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Summary: Simotinib (SIM6802) is a selective epidermal growth factor receptor tyrosine kinase inhibitor and is used for the treatment of lung cancer.Recently, we discovered that it inhibits the P-glycoprotein (P-gp), which is an ATP binding cassette transporter.P-glycoprotein pumps multiple types of drugs out of the cell using energy generated from ATP, and confers multidrug resistance on cancer cells.We aimed to elucidate the impact of simotinib on P-glycoprotein activity.