Kinase Therapeutic Pipelines: An Assessment of Targets and Agents in Development

Table of Contents

Chapter 1: KINASES

• 1.1. The Function of Kinases
• 1.2. The Human Kinome
• 1.3. Kinase Classification
• AGC Family
• CAMK Family
• CMGC Family
• CK1 Family
• STE Family
• TK Family
• TKL Family
• Atypical Protein Kinases
• 1.4. Kinase Structure
• 1.5. Kinases as Drug Targets

Chapter 2: CURRENT COMMERCIAL SUCCESSES

• 2.1. Small-Molecule Kinase Inhibitors
• Gleevec
• Iressa and Tarceva
• Nexavar
• Sutent
• Rapamune and Certican
• 2.2. Biological Agents

Chapter 3: INDICATIONS FOR THE USE OF KINASE INHIBITORS

• 3.1. Cancer
• 3.2. Angiogenic Conditions
• 3.3. Inflammatory Diseases
• 3.4. Metabolic Disorders
• 3.5. Central Nervous System Conditions
• 3.6. Cardiovascular Disease

Chapter 4: STRATEGIES FOR DEVELOPING KINASE INHIBITORS

• 4.1. Which Domain to Target?
• 4.2. Screening Approaches
• 4.3. Achieving Cellular Activity
• 4.4. Selectivity Profile
• 4.5. Pitfalls Encountered
• 4.6. Intellectual Property Issues
• 4.7. SWOT Analysis
• Strengths
• Opportunities
• Weaknesses
• Threats

Chapter 5: CURRENT PIPELINES

• 5.1. Overview of Major Company Approaches
• Abbott
• Amgen
• AstraZeneca
• Bayer Schering
• Boehringer Ingelheim
• Bristol-Myers Squibb
• Daiichi Sankyo
• Eli Lilly
• GlaxoSmithKline
• Johnson & Johnson
• Merck & Co.
• Merck Serono
• Novartis
• Pfizer
• Roche
• Sanofi-aventis
• Schering-Plough
• Takeda
• Wyeth
• 5.2. Popular Targets
• 5.3. Drugs Targeting Protein Kinases that Have Recently Been Approved or Are Awaiting Approval
• Lapatinib
• Nilotinib
• Dasatinib
• Sunitinib
• Sorafenib
• Panitumumab
• 5.4. Kinase Inhibitors in Phase III
• Motesanib
• Pazopanib
• Aflibercept
• Vandetanib
• Cediranib
• BIBW-2992
• Enzastaurin and Ruboxistaurin
• Deforolimus
• Lestaurtinib
• Alvocidib
• 5.5. Kinase Inhibitors in Phase II
• p38 MAP Kinase Inhibitors
• VX-702
• SCIO-469
• Pamapimod
• 681323 and 856553
• KC-706
• Other MAP Kinase Inhibitors
• Atypical MAP Kinase Inhibitors
• MEK Inhibitors
• PD-325901
• ARRY-142886
• PI3K Inhibitors
• Akt Inhibitors
• Triciribine
• Perifosine
• INCB-18424
• CDK and Chk Inhibitors
• Chk1 Inhibitors
• CDK Inhibitors
• Seliciclib
• Abl Inhibitors
• INNO-406
• AT-9283
• MK-0457
• AZD-0530
• Bosutinib
• Anti-angiogenic Kinase Inhibitors
• ABT-869
• AEE-788
• BIBF-1120
• Brivanib
• RTA-402
• SU-14813
• SU-6668
• TG-100801
• XL-880
• IGFR Inhibitors
• INSM-18
• IMC-A12
• CP-751871
• EGFR and ErbB2 Inhibitors
• Neratinib
• Flt3 Inhibitors
• Lestaurtinib
• Tandutinib
• Inhibitors of Other Kinases
• ABT-263
• Masatinib
• CMI X-11S
• Cethrin
• R-788
• CP-690550
• PHA-739358
• BI-2536
• 5.6. Kinase Inhibitors in Phase I
• Aurora Kinases
• Raf Kinase
• FGF Inhibitors
• Other Kinases
• 5.7. Outlook

Chapter 6: SPECIALIST COMPANIES

• 6.1. Structure-Based Approaches
• Vertex Pharmaceuticals
• 6.2. High-Throughput Crystallography
• Astex Therapeutics
• SGX Pharmaceuticals
• 6.3. Indication-Based Approaches
• AVEO Pharmaceuticals
• Cyclacel Pharmaceuticals
• Kinex Pharmaceuticals
• Oncalis AG
• TargeGen
• 6.4. Domain-Focused Approaches
• Ariad Pharmaceuticals
• Rigel Pharmaceuticals
• Kemia
• Piramed Pharma
• 6.5. Screening-Based Approaches
• Ambit Biosciences
• Galapagos
• Sunesis Pharmaceuticals
• Upstate
• 6.6. Computational Approaches
• 4SC AG
• Amphora Discovery
• Aureus Pharma
• Emiliem
• Locus Pharmaceuticals

Chapter 7: EXPERT INTERVIEWS: A VIRTUAL ROUNDTABLE

• Stephen Burley, MD, DPhil, SGX Pharmaceuticals
• Jose Duca, PhD, Schering-Plough Research Institute
• David Hayes, PhD, Millipore
• Alcide Barberis, PhD, Oncalis AG
• Neil Gibson, PhD, OSI Pharmaceuticals
• Professor Sir Philip Cohen, FRS, FRSE, Medical Research Council Protein Phosphorylation Unit, University of Dundee
• Jeffrey Settleman, PhD, Department of Medicine, Harvard Medical School
• References
• Company Index with Web Addresses