Capecitabine is a novel fluoropyrimidine carbamate, which has a broader spectrum of antitumor activity than other fluoropyrimidines, such as 5-FU, DFUR, or UFT; it has proved effective over a wide dose range. Recent research has suggested that frequent administration of lower doses of certain chemotherapeutic drugs might enhance their antiangiogenic effect. The present study investigated the antiangiogenic effect of capecitabine on breast cancer. In order to augment its efficacy, we combined capecitabine chemotherapy with ginsenoside Rg3. Our results indicate that a metronomic regimen of capecitabine inhibited angiogenesis in breast cancer, and its antiangiogenic effects may be further enhanced by the concurrent administration of ginsenoside Rg3. As an antiangiogenic method, this regimen presented better antitumor effects, less toxicity, and reduced susceptibility to drug resistance.