Our results suggest that cariprazine significantly reverses ABCG2-mediated MDR and re-sensitizes both lung and colon cancer cell lines overexpressing ABCG2 transporters to substrate antineoplastic drugs like MX by inhibiting the efflux function of the transporter and downregulating the expression levels of ABCG2 transporter. Here, ABCG2 is linked to colonic neoplasm.