in Drug Discovery – Top 5 Companies as per Number of Molecules in NDA Filed and in Phase III 128

8.2.1 Merck & Co., Inc. 128

8.2.2 Novartis AG 130

8.2.3 Pfizer Inc. 131

8.2.4 Eli Lilly and Company 132

8.2.5 Johnson and Johnson 133

9 GPCRs in Drug Discovery – Strategic Consolidations 134

9.1 AstraZeneca Enters Into Co-Development Agreement With Heptares 134

9.2 Heptares Therapeutics Enters Into Option Licensing Agreement With Shire For Adenosine A2A 134

9.3 Dimerix Bioscience Enters Into Research Agreement With Takeda Cambridge 135

9.4 Heptares Therapeutics Enters Into Drug Discovery Collaboration With Takeda Pharmaceutical Company Ltd. 135

9.5 ACADIA Pharmaceuticals Extends Drug Discovery Collaboration With Allergan 136

9.6 Omeros Expands Licensing Agreement With Daiichi Sankyo 136

9.7 Domain Therapeutics Enters Into Licensing Agreement With Merck Serono 137

9.8 Receptos Enters Into Collaboration with Eli Lilly 137

9.9 Receptos Enters Into Licensing Agreement With Ortho-McNeil-Janssen Pharmaceuticals 138

9.10 Anchor Therapeutics Enters Into Licensing Agreement with Ortho-McNeil-Janssen 138

10 GPCRs in Drug Discovery – Appendix 139

10.1 Market Definitions 139

10.2 Abbreviations 139

10.3 Research Methodology 139

10.3.1 Coverage 139

10.3.2 Secondary Research 140

10.3.3 Primary Research 140

10.3.4 Expert Panel Validation 140

10.3.5 Section-wise Methodology 141

10.4 Contact Us 143

10.5 Disclaimer 143

10.6 Sources 143

1.1 List of Tables

Table 1: GPCRs in Drug Discovery, The Rhodopsin Receptor Family 16

Table 2: GPCRs in Drug Discovery, Isoforms of the Heterotrimeric G Proteins 18

Table 3: GPCRs in Drug Discovery, Types of Mammalian PLC Enzymes 21

Table 4: GPCRs in Drug Discovery, RhoGEF Regulated by G12/13 21

Table 5: GPCRs in Drug Discovery, Effects of Protein Kinase C Activation in the Human Body 23

Table 6: GPCRs in Drug Discovery, Orphan Receptors as per the Traditional Classification System 37

Table 7: GPCRs in Drug Discovery, De-orphanized GPCRs, 2005-2009 38

Table 8: GPCRs in Drug Discovery, Pipeline Status of the Top 10 Therapy Areas under GPCRs, 2011 43

Table 9: GPCRs in Drug Discovery, Pipeline Status of Other Therapy Areas under GPCRs, 2011 44

Table 10: GPCRs in Drug Discovery, Central Nervous System, Number of Molecules Targeting GPCRs By Phase, 2011 46

Table 11: GPCRs in Drug Discovery, Central Nervous System, Top 10 Indications By Total Molecules In Pipeline, 2011 48

Table 12: GPCRs in Drug Discovery, Major Phase III Molecules for CNS Indications, 2011 48

Table 13: GPCRs in Drug Discovery, Oncology, Number of Molecules Targeting GPCRs By Phase, 2011 52

Table 14: GPCRs in Drug Discovery, Oncology, Top 10 Indications By Total Molecules In Pipeline, 2011 54

Table 15: GPCRs in Drug Discovery, Major Phase III Molecules for Oncology Indications, 2011 55

Table 16: GPCRs in Drug Discovery, Cardiovascular System, Number of Molecules Targeting GPCRs By Phase, 2011 56

Table 17: GPCRs in Drug Discovery, Cardiovascular System, Top 10 Indications By Total Molecules In Pipeline, 2011 58

Table 18: GPCRs in Drug Discovery, Major Phase III Molecules for CVS Indications, 2011 59

Table 19: GPCRs in Drug Discovery, Metabolic Disorders, Number of Molecules Targeting GPCRs By Phase, 2011 60

Table 20: GPCRs in Drug Discovery, Metabolic Disorders, Top 10 Indications By Total Molecules In Pipeline, 2011 62

Table 21: GPCRs in Drug Discovery, Major Phase III Molecules for Metabolic Disorders Indications, 2011 63

Table 22: GPCRs in Drug Discovery, Gastrointestinal Disorders, Number of Molecules Targeting GPCRs By Phase, 2011 64

Table 23: GPCRs in Drug Discovery, Gastrointestinal Disorders, Top 10 Indications By Total Molecules In Pipeline, 2011 65

Table 24: GPCRs in Drug Discovery, Major Phase III Molecules for Gastrointestinal Indications, 2011 66

Table 25: GPCRs in Drug Discovery, Respiratory Diseases, Number of Molecules Targeting GPCRs By Phase, 2011 67

Table 26: GPCRs in Drug Discovery, Respiratory Diseases, Top 10 Indications By Total Molecules In Pipeline, 2011 69

Table 27: GPCRs in Drug Discovery, Major Phase III Molecules for Respiratory Diseases Indications, 2011 70

Table 28: GPCRs in Drug Discovery, Immunology, Number of Molecules Targeting GPCRs By Phase, 2011 71

Table 29: GPCRs in Drug Discovery, Immunology, Top 10 Indications By Total Molecules In Pipeline, 2011 73

Table 30: GPCRs in Drug Discovery, Major Phase III Molecules for Immunology Indications, 2011 73

Table 31: GPCRs in Drug Discovery, Women's Health, Number of Molecules Targeting GPCRs By Phase, 2011 74

Table 32: GPCRs in Drug Discovery, Women's Health, Top 10 Indications By Total Molecules In Pipeline, 2011 76

Table 33: GPCRs in Drug Discovery, Major Phase III Molecules for Women's Health Indications, 2011 77

Table 34: GPCRs in Drug Discovery, Ophthalmology, Number of Molecules Targeting GPCRs By Phase, 2011 78

Table 35: GPCRs in Drug Discovery, Ophthalmology, Top 10 Indications By Total Molecules In Pipeline, 2011 80

Table 36: GPCRs in Drug Discovery, Major Phase III Molecules for Ophthalmology Indications, 2011 81

Table 37: GPCRs in Drug Discovery, Genito-Urinary System and Sex Hormones, Number of Molecules Targeting GPCRs By Phase, 2011 82

Table 38: GPCRs in Drug Discovery, Genito-Urinary System and Sex Hormones, Top 10 Indications By Total Molecules In Pipeline, 2011 83

Table 39: GPCRs in Drug Discovery, Major Phase III Molecules for Genito-Urinary System and Sex Hormones Indications, 2011 84

Table 40: GPCRs in Drug Discovery, Top 10 Indications By Total Molecules in Pipeline, 2011 86

Table 41: GPCRs in Drug Discovery, Diabetes, Number of Molecules Targeting GPCRs By Phase, 2011 88

Table 42: GPCRs in Drug Discovery, Parkinson's Disease, Number of Molecules Targeting GPCRs By Phase, 2011 91

Table 43: GPCRs in Drug Discovery, Pain, Number of Molecules Targeting GPCRs By Phase, 2011 94

Table 44: GPCRs in Drug Discovery, Schizophrenia, Number of Molecules Targeting GPCRs By Phase, 2011 97

Table 45: GPCRs in Drug Discovery, Obesity, Number of Molecules Targeting GPCRs By Phase, 2011 100

Table 46: GPCRs in Drug Discovery, Hypertension, Number of Molecules Targeting GPCRs By Phase, 2011 103

Table 47: GPCRs in Drug Discovery, Asthma, Number of Molecules Targeting GPCRs By Phase, 2011 106

Table 48: GPCRs in Drug Discovery, Prostate Cancer, Number of Molecules Targeting GPCRs By Phase, 2011 109

Table 49: GPCRs in Drug Discovery, COPD, Number of Molecules Targeting GPCRs By Phase, 2011 112

Table 50: GPCRs in Drug Discovery, Glaucoma, Number of Molecules Targeting GPCRs By Phase, 2011 115

Table 51: GPCRs in Drug Discovery, Heptares Therapeutics Ltd., GPCR Research Profile, 2011 118

Table 52: GPCRs in Drug Discovery, Receptos Inc., GPCR Research Profile, 2011 118

Table 53: GPCRs in Drug Discovery, 7TM Pharma A/S, GPCR Research Profile, 2011 119

Table 54: GPCRs in Drug Discovery, Trevena Inc., GPCR Research Profile, 2011 120

Table 55: GPCRs in Drug Discovery, Cara Therapeutics Inc., GPCR Research Profile, 2011 120

Table 56: GPCRs in Drug Discovery, Addex Pharmaceuticals, GPCR Research Profile, 2011 121

Table 57: GPCRs in Drug Discovery, Domain Therapeutics, GPCR Research Profile, 2011 122

Table 58: GPCRs in Drug Discovery, Euroscreen S.A., GPCR Research Profile, 2011 122

Table 59: GPCRs in Drug Discovery, Arena Pharmaceuticals, GPCR Research Profile, 2011 123

Table 60: GPCRs in Drug Discovery, Compugen Ltd., GPCR Research Profile, 2011 124

Table 61: GPCRs in Drug Discovery, Tranzyme Pharma Inc., GPCR Research Profile, 2011 124

Table 62: GPCRs in Drug Discovery, Acadia Pharmaceuticals Inc. GPCR Research Profile, 2011 126

Table 63: GPCRs in Drug Discovery, Actelion Ltd., GPCR Research Profile, 2011 127

Table 64: GPCRs in Drug Discovery, Merck & Co., Inc. Pipeline Profile, 2011 128

Table 65: GPCRs in Drug Discovery, Novartis AG Pipeline Profile, 2011 130

Table 66: GPCRs in Drug Discovery, Pfizer Inc. Pipeline Profile, 2011 131

Table 67: GPCRs in Drug Discovery, Eli Lilly and Company Pipeline Profile, 2011 132

Table 68: GPCRs in Drug Discovery, Johnson and Johnson Pipeline Profile, 2011 133

Table 69: GPCRs in Drug Discovery, AstraZeneca-Heptares Partnership Details 134

Table 70: GPCRs in Drug Discovery, Heptares-Takeda Partnership Details 135

Table 71: GPCRs in Drug Discovery, Domain-Merck Licensing Agreement Details 137

1.2 List of Figures

Figure 1: GPCRs in Drug Discovery, G-Protein Mediated Signaling of 7TM Receptors 13

Figure 2: GPCRs in Drug Discovery, The GRAFS Classification System 15

Figure 3: GPCRs in Drug Discovery, The cAMP Signaling Pathway 20

Figure 4: GPCRs in Drug Discovery, Classification of Oligomers 34

Figure 5: GPCRs in Drug Discovery, De-orphanization Rate of GPCRs, 2000-2009 38

Figure 6: GPCRs in Drug Discovery, The Receptor Pharmacology Process for De-orphanization 39

Figure 7: GPCRs in Drug Discovery, Molecules Targeting GPCRs in Development for Top 10 Therapy Areas, 2011 42

Figure 8: GPCRs in Drug Discovery, Molecules Targeting GPCRs in Development for Other Therapy Areas, 2011 44

Figure 9: GPCRs in Drug Discovery, Pipeline Analysis for Molecules Targeting GPCRs by Phase, 2011 45

Figure 10: GPCRs in Drug Discovery, Central Nervous System, Number of Molecules Targeting GPCRs By Phase, 2011 46

Figure 11: GPCRs in Drug Discovery, Central Nervous System, Top 10 Indications By Total Molecules In Pipeline, 2011 47

Figure 12: GPCRs in Drug Discovery, Oncology, Number of Molecules Targeting GPCRs By Phase, 2011 52

Figure 13: GPCRs in Drug Discovery, Oncology, Top 10 Indications By Total Molecules In Pipeline, 2011 53

Figure 14: GPCRs in Drug Discovery, Cardiovascular System, Number of Molecules Targeting GPCRs By Phase, 2011 56

Figure 15: GPCRs in Drug Discovery, Cardiovascular System, Top 10 Indications By Total Molecules In Pipeline, 2011 57

Figure 16: GPCRs in Drug Discovery, Metabolic Disorders, Number of Molecules Targeting GPCRs By Phase, 2011 60

Figure 17: GPCRs in Drug Discovery, Metabolic Disorders, Top 10 Indications By Total Molecules In Pipeline, 2011 61

Figure 18: GPCRs in Drug Discovery, Gastrointestinal Disorders, Number of Molecules Targeting GPCRs By Phase, 2011 64

Figure 19: GPCRs in Drug Discovery, Gastrointestinal Disorders, Top 10 Indications By Total Molecules In Pipeline, 2011 65

Figure 20: GPCRs in Drug Discovery, Respiratory Diseases, Number of Molecules Targeting GPCRs By Phase, 2011 67

Figure 21: GPCRs in Drug Discovery, Respiratory Diseases, Top 10 Indications By Total Molecules In Pipeline, 2011 68

Figure 22: GPCRs in Drug Discovery, Immunology, Number of Molecules Targeting GPCRs By Phase, 2011 71

Figure 23: GPCRs in Drug Discovery, Immunology, Top 10 Indications By Total Molecules In Pipeline, 2011 72

Figure 24: GPCRs in Drug Discovery, Women's Health, Number of Molecules Targeting GPCRs By Phase, 2011 74

Figure 25: GPCRs in Drug Discovery, Women's Health, Top 10 Indications By Total Molecules In Pipeline, 2011 75

Figure 26: GPCRs in Drug Discovery, Ophthalmology, Number of Molecules Targeting GPCRs By Phase, 2011 78

Figure 27: GPCRs in Drug Discovery, Ophthalmology, Top 10 Indications By Total Molecules In Pipeline, 2011 79

Figure 28: GPCRs in Drug Discovery, Genito-Urinary System and Sex Hormones, Number of Molecules Targeting GPCRs By Phase, 2011 82

Figure 29: GPCRs in Drug Discovery, Genito-Urinary System and Sex Hormones, Top 10 Indications By Total Molecules In Pipeline, 2011 83

Figure 30: GPCRs in Drug Discovery, Top 10 Indications By Total Molecules in Pipeline, 2011 85

Figure 31: GPCRs in Drug Discovery, Top 10 Indications By Phase, 2011 87

Figure 32: GPCRs in Drug Discovery, Diabetes, Number of Molecules Targeting GPCRs By Phase, 2011 88

Figure 33: GPCRs in Drug Discovery, Diabetes, Major Targets for Pipeline Molecules, 2011 89

Figure 34: GPCRs in Drug Discovery, Diabetes, Comparison of Major Targets with Stage of Development, 2011 90

Figure 35: GPCRs in Drug Discovery, Parkinson's Disease, Number of Molecules Targeting GPCRs By Phase, 2011 91

Figure 36: GPCRs in Drug Discovery, Parkinson's Disease, Major Targets for Pipeline Molecules, 2011 92

Figure 37: GPCRs in Drug Discovery, Parkinson's Disease, Comparison of Major Targets with Stage of Development, 2011 93

Figure 38: GPCRs in Drug Discovery, Pain, Number of Molecules Targeting GPCRs By Phase, 2011 94

Figure 39: GPCRs in Drug Discovery, Pain, Major Targets for Pipeline Molecules, 2011 95

Figure 40: GPCRs in Drug Discovery, Pain, Comparison of Major Targets with Stage of Development, 2011 96

Figure 41: GPCRs in Drug Discovery, Schizophrenia, Number of Molecules Targeting GPCRs By Phase, 2011 97

Figure 42: GPCRs in Drug Discovery, Schizophrenia, Major Targets for Pipeline Molecules, 2011 98

Figure 43: GPCRs in Drug Discovery, Schizophrenia, Comparison of Major Targets with Stage of Development, 2011 99

Figure 44: GPCRs in Drug Discovery, Obesity, Number of Molecules Targeting GPCRs By Phase, 2011 100

Figure 45: GPCRs in Drug Discovery, Obesity, Major Targets for Pipeline Molecules, 2011 101

Figure 46: GPCRs in Drug Discovery, Obesity, Comparison of Major Targets with Stage of Development, 2011 102

Figure 47: GPCRs in Drug Discovery, Hypertension, Number of Molecules Targeting GPCRs By Phase, 2011 103

Figure 48: GPCRs in Drug Discovery, Hypertension, Major Targets for Pipeline Molecules, 2011 104

Figure 49: GPCRs in Drug Discovery, Hypertension, Comparison of Major Targets with Stage of Development, 2011 105

Figure 50: GPCRs in Drug Discovery, Asthma, Number of Molecules Targeting GPCRs By Phase, 2011 106

Figure 51: GPCRs in Drug Discovery, Asthma, Major Targets for Pipeline Molecules, 2011 107

Figure 52: GPCRs in Drug Discovery, Asthma, Comparison of Major Targets with Stage of Development, 2011 108

Figure 53: GPCRs in Drug Discovery, Prostate Cancer, Number of Molecules Targeting GPCRs By Phase, 2011 109

Figure 54: GPCRs in Drug Discovery, Prostate Cancer, Major Targets for Pipeline Molecules, 2011 110

Figure 55: GPCRs in Drug Discovery, Prostate Cancer, Comparison of Major Targets with Stage of Development, 2011 111

Figure 56: GPCRs in Drug Discovery, COPD, Number of Molecules Targeting GPCRs By Phase, 2011 112

Figure 57: GPCRs in Drug Discovery, COPD, Major Targets for Pipeline Molecules, 2011 113

Figure 58: GPCRs in Drug Discovery, COPD, Comparison of Major Targets with Stage of Development, 2011 114

Figure 59: GPCRs in Drug Discovery, Glaucoma, Number of Molecules Targeting GPCRs By Phase, 2011 115

Figure 60: GPCRs in Drug Discovery, Glaucoma, Major Targets for Pipeline Molecules, 2011 116

Figure 61: GPCRs in Drug Discovery, Glaucoma, Comparison of Major Targets with Stage of Development, 2011 117

Figure 62: GPCRs in Drug Discovery, Merck & Co., Inc. Pipeline Profile, 2011 129

Figure 63: GPCRs in Drug Discovery, Novartis AG Pipeline Profile, 2011 130

Figure 64: GPCRs in Drug Discovery, Pfizer Inc. Pipeline Profile, 2011 131

Figure 65: GPCRs in Drug Discovery, Eli Lilly and Company Pipeline Profile, 2011 132

Companies Mentioned

Heptares Therapeutics Ltd.

Receptos Inc.

7TM Pharma A/S

Dimerix Biosciences Pvt. Ltd.

Trevena, Inc.

Cara Therapeutics, Inc.

Addex Pharmaceuticals

Anchor Therapeutics

Domain Therapeutics

Euroscreen S.A.

Omeros Corporation

Arena Pharmaceuticals

Compugen, Ltd.

Tranzyme Pharma, Inc.

Oxagen Limited

Prosarix Ltd.

Acadia Pharmaceuticals Inc.

Actelion Ltd.

AcurePharma AB

DiscoveRx

Merck & Co., Inc.

Novartis AG

Pfizer Inc.

Eli Lilly and Company

Johnson and Johnson

To order this report:

In Vitro Diagnostic Industry: GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing

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