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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...

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Detalles Bibliográficos
Autores principales: Gouda, Mohamed A., Subbiah, Vivek
Formato: Online Artículo Texto
Lenguaje:English
Publicado: SAGE Publications 2023
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.
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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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