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Targeting RET Solvent-Front Mutants with Alkynyl Nicotinamide-Based Inhibitors

18 Apr 2023

Abstract excerpt

Selpercatinib (LOXO292) and pralsetinib (BLU667) are RET protein tyrosine kinase inhibitors (TKIs) recently approved for treating RET-altered cancers. However, RET mutations that confer selpercatinib/pralsetinib resistance have been identified, necessitating development of next-generation RET TKIs. While acquired RET G810C/R/S/V mutations were reported in selpercatinib-treated patients, it was unclear whether all...

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PMID: 37070927
DOI: 10.1158/1535-7163.mct-22-0629

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