Chemoresistance is one of the major challenges for the breast cancer treatment. Owing to its heterogeneous nature, the chemoresistance mechanisms of breast cancer are complicated, and not been fully elucidated. The existing treatments fall short of offering adequate solution to drug resistance, so more effective approaches are desperately needed to improve existing therapeutic regimens. To overcome this hurdle, a number of strategies are being investigated, such as novel agents or drug carriers and combination treatment. In addition, some new therapeutics including gene therapy and immunotherapy may be promising for dealing with the resistance. In this article, we review the mechanisms of chemoresistance in breast cancer. Furthermore, the potential therapeutic methods to overcome the resistance were discussed.