• Alias: GSK458, GSK2126458
    • A small-molecule pyridylsulfonamide inhibitor of PI3K
    • Currently in phase 1 clinical trials
    • Recommended phase 2 dose: 2.5 mg PO daily on empty stomach, 2 hours before food and stay fasted for 1 hour after dosing
    • Half-life: 10 hours
    • Metabolism: Substrate for P-glycoproteins (PgP1) and an inhibitor of CYP3A4
    • Common side effects: Rash, fatigue, nausea, diarrhea
    (Munster et al., 2011)
    Other topics in Targeted and Immunotherapy Agents