• Alias: AP24534
    • A multitargeted RTK inhibitor of wild-type and all mutated forms of BCR-ABL, including T315I, the highly drug therapy–resistant missense mutation of BCR-ABL
    • Also inhibits VEGFR, FGFR, TIE2, and FMS-related tyrosine kinase receptor-3 (FLT3)
    • FDA approved for chronic myeloid leukemia and Ph+ acute lymphoblastic leukemia
    • NOTE: Withdrawn from the US market for newly diagnosed chronic CML patients in November 2013
    • Recommended dose: 45 mg orally with or without food
    • Half-life: â™24 hours
    • Metabolism: Moderate CYP3A4 substrate
    • Common side effects: Hypertension, peripheral edema, rash, nausea/vomiting, abdominal pain, myelosuppression, fatigue/weakness, diarrhea or perglycemia, arterial thrombosis/hepatotoxicity (US box warning)
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