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Rearranged during transfection (RET) proto-oncogene rearrangements have been validated as an additional oncogenic driver that occurs in 1-2% of NSCLC. Prior efforts to target RET in lung cancer patients were hampered by the lack of potent and selective RET tyrosine kinase inhibitors (TKIs), necessitating the re-purposed use of multikinase inhibitors such as cabozantinib or vandetanib, which are encumbered by suboptimal efficacy and significant toxicities. Recently, novel, oral, highly potent, and selective RET TKIs—BLU-667 (pralsetinib) and LOXO-292 (selpercatinib)—have entered the clinic.
Video Overview: https://youtu.be/XkWV7eZqc8E
Jessica J. Lin, MD
Massachusetts General Hospital
STO gratefully acknowledges educational grants in partial support of this activity from:
Novartis Pharmaceuticals Corp.