The aim of this study was to evaluate the efficacy and the toxicity of capecitabine therapy in metastatic breast cancer. A total of 103 patients treated between December 2001 and December 2005 were evaluated retrospectively. Capecitabine was used at a dose of 2500 mg/m(2)/day for 14 days, with 3 weeks of intervals between cyclesevery 3 weeks. There were 20 patients (19.4%) with brain metastasis at the start of capecitabine regimen. Median cycle of capecitabine was 6 cycles (range 1-24 cycles) mainly as 3rd line therapy (range 1.-9. line). The overall response rate was 48.6% (3.9% complete response plus 44.7% partial response). The rates of progressive and stable disease were 23.3% and 28.2%, respectively. Thirty patients (29%) required dose reduction due to adverse side effects, and treatment was discontinued in 4 patients (3.8%). Capecitabine is an effective and safe drug in the treatment of metastatic breast cancer, and it has also shown promising activity in the treatment for brain metastases in patients with breast cancer.