• Aliases: BEZ235, NVP-BEZ235
    • Orally bioavailable imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTORC1 kinase activity by binding to the ATP-binding cleft of these enzymes
    • Currently under investigation in phase 1/2 trials for renal cell carcinoma and for pancreatic, prostate, and breast cancer
    • Recommended phase 2 dose: 1,200 mg PO daily or 400 to 800 mg PO daily (in combination with chemotherapy). Taken with food/breakfast. No Seville orange juice or grapefruit juice
    • Half-life: â™4 to 8 hours
    • Common side effects: Nausea/vomiting, fatigue/asthenia, anemia, anorexia, diarrhea
    (Burris et al., 2010)
    Other topics in Targeted and Immunotherapy Agents