Selpercatinib in the treatment of medullary and radioiodine-refractory differentiated thyroid cancer with RET mutation (literature review)
Selpercatinib is a novel, highly selective, small-molecule inhibitor of RET kinase that competes with adenosine triphosphate. In experimental models, this drug has demonstrated nanomolar activity against various RET gene alterations, including an acquired resistance mutation in the gatekeeper gene a...
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| Format: | Article |
| Language: | Russian |
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ABV-press
2025-03-01
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| Series: | Опухоли головы и шеи |
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| Online Access: | https://ogsh.abvpress.ru/jour/article/view/1045 |
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| _version_ | 1850024048877109248 |
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| author | E. V. Borodavina S. I. Kutukova Т. V. Kekeeva Р. A. Isaev |
| author_facet | E. V. Borodavina S. I. Kutukova Т. V. Kekeeva Р. A. Isaev |
| author_sort | E. V. Borodavina |
| collection | DOAJ |
| description | Selpercatinib is a novel, highly selective, small-molecule inhibitor of RET kinase that competes with adenosine triphosphate. In experimental models, this drug has demonstrated nanomolar activity against various RET gene alterations, including an acquired resistance mutation in the gatekeeper gene at residue V804, as well as antitumor activity in the brain. Selpercatinib inhibits wild-type and various mutated forms of RET, as well as vascular endothelial growth factor receptors (VEGFR1 and VEGFR3) with half-maximal inhibitory concentrations from 0.92 to 67.8 nM, and fibroblast growth factor receptors (FGFR1, FGFR2, and FGFR3).The article presents results of clinical studies on the efficacy and safety of selpercatinib in patients with radioiodine refractory differentiated thyroid cancer with alterations in RET gene and in patients with medullary thyroid cancer with a germinal or somatic mutation in this gene. |
| format | Article |
| id | doaj-art-3a1706bed7dc47d7baa6b20ce679082f |
| institution | DOAJ |
| issn | 2222-1468 2411-4634 |
| language | Russian |
| publishDate | 2025-03-01 |
| publisher | ABV-press |
| record_format | Article |
| series | Опухоли головы и шеи |
| spelling | doaj-art-3a1706bed7dc47d7baa6b20ce679082f2025-08-20T03:01:13ZrusABV-pressОпухоли головы и шеи2222-14682411-46342025-03-01151748810.17650/2222-1468-2025-15-1-74-88628Selpercatinib in the treatment of medullary and radioiodine-refractory differentiated thyroid cancer with RET mutation (literature review)E. V. Borodavina0S. I. Kutukova1Т. V. Kekeeva2Р. A. Isaev3A.F. Tsyb Medical Radiological Research Center – branch of the National Medical Research Radiological Centre, Ministry of Health of RussiaCity Clinical Oncological Dispensary; Pavlov University, Ministry of Health of RussiaResearch Centre for Medical GeneticsA.F. Tsyb Medical Radiological Research Center – branch of the National Medical Research Radiological Centre, Ministry of Health of RussiaSelpercatinib is a novel, highly selective, small-molecule inhibitor of RET kinase that competes with adenosine triphosphate. In experimental models, this drug has demonstrated nanomolar activity against various RET gene alterations, including an acquired resistance mutation in the gatekeeper gene at residue V804, as well as antitumor activity in the brain. Selpercatinib inhibits wild-type and various mutated forms of RET, as well as vascular endothelial growth factor receptors (VEGFR1 and VEGFR3) with half-maximal inhibitory concentrations from 0.92 to 67.8 nM, and fibroblast growth factor receptors (FGFR1, FGFR2, and FGFR3).The article presents results of clinical studies on the efficacy and safety of selpercatinib in patients with radioiodine refractory differentiated thyroid cancer with alterations in RET gene and in patients with medullary thyroid cancer with a germinal or somatic mutation in this gene.https://ogsh.abvpress.ru/jour/article/view/1045medullary thyroid cancerradioiodine refractory thyroid cancerprogressioncalcitoninret mutationtargeted therapyselpercatinib |
| spellingShingle | E. V. Borodavina S. I. Kutukova Т. V. Kekeeva Р. A. Isaev Selpercatinib in the treatment of medullary and radioiodine-refractory differentiated thyroid cancer with RET mutation (literature review) Опухоли головы и шеи medullary thyroid cancer radioiodine refractory thyroid cancer progression calcitonin ret mutation targeted therapy selpercatinib |
| title | Selpercatinib in the treatment of medullary and radioiodine-refractory differentiated thyroid cancer with RET mutation (literature review) |
| title_full | Selpercatinib in the treatment of medullary and radioiodine-refractory differentiated thyroid cancer with RET mutation (literature review) |
| title_fullStr | Selpercatinib in the treatment of medullary and radioiodine-refractory differentiated thyroid cancer with RET mutation (literature review) |
| title_full_unstemmed | Selpercatinib in the treatment of medullary and radioiodine-refractory differentiated thyroid cancer with RET mutation (literature review) |
| title_short | Selpercatinib in the treatment of medullary and radioiodine-refractory differentiated thyroid cancer with RET mutation (literature review) |
| title_sort | selpercatinib in the treatment of medullary and radioiodine refractory differentiated thyroid cancer with ret mutation literature review |
| topic | medullary thyroid cancer radioiodine refractory thyroid cancer progression calcitonin ret mutation targeted therapy selpercatinib |
| url | https://ogsh.abvpress.ru/jour/article/view/1045 |
| work_keys_str_mv | AT evborodavina selpercatinibinthetreatmentofmedullaryandradioiodinerefractorydifferentiatedthyroidcancerwithretmutationliteraturereview AT sikutukova selpercatinibinthetreatmentofmedullaryandradioiodinerefractorydifferentiatedthyroidcancerwithretmutationliteraturereview AT tvkekeeva selpercatinibinthetreatmentofmedullaryandradioiodinerefractorydifferentiatedthyroidcancerwithretmutationliteraturereview AT raisaev selpercatinibinthetreatmentofmedullaryandradioiodinerefractorydifferentiatedthyroidcancerwithretmutationliteraturereview |