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
Descripción
Sumario: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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