Abstract

First-, second-, and third-generation (G) epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are now available in clinical practice. Since acquisition of T790M and C797S mutations confer resistance to 1G/2G and 3G EGFR-TKIs, respectively, several 4G EGFR-TKIs that can inhibit triple mutations of activating mutation/T790M/C797S are now being developed. In this study, we evaluated an in vitro activity and potential resistance mutations to one of the 4G EGFR-TKIs, BI-4020, using Ba/F3 models.

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