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Review
. 2021 Jan 15:210:112995.
doi: 10.1016/j.ejmech.2020.112995. Epub 2020 Nov 16.

The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation

Jie He  1 , Zhihui Zhou  1 , Xin Sun  1 , Zunhua Yang  2 , Pengwu Zheng  1 , Shan Xu  3 , Wufu Zhu  4
Affiliations
Review

The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation

Jie He et al. Eur J Med Chem. .

Abstract

Epidermal growth factor receptor (EGFR) is a receptor for epithelial growth factor (EGF) cell proliferation and signaling, which is related to the inhibition of tumor cell proliferation, angiogenesis, tumor invasion, metastasis, and apoptosis. Thus, it has become an important target for the treatment of non-small cell lung cancer (NSCLC). The first to the third-generation EGFR inhibitors have demonstrated powerful efficacy and brought a prospect to patients. Unfortunately, after 9-15 months of treatment, they all developed resistance without exception. As for the resistance of third-generation inhibitors, no major breakthrough has been made in this field. In this review, we discussed the recent advances in medicinal chemistry of fourth-generation EGFR-TKIs, as well as further discussed the clinical challenges and future prospects of treating patients with EGFR mutations resistant to third-generation EGFR-TKIs.

Keywords: C797S; EGFR; NSCLC; The fourth-generation inhibitors.

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Conflict of interest statement

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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