Protein kinase inhibitor

Cytotoxic agents.

Imatinib

BCR-ABL and c-KIT tyrosine kinase inhibitors

• Inhibition of autophosphorylation and activation of multiple proteins by tyrosine kinases (e.g.,BCR-ABL, c-KIT)

• Chronic myeloid leukemia

• BCR-ABL positive ALL

• Kit (CD117)-positive gastrointestinal stromal tumors

• Aggressive systemic mastocytosis (imatinib)

• Dermatofibrosarcoma protuberans (imatinib)

• Hypereosinophilic syndrome (imatinib)

• Chronic eosinophilic leukemia (imatinib)

• Myelodysplastic/Myeloproliferative diseases (imatinib)

• General

  • Fluid retention and edema

  • Myelosuppression

  • Hepatotoxicity (e.g., ↑ LFTs)

  • Myalgia

• For imatinib

  • Neurotoxicity

  • Bullous dermatologic reactions

  • Hemorrhage

  • Nephrotoxicity

• For dasatinib:

  • Cardiotoxicity

  • Skin rash

  • Hemorrhage

  • Pulmonary arterial hypertension

  • QT prolongation