Abstract

Abstract Breast cancer is the most common and lethal cancer type in women. Even with the use of newly developed chemotherapy drugs, their effectiveness for breast cancer treatment tends to substantially decline when the disease progresses due to a multitude of chemoresistance mechanisms. The multidrug resistance (MDR) phenotype mediated by drug efflux transporters such as P-glycoprotein has long been recognized as one of these key chemoresistance mechanisms. MDR may be intrinsic or acquired in response to chemotherapy. As chemotherapy is the primary treatment option for the highly aggressive triple negative breast cancer, and is also commonly included in the regimens for other breast cancer subtypes in advanced stage, this chemoresistance mechanism deserves a focused review and discussion. In this chapter, we will provide a general overview of the breast cancer disease and discuss the role of drug efflux transporters in mediating chemoresistance of this malignant disease. Several strategies to address this problem ranging from the use of MDR reversal agents to the development of novel nanotherapeutics will be discussed.

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