Combination of cisplatin and belinostat is synergistic in NSCLC. Belinostat apparently circumvent cisplatin resistance. Belinostat increased cellular cisplatin accumulation by inhibiting ABCC2 efflux. Belinostat downregulated ABCC2 by increasing binding of a repressor to the promoter. Belinostat inhibited DNA repair by downregulating the DNA repair gene ERCC1.