• Alias: LDK378
    • An orally available inhibitor of the RTK activity of ALK that binds to and inhibits wild-type ALK kinase, ALK fusion proteins, and ALK point mutation variants. Inhibition of ALK leads to both the disruption of ALK-mediated signaling and the inhibition of cell growth in ALK-overexpressing tumor cells.
    • FDA approved for metastatic NSCLC with ALK-positive mutation.
    • Recommended dose: 750 mg daily on empty stomach, 1 hour before or 2 hours after meal. Avoid grapefruit and grapefruit juice.
    • Metabolism: Major CYP3A4 substrate
    • Half-life: 41 hours
    • Common side effects: QT prolongation, nausea/vomiting, fatigue, skin rash, hyperglycemia, increased lipase, transaminitis, hyperbilirubinemia, visual impairment
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