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An early look at selective RET inhibitor resistance: new challenges and opportunities.


ABSTRACT: Two RET inhibitors, selpercatinib and pralsetinib, recently received approval for the treatment of advanced RET fusion-positive lung cancer. Acquired resistance to these inhibitors will be a major challenge. We have shown that resistance can emerge due to recurrent RET kinase domain mutations and, in most cases, due to RET-independent mechanisms.

SUBMITTER: Lin JJ 

PROVIDER: S-EPMC8144197 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature

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An early look at selective RET inhibitor resistance: new challenges and opportunities.

Lin Jessica J JJ   Gainor Justin F JF  

British journal of cancer 20210323 11


Two RET inhibitors, selpercatinib and pralsetinib, recently received approval for the treatment of advanced RET fusion-positive lung cancer. Acquired resistance to these inhibitors will be a major challenge. We have shown that resistance can emerge due to recurrent RET kinase domain mutations and, in most cases, due to RET-independent mechanisms. ...[more]

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2014-03-25 | GSE54583 | GEO