Article
Discovery of YK-029A, a novel mutant EGFR inhibitor targeting both T790 M and exon 20 insertion mutations, as a treatment for NSCLC.
European journal of medicinal chemistry - 5 Oct 2023
Liu Bin, Gao Feng, Zhao Hui, Yuan Shuai, Peng Xingzhe, Zhang Pengzhi, Wang Jing, Zhang Tongmei, Duan Maosheng, Guo Yongqi
Abstract excerpt
Although traditional EGFR-TKIs have advanced the treatment landscape of NSCLC with sensitive driver mutations (del19 or L858R), some NSCLC patients with EGFR exon 20 insertion mutations have been left with few effective therapies. The development of novel TKIs is still in progress. Herein, we describe the structure-guided design of a novel selective and orally bioavailable inhibitor, YK-029A, which could overcome...
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