Abstract: Docetaxel has been used widely for the treatment of breast cancer in neoadjuvant, adjuvant and metastatic settings. However, its therapeutic usefulness is limited by innate or acquired resistance. The known mechanisms of docetaxel resistance in breast cancer include the alteration of drug target, the activation of detoxifying enzymes, the aberrant expression of apoptosis-related genes, the DNA methylation status, the overexpression of the ATP-binding cassette transporters, and the abnormal microRNA expression.