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Imatinib, Dasatinib

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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