2. Academic Validation
  3. The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation

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

  • Eur J Med Chem. 2021 Jan 15:210:112995. doi: 10.1016/j.ejmech.2020.112995.
Jie He 1,  Zhihui Zhou 1,  Xin Sun 1,  Zunhua Yang 2,  Pengwu Zheng 1,  Shan Xu 3,  Wufu Zhu 4
Affiliations

Affiliations

  • 1 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, 605 Fenglin Road, Nanchang, Jiangxi, 330013, China.
  • 2 College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
  • 3 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, 605 Fenglin Road, Nanchang, Jiangxi, 330013, China. Electronic address: shanxu9891@126.com.
  • 4 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, 605 Fenglin Road, Nanchang, Jiangxi, 330013, China. Electronic address: zhuwufu-1122@163.com.
PMID: 33243531 DOI: 10.1016/j.ejmech.2020.112995
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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