USMLE

Imatinib, Dasatinib

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Oncology Pharm
  1. Bleomycin
  2. Dactinomycin, Actinomycin D
  3. Doxorubicin, Daunorubicin
  4. Azathioprine, 6-MP
  5. Cladribine
  6. Cytarabine
  7. Busulfan
  8. Cyclophosphamide, Ifosfamide
  9. Nitrosoureas
  10. Paclitaxel
  11. Vincristine, Vinblastine
  12. Cisplatin, Carboplatin, Oxaliplatin
  13. Etoposide, Teniposide
  14. Irinotecan, Topotecan
  15. Bevacizumab
  16. Erlotinib
  17. Cetuximab, Panitumumab
  18. Imatinib, Dasatinib
  19. Rituximab
  20. Bortezomib, Carfilzomib
  21. Trastuzumab
  22. Dabrafenib, Vemurafenib
  23. Raloxifene and Tamoxifen
  24. Hydroxyurea
  25. Procarbazine

Summary

Imatinib and dasatinib are tyrosine kinase inhibitors that inhibit the bcr-abl and c-kit tyrosine kinase proteins. Bcr-abl is encoded by the Philadelphia chromosome, which is a t(9;22) fusion gene in CML. Therefore, since they inhibit bcr-abl, imatinib and dasatinib are effective in targeting neoplastic cells in CML. Finally, patients taking imatinib and dasatinib may experience fluid retention as a potential side effect. 

Key Points

  • Imatinib, Dasatinib
    • Mechanism
      • Tyrosine kinase inhibitor of bcr-abl and c-kit
      • Bcr-abl encoded by the Philadelphia chromosome t(9;22) fusion gene of CML
    • Clinical Use
      • CML
      • GI stromal tumors (GIST)
    • Adverse Effects
      • Fluid retention