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- W2952344688 abstract "First generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (gefitinib and erlotinib) demonstrate excellent clinical efficacy for NSCLC patients carrying EGFR oncogenic mutations (L858R, del exon 19 deletions between amino acids 746 and 750). Invariable, drug resistance occurs with around 60% of it driven by the EGFR-T790M gatekeeper mutation. To counter the T790M-dependent resistance, third generation covalent EGFR inhibitors have been developed with high potency toward T790M containing mutants and selectivity over WT EGFR. This review provides an overview of the third generation drugs currently in clinical trials and also encompasses novel methodologies developed to discover third generation covalent EGFR drugs." @default.
- W2952344688 created "2019-06-27" @default.
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- W2952344688 date "2016-05-01" @default.
- W2952344688 modified "2023-09-26" @default.
- W2952344688 title "ChemInform Abstract: Recent Progress on Third Generation Covalent EGFR Inhibitors" @default.
- W2952344688 cites W2281446905 @default.
- W2952344688 doi "https://doi.org/10.1002/chin.201621272" @default.
- W2952344688 hasPublicationYear "2016" @default.
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