Adverse Events and Oncotargeted Kinase Inhibitors gathers and evaluates data on adverse events associated with tyrosine kinase inhibitors (TKIs), a powerful anti-tumor drug class that has recently been introduced for human therapy. This book compiles a comprehensive safety profile of each TKI from experiences in official therapeutic indications, also exploring off-label exploratory investigations and postmarketing pharmaceutical surveillance databases.
A brief history of each drug’s development and submission is provided, along with a more detailed analysis of the mechanism(s) of action involved in therapeutic activity or related to the insurgence of specific adverse events. Early chapters focus on general characteristics of TKIs, typology, and classification of adverse events, while the final chapters analyze TKIs as AE inducers and classes of AEs by system or organ involvement.
This comprehensive resource compiles and critically reviews all of the relevant safety data for this class of drugs, with the goal of improving the understanding of pathogenesis and facilitating the prevention, monitoring, and management of these adverse events.
1. Chapter 1. Introduction - p. 3 2. Chapter 2. Kinases - p. 9 3. 2.1. Protein Kinases - p. 12 4. 2.2. Protein Phosphatases and Downregulation of Kinases - p. 48 5. Chapter 3. Kinase Inhibitors - p. 57 6. Chapter 4. Adverse Events - p. 81 7. Part II. Oncotargeted Kinase Inhibitors - p. 93 8. Chapter 5. Imatinib - p. 97 9. Chapter 6. Gefitinib - p. 123 10. Chapter 7. Erlotinib - p. 145 11. Chapter 8. Sorafenib - p. 167 12. 8.1. Mechanism of Action - p. 169 13. 8.2. Adverse Events - p. 174 14. 8.3. Off-label Experience - p. 178 15. 8.4. Postmarketing Surveillance - p. 184 16. 8.5. Remarks - p. 185 17. Chapter 9. Sunitinib - p. 199 18. Chapter 10. Dasatinib - p. 221 19. Chapter 11. Lapatinib - p. 243 20. Chapter 12. Nilotinib - p. 265 21. Chapter 13. Pazopanib - p. 283 22. Chapter 14. Vandetanib - p. 305 23. Chapter 15. Vemurafenib - p. 331 24. Chapter 16. Crizotinib - p. 353 25. Chapter 17. Ruxolitinib - p. 375 26. Chapter 18. Axitinib - p. 395 27. Chapter 19. Bosutinib - p. 415 28. Chapter 20. Regorafenib - p. 435 29. Chapter 21. Cabozantinib - p. 457 30. Chapter 22. Ponatinib - p. 481 31. Chapter 23. Dabrafenib - p. 505 32. 23.1. Mechanism of Action - p. 506 33. 23.2. Adverse Events - p. 513 34. 23.3. Off-label Experience - p. 519 35. 23.4. Postmarketing Surveillance - p. 521 36. 23.5. Remarks - p. 522 37. Chapter 24. Trametinib - p. 531 38. 24.1. Mechanism of Action - p. 533 39. 24.2. Adverse Events - p. 539 40. 24.3. Off-Label Experience - p. 546 41. 24.4. Postmarketing Surveillance - p. 551 42. 24.5. Remarks - p. 552 43. Chapter 25. Afatinib - p. 561 44. 25.1. Mechanism of Action - p. 562 45. 25.2. Adverse Events - p. 568 46. 25.3. Off-label Experience - p. 573 47. 25.4. Postmarketing Surveillance - p. 579 48. 25.5. Remarks - p. 580 49. Chapter 26. Idelalisib - p. 591 50. Chapter 27. Ibrutinib - p. 609 51. 27.1. Mechanism of Action - p. 610 52. 27.2. Adverse Events - p. 619 53. 27.3. Off-Label Experience - p. 626 54. 27.4. Postmarketing Surveillance - p. 630 55. 27.5. Remarks - p. 631 56. Part III. Overview - p. 637 57. Chapter 28. Overview - p. 641 58. 28.1. Kinase Inhibitors as Adverse Event Inducers - p. 659 59. 28.2. Analysis of Nondrug Class Kinase Inhibitors as Adverse Event Inducers - p. 678 60. 28.3. Toxicities at Large and Small - p. 680 61. Chapter 29. Conclusion and Perspectives - p. 695 62. Index - p. 707
Adverse Events and Oncotargeted Kinase Inhibitors gathers and evaluates data on adverse events associated with tyrosine kinase inhibitors (TKIs), a powerful anti-tumor drug class that has recently been introduced for human therapy. This book compiles a comprehensive safety profile of each TKI from experiences in official therapeutic indications, also exploring off-label exploratory investigations and postmarketing pharmaceutical surveillance databases.
A brief history of each drug’s development and submission is provided, along with a more detailed analysis of the mechanism(s) of action involved in therapeutic activity or related to the insurgence of specific adverse events. Early chapters focus on general characteristics of TKIs, typology, and classification of adverse events, while the final chapters analyze TKIs as AE inducers and classes of AEs by system or organ involvement.
This comprehensive resource compiles and critically reviews all of the relevant safety data for this class of drugs, with the goal of improving the understanding of pathogenesis and facilitating the prevention, monitoring, and management of these adverse events.
1. Chapter 1. Introduction - p. 3 2. Chapter 2. Kinases - p. 9 3. 2.1. Protein Kinases - p. 12 4. 2.2. Protein Phosphatases and Downregulation of Kinases - p. 48 5. Chapter 3. Kinase Inhibitors - p. 57 6. Chapter 4. Adverse Events - p. 81 7. Part II. Oncotargeted Kinase Inhibitors - p. 93 8. Chapter 5. Imatinib - p. 97 9. Chapter 6. Gefitinib - p. 123 10. Chapter 7. Erlotinib - p. 145 11. Chapter 8. Sorafenib - p. 167 12. 8.1. Mechanism of Action - p. 169 13. 8.2. Adverse Events - p. 174 14. 8.3. Off-label Experience - p. 178 15. 8.4. Postmarketing Surveillance - p. 184 16. 8.5. Remarks - p. 185 17. Chapter 9. Sunitinib - p. 199 18. Chapter 10. Dasatinib - p. 221 19. Chapter 11. Lapatinib - p. 243 20. Chapter 12. Nilotinib - p. 265 21. Chapter 13. Pazopanib - p. 283 22. Chapter 14. Vandetanib - p. 305 23. Chapter 15. Vemurafenib - p. 331 24. Chapter 16. Crizotinib - p. 353 25. Chapter 17. Ruxolitinib - p. 375 26. Chapter 18. Axitinib - p. 395 27. Chapter 19. Bosutinib - p. 415 28. Chapter 20. Regorafenib - p. 435 29. Chapter 21. Cabozantinib - p. 457 30. Chapter 22. Ponatinib - p. 481 31. Chapter 23. Dabrafenib - p. 505 32. 23.1. Mechanism of Action - p. 506 33. 23.2. Adverse Events - p. 513 34. 23.3. Off-label Experience - p. 519 35. 23.4. Postmarketing Surveillance - p. 521 36. 23.5. Remarks - p. 522 37. Chapter 24. Trametinib - p. 531 38. 24.1. Mechanism of Action - p. 533 39. 24.2. Adverse Events - p. 539 40. 24.3. Off-Label Experience - p. 546 41. 24.4. Postmarketing Surveillance - p. 551 42. 24.5. Remarks - p. 552 43. Chapter 25. Afatinib - p. 561 44. 25.1. Mechanism of Action - p. 562 45. 25.2. Adverse Events - p. 568 46. 25.3. Off-label Experience - p. 573 47. 25.4. Postmarketing Surveillance - p. 579 48. 25.5. Remarks - p. 580 49. Chapter 26. Idelalisib - p. 591 50. Chapter 27. Ibrutinib - p. 609 51. 27.1. Mechanism of Action - p. 610 52. 27.2. Adverse Events - p. 619 53. 27.3. Off-Label Experience - p. 626 54. 27.4. Postmarketing Surveillance - p. 630 55. 27.5. Remarks - p. 631 56. Part III. Overview - p. 637 57. Chapter 28. Overview - p. 641 58. 28.1. Kinase Inhibitors as Adverse Event Inducers - p. 659 59. 28.2. Analysis of Nondrug Class Kinase Inhibitors as Adverse Event Inducers - p. 678 60. 28.3. Toxicities at Large and Small - p. 680 61. Chapter 29. Conclusion and Perspectives - p. 695 62. Index - p. 707
