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創薬におけるGPCR(Gタンパク質共役受容体):標的GPCRの脱オーファン化への取り組みの拡大

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

発行 GBI Research 商品コード 219214
出版日 ページ情報 英文 143 Pages
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創薬におけるGPCR(Gタンパク質共役受容体):標的GPCRの脱オーファン化への取り組みの拡大 GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing
出版日: 2011年11月01日 ページ情報: 英文 143 Pages
概要

当レポートでは、創薬におけるGPCR(Gタンパク質共役受容体)の重要性について技術面および商業面から調査分析し、GPCR(Gタンパク質共役受容体)の概要・構造、GPCRを標的とする創薬のための革新的研究手法、オーファンGPCRの重要性と脱オーファン化の手法、各開発フェーズのパイプライン分析(疾患クラス・適応症別)、主要企業と競合環境などをまとめ、概略以下の構成でお届けいたします。

第1章 目次

第2章 イントロダクション

第3章 概要

  • イントロダクション
  • ヒトゲノムのGPCR
  • GPCRの構造
  • Gタンパク質の構造
  • Gタンパク質のカップリング
  • GPCRのセカンドメッセンジャー
  • 翻訳後修飾

第4章 GPCRを標的とする創薬と革新的研究手法

  • イントロダクション
  • 構造に基づく研究
  • フラグメントに基づく創薬
  • LiSS
  • アロステリズムとGPCR
  • GPCR二量体(ダイマー)
  • GPCRオリゴマー形成
    • イントロダクション
    • 新たな手段
    • ケーススタディ、など

第5章 オーファンGPCR

  • イントロダクション
  • 脱オーファン化に利用される現在の手法
  • 脱オーファン化の機能アッセイ

第6章 パイプライン分析:疾患クラス別

  • 中枢神経系
  • 心織血管系
  • 代謝障害
  • 胃腸疾患
  • 呼吸器系疾患
  • 免疫疾患
  • 女性特有の疾患
  • 眼科
  • 泌尿器生殖器系・性ホルモン
    • イントロダクション
    • パイプラインプロファイル
    • 主な適応症

第7章 パイプライン分析:適応症別

  • 糖尿病
  • パーキンソン病
  • 疼痛
  • 合失調症
  • 肥満症
  • 高血圧
  • 喘息
  • 前立腺癌
  • COPD(慢性閉塞性肺疾患)
  • 緑内障
    • イントロダクション
    • パイプラインプロファイル
    • 主要標的の分析

第8章 競合環境

  • 主要企業

第9章 企業間の戦略的統合

  • AstraZeneca:Heptaresとの共同開発契約を締結
  • Heptares Therapeutics:ShireとAdenosine A2Aのオプションライセンシング契約を締結
  • Dimerix Bioscience:Takeda Cambridgeとの研究契約を締結
  • Heptares Therapeutics:武田製薬と創薬部門の提携を確立
  • ACADIA Pharmaceuticals:Allerganとの創薬部門の提携を延長
  • Omeros:第一三共とのライセンス契約を延長
  • Domain Therapeutics:Merck Seronoとライセンシング契約を締結
  • Receptos:Eli Lillyとの提携を確立
  • Receptos:Ortho-McNeil-Janssen Pharmaceuticalsとライセンシング契約を締結
  • Anchor Therapeutics:Ortho-McNeil-Janssenとライセンシング契約を締結

第10章 付録

図表

目次
Product Code: GBIHC137MR

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.

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

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

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

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
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