Selpercatinib: First approved selective RET inhibitor.
review · Level V
Where this comes from
- Record sourced from PubMed, PMID 37059058.
- Also identified by DOI 10.1016/j.cell.2023.02.040.
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Abstract
Selpercatinib is a small molecule that binds at the RET kinase active site. It inhibits activity of constitutively dimerized RET fusion proteins and activated point mutants, thereby blocking downstream signals for proliferation and survival. It is the first selective RET inhibitor to be FDA approved for tumor agnostic targeting of oncogenic RET fusion proteins. To view this Bench to Bedside, open or download the PDF.
Medical subject headings
- Neoplasms
- Protein Kinase Inhibitors
- Proto-Oncogene Proteins c-ret