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Lapatinib, a tyrosine kinase inhibitor (TKI), is used in the treatment of advanced or metastatic breast cancer overexpressing human epidermal receptor 2 (HER2).Lapatinib can modulate the function of ATP-binding cassette (ABC) transporters (ABCB1 and ABCG2) which are the major mechanism responsible for multidrug resistance (MDR) in cancer.In this study, we investigated the effect of lapatinib on multidrug resistance-associated protein 1(MRP1/ABCC1), MRP2 (ABCC2), MRP4 (ABCC4) and lung relative resistance protein (LRP) drug efflux pump.