A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib

KRAS(G12C) is one of the most common oncogenes in non-small cell lung cancer (NSCLC) and is associated with a poor prognosis. Historically, KRAS mutations have been difficult to target due to lack of binding sites and exceptionally high affinity for guanosine triphosphate/guanosine diphosphate (GTP/...

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Detalles Bibliográficos
Autores principales: Brazel, Danielle, Arter, Zhaohui, Nagasaka, Misako
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove 2022
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9662012/
https://www.ncbi.nlm.nih.gov/pubmed/36387582
http://dx.doi.org/10.2147/LCTT.S383662
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author Brazel, Danielle
Arter, Zhaohui
Nagasaka, Misako
author_facet Brazel, Danielle
Arter, Zhaohui
Nagasaka, Misako
author_sort Brazel, Danielle
collection PubMed
description KRAS(G12C) is one of the most common oncogenes in non-small cell lung cancer (NSCLC) and is associated with a poor prognosis. Historically, KRAS mutations have been difficult to target due to lack of binding sites and exceptionally high affinity for guanosine triphosphate/guanosine diphosphate (GTP/GDP). Recently, KRAS(G12C) selective inhibitors have shown promising results in Phase I/II studies. Here we discuss the mechanism of action, pharmacokinetic and pharmacodynamic properties, efficacy, and tolerability of adagrasib (MRTX849).
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spelling pubmed-96620122022-11-15 A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib Brazel, Danielle Arter, Zhaohui Nagasaka, Misako Lung Cancer (Auckl) Review KRAS(G12C) is one of the most common oncogenes in non-small cell lung cancer (NSCLC) and is associated with a poor prognosis. Historically, KRAS mutations have been difficult to target due to lack of binding sites and exceptionally high affinity for guanosine triphosphate/guanosine diphosphate (GTP/GDP). Recently, KRAS(G12C) selective inhibitors have shown promising results in Phase I/II studies. Here we discuss the mechanism of action, pharmacokinetic and pharmacodynamic properties, efficacy, and tolerability of adagrasib (MRTX849). Dove 2022-11-10 /pmc/articles/PMC9662012/ /pubmed/36387582 http://dx.doi.org/10.2147/LCTT.S383662 Text en © 2022 Brazel et al. https://creativecommons.org/licenses/by-nc/3.0/This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/ (https://creativecommons.org/licenses/by-nc/3.0/) ). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php).
spellingShingle Review
Brazel, Danielle
Arter, Zhaohui
Nagasaka, Misako
A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib
title A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib
title_full A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib
title_fullStr A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib
title_full_unstemmed A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib
title_short A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib
title_sort long overdue targeted treatment for kras mutations in nsclc: spotlight on adagrasib
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9662012/
https://www.ncbi.nlm.nih.gov/pubmed/36387582
http://dx.doi.org/10.2147/LCTT.S383662
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