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Biomedicines, Volume 12, Issue 7 (July 2024) – 249 articles

Cover Story (view full-size image): EGFR tyrosine kinase inhibitors (TKIs) are key drugs in the treatment of non-small cell lung cancer patients with EGFR-activating mutations. First-, second-, and third-generation (abbreviated as 1G, 2G, and 3G) EGFR-TKIs have been applied in clinical use, and osimertinib (3G-TKI) is now the standard-of-care as front-line treatment in many countries. In this study, we searched for an optimal TKI after front-line osimertinib failure using in vitro models harboring EGFR-activating mutation plus osimertinib-resistant secondary mutation by comparing erlotinib (1G-TKI), novel 3G-TKIs, and BI4020 (4G-TKI). We also explored acquired resistance mechanisms to BI4020 assuming that it may be used as a front-line TKI in the near future. View this paper
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