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Osimertinib is a third-generation, CNS-active, irreversible, oral epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) that potently and selectively inhibits both EGFR-TKI-sensitizing and T790M resistance mutations, but it does not bind to healthy, unmutated HER1/EGFR/ErbB-1 (epidermal growth factor receptor). Instead, Osimertinib binds irreversibly to HER1/EGFR/ErbB-1 (epidermal growth factor receptor) (MUT) (mutations in L858R and exon 19 deletion)
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