Difference between revisions of "Selpercatinib (Retevmo)"
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==Mechanism of action== | ==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. | + | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/selpercatinib 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== | |
| − | ==Diseases for which it is | ||
*[[Non-small cell lung cancer, RET-positive|RET-positive NSCLC]] | *[[Non-small cell lung cancer, RET-positive|RET-positive NSCLC]] | ||
| − | *RET-mutant medullary thyroid cancer | + | *RET-mutant [[Thyroid cancer, medullary|medullary thyroid cancer]] |
| − | *RET-positive thyroid cancer | + | *[[Thyroid_cancer,_RET-positive|RET-positive thyroid cancer]] |
| + | *[[Malignant solid neoplasm, RET-mutated|RET+ solid tumors (tissue-agnostic)]] | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| − | * | + | ===[[Non-small cell lung cancer]]=== |
| − | + | *2020-05-08: Granted accelerated approval for adult patients with metastatic [[Biomarkers#RET|RET]] [[Biomarkers#fusion|fusion-positive]] [[Non-small cell lung cancer|non-small cell lung cancer (NSCLC)]]. ''(Based on LIBRETTO-001<sub>NSCLC</sub>)'' | |
| − | ** | + | **2022-09-21: Granted regular approval for adult patients with locally advanced or metastatic [[Non-small cell lung cancer|non-small cell lung cancer (NSCLC)]] with a [[Biomarkers#RET|rearranged during transfection (RET) gene]] [[Biomarkers#fusion|fusion]]. ''(Based on LIBRETTO-001<sub>NSCLC</sub>)'' |
| − | ** | + | ===[[RET|RET (tissue-agnostic)]]=== |
| + | *2022-09-21: Granted accelerated approval for adult patients with locally advanced or metastatic [[Malignant solid neoplasm, RET-mutated|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-001<sub>RET</sub>)'' | ||
| + | *2024-05-29: Granted accelerated approval for pediatric patients two years of age and older with locally advanced or metastatic [[Malignant solid neoplasm, RET-mutated|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 [[Biomarkers#RET|RET]]-[[Biomarkers#Alterations|mutant]] [[Thyroid cancer, medullary|medullary thyroid cancer]] (MTC) who require systemic therapy. ''(Based on LIBRETTO-001<sub>thyroid</sub>)'' | ||
| + | *2020-05-08: Granted accelerated approval for adult and pediatric patients at least 12 years of age with advanced or metastatic [[Biomarkers#RET|RET]] [[Biomarkers#fusion|fusion-positive]] [[thyroid cancer]] who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate). ''(Based on LIBRETTO-001<sub>thyroid</sub>)'' | ||
| + | **2023-06-12: Regular approval for adult and pediatric patients 2 years of age and older with advanced or metastatic [[Biomarkers#RET|RET]] [[Biomarkers#fusion|fusion-positive]] [[thyroid cancer]] who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate). ''(Based on LIBRETTO-001<sub>thyroid</sub>)'' | ||
| + | *2024-05-29: Granted accelerated approval for pediatric patients two years of age and older with advanced or metastatic [[Thyroid cancer, medullary|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|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 [[Thyroid cancer, medullary|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 [[Thyroid cancer, differentiated|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 [[Thyroid cancer, medullary|medullary thyroid cancer]]. | ||
==Also known as== | ==Also known as== | ||
*'''Code name:''' LOXO-292 | *'''Code name:''' LOXO-292 | ||
| − | *'''Brand | + | *'''Brand names:''' Retevmo, Retsevmo |
[[Category:Drugs]] | [[Category:Drugs]] | ||
[[Category:Oral medications]] | [[Category:Oral medications]] | ||
| + | [[Category:Mutation-specific medications]] | ||
[[Category:RET inhibitors]] | [[Category:RET inhibitors]] | ||
[[Category:Non-small cell lung cancer medications]] | [[Category:Non-small cell lung cancer medications]] | ||
| + | [[Category:Malignant solid neoplasm, RET-mutated medications]] | ||
[[Category:Thyroid cancer medications]] | [[Category:Thyroid cancer medications]] | ||
| + | |||
| + | [[Category:EMA approved in 2021]] | ||
[[Category:FDA approved in 2020]] | [[Category:FDA approved in 2020]] | ||
| + | [[Category:Health Canada approved in 2021]] | ||
| + | [[Category:PMDA approved in 2021]] | ||
Latest revision as of 23:00, 12 June 2024
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
- RET-positive NSCLC
- RET-mutant medullary thyroid cancer
- RET-positive thyroid cancer
- RET+ solid tumors (tissue-agnostic)
History of changes in FDA indication
Non-small cell lung cancer
- 2020-05-08: Granted accelerated approval for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC). (Based on LIBRETTO-001NSCLC)
- 2022-09-21: Granted regular approval for adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with a rearranged during transfection (RET) gene fusion. (Based on LIBRETTO-001NSCLC)
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)
- 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