Selpercatinib (Retevmo)

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

• 5/8/2020: Granted accelerated approval for the following indications:
  • Adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC)
  • Adult and pediatric patients ≥12 years of age with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy
  • 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