Pralsetinib (Gavreto)

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Mechanism of action

From the NCI Drug Dictionary: An orally bioavailable selective inhibitor of mutant forms of and fusion products involving the proto-oncogene receptor tyrosine kinase RET, with potential antineoplastic activity. Upon administration, BLU-667 binds to and targets various RET mutants and RET-containing fusion product.

Diseases for which it is used

History of changes in FDA indication

  • 9/4/2020: Granted accelerated approval for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC)
  • 12/1/2020: Approved for adult and pediatric patients 12 years of age and older with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy.
  • 12/1/2020: Approved for adult and pediatric patients 12 years of age and older with 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: BLU-667
  • Brand name: Gavreto