• Alias: INCB028060
    • Selectively binds to proto-oncogene MET, thereby inhibiting c-MET phosphorylation and disrupting MET signal transduction pathways
    • Currently under investigation in phase 1/2 trials in solid tumors
    • Phase 1 dose range: 100 to 400 mg orally daily
    • Preliminary half-life: 6.8 hours
    • Metabolism: Major CYP3A4 and P-glycoprotein inhibitor
    • Common side effects: Fatigue, headache, nausea/diarrhea, QTc prolongation, tremors
    (Donehower et al., 2011)
    Other topics in Targeted and Immunotherapy Agents