Author: Peter Norman, PhD, MBA
FIGURES
Figure 1.1. The Human Kinome
Figure 2.1. Schematic of PI3K-Akt Kinase Cascade
Figure 5.1. Kinase Inhibitors in Development in 2006 and 2009, by Development Phase
Figure 5.2. Kinase Inhibitors in Development in 2009 by Indication
Figure 5.3. Kinase Inhibitors in Development in 2009 by Non-Oncology Indication
Figure 6.1. Small-Molecule Kinase Inhibitors in Major Company Pipelines by Phase of Development
TABLES
Table 1.1. The AGC Family of Protein Kinases, Listed In Order of Phylogenetic Similarity
Table 1.2. The CAMK Family of Protein Kinases, Listed In Order of Phylogenetic Similarity
Table 1.3. The CMGC Family of Protein Kinases, Listed In Order of Phylogenetic Similarity
Table 1.4. The CK1 Family of Protein Kinases, Listed In Order of Phylogenetic Similarity
Table 1.5. The STE Family of Protein Kinases, Listed In Order of Phylogenetic Similarity
Table 1.6. The TK Family of Protein Kinases, Listed In Order of Phylogenetic Similarity
Table 1.7. The TKL Family of Protein Kinases, Listed In Order of Phylogenetic Similarity
Table 1.8. The Families of Atypical Protein Kinases
Table 3.1. Kinases Identified as Having Poorer Selectivity Than Initially Believed
Table 4.1. 2008 and 2009 Sales of Marketed Kinase Inhibitors
Table 4.2. Sales of Marketed Recombinant Products Targeting Growth Factors, 2008 and First Half of 2009
Table 5.1. Kinase Inhibitors in Phase III Clinical Studies
Table 5.2. Kinase Inhibitors in Phase II or Phase I/II Clinical Studies
Table 5.3. Kinase Inhibitors in Phase I Clinical Studies
Table 5.4. ErbB Family Kinase Inhibitors in Development
Table 5.5. FGFR Inhibitors in Clinical Development
Table 5.6. IGFR Inhibitors in Development
Table 5.7. VEGFR Inhibitors in Clinical Development
Table 5.8. Multi-Kinase Inhibitors in Clinical Development
Table 5.9. Flt3 Inhibitors in Development
Table 5.10. PI3K Inhibitors in Development
Table 5.11. Selective mTOR Inhibitors In Development
Table 5.12. Selective Akt and S6K Inhibitors In Development
Table 5.13. Raf Inhibitors In Development
Table 5.14. MEK and Erk Inhibitors In Development
Table 5.15. JAK1 and JAK2 Inhibitors In Development
Table 5.16. Cyclic-Dependent Kinase Inhibitors In Development
Table 5.17. Checkpoint Kinase Inhibitors In Development
Table 5.18. Polo-Like Kinase Inhibitors In Development
Table 5.19. Abl and Bcr-Abl Inhibitors In Development
Table 5.20. p38 Inhibitors In Development
Table 5.21. GSK-3 Inhibitors in Development
Table 5.22. Protein Kinase C (PKC) Inhibitors In Development
Table 5.23. Aurora Kinase Inhibitors In Development
Table 5.24. Inhibitors of c-Met or Recombinant HGF Antagonists In Development
Table 5.25. Inhibitors of Rho Kinases (ROCK1 and ROCK2) In Development
Table 5.26. Inhibitors of c-Jun Kinases (JNKs) In Development
Table 5.27. Inhibitors of Src Family Kinases In Development
Table 5.28. IKK2 Inhibitors In Development
Table 5.29. Syk and Zap-70 Inhibitors In Development
Table 5.30. JAK3 Inhibitors In Development
Table 5.31. Inhibitors of Other Serine Kinases In Development
Table 5.32. Inhibitors of Other Tyrosine Kinases In Development
Table 5.33. Inhibitors of Other Tyrosine-Like and CAMK (*) Kinases In Development
Table 6.1. Abbott’s Kinase Inhibitor Pipeline
Table 6.2. Amgen’s Kinase Inhibitor Pipeline
Table 6.3. Astellas’ Kinase Inhibitor Pipeline
Table 6.4. AstraZeneca’s Kinase Inhibitor Pipeline
Table 6.5. Bayer’s Kinase Inhibitor Pipeline
Table 6.6. Boehringer Ingelheim’s Kinase Inhibitor Pipeline
Table 6.7. Bristol-Myers Squibb’s Kinase Inhibitor Pipeline
Table 6.8. Daiichi Sankyo’s Kinase Inhibitor Pipeline
Table 6.9. Eisai’s Kinase Inhibitor Pipeline
Table 6.10. Eli Lilly’s Kinase Inhibitor Pipeline
Table 6.11. GlaxoSmithKline’s Kinase Inhibitor Pipeline
Table 6.12. Johnson & Johnson’s Kinase Inhibitor Pipeline
Table 6.13. Merck & Co.’s Kinase Inhibitor Pipeline
Table 6.14. Merck Serono’s Kinase Inhibitor Pipeline
Table 6.15. Novartis’ Kinase Inhibitor Pipeline
Table 6.16. Pfizer’s Kinase Inhibitor Pipeline
Table 6.17. Roche’s Kinase Inhibitor Pipeline
Table 6.18. sanofi-aventis’ Kinase Inhibitor Pipeline
Table 6.19. Takeda’s Kinase Inhibitor Pipeline
Table 6.20. Array BioPharma’s Kinase Inhibitor Pipeline
Table 6.21. Exelixis’ Kinase Inhibitor Pipeline
Table 6.22. Nerviano’s Kinase Inhibitor Pipeline
Table 6.23. Rigel’s Kinase Inhibitor Pipeline
Table 6.24. Vertex’ Kinase Inhibitor Pipeline
Table 6.25. Ambit’s Kinase Inhibitor Pipeline