Abstract
D&MD' s "Market Opportunity in the G-Protein Coupled Receptors (GPCRs) Target Space: Qualitative and Quantitative Market Metrics" is a focused market analysis report that provides the latest analysis of the GPCR target space in terms of druggable targets available, quantitative metrics defining the space, and therapeutic candidates in various clinical stages of the developmental pipeline.
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
