Article
Activity of tarloxotinib-E in cells with EGFR exon-20 insertion mutations and mechanisms of acquired resistance.
Thoracic cancer - 1 May 2021
Nishino Masaya, Suda Kenichi, Koga Takamasa, Ohara Shuta, Fujino Toshio, Soh Junichi, Tirunagaru Vijaya, Vellanki Avanish, Doebele Robert C, Mitsudomi Tetsuya
Abstract excerpt
BACKGROUND: Approximately 10% of non-small cell lung cancers (NSCLCs) that harbor epidermal growth factor receptor (EGFR) gene mutations have in-frame insertions in exon 20 of the EGFR gene. These tumors do not usually respond to currently available EGFR-tyrosine kinase inhibitors (TKIs). Tarloxotinib is a novel hypoxia-activated prodrug that releases a potent, irreversible pan-ERBB TKI (tarloxotinib-E) under...
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