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Kinase Therapeutics: A Wealth of Targets Sparks a Highly Active Market

Published by: CHI Insight Pharma Reports

Published: May. 1, 2006 - 125 Pages


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-¥á

PKC-©¬

ROCK

PI3 Kinase Pathway

mTOR

CDK

Aurora

PLK

CHK


2.5 Serine-Threonine Kinase Inhibitors for Diseases Other than Cancer


PKC-¥ä

p38 MAP Kinase

JNK

MLK

NF-†B 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




Appendix: Kinase Names




Company Index with Web Addresses




List of Figures

Figure 1.1. Signaling Pathway Activation

Figure 1.2. The Human Kinome

Figure 1.3. Mechanisms of Activation of Normal Tyrosine Kinases




List of Tables

Table 2.1. Receptor Tyrosine Kinase Inhibitors in Clinical Trials

Table 2.2. Non-receptor Tyrosine Kinase Inhibitors in Clinical Trials

Table 2.3. Serine-Threonine Kinase Inhibitors in Clinical Trials for Cancer

Table 2.4. Serine-Threonine Kinase Inhibitors in Clinical Trials for Diseases Other than Cancer

Table 3.1. Estimated New Cases of Cancer in the United States, Total and Selected Types

Table 3.2. Sales of Kinase Inhibitors for Cancer, 2004 and 2005

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.

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