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