• Alias: BKM120
    • Orally bioavailable pan-class I PI3K inhibitor
    • Currently under investigation in phase 3 trials with hormone receptor–positive, HER2-negative metastatic breast cancer
    • Recommended phase 3 dose: 100 mg PO daily in combination with fulvestrant. Take dose 1 hour after breakfast and fast for 2 hours after dosing.
    • Half-life: â™40 hours
    • Metabolism: moderate/reversible inhibitor of CYP3A4
    • Common side effects: Rash, anorexia, mood alteration, diarrhea, hyperglycemia
    (Baselga et al., 2017)
    Other topics in Targeted and Immunotherapy Agents