Selpercatinib (Retevmo)

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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 established

History of changes in FDA indication

Non-small cell lung cancer

RET (tissue-agnostic)

  • 2022-09-21: Granted accelerated approval for adult patients with locally advanced or metastatic solid tumors with a rearranged during transfection (RET) gene fusion that have progressed on or following prior systemic treatment or who have no satisfactory alternative treatment options. (Based on LIBRETTO-001RET)
  • 2024-05-29: Granted accelerated approval for pediatric patients two years of age and older with locally advanced or metastatic solid tumors with a RET gene fusion, as detected by an FDA-approved test, that have progressed on or following prior systemic treatment or who have no satisfactory alternative treatment options. (Based on LIBRETTO-121)

Thyroid cancer

  • 2020-05-08: Granted accelerated approval for adult and pediatric patients at least 12 years of age with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy. (Based on LIBRETTO-001thyroid)
    • 2024-09-27: Granted regular approval for adult and pediatric patients 2 years of age and older with advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an FDA-approved test, who require systemic therapy. (Based on LIBRETTO-531)
  • 2020-05-08: Granted accelerated approval for adult and pediatric patients at least 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-001thyroid)
    • 2023-06-12: Regular approval for adult and pediatric patients 2 years of age and older 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-001thyroid)
  • 2024-05-29: Granted accelerated approval for pediatric patients two years of age and older with advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an FDA-approved test, who require systemic therapy. (Based on LIBRETTO-121)
  • 2024-05-29: Granted accelerated approval for pediatric patients two years of age and older with advanced or metastatic thyroid cancer with a RET gene fusion, as detected by an FDA-approved test, who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate). (Based on LIBRETTO-121)

History of changes in EMA indication

  • 2021-02-11: Initial conditional authorization as Retsevmo.

History of changes in Health Canada indication

  • 2021-06-15: Initial notice of compliance with conditions as monotherapy for the treatment of metastatic RET fusion-positive non-small cell lung cancer (NSCLC) in adult patients.
  • 2021-06-15: Initial notice of compliance with conditions as monotherapy for the treatment of RET-mutant medullary thyroid cancer (MTC) in adult and pediatric patients 12 years of age and older with unresectable advanced or metastatic disease.
  • 2021-06-15: Initial notice of compliance with conditions as monotherapy for the treatment of RET fusion-positive differentiated thyroid carcinoma in adult patients with advanced or metastatic disease (not amenable to surgery or radioactive iodine therapy) following prior treatment with sorafenib and/or lenvatinib.

History of changes in PMDA indication

  • 2021-09-27: Newly indicated for the treatment of RET fusion gene-positive unresectable advanced or recurrent non-small cell lung cancer.
  • 2022-02-25: New indication and a new dosage for the treatment of RET fusion gene-positive unresectable thyroid cancer.
  • 2022-02-25: New indication and a new dosage for the treatment of RET gene mutation-positive unresectable medullary thyroid cancer.

Also known as

  • Code name: LOXO-292
  • Brand names: Retevmo, Retsevmo
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