What is Imatinib?
Imatinib is a Protein Tyrosine Kinase Inhibitor
-inhibits platelet-derived growth factor receptro (PDGFR) tyrosine kinase, the cytoplasmic ABL tyrosine kinase, and the receptor tyrosine kinase KIT.
-treats cancers which the ABL, KIT, or PDGFR have dominate roles in driving tumor proliferation (mutation results in constitutive activation of kinases)
-therapeutic efficacy in chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs), chronic myelomonocytic leukemia (CMML), and hypereosinophilic syndrom (HES)
-Aquired Resistance: mutations in the kinase domain
-Adverse effects: nausea, vomiting, edema, muscle cramps