Anthracycline, taxane or trastuzumab play a central role in systemic chemotherapy for breast cancer. The standard of subsequent treatment is capecitabine, S-1, vinorelbine, irinotecan or gemcitabine. Ixabepilone or nanoparticle paclitaxel is effective for taxane-resistant breast cancer. Lapatinib proves effective for trastuzumab-resistant HER2-overexpressing breast cancer and also for brain metastasis. Trastuzumab-DM1, pertuzumab and neratinib are promising drugs. In terms of antiangiogenic agents, bevacizumab in combination with taxane demonstrates efficacy. Axitinib, sunitinib or pazopanib is under investigation. It is necessary to study the best manner of sequence and combination in these drugs.