Selpercatinib (Retevmo)
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Mechanism of action
From the NCI Drug Dictionary: An orally bioavailable selective inhibitor of wild-type, mutant and fusion products involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, LOXO-292 selectively binds to and targets various RET mutants and RET-containing fusion products. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity.
Diseases for which it is used
- RET-positive NSCLC
- RET-mutant medullary thyroid cancer
- RET-positive thyroid cancer
History of changes in FDA indication
Non-small cell lung cancer
- 5/8/2020: Granted accelerated approval for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC)
Thyroid cancer
- 5/8/2020: Granted accelerated approval for adult and pediatric patients ≥12 years of age with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy
- 5/8/2020: Granted accelerated approval for adult and pediatric patients ≥12 years of age with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate).
Also known as
- Code name: LOXO-292
- Brand name: Retevmo