Journal
NPJ PRECISION ONCOLOGY
Volume 5, Issue 1, Pages -Publisher
NATURE RESEARCH
DOI: 10.1038/s41698-021-00188-x
Keywords
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Categories
Funding
- National Institutes of Health [R01CA242845]
- Oklahoma Tobacco Settlement Endowment Trust
- Peggy and Charles Stephenson Endowed Chair fund
- Cancer Prevention and Research Institute of Texas [RP1100584]
- Sheikh Khalifa Bin Zayed Al Nahyan Institute for Personalized Cancer Therapy [1U01 CA180964]
- NCATS [UL1 TR000371]
- MD Anderson Cancer Center Support Grant [P30 CA016672]
- NIH/National Institute of General Medical Sciences [P20GM103639, P20GM103640]
- NIH/National Cancer Institute [P30CA225520]
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Recently FDA-approved pralsetinib and selpercatinib are RET-selective protein tyrosine kinase inhibitors for treating RET-altered cancers. Selpercatinib was found to effectively inhibit certain resistant mutations that were strongly resistant to pralsetinib, showing better activity in those cases.
Recently Food and Drug Administration (FDA)-approved pralsetinib (BLU-667) and selpercatinib (LOXO-292) are RET-selective protein tyrosine kinase inhibitors for treating RET-altered cancers, but whether they have distinct activity was unknown. The L730V/I mutations at the roof of the solvent-front site of the RET kinase were identified as strongly resistant to pralsetinib but not to selpercatinib. Selpercatinib effectively inhibited these mutants and the KIF5B-RET(L730V/I) oncogene-driven tumors.
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