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

Pharmaceutics

Jing Zhu¹  Weiguo Xu¹  Qian Yang² 

[1] Respiratory and Critical Care Medicine, Mianyang Central Hospital, Mianyang 621000, China;Sichuan Province College Key Laboratory of Structure-Specific Small Molecule Drugs, School of Pharmacy, Chengdu Medical College, No. 783, Xindu Avenue, Xindu District, Chengdu 610500, China;

关键词: epidermal growth factor receptor tyrosine kinase inhibitors;    EGFR mutations;    molecular targeted therapy;    non-small cell lung cancer;    resistance mechanism;   

DOI  :  10.3390/pharmaceutics13091500

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown