Cargando…

Iterative Upgrading of Small Molecular Tyrosine Kinase Inhibitors for EGFR Mutation in NSCLC: Necessity and Perspective

Molecular targeted therapy has been reported to have fewer adverse effects, and offer a more convenient route of administration, compared with conventional chemotherapy. With the development of sequencing technology, and research on the molecular biology of lung cancer, especially whole-genome infor...

Descripción completa

Detalles Bibliográficos
Autores principales: Zhu, Jing, Yang, Qian, Xu, Weiguo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8468657/
https://www.ncbi.nlm.nih.gov/pubmed/34575576
http://dx.doi.org/10.3390/pharmaceutics13091500
_version_ 1784573727182159872
author Zhu, Jing
Yang, Qian
Xu, Weiguo
author_facet Zhu, Jing
Yang, Qian
Xu, Weiguo
author_sort Zhu, Jing
collection PubMed
description Molecular targeted therapy has been reported to have fewer adverse effects, and offer a more convenient route of administration, compared with conventional chemotherapy. With the development of sequencing technology, and research on the molecular biology of lung cancer, especially whole-genome information on non-small cell lung cancer (NSCLC), various therapeutic targets have been unveiled. Among the NSCLC-driving gene mutations, epidermal growth factor receptor (EGFR) mutations are the most common, and approximately 10% of Caucasian, and more than 50% of Asian, NSCLC patients have been found to have sensitive EGFR mutations. A variety of targeted therapeutic agents for EGFR mutations have been approved for clinical applications, or are undergoing clinical trials around the world. This review focuses on: the indications of approved small molecular kinase inhibitors for EGFR mutation-positive NSCLC; the mechanisms of drug resistance and the corresponding therapeutic strategies; the principles of reasonable and precision molecular structure; and the drug development discoveries of next-generation inhibitors for EGFR.
format Online
Article
Text
id pubmed-8468657
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-84686572021-09-27 Iterative Upgrading of Small Molecular Tyrosine Kinase Inhibitors for EGFR Mutation in NSCLC: Necessity and Perspective Zhu, Jing Yang, Qian Xu, Weiguo Pharmaceutics Review Molecular targeted therapy has been reported to have fewer adverse effects, and offer a more convenient route of administration, compared with conventional chemotherapy. With the development of sequencing technology, and research on the molecular biology of lung cancer, especially whole-genome information on non-small cell lung cancer (NSCLC), various therapeutic targets have been unveiled. Among the NSCLC-driving gene mutations, epidermal growth factor receptor (EGFR) mutations are the most common, and approximately 10% of Caucasian, and more than 50% of Asian, NSCLC patients have been found to have sensitive EGFR mutations. A variety of targeted therapeutic agents for EGFR mutations have been approved for clinical applications, or are undergoing clinical trials around the world. This review focuses on: the indications of approved small molecular kinase inhibitors for EGFR mutation-positive NSCLC; the mechanisms of drug resistance and the corresponding therapeutic strategies; the principles of reasonable and precision molecular structure; and the drug development discoveries of next-generation inhibitors for EGFR. MDPI 2021-09-18 /pmc/articles/PMC8468657/ /pubmed/34575576 http://dx.doi.org/10.3390/pharmaceutics13091500 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Zhu, Jing
Yang, Qian
Xu, Weiguo
Iterative Upgrading of Small Molecular Tyrosine Kinase Inhibitors for EGFR Mutation in NSCLC: Necessity and Perspective
title Iterative Upgrading of Small Molecular Tyrosine Kinase Inhibitors for EGFR Mutation in NSCLC: Necessity and Perspective
title_full Iterative Upgrading of Small Molecular Tyrosine Kinase Inhibitors for EGFR Mutation in NSCLC: Necessity and Perspective
title_fullStr Iterative Upgrading of Small Molecular Tyrosine Kinase Inhibitors for EGFR Mutation in NSCLC: Necessity and Perspective
title_full_unstemmed Iterative Upgrading of Small Molecular Tyrosine Kinase Inhibitors for EGFR Mutation in NSCLC: Necessity and Perspective
title_short Iterative Upgrading of Small Molecular Tyrosine Kinase Inhibitors for EGFR Mutation in NSCLC: Necessity and Perspective
title_sort iterative upgrading of small molecular tyrosine kinase inhibitors for egfr mutation in nsclc: necessity and perspective
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8468657/
https://www.ncbi.nlm.nih.gov/pubmed/34575576
http://dx.doi.org/10.3390/pharmaceutics13091500
work_keys_str_mv AT zhujing iterativeupgradingofsmallmoleculartyrosinekinaseinhibitorsforegfrmutationinnsclcnecessityandperspective
AT yangqian iterativeupgradingofsmallmoleculartyrosinekinaseinhibitorsforegfrmutationinnsclcnecessityandperspective
AT xuweiguo iterativeupgradingofsmallmoleculartyrosinekinaseinhibitorsforegfrmutationinnsclcnecessityandperspective