• Alias: SCH 900242
    • Inhibits MDM2, allowing TP53 to function and arrest cancer cell growth
    • For MK-8242 to work, TP53 itself has to be wild type, because increasing the amount of abnormal TP53 would probably not stop cancer cells from growing.
    • Currently under investigation in phase 1 clinical trials in solid tumors and acute myelogenous leukemia
    • Metabolism: CYP3A4 and possible major inhibitor of CYP3A4
    • Phase 1 dose: Oral dosing b.i.d. on fasting stomach 1 hour prior to dosing and remain in fasting for 1 hour after dosing
    • Preclinical half-life: 6.5 to .9 hours
    Other topics in Targeted and Immunotherapy Agents