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170 pages

Date published 
April 2007

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Metabolic and Inflammatory Disease R&D Table of Contents

Metabolic and Inflammatory Disease R&D: An Assessment of 5 Highly Promising Therapeutic Classes

By Peter Norman, MBA, PhD
 

Chapter 1
INTRODUCTION
1.1 Target-Based Approaches to Drug Discovery
1.2 Identification of Current High-Profile Targeted Approaches
Inflammatory and Immune Diseases
Metabolic Diseases
1.3 Does Extensive Activity Predict Success?
Success from High Activity
Leukotriene CysLT1 Receptor Antagonists
PDE5 Inhibitors
COX-2 Inhibitors
Failures Despite Intense Efforts
5-Lipoxygenase Inhibitors
Renin Inhibitors
Thromboxane Antagonists
Long-lived Efforts
p38 MAP Kinase
PDE4 Inhibitors
1.4 Reasons for Failures

Chapter 2
METHODOLOGY: IDENTIFYING HIGH-PROFILE AREAS OF EFFORT
2.1. Medical Advances
2.2. Literature Activity
2.3. Meetings
2.4. Patenting Activity
2.5. Commercial Deals

Chapter 3
HIGH-PROFILE TOPICS IN INFLAMMATORY AND METABOLIC DISEASES
3.1. Inflammatory Diseases
Respiratory Diseases
Arthritis
3.2. Metabolic Diseases
Diabetes
Obesity
Metabolic Syndrome
Lipid Disorders

Chapter 4
CHEMOKINE ANTAGONISTS
4.1. Chemokines
4.2. Targets
CCR Receptors
CXCR Receptors
4.3. Pathophysiological Role(s)
Inflammatory Processes
HIV Infection
4.4. Potential Therapeutic Indications
Atherosclerosis
Allergic Rhinitis
Asthma
Chronic Obstructive Pulmonary Disease
Multiple Sclerosis
Rheumatoid Arthritis
Cancer
4.5. Possible Pitfalls
CCR Receptors
CXCR Receptors
CCR1 Antagonists
SH-T-04268-H
CCR2 Antagonists
Chemokine Antagonists: Strong Evidence … Well Validated. Q&A with Dr. Kris Vaddi, vice president, Preclinical Biology, Incyte, and Dr. Robert Newton, Drug Discovery Biology, Incyte
CCR3 Antagonists
CCX-282
CXCR2 Antagonists
SCH-527123
GSK-656933
DF-1681
CTCE-9908
Preclinical Efforts
4.6. Active Major Companies
Amgen
Astellas
AstraZeneca
Bayer Schering
Boehringer Ingelheim
Bristol-Meyers Squibb
Daiichi Sankyo
GlaxoSmithKline
Hoffmann-La Roche
Janssen
Merck
Novartis
Pfizer
sanofi-aventis
Schering-Plough
Takeda
Wyeth
4.7. Other Active Companies
AnorMED
ChemoCentryx
Chemokine Therapeutics
Dompé
Incyte
Millennium Pharmaceuticals
Ono Pharmaceutical
Pharmacopeia Drug Discovery
UCB SA
4.8. Significant Commercial Deals
4.9. Current Outlook

Chapter 5
TOLL-LIKE RECEPTOR MODULATORS
5.1. Pathophysiological Role(s)
5.2. Potential Therapeutic Indications
5.3. Possible Pitfalls
5.4. Level of Activity, 2000 to 2006
5.5. Development Compounds
TLR-3 Agonists
Ampligen
TLR-4 Modulators
Eritoran
TAK-242
CRX-675
TLR-7 Agonists
852A
Isatoribine and ANA-975
ANA-773
Toll-like Receptors: Opportunities in Numerous Disease States. Q&A with Professor Luke O’Neill, Opsana Therapeutics
TLR-9 Agonists
PF-3512676
Tolamba, Heplisav, and ISS-1018
CpG-10101
IMO-2055
Preclinical Agents
5.6. Active Major Companies
AstraZeneca
Eisai
GlaxoSmithKline
Novartis
Pfizer
sanofi-aventis
Takeda
5.7. Other Active Companies
3M Pharmaceuticals
Anadys
Coley Pharmaceuticals
Dynavax Technologies
Hemispherx Biopharma
Idera Pharmaceuticals
Innate Pharma
Opsona Therapeutics
5.8. Significant Commercial Deals
5.9. Current Outlook

Chapter 6
11β-HYDROXYSTEROID DEHYDROGENASE INHIBITORS
6.1. 11β-Hydroxysteroid Dehydrogenase
11β-HSD1
11β-HSD2
6.2. Pathophysiological Role(s)
6.3. Potential Therapeutic Indications
Type 2 Diabetes
11β-HSD Inhibitors: Broad Applications in Metabolic Disease. Q&A with Dr. Greg Hollis, vice president, Advanced Technology, Incyte; Dr. Deborah Hunter, leader, Incyte; and Dr. Nigel Vicker, group leader, Discovery Chemistry, Ipsen
Metabolic Syndrome
Obesity
Memory Disorders
Inflammation
6.4. Possible Pitfalls
INCB-13739
AMG-221
Preclinical Efforts
6.5. Active Major Companies
Abbott
Amgen
AstraZeneca
Hoffman-La Roche
Janssen
Merck
Pfizer
Takeda
Wyeth
6.6. Other Active Companies
Bionetworks GmbH
Biovitrum AB
Evotec AG
Incyte
Sterix
6.7. Significant Commercial Deals
6.8. Current Outlook

Chapter 7
MELANOCORTIN RECEPTOR MODULATORS
7.1. Melanocortin Receptors
7.2. Drug Targets
7.3. Pathophysiological Role(s)
7.4. Potential Therapeutic Indications
Obesity
Sexual Dysfunction
Depression and Anxiety
7.5. Possible Pitfalls
Bremelanotide
AP-214
Preclinical Efforts
MC4 Agonists
MC4 Antagonists
7.6. Active Major Companies
Eli Lilly
Merck
Novartis
Novo Nordisk
Roche
7.7. Other Active Companies
Action Pharma
Ipsen
Millennium Pharmaceuticals
Neurocrine Biosciences
Palatin Technologies
Procter & Gamble
Santhera
Taisho
7.8. Significant Commercial Deals
7.9. Commercial Outlook

Chapter 8
MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISTS
8.1. Melanin-Concentrating Hormone
8.2. MCH-1 Receptor
8.3. Pathophysiological Role(s)
8.4. Potential Therapeutic Indications
Obesity
Depression and Anxiety
8.5. Possible Pitfalls
8.6. Development Compounds
8.7. Clinical Compounds
AMG-076
856464
NGD-4715
Preclinical Efforts
8.8. Active Major Companies
Abbott Laboratories
Amgen
AstraZeneca
Boehringer Ingelheim
Eli Lilly
GlaxoSmithKline
Merck
sanofi-aventis
Schering-Plough
Takeda
8.9. Other Active Companies
7TM Pharma A/S
Arena Pharmaceuticals
Biovitrum
Lundbeck
Neurocrine Biosciences
Neurogen
Procter & Gamble
Taisho Pharmaceuticals
8.10. Significant Commercial Deals
8.11. Current Outlook

References

Glossary of Selected Terms

Company Index with Web Addresses