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市場調査レポート
創薬におけるキナーゼ標的
Targeting Kinases for Drug Discovery
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Abstract
Introduction
Protein kinases - intracellular enzymes that modulate cellular functions -
play a pivotal role in the signal transduction processes that regulate many
key biological processes. Abnormalities in these signal transduction pathways
are implicated in the etiology of numerous diseases, which has motivated
pharmaceutical companies to pursue protein kinases as drug targets - a trend
that now accounts for 20-30% of all drug discovery programs.
Get the Answers You Need to Shape Your Strategy
- The protein kinase family is a mostly unexploited class of drug targets.
Novartis' s kinase inhibitor Gleevec, approved in 2001 for CMS, boasts sales of
$3 billion worldwide in 2007. What effect has Gleevec' s success had on the
development of new kinase inhibitors?
- Most major pharmaceutical companies are avidly pursuing kinase inhibitor
development both internally and/or in collaboration with biotech companies.
Which Big Pharma players have kinase inhibitor development programs underway?
What are some of the key collaborations and alliances that have formed around
kinase targets? What is the current state of the kinase inhibitor development
pipeline?
- Whereas development of kinase inhibitors in the past has been hindered by
the perceived complexity of the process, technological advances will drive the
future development of kinase inhibitors. What are some of the technologies
that have aided the development of new kinase inhibitors? How has technology
altered the choice of drug targets and disease indications being pursued by
pharma companies?
- At present, oncology patients have derived the most benefit from kinase
inhibitors, although the potential exists for patients with longer-term
chronic conditions to benefit. What chronic conditions are under investigation
for treatment with kinase inhibitors? What difficulties or opportunities lie
on the path of such agents' approval?
Scope
- Commercial potential: current state of the kinase inhibitor market;
potential market influences.
- About protein kinases: protein kinase family classifications; structure
and function of the kinase and its inhibitors; current screening procedures.
- Kinase inhibitor selectivity: why selectivity is important and how it
can be determined.
- Development challenges: the influences of mutations and drug
resistance; p38 MAP kinases.
- Pharmacogenomics: the influence of genetic variation on kinase
inhibitor efficacy.
- Profiles: select companies employing novel technologies and strategies
in kinase research.
- Market outlook: our general forecast for the direction and success
of protein kinase inhibitors.
Table of Contents
- Executive Summary
- Strategic Considerations
- Stakeholder Implications
- Introduction
- Commercial Potential of Small-Molecule Kinase Inhibitors
- Mechanism/Structure/Discovery/Design.
- Protein Kinase Classification
- Protein Kinase Structure and Function
- Screening for Kinase Inhibitors
- Kinase Inhibitor Selectivity
- The Relative Importance of Selectivity
- Kinase Profiling
- Challenges in Kinase Inhibitor Development
- Influence of Mutations in the Target Kinase
- Acquired Drug Resistance
- p38α MAP Kinase Inhibitor Development
- Pharmacogenomics in Kinase Inhibitor Development
- Profiles in Innovation
- Astex Therapeutics
- SGX Pharmaceuticals
- Locus Pharmaceuticals
- Kinex Pharmaceuticals
- Ambit Biosciences
- Emiliem
- TargeGen
- Exelixis
- Outlook for Kinase Inhibitors
Tables
- 1. Global Sales of Marketed Kinase Inhibitors, 2006-2007
- 2. Orphan Designations for Gleevec in the United States
- 3. Select Kinase Inhibitors in Development
- 4. Select Kinases of Current Interest for Pharmaceutical Development
- 5. Companies Offering Kinase Profiling and Screening Services
- 6. Select Kinase-Based Deals
Figures
- 1. Growth in Global Sales of Herceptin, Gleevec, and Tarceva
- 2. X-Ray Crystal Structure of ATP Bound to Protein Kinase A
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