Article
CH7233163 Overcomes Osimertinib-Resistant EGFR-Del19/T790M/C797S Mutation.
Molecular cancer therapeutics - 1 Nov 2020
Kashima Kenji, Kawauchi Hiroki, Tanimura Hiromi, Tachibana Yukako, Chiba Takashi, Torizawa Takuya, Sakamoto Hiroshi
Abstract excerpt
Osimertinib is the only EGFR-tyrosine kinase inhibitor (TKI) capable of overcoming EGFR-T790M-mutated NSCLC, but osimertinib-resistant EGFR triple mutations (Del19/T790M/C797S or L858R/T790M/C797S) have been reported. Although allosteric EGFR TKIs (e.g., EAI-045) that potentially overcome L858R/T790M/C797S have been identified, there are no effective inhibitors against Del19/T790M/C797S. In this study, we...
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