Market Opportunity in the G-Protein Coupled Receptors (GPCRs) Target Space: Qualitative and Quantitative Market Metrics

Table of Contents

CHAPTER 1: EXECUTIVE SUMMARY

• Introduction to GPCRs and Focus of This Report
• GPCR Categories, Signaling and Drug Discovery
• Market Opportunity in the GPCRs Space

CHAPTER 2: MOLECULAR DETAILS OF GPCR CLASSIFICATION, BIOLOGY, AND TECHNOLOGIES FOR THEIR INTERROGATION AND SCREENING

• Scope of This Chapter
• Overview of the GPCR Space
• GPCR Signaling Cascades In Vivo- The Molecular Events Triggered Upon GPCR Activation
• New Paradigms of GPCR Signaling
• GPCR Cross Talk and Dimerization
• RGS Proteins
• GPCR Kinases (GRKs) and Desensitization of GPCRs
• Orphan GPCRs (oGPCRs)
• Structural Approaches: A Major Hurdle in GPCR Drug Discovery
• GPCR Assay Technologies- How to Study GPCRs for Screening and Analysis Especially in Drug Discovery
• Environments
• Receptor Ligand Binding and GTP Binding Assays
• Second Messenger Assays
• Protein Interaction Assays
• GPCR Trafficking Assays
• Gene Reporter Assays
• Bioimpedance Assays
• Selected Technical References on GPCRs

CHAPTER 3: BUSINESS ANALYSIS OF THE G PROTEIN-COUPLED RECEPTORS (GPCRS) SPACE

• Scope of this Chapter
• Analysis of the Pharmaceutical Targets Space and Overview of Druggability of Targets- Qualitative and
• Quantitative Trends
• GPCRs as Drug Targets
• Market Trends in the GPCR Interrogation/Analysis Space- Qualitative and Quantitative Market Trends3-
• Size of GPCR Interrogation/Analysis Screening Campaigns and the Overall Market Size
• Qualitative Impressions of the GPCR Marketplace, Trends Therein, and Open Questions
• The Intellectual Property Landscape for GPCRs and Other Biologics
• References

CHAPTER 4: THERAPEUTICS PIPELINE: GPCR-ADDRESSING POTENTIAL DRUGS AND TARGETS ADDRESSED

• Scope of This Chapter

CHAPTER 5: COMPANY PROFILES

• 3M Pharmaceuticals
• 7TM Pharma
• Arena
• atugen
• Euroscreen

APPENDIX 1: INTELLECTUAL PROPERTY OVERVIEW

• Trademarks and Service Marks: Logos and Brand Names
• Copyright: Written and Audiovisual Works
• Trade Secrets: A Grab-Bag of Perpetual Secrets
• A Short Patent Primer
• Patents: Procedures and Players
• After the Grant: Patent Litigation and Licensing
• Patenting GPCRs and Other Proteins
• The Four Key Elements of Patents: Patentable Subject Matter, Usefulness, Novelty, and Non-obviousness
• Subject Matter: What Can Be Claimed?
• Usefulness: Proving the Receptor' s Function
• Changes in the Utility Examination Guidelines
• Meeting the New Utility Test: Characterizing Receptor Function
• Novelty and Non-obviousness: Searching for Prior Art
• Two More Elements: Adequate Written Descriptions and Enablement
• Forging an IP-Savvy Business Model
• Managing the Tradeoffs
• Tradeoff #1: Patenting Early vs. Patenting Strong
• Tradeoff #2: Patent Strength vs. Patent Cost
• Tradeoff #3: Litigation and Licensing vs. The Core Business
• When You Find Prior Art: Patenting a GPCR in the Face of Prior Discovery
• Equivalent Inventions- The Impact of the Festo Case
• Notes and References

APPENDIX 2: IMPORTANT AND EMERGING THEMES IN THE GPCRS SPACE

TABLE OF EXHIBITS

• Exhibit 1.1 Molecular Targets of Currently-Approved Drugs
• Exhibit 1.2 Intracellular Signaling Upon GPCR Stimulation
• Exhibit 1.3 ADescription of Drug Targets within the GPCR Target Space
• Exhibit 1.3 BGPCR Receptor Types, Mechanism of Action, Common Drug Examples
• Exhibit 1.4 The Market For Various Assays to Interrogate GPCRs In Drug Discovery
• Exhibit 2.1 Schematic of Typical GPCR Structure*
• Exhibit 2.2 Classification of the Various GPCR Families and Sub-Families**
• Exhibit 2.3 Endogenous Cognate Ligands of the GPCRs**
• Exhibit 2.4 Signaling Cascades Proximal to the GPCR
• Exhibit 2.5 Reverse Pharmacology and How It Differs from "Traditional" Drug Discovery
• Exhibit 2.6 X-Ray Crystal Structure of Bacterial Rhodopsin Complexed with Retinal
• Exhibit 2.7 Summary of Assay Types Deployed to Study GPCRs
• Exhibit 2.8 Approaches to Screening Modulators of GPCRs Based on Protein-Protein Interaction
• Exhibit 2.9 Formats of GPCR Trafficking Assays
• Exhibit 3.1 Number of Targets Around Which All FDA-approved Drugs Are Built Around
• Exhibit 3.2 Comparison of the Druggable Genomes of Selected Eukaryotes
• Exhibit 3.3 Drug-Target Families and The Druggable Genome
• Exhibit 3.4 A Description of Drug Targets within the GPCR Target Space
• Exhibit 3.4B GPCR Receptor Types, Mechanism of Action, Common Drug Examples
• Exhibit 3.5 The Pharmacological Target Space- Comparison of the Various Target Classes
• Exhibit 3.6 Percentage of R&D Efforts Directed at Different GPCR Subclasses
• Exhibit 3.7 The Growth of the GPCR Interrogation/Analysis Marketplace
• Exhibit 3.8 Monthly Research Spending Interrogating/Analyzing GPCRs
• Exhibit 3.9 R&D Dollar Spending Breakout on Various Assays to Interrogate GPCRs
• Exhibit 3.10 Growth or Decline of Different GPCR Interrogation/Analysis Approaches in Pharmaceutical and Biotechnology Companies
• Exhibit 3.11 Distribution of Experiments Run by Pharmaceutical Respondents versus Biotechnology Respondents in terms of Interrogating/Analyzing GPCRs
• Exhibit 3.12 Market Size for GPCR Interrogation/Analysis in terms of Industry Dollars and Experiments Assays
• Exhibit 3.13 Top GPCR Targeted Drug Development Projects
• Exhibit 4.1 All GPCR-directed Therapeutics in Various Stages of the Developmental Pipeline
• Exhibit 4.2 Leading Compounds Targeted to the Various GPCR Targets that are Showing Faster-than- Average Progression Through Development
• Exhibit App1.1 Likely Spectrum of Protein Patentability Based on Utility Requirements
• Exhibit App1.2 Useful Sources for Patent Prior Art Searches