To evaluate whether the HSA–NAMI-A–Cu(BpT)Br–DOX complex overcome the resistance of MCF-7 breast cancer cells to DOX, we investigated the cytotoxicity of the HSA–NAMI-A–Cu(BpT)Br–DOX complex to MCF-7/ADR and MCF-7 breast cancer cells. Here, ALB is linked to breast carcinoma.