• Aliases: GSK572016, GW2016, GW-572016
    • Reversibly blocks phosphorylation of the EGFR, HER2, and the ERK-1 and -2, and AKT kinases
    • Inhibits cyclin D protein levels in human tumor cell lines and xenografts
    • FDA approved for metastatic or advanced breast cancer with HER2 overexpression
    • Recommended dose: 1,250 mg once daily in combination with capecitabine 2,000 mg/m2 daily, 1,500 mg once daily in combination with letrozole 2.5 mg once daily. Take 1 hour before or 1 hour after meals and avoid grapefruit juice.
    • Half-life: 24 hours
    • Metabolism: Major CYP3A4 and P-glycoprotein substrate
    • Common ide effects:
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