Selpercatinib (Retevmo)

From HemOnc.org - A Hematology Oncology Wiki
Jump to navigation Jump to search

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

Non-small cell lung cancer

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. (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)

Also known as

  • Code name: LOXO-292
  • Brand name: Retevmo