Epirubicin, a member of the anthracycline family of chemotherapeutic agents, has been widely used throughout the world both as adjuvant therapy in early breast cancer and in metastatic breast cancer. Clinical trials with epirubicin have examined the importance of a dose-response relationship, therapeutic dose, and optimum duration of chemotherapy. In addition, pharmacokinetic studies have provided data on ideal combinations with other agents. Epirubicin-containing regimens are considered to be superior to those containing cyclophosphamide, methotrexate, and fluorouracil (CMF) and are also used in patients with locally advanced stage IIIA/IIIB breast cancer. Combinations with other chemotherapeutic agents (eg, epirubicin plus a taxane, sequential or combined use of these agents) are being evaluated in ongoing clinical trials. Moreover, recent studies have suggested that biologic markers, such as tumor HER2/neu overexpression, predict responses to dose-intensive anthracycline chemotherapy, and combinations with nonchemotherapeutic regimens (eg, trastuzumab) may provide additional benefits, but such strategies require further evaluation.