Global G-Protein Coupled Receptors (GPCRs) Industry

  • April 2012
  • -
  • Global Industry Analysts
  • -
  • 299 pages

This report analyzes the Global market for G-Protein Coupled Receptors (GPCRs) in US$ Billion. Annual estimates and forecasts are provided for the period 2009 through 2017. Also, a six-year historic analysis is provided for this market. The report profiles 43 companies including 7TM Pharma A/S, Actelion Pharmaceuticals Ltd., Acure Pharma AB, Anchor Therapeutics, Arena Pharmaceuticals, Inc., Addex Pharmaceuticals, Acadia Pharmaceuticals Inc., Cara Therapeutics, Inc., DiscoveRx Corporation, Dimerix Bioscience Pty Ltd., Domain Therapeutics, Euroscreen SA, and Trevena, Inc. Market data and analytics are derived from primary and secondary research. Company profiles are primarily based upon search engine sources in the public domain.

Table Of Contents

Study Reliability and Reporting Limitations I-1
Disclaimers I-2
Data Interpretation and Reporting Level I-3
Quantitative Techniques and Analytics I-3
Product Definitions and Scope of Study I-3


A Quick Primer II-1
Why GPCRs Are Important? II-1
Illustrative Examples of Currently Available Pharmaceutical
Drugs Targeting GPCRs II-1
Untapped Pharmacological Potential of GPCRs Ignites Interest II-2
Popular Types of GPCRs of Therapeutic Interest Currently
Being Studied Include: II-3
Current Knowledge of GPCR Crystal Structures Just the Tip of
the Iceberg II-3
NMR Spectroscopy: An Invaluable Tool to Study GPCR Structures II-4
Orphan GPCRs: A Promising Area for Drug Discovery II-4
Developments in Screening Technology for GPCRs II-5
Cell Membrane Assays for GPCR Quantitative Analysis II-5
What’s in for the Pharmaceutical Industry? II-5
Challenges Aplenty in the GPCR Space II-6
Addressing Orphan GPCRs II-6
Lack of Structural Information II-6
Identification and Classification of Allosteric Sites II-6

GPCR: Gateways to Cell II-7
Classification of GPCRs II-7
Table 1: List of Identified Known and Orphan (Non-Sensory)
GPCRs in Human Genome (includes corresponding Graph/Chart) II-8
Orphan GPCRs and Deorphanization II-8
List of oGPCR-Ligand Pairings Identified By Using Reverse
Pharmacology Approach II-9
Structural Information II-9
Rhodopsin: A Well Studied GPCR II-10
Crystal Structure of Human Beta-2 Adrenergic GPCR II-10
Structure of Human A2A Adenosine Receptor II-10
Significance of GPCR Crystal Structures II-11
GPCR Signaling Pathways II-11
Physiological Roles Performed by GPCRs II-11
Visual Sense II-11
Cell-density Sensing II-11
Regulation of mood and behavior II-11
Smelling Sense II-12
Regulating Immune-System Inflammation and Activity II-12
Automatic Transmission of Nervous System II-12
Receptor - Ligand Interaction II-12
Types of Ligands II-12
Therapeutic Potential of GPCRs II-12
List of Major Disease States and Associated Known GPCRs II-13
Allosteric Modulators and Implication of Allostery in Drug
Discovery II-13
Advantages of Allosteric Modulators II-13
Dimerisation and Role of Dimers in Drug Discovery II-14
Oligomerisation and Role of Oligomers in Drug Discovery II-14
Functional Selectivity II-14
Existing Drug Candidates in GPCR Space II-15
List of Existing GPCR-Based Drugs Available In Market Along
With Their Target Receptor and Indication II-15
Pipeline GPCR Drug Candidates II-15
Ion Channels II-16
Approaches to Drug Discovery in GPCR Space II-16
Structure-Based Drug Discovery II-16
Ligand-Based Drug Discovery II-16
Target-Based Drug Discovery II-16
GPCR Screening and Targeting Technologies II-16
Cell-Based Screening Assays II-17
Virtual Screening II-18
Fragment screening II-18

Domain Therapeutics Enters into an Agreement with Merck Serono II-19
Anchor Therapeutics Makes a Breakthrough in GPCR Collaboration II-19
Receptos Collaborates with Lilly GPCR target II-19
Sanofi-aventis Enters into Licensing Agreement with Metabolex II-20
Neurocrine and Boehringer Ingelheim Join Hands to Develop
GPR119 Agonists II-20
Affitech Enters into Research Collaboration with NTS Plus II-20
Takeda Cambridge Inks an Agreement to Utilize Dimerix’ GPCR-
HIT Platform II-21
PerkinElmer Unveils New Detection Kit for Profiling and
Screeing GPCRs II-21
Omeros Completes Acquisition of GPCR Assay Technology from
Patobios II-22
DiscoveRx Corporation Takes Over KINOMEscanâ„¢ II-22
Roche and ATCC Collaborate on Real-Time Endogenous GPCR
Function Research II-22
Millipore Launches Luminescent GPCR Reporter Frozen Cells II-22
Ascent Therapeutics re-christened as Anchor Therapeutics II-22
Affitech Sells Cancer Vaccine Project to Focus on GPCR Research II-23
Medarex Releases Pre-clinical Data for MDX-1338 II-23
Compugen Declares Positive Therapeutic Effects of CGEN-25009 II-23
Addex Releases Clinical Data for ADX10059 II-23
Arana Receives Patent Approval for PMX53 and Related GPCR
Compounds II-24
Epix Pharmaceuticals Receives Patent Approval for PRX-03140
and Related Compounds II-24
Odyssey Thera Receives Patent Approval for Fluorescence-Based
Assays II-24
Cisbio Bioassays Introduces Cellul'erk Assay II-24
DiscoveRx Introduces Products and Services to Assays and
Reagents Portfolio II-25
PerkinElmer Introduces Novel Ion Channel and GPCR Cell Lines II-25
Millipore Launches New AllostericProfilerTM Service II-25
Ligand Pharmaceuticals and Trevena Enter into Agreement II-25
ChanTest Takes Over ACS II-26
PerkinElmer Enters into Collaboration with Sangmyung University II-26
Debiopharm Group Inks Exclusive Agreement with MSM Protein
Technologies II-26
GVK Biosciences and University of Tokyo Sign Agreement II-26
MSM Protein Technologies Enters into Alliance with Merck Serono II-27
Xenome Enters into Agreement with Axxam II-27
DiscoveRx and GlaxoSmithKline Inks Global Agreement II-27
Sygnature Enters into Contract Chemistry Agreement with
Heptares Therapeutics II-27
Enzo Life Sciences Enters into Partnership with BioTek
Instruments II-28
Heptares Therapeutics Enters into Agreement with Novartis
Option Fund II-28
CellAura Enters into Partnership with Cisbio Bioassays II-28
Euroscreen and Novartis Ink Research Collaboration Agreement II-28
Evotec Enters into Co-marketing Agreement with DiscoveRx II-29
Jubilant Biosys Inks Co-marketing Agreement with DiscoveRx II-29
Faust Pharmaceuticals Changes Name to Domain Therapeutics II-29
GSK, MRCT and DiscoveRx Collaborate for Deorphanization of GPCRs II-29
DiscoveRx Inks Agreement with BioFocus II-30
Actelion's S1P1 Receptor Agonist to Enter into Phase II
Clinical Trial II-30
AnaSpec Introduces Two Isoform Specific Antibodies II-30
Millipore Introduces MultiScreen®HTS+ Filter Plates II-30
Faust and Takeda Enter into Research Agreement II-31
Caliper Life Sciences Collaborates with DiscoveRx II-31
Compugen Inks Agreement with Merck Serono II-31
BioFocus and Amgen Extend Drug Discovery Agreement II-31
DiscoveRx Selects Cosmo Bio to Distribute GPCR Profiling
Service across Japan II-31
Euroscreen Extends Agreement with Cephalon II-32
BioFocus DPI Introduces Novel Version of GPCR SARfari II-32
PerkinElmer Takes Over Euroscreen Products II-32

7TM Pharma A/S (Denmark) II-33
Actelion Pharmaceuticals Ltd. (Switzerland) II-33
Acure Pharma AB (Sweden) II-33
Anchor Therapeutics (USA) II-34
Arena Pharmaceuticals, Inc. (US) II-34
Addex Pharmaceuticals (Switzerland) II-34
Acadia Pharmaceuticals Inc., (USA) II-35
Cara Therapeutics, Inc. (USA) II-36
DiscoveRx Corporation (USA) II-36
Dimerix Bioscience Pty Ltd (Australia) II-36
Domain Therapeutics (France) II-37
Euroscreen SA (Belgium) II-37
Trevena, Inc. (USA) II-37

Table 2: World Recent Past, Current and Future Market Analysis
for G-Protein Coupled Receptors (GPCRs) Targeting Drugs
Analyzed with Annual Sales Figures in US$ Billion for Years
2009 through 2017 (includes corresponding Graph/Chart) II-38

Table 3: World Historic Review for G-Protein Coupled Receptors
(GPCRs) Targeting Drugs Analyzed with Annual Sales Figures in
US$ Billion for Years 2003 through 2008 (includes
corresponding Graph/Chart) II-39


Total Companies Profiled: 43

Region/Country Players
The United States 24
Europe 15
France 2
Germany 1
The United Kingdom 3
Italy 1
Rest of Europe 8
Asia-Pacific (Excluding Japan) 3
Middle East 1

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