• A synthetic small-molecule γ-secretase that inhibits the notch signaling pathway
    • Currently under investigation in phase 1/2 clinical trials for T-cell leukemia, breast cancer, brain tumors (gliomas), pancreatic cancer, colon cancer, cervical cancer, and salivary gland carcinoma
    • Recommended expanded dose: 350 mg orally 3 days on, 4 days off every week for 28 days; 1,500 to 1,800 mg orally once a week with or without food
    • Half-life: â™15 hours (terminal)
    • Preliminary phase 1 side effects: Nausea/vomiting, diarrhea, fatigue, lymphopenia, hypokalemia, constipation
    (Krop et al., 2012)
    Other topics in Targeted and Immunotherapy Agents