The medical approach to the management of metastatic breast cancer has changed through the years following the introduction of new cytotoxic agents and the demonstration of their antitumor activity. In general, combination drug regimens are the initial treatments of choice when chemotherapy is indicated for patients with metastatic breast cancer. However, the single-agent activity of some of the newer agents rivals that of older combination chemotherapy treatments. Compared with older therapies, improved objective response rates and/or improved duration of response recently have been reported in studies evaluating optimal dosing and sequencing of these newer agents, alone or in combination with other drugs. Although there is no rigid standard for the sequencing of therapy for management of metastatic breast cancer, chemotherapy has a role in the treatment program for nearly all patients with this disease. The goal of treatment remains meaningful palliation of patients with complications of progressive cancer.