| D&MD’s Transmembrane Transporters: High Sales, High Potential as Drug Targets market report comprehensively reviews transmembrane transporters (including ion channels) and assesses their importance as drug targets. Data presented in this report demonstrates that among the top 100 best-selling drugs in the United States in 2004, transporters represent the most abundant class of targets. This report will help readers assess or reassess their strategies with respect to this target class. An online survey conducted specially for this report shows that transporters (alongside protein kinases), are regarded as commercially the most promising targets available to the drug industry. Although much has been learned about transporters as drug targets, only recently have scientists been able to directly examine three-dimensional ion channel and other integral membrane transporter structures.
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- Chapter 1: Executive Summary
- Chapter 2: Why Target Transporters?
- Introduction
- Functions of Transporters
- Transport Mechanisms
- TC Classification System for Transporters
- Transporter Families and Superfamilies
- Progress in Structure Elucidation
- Top-Selling Transporter-Targeted Drugs
- Chapter 3: Ion Transporters
- Introduction
- Ion Pumps
- Overview
- Ion Pumps As Drug Targets
- The ABC Superfamily
- The P-ATPase Superfamily
- Ion Channels
- Overview
- Structural Architectures
- Screening Technologies
- Sodium Channels As Drug Targets
- The Voltage-gated Ion Channel Superfamily
- Other Voltage-gated Channels
- The Epithelial Na+ Channel Family
- Potassium Channels As Drug Targets
- The Voltage-gated Ion Channel Superfamily
- The Inward Rectifier K+ Channel Family
- The Ca2+-activated Auxiliary Subunit Slo รข Family
- Calcium Channels As Drug Targets
- The Voltage-gated Ion Channel Superfamily
- Other Calcium Channels
- Chloride Channels As Drug Targets
- The Epithelial Chloride Channel Family
- The Chloride Channel Family
- Solute (Ion) Carriers
- Overview
- Solute Carriers As Drug Targets
- The Cation-Chloride Cotransporter Family
- The Major Facilitator Superfamily
- The Cation:Proton Antiporter1 Family
- Other Solute Carriers
- Miscellaneous Targets
- Chapter 4: Neurotransmitter-binding Transporters
- Introduction
- Major Neurotransmitters and Their Functions
- Role of Membrane Transporters in Neurotransmission
- Ionotropic Receptors as Drug Targets
- Overview
- The Ligand-gated Ion Channel Family
- GABA-A Receptors
- 5-HT3 Receptor
- Nicotinic Acetylcholine Receptor
- Glycine Receptor
- The Glutamate-gated Ion Channel Family
- NMDA Receptor
- AMPA Receptor
- Kainate Receptor
- The ATP-gated Cation Channel Family
- Solute Carriers as Drug Targets
- Overview
- The Neurotransmitter:Sodium Symporter Family
- Serotonin Transporter
- Noradrenalin Transporter
- Dopamine Transporter
- GABA Transporters
- Glycine Transporter
- The Dicarboxylate/Amino Acid:Cation Symporter Family
- The Major Facilitator Superfamily
- Chapter 5: Lipid, Bile Acid, and Carbohydrate Transporters
- Lipid and Bile Acid Transporters as Drug Targets
- Introduction
- The ABC Superfamily
- ABCA1 Transporter
- ABCG5 and ABCG8 Transporters
- The Bile Acid:Na+ Symporter Family
- IBAT Transporter
- The Putative Fatty Acid Transporter Family
- FATP4 Transporter
- Carbohydrate Transporters as Drug Targets
- Introduction
- The Major Facilitator Superfamily
- GLUT4 Transporter
- The Solute:Sodium Symporter Family
- SGLT1 and SGLT2 Transporters
- Chapter 6: Other Areas of Research
- Transporters in Cancer Drug Resistance
- Role of MDR-ABC Transporters
- MDR1 Transporter
- MRP1 Transporter
- MXR Transporter
- Other Transporters
- Pharmacological Modulation of MDR Transporters
- Transporters in ADME/Tox
- ABC Transporter Assays for ADME/Tox Prediction
- Ion Channel Assays For Cardiac Toxicity
- Transporters in Infectious Diseases
- Transporters in Drug Delivery
- Chapter 7: Market Considerations and Forecasts
- Introduction
- The Survey
- Preliminary Remarks
- Questions and Answers
- Conclusions
- The World Pharmaceutical Market
- The Market for Transporter-Targeted Products
- Cardiovascular Market
- Central Nervous System (CNS) Market
- Alimentary/Metabolic Market
- Transporter Drug R&D: Leading Indications
- Transporter Drug R&D: Leading Companies
- Transporter Drug Companies and Applications
- Transporter Drug Companies and Targets
- Transporter Market Analysis and Forecasts to 2010
- Chapter 8: Trends and Opportunities
- Transporters Embraced by Big Pharma
- Over 100 Transporter Targets Under Investigation
- The Most Popular Targets and Indications
- Opportunities in Analgesia
- Next-Generation Ion Channel Modulators
- Next-Generation Ligand-Gated Ion Channel Modulators
- Next-Generation Neurotransmitter Re-uptake Inhibitors
- Next-Generation Glutamate-Gated Ion Channel Modulators
- Exploring New Transporter Targets
- Towards Gene Family-Based Transporter Drug Discovery
- Expanding Applications Outside Drug Discovery
- Chapter 9: Company Profiles
- Abbott
- Akzo Nobel
- Astellas Pharma Inc
- AstraZeneca
- Bayer AG
- Biovail
- Boehringer Ingelheim GmbH
- Bristol-Myers Squibb
- Cortex Pharmaceuticals Inc
- Daiichi Sankyo Co Ltd
- Elan Plc
- Eli Lilly and Company
- GlaxoSmithKline Plc
- Hoffman-La Roche
- ICagen Inc
- Johnson & Johnson
- Lundbeck A/S
- Merck KGaA
- Merck & Co Inc
- Mitsubishi Pharma
- NeuroSearch A/S
- Novartis AG
- Novo Nordisk A/S
- NPS Pharmaceuticals
- Pfizer Inc
- Sanofi-Aventis
- Sepracor Inc
- Servier
- Takeda Pharmaceutical Company Ltd
- Wyeth
- Table Of Exhibits
- 2.1 Transport Mechanisms During the 1990s
- 2.2 Transporter Classes
- 2.3 TC Superfamilies
- 2.4 Targets of Top 100 Drugs by US Sales in 2004
- 2.5 Top 10 Drugs for 2004 Ranked by US Sales
- 2.6 Top 10 Drugs for 2004 Ranked by US Sales Growth Rates
- 2.7 Top-selling Transporter-targeted Drugs for 2004 by US Sales
- 2.8 Leading Transporter Companies by US Top 100 Sales in 2003 and 2004
- 3.1 Ion Transporters: Summary of Drug Targets
- 3.2 Drugs Targeting ATP-Binding Cassette Transporters (ABC Transporters)
- 3.3 Drugs Targeting ATPases
- 3.4 Drugs Targeting Sodium Channels (SCNs)
- 3.5 Drugs Targeting Potassium Channels (KCNs)
- 3.6 Drugs Targeting Calcium Channels (CACNs)
- 3.7 Drugs Targeting Chloride Channels
- 3.8 Drugs Targeting Solute Carriers (SLCs)
- 3.9 Drugs Targeting Other Transporter Targets
- 4.1 Neurotransmitter-Binding Transporters: Summary of Drug Targets
- 4.2 Drugs Targeting Ionotropic Receptors
- 4.3 Drugs Targeting Solute Carriers (SLCs)
- 5.1 Lipid, Bile Acid, and Carbohydrate Transporters: Summary of Drug Targets
- 5.2 Drugs Targeting Lipid, Bile Acid, and Carbohydrate Transporters
- 7.1 Job Functions of Survey Respondents
- 7.2 Target Classes by Commercial Potential
- 7.3 Transporter Target Subclasses by Commercial Potential
- 7.4 Transporters: Toxicology versus Therapeutics
- 7.5 Respondents Developing Transporter Drugs
- 7.6 Transporter Indications in Development
- 7.7 Transporter Subclasses in Development
- 7.8 Respondents Marketing Transporter-Targeted Drugs
- 7.9 Indications of Marketed Transporter-Targeted Drugs
- 7.10 Targets of Marketed Transporter Drugs
- 7.11 High-Potential Transporter Indications
- 7.12 Target Acquisition Strategies
- 7.13 Target Development Strategies
- 7.14 World Pharma Market by Region in 2005 and 2010
- 7.15 World Pharma Market by Indication in 2005 and 2010
- 7.16 Transporter Drug Indications by Development Stage
- 7.17 Transporter Companies by Product Portfolio
- 7.18 Transporter Indications by Top 20 Companies
- 7.19 Top Transporter Companies by Top Targets
- 7.20 Top Transporter Indications by Target
- 7.21 Transporter Market Forecasts by Indication, 2005-2010
- 7.22 Transporter Market Forecasts by Region, 2005-2010
- 9.1 Product Portfolio for Abbott by Target
- 9.2 Product Portfolio for Akzo Nobel by Target
- 9.3 Product Portfolio for Astellas by Target
- 9.4 Product Portfolio for AstraZeneca by Target
- 9.5 Product Portfolio for Bayer by Target
- 9.6 Product Portfolio for Biovail by Target
- 9.7 Product Portfolio for Boehringer Ingelheim by Target
- 9.8 Product Portfolio for Bristol-Myers Squibb by Target
- 9.9 Product Portfolio for Cortex Pharmaceuticals by Target
- 9.10 Product Portfolio for Daiichi Sankyo by Target
- 9.11 Product Portfolio for Elan by Target
- 9.12 Product Portfolio for Eli Lilly by Target
- 9.13 Product Portfolio for GlaxoSmithKline by Target
- 9.14 Product Portfolio for Hoffmann-La Roche by Target
- 9.15 Product Portfolio for Icagen by Target
- 9.16 Product Portfolio for Johnson & Johnson by Target
- 9.17 Product Portfolio for Lundbeck by Target
- 9.18 Product Portfolio for Merck KGaA by Target
- 9.19 Product Portfolio for Merck & Co by Target
- 9.20 Product Portfolio for Mitsubishi Pharma by Target
- 9.21 Product Portfolio for NeuroSearch by Target
- 9.22 Product Portfolio for Novartis by Target
- 9.23 Product Portfolio for Novo Nordisk by Target
- 9.24 Product Portfolio for NPS Pharmaceuticals by Target
- 9.25 Product Portfolio for Pfizer by Target
- 9.26 Product Portfolio for Sanofi-Aventis by Target
- 9.27 Product Portfolio for Sepracor by Target
- 9.28 Product Portfolio for Servier by Target
- 9.29 Product Portfolio for Takeda by Target
- 9.30 Product Portfolio for Wyeth by Target
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