2. Academic Validation
  3. Recent advances of novel fourth generation EGFR inhibitors in overcoming C797S mutation of lung cancer therapy

Recent advances of novel fourth generation EGFR inhibitors in overcoming C797S mutation of lung cancer therapy

  • Eur J Med Chem. 2023 Jan 5;245(Pt 1):114900. doi: 10.1016/j.ejmech.2022.114900.
Li Xu 1,  Bing Xu 1,  Jianshe Wang 2,  Yuan Gao 1,  Xingrui He 3,  Tian Xie 4,  Xiang-Yang Ye 5
Affiliations

Affiliations

  • 1 School of Pharmacy, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, China; Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, China.
  • 2 Drug Discovery, Hangzhou PurpleCrystal Pharma Co., LTD, Hangzhou, Zhejiang, 311121, China.
  • 3 School of Pharmacy, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, China; Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, China. Electronic address: hexingrui163@163.com.
  • 4 School of Pharmacy, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, China; Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, China. Electronic address: xbs@hznu.edu.cn.
  • 5 School of Pharmacy, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, China; Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, China. Electronic address: xyye@hznu.edu.cn.
PMID: 36417820 DOI: 10.1016/j.ejmech.2022.114900
Abstract

Lung Cancer is the second place among the global Cancer population in term of the morbidity and mortality, while non-small cell lung Cancer (NSCLC) accounts for the largest proportion of all lung Cancer patient. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are commonly used in the treatment of NSCLC. Despite of the success in coping with EGFR kinase resistance lung Cancer using the first three generations of EGFR-TK inhibitors (EGFR-TKIs), the new problem of resistance to Osimertinib occurred due to the newly developed EGFRC797S mutation. In recent years, scientists have proposed several pharmacochemical strategies for the treatment of Osimertinib-resistant NSCLC patients. This paper intends to collect the references in this field since 2021 and to summarize the pharmacochemical processes and strategies in discovery of novel EGFR-TKIs for overcoming C797S mutation in lung Cancer patients. It could serve as quick information provider for further structural modifications and drug discovery.

Keywords

C797S mutation; Epidermal growth factor receptor (EGFR); Non-small cell lung cancer (NSCLC); Tyrosine kinase inhibitors (TKIs).

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