• Alias: TKI258, CHIR-258
    • A multitargeted RTK inhibitor, mostly for class III (FLT3/KIT), and also potent to class IV (FGFR1/3) and class V (VEGFR1–4) RTKs; less potent to EGFR, MET, EphA2, TIE2, IGF-1R, and HER2
    • Currently under investigation in phase 2 and 3 studies for GI stromal tumors, and FGFR-amplified breast cancer
    • Recommended phase 3 dose: 400 to 500 mg orally once daily (5 days on/2 days off)
    • Half-life: â™13 hours
    • Metabolism: CYP1A2 substrate
    • Common side effects: Fatigue, diarrhea, nausea
    (Kim et al., 2011)
    Other topics in Targeted and Immunotherapy Agents