It turns out that combination therapy, which involves a chemotherapeutic drug with a reversal reagent, is the prospective approach to regulate the aberrant function of ABC transporters.[4] TKIs used for certain cancer treatments generally have “off-target” impacts.[44,45] In past decades, TKIs exhibit potential re-sensitization effects to overcome ABC transporter-mediated MDR in combination with other chemotherapeutic drugs.[46] Hence, the usage of TKIs to restore the effect of traditional anticancer drugs is regarded as an alternative therapy in ABC transporter-associated MDR. Here, ABCG2 is linked to cancer.