• Alias: Ro-31-7453
    • An orally bioavailable, small-molecule bisindolylmaleimide cell cycle inhibitor that inhibits tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis
    • Also shown to inhibit the activities of the oncogenic kinase AKT, the mTOR pathway, and importin-β, a protein essential to the transport of other proteins from the cytosol into the nucleus
    • Phase 1b/2 studies are ongoing in NSCLC, metastatic pancreatic cancer, metastatic ovarian cancer, and metastatic breast cancer.
    • Recommended phase 2 dose: Up to 1,000 mg PO for 4 days of each cycle
    Other topics in Targeted and Immunotherapy Agents