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Selpercatinib: First approved selective RET inhibitor
Larissa C B Oliveira1, Lois M Mulligan1
1Division of Cancer Biology and Genetics, Cancer Research Institute, and Department of Pathology and Molecular Medicine, Queen's University, Kingston, ON, K7L 3N6, Canada.
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.
Insights
Selpercatinib, a novel RET inhibitor, effectively targets RET fusion proteins and mutants. This FDA-approved therapy blocks cancer cell proliferation and survival signals, offering new hope for targeted cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- The RET proto-oncogene plays a critical role in various cancers when altered by fusions or mutations.
- Targeting RET signaling pathways is a promising strategy for cancer therapy.
Purpose of the Study:
- To introduce Selpercatinib, a potent and selective RET kinase inhibitor.
- To highlight its mechanism of action in inhibiting oncogenic RET alterations.
Main Methods:
- Selpercatinib binds to the RET kinase active site.
- It inhibits constitutively dimerized RET fusion proteins and activated point mutants.
Main Results:
- Selpercatinib effectively blocks downstream signals essential for cancer cell proliferation and survival.
- It represents a significant advancement in targeted cancer therapy.
Conclusions:
- Selpercatinib is the first FDA-approved drug for tumor-agnostic targeting of oncogenic RET fusion proteins.
- This selective RET inhibitor offers a new therapeutic option for patients with RET-altered cancers.
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