• Aliases: PX-866, CHEBI:65345, DJM-166
    • An irreversible, small-molecule wortmannin analog inhibitor of the α-, γ-, and δ- isoforms of PI3K
    • Currently under investigation in phase 1/2 clinical trials for colorectal cancer, melanoma, glioblastoma multiforme, SCCHN, and prostate cancer
    • Phase 2 recommended dose: 8 mg PO daily on fasting stomach 2 hours before meals and fast for 1 hour after dosing
    • Half-life: â™4 hours
    • Common side effects (phase 1): Nausea/vomiting, diarrhea, fatigue, thrombocytopenia, increased AST
    (Hong et al., 2012)
    Other topics in Targeted and Immunotherapy Agents