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Precision oncology with selective RET inhibitor selpercatinib in RET-rearranged cancers
Rearranged during transfection (RET) is a protooncogene that encodes for receptor tyrosine kinase with downstream effects on multiple cellular pathways. Activating RET alterations can occur and lead to uncontrolled cellular proliferation as a hallmark of cancer development. Oncogenic RET fusions are...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
SAGE Publications
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10288430/ https://www.ncbi.nlm.nih.gov/pubmed/37360768 http://dx.doi.org/10.1177/17588359231177015 |
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author | Gouda, Mohamed A. Subbiah, Vivek |
author_facet | Gouda, Mohamed A. Subbiah, Vivek |
author_sort | Gouda, Mohamed A. |
collection | PubMed |
description | Rearranged during transfection (RET) is a protooncogene that encodes for receptor tyrosine kinase with downstream effects on multiple cellular pathways. Activating RET alterations can occur and lead to uncontrolled cellular proliferation as a hallmark of cancer development. Oncogenic RET fusions are present in nearly 2% of patients with non-small cell lung cancer (NSCLC), 10–20% of patients with thyroid cancer, and <1% across the pan-cancer spectrum. In addition, RET mutations are drivers in 60% of sporadic medullary thyroid cancers and 99% of hereditary thyroid cancers. The discovery, rapid clinical translation, and trials leading to FDA approvals of selective RET inhibitors, selpercatinib and pralsetinib, have revolutionized the field of RET precision therapy. In this article, we review the current status on the use of the selective RET inhibitor, selpercatinib, in RET fusion-positive tumors: NSCLC, thyroid cancers, and the more recent tissue-agnostic activity leading to FDA approval. |
format | Online Article Text |
id | pubmed-10288430 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | SAGE Publications |
record_format | MEDLINE/PubMed |
spelling | pubmed-102884302023-06-24 Precision oncology with selective RET inhibitor selpercatinib in RET-rearranged cancers Gouda, Mohamed A. Subbiah, Vivek Ther Adv Med Oncol Review Rearranged during transfection (RET) is a protooncogene that encodes for receptor tyrosine kinase with downstream effects on multiple cellular pathways. Activating RET alterations can occur and lead to uncontrolled cellular proliferation as a hallmark of cancer development. Oncogenic RET fusions are present in nearly 2% of patients with non-small cell lung cancer (NSCLC), 10–20% of patients with thyroid cancer, and <1% across the pan-cancer spectrum. In addition, RET mutations are drivers in 60% of sporadic medullary thyroid cancers and 99% of hereditary thyroid cancers. The discovery, rapid clinical translation, and trials leading to FDA approvals of selective RET inhibitors, selpercatinib and pralsetinib, have revolutionized the field of RET precision therapy. In this article, we review the current status on the use of the selective RET inhibitor, selpercatinib, in RET fusion-positive tumors: NSCLC, thyroid cancers, and the more recent tissue-agnostic activity leading to FDA approval. SAGE Publications 2023-06-21 /pmc/articles/PMC10288430/ /pubmed/37360768 http://dx.doi.org/10.1177/17588359231177015 Text en © The Author(s), 2023 https://creativecommons.org/licenses/by/4.0/This article is distributed under the terms of the Creative Commons Attribution 4.0 License (https://creativecommons.org/licenses/by/4.0/) which permits any use, reproduction and distribution of the work without further permission provided the original work is attributed as specified on the SAGE and Open Access page (https://us.sagepub.com/en-us/nam/open-access-at-sage). |
spellingShingle | Review Gouda, Mohamed A. Subbiah, Vivek Precision oncology with selective RET inhibitor selpercatinib in RET-rearranged cancers |
title | Precision oncology with selective RET inhibitor selpercatinib in RET-rearranged cancers |
title_full | Precision oncology with selective RET inhibitor selpercatinib in RET-rearranged cancers |
title_fullStr | Precision oncology with selective RET inhibitor selpercatinib in RET-rearranged cancers |
title_full_unstemmed | Precision oncology with selective RET inhibitor selpercatinib in RET-rearranged cancers |
title_short | Precision oncology with selective RET inhibitor selpercatinib in RET-rearranged cancers |
title_sort | precision oncology with selective ret inhibitor selpercatinib in ret-rearranged cancers |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10288430/ https://www.ncbi.nlm.nih.gov/pubmed/37360768 http://dx.doi.org/10.1177/17588359231177015 |
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