• An orally bioavailable selective inhibitor of wild-type, mutant, and fusion products involving the proto-oncogene RTK rearranged during transfection (RET), thereby inhibiting the growth of tumor cells that exhibit increased RET activity.
    • Currently studied in RET fusion–positive lung cancer and medullary thyroid cancer
    • Phase 1 dose: Range from 20 to 100 mg PO twice daily
    • Metabolism: A potent substrate of CYP3A4
    (IASLC, 2017)
    Other topics in Targeted and Immunotherapy Agents