Abstract
Kinase Therapeutics: A Wealth of Targets Sparks a Highly Active Market reviews the considerable array of drug development efforts directed at kinases. This new CHA Advances report describes the various classes of kinases for which inhibitors are being developed, and examines the general strategies and technologies being employed to commercialize kinase inhibitors, including those underway at major pharmaceutical companies.
The ubiquity of kinases as potential targets means that eventually they will be exploited for virtually every human disease, particularly diabetes, inflammatory disorders, and especially cancer. The success of Novartis' Gleevec and Roche's Herceptin has demonstrated that kinase inhibitors for cancer that are effective and well-tolerated can enjoy strong sales.
Kinase modulation is without doubt a novel and promising approach to treating disease, but challenges remain. Those evaluated in the report include:
- Ensuring target relevance and specificity.
- Overcoming resistance.
- Designing clinical trials to maximize the response to a drug.
- Addressing the high cost of novel therapeutics.
Kinase Therapeutics: A Wealth of Targets Sparks a Highly Active Market evaluates the market potential for kinase-targeting compounds in development for a variety of diseases. Only those conditions for which drug candidates have reached at least mid-stage clinical development are covered. The report addresses the major disease categories, including:
- Patient numbers for diseases of interest to developers of kinase modulators.
- Competing therapeutics already on the market, particularly those that have recently gained regulatory approval.
- Evaluation of the pros and cons of various targets and therapeutic approaches
- Estimates of market sizes in dollars, where available.
Kinases represent perhaps the largest druggable class of targets. And yet researchers have only started to scratch the surface. Most, if not all, big pharmas have programs in this area, and are in fact among the leaders in the field. This report is crucial reading for executives who need to stay on top of the technical and commercial developments in the area of kinase therapeutics.
About the Author
Mark C. Via, an editor at CTB International Publishing, has ten years' experience writing and editing for pharmaceutical trade publications. Mr. Via holds a B.A. degree in history from Williams College. Mr. Via has authored previous Advances reports, including Inflammatory Disease Therapeutics: Pipelines and Competitive Dynamics.
Table of Contents
Chapter 1. Background and Scientific Overview:
Kinases Are Important Cellular Signaling Enzymes
- 1.1 The Function of Kinases
- 1.2 Classifying Kinases
- 1.3 Kinases: Ubiquitous Drug Targets
- The Established Link to Cancer
- Targeting Receptor Tyrosine Kinases
- Targeting Non-receptor Tyrosine Kinases
- Targeting Serine-Threonine Kinases for Cancer
- Targeting Serine-Threonine Kinases for Diseases Other than Cancer
- 1.4 Overview of the Field
Chapter 2. Kinase Inhibitors in Development:
Tapping into a Wealth of Targets
- 2.1 Types of Kinase Inhibitors: Small Molecules and Their Alternatives
- 2.2 Receptor Tyrosine Kinase Inhibitors
- EGFR Family
- Split Kinase Domain Family
- Targeting VEGF with RNAi for Opthalmic Diseases
- 2.3 Non-receptor Tyrosine Kinase Inhibitors
- Abl
- Tec Family Kinases
- Syk
- JAK
- 2.4 Serine-Threonine Kinase Inhibitors for Cancer
- Ras-Raf-MEK-ERK Pathway
- ALK5
- PKC-α
- PKC-β
- ROCK
- PI3 Kinase Pathway
- mTOR
- CDK
- Aurora
- PLK
- CHK
- 2.5 Serine-Threonine Kinase Inhibitors for Diseases Other than Cancer
- PKC-δ
- p38 MAP Kinase
- JNK
- MLK
- NF-κB Pathway
- PI3 Pathway
- GSK3
- mTOR
- AMPK
- PDHK
Chapter 3. Business and Strategic Outlook:
Market Potential for Kinase-Targeted Drugs
- 3.1 Special Challenges in Developing Kinase Modulators
- Target Relevance and Specificity
- Resistance
- Trial Design
- Cost
- 3.2 Markets for Kinase-Based Drugs
- Cancer
- Age-Related Macular Degeneration
- Immune and Inflammatory Diseases
- Diabetic Complications
Chapter 4. Expert Commentaries
- 4.1 Shripad Bhagwat, PhD, SVP, Drug Discovery, Ambit Biosciences
- 4.2 Sean G. Buchanan, PhD, Senior Director, Biology, SGX Pharmaceuticals
- 4.3 K. Peter Hirth, Phd, CEO, Plexxikon
- 4.4 Tony Hunter, PhD, Professor, Salk Institute for Biological Studies
- 4.5 Michael Melnick, VP, Business and Corporate Development, Cell Signaling Technology
Chapter 5. Company Profiles
- 5.1. Ambit Biosciences
- 5.2. Amgen
- 5.3. Amphora Discovery
- 5.4. ARIAD Pharmaceuticals
- 5.5. Astex Therapeutics
- 5.6. AstraZeneca
- 5.7. BioFocus
- 5.8. Bristol-Myers Squibb
- 5.9. Cell Signaling Technology
- 5.10 CGI Pharmaceuticals
- 5.11 Cyclacel Pharmaceuticals
- 5.12. Eli Lilly & Co.
- 5.13. Exelixis
- 5.14. Millennium Pharmaceuticals
- 5.15. Novartis
- 5.16. Pfizer
- 5.17. Rigel Pharmaceuticals
- 5.18. Sanofi-Aventis
- 5.19. Semafore Pharmaceuticals
- 5.20. SGX Pharmaceuticals
- 5.21. Sunesis Pharmaceuticals
- 5.22. Upstate
- 5.23. Vertex Pharmaceuticals










