Precision therapy for RET-altered cancers with RET inhibitors

Kyaw Z. Thein, Vamsidhar Velcheti, Blaine H.M. Mooers, Jie Wu, Vivek Subbiah

Research output: Contribution to journalReview articlepeer-review

1 Scopus citations

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 languageEnglish (US)
Pages (from-to)1074-1088
Number of pages15
JournalTrends in Cancer
Volume7
Issue number12
DOIs
StatePublished - 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

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