• Alias: MDV-3100
    • An AR antagonist that works by competitively inhibiting androgen binding to ARs and by inhibiting AR nuclear translocation and coactivator recruitment of the ligand-receptor complex.
    • FDA approved for metastatic castration-resistant prostate cancer in August 2012
    • Recommended dose: 160 mg PO daily
    • Half-life: 5.8 days (range 2–10 days)
    • Metabolism: Major CYP2C8 and CYP3A4 substrates
    • Side effects: Peripheral edema, fatigue, hot flashes, back pain/arthralgia, upper respiratory infection, neutropenia
    Other topics in Targeted and Immunotherapy Agents