• Alias: MLN8237
    • Second-generation, orally bioavailable, selective AURKA inhibitor that has >200-fold higher selectivity for Aurora A than Aurora B
    • Currently under investigation in phase 3 trial for treatment of relapsed or refractory PTCL (failed to meet primary endpoint in May 2015, therefore study terminated). Continue phase 2 in SCLC and in high-risk AML
    • Recommended phase 3 dose: 50 mg twice daily for 7 consecutive days of the 21-day cycle (10 mg enteric coated tablet). Fast 2 hours before and 1 hour after dosing.
    • Half-life: 19 to 23 hours
    • Metabolism: Excreted primarily unchanged
    Other topics in Targeted and Immunotherapy Agents