Fig. 7

Schematic diagram of dacomitinib reversing MDR. In the absence of dacomitinib, ABCG2 transporters utilize energy derived from the hydrolysis of ATP to efflux its substrates agents crossing the membrane (a). However, in the presence of dacomitinib, dacomitinib may bind to the ATP binding site of ABCG2, thereby blocking the efflux of the transporter substrates and increasing the intracellular accumulation of the substrate drugs. Therefore, dacomitinib could increase the efficacy of conventional chemotherapeutic drug in ABCG2 overexpressing cancer cells (b)