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
History of changes in FDA indication
- 5/8/2020: Granted accelerated approval for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC). (Based on LIBRETTO-001)
- 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. (Based on LIBRETTO-001)
- 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). (Based on LIBRETTO-001)
History of changes in EMA indication
- 2/11/2021: Initial marketing authorization as Retsevmo.
Also known as
- Code name: LOXO-292
- Brand names: Retevmo, Retsevmo