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Purpose: To analyse and compare the clinical effects and safety of capecitabine and tegafur/gimeracil/oteracil (S-1) in the treatment of advanced breast carcinoma.Methods: Eighty-four metastatic breast cancer elderly patients for whom first or second-line treatment had failed, were selected from among those admitted to the oncology ward of Binjiang People’s Hospital, China between January 2014 and June 2015. They were randomly divided into S-1 group (n =41) and capecitabine group (n = 41) and received varying doses of those drugs according to body surface area. Clinical effects, progression-free survival, and incidence of adverse reactions were compared for the two groups following treatment.Results: Disease control rate (CR) in S-1 group was 55.6 %, much higher than 35.1 % observed for capecitabine group (p < 0.05). The disease control rate for the S-1 group was 93.7 %, also much higher than the 70.6 % found in capecitabine group. Survival analysis showed that the median survival times of the two groups did not differ significantly (p > 0.05). Furthermore, some adverse reactions such as myelosuppression and lack of strength, did not differ significantly between the two groups (p > 0.05), whereas others, including leukopenia, nausea and vomiting and hand-foot syndrome were more serious and frequent in capecitabine group than in S-1 group (p < 0.05).Conclusion: Monotherapy with S-1 is more effective than that with capecitabine. Adverse reactions are minimal for both drugs.Keywords: Breast carcinoma, Capecitabine, S-1, Adverse reactions, Myelosuppression, Leukopenia, Hand-foot syndrome