Abstract
Rearranged during transfection (RET) is involved in the physiological development of some organ systems. Activating RET alterations via either gene fusions or point mutations are potent oncogenic drivers in non-small cell lung cancer, thyroid cancer, and in multiple diverse cancers. RET-altered cancers were initially treated with multikinase inhibitors (MKIs). The efficacy of MKIs was modest at the expense of notable toxicities from their off-target activity. Recently, highly potent and RET-specific inhibitors selpercatinib and pralsetinib were successfully translated to the clinic and FDA approved. We summarize the current state-of-the-art therapeutics with preclinical and clinical insights of these novel RET inhibitors, acquired resistance mechanisms, and future outlooks.
Original language | English (US) |
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Pages (from-to) | 1074-1088 |
Number of pages | 15 |
Journal | Trends in Cancer |
Volume | 7 |
Issue number | 12 |
DOIs | |
State | Published - Dec 2021 |
Keywords
- BLU-667 (pralsetinib)
- LOXO-292 (selpercatinib)
- RET-altered cancers
- lung cancer
- multikinase inhibitors
- thyroid cancer
ASJC Scopus subject areas
- Oncology
- Cancer Research