Pralsetinib (Gavreto)

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

• RET-positive NSCLC
• Thyroid cancer, RET-positive

History of changes in FDA indication - PARTIALLY WITHDRAWN

• 2020-09-04: Accelerated approval for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC). (Based on ARROW_RET-NSCLC)
• 2020-12-01: Accelerated approval 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. (Based on ARROW_RET-thyroid)
  • 2023-07-20: Accelerated approval 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of age and older with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy withdrawn.
• 2020-12-01: Accelerated approval 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). (Based on ARROW_RET-thyroid)
• 2023-08-09: Granted regular approval for adult patients with metastatic rearranged during transfection (RET) fusion-positive non-small cell lung cancer (NSCLC) as detected by an FDA-approved test. (Based on ARROW_RET-NSCLC)

History of changes in EMA indication

• 2021-11-18: Initial conditional authorization

History of changes in Health Canada indication

• 2021-06-30: Initial notice of compliance with conditions for the treatment of adult patients with rearranged during transfection (RET) fusion-positive locally advanced unresectable or metastatic non-small cell lung cancer (NSCLC)

Also known as

• Code name: BLU-667
• Brand name: Gavreto