As a result of increasing anthracycline use earlier in the course of breast cancer, oncologists are frequently faced with the challenge of treating patients whose disease has progressed during or following anthracycline therapy or who are ineligible for further anthracycline therapy. Many of these women remain candidates for cytotoxic chemotherapy, and several treatment options exist. Until recently, the taxanes, docetaxel in particular, were widely regarded as the most effective therapy for these patients, based on a survival advantage observed with docetaxel. However, a recent phase III study demonstrated that the addition of capecitabine to docetaxel results in superior overall survival (with a 3-month improvement in median survival), superior time to disease progression, and a superior response rate, with a manageable safety profile. Capecitabine/docetaxel is the first cytotoxic combination to improve survival over standard monotherapy in patients with anthracycline-pretreated metastatic breast cancer. Moreover, the survival benefit can be attributed to the addition of capecitabine, as it was achieved despite the lower dose of docetaxel administered in the combination arm. Quality of life was maintained with capecitabine/docetaxel combination therapy, which further supports the use of this regimen in patients with anthracycline-pretreated metastatic breast cancer. Pharmacoeconomic modeling using the data from the phase III trial has shown that the capecitabine/docetaxel combination therapy is highly cost effective when compared with other cancer treatments that improve survival. This review describes several treatment options for patients with anthracycline-pretreated breast cancer, including the phase III data (efficacy, tolerability, quality of life, and pharmacoeconomics) for capecitabine plus docetaxel in this setting.