Figure 7.

Schematic diagram showing the mechanism of rociletinib. (A) ABCG2 transporters utilize energy derived from the hydrolysis of ATP to efflux its substrates agents across the cell membrane in the absence of rociletinib. (B) Rociletinib 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, rociletinib could increase the efficacy of conventional chemotherapeutic drugs in ABCG2-overexpressing MDR cancer cells.