Abstract: Human epidermal growth factor receptor-2 (HER-2) gene amplification and protein overexpression occur in approximately 15% to 20% of breast cancer patients, resulting in a clinically aggressive tumor type that is associated with a poor prognosis. HER-2-targeted therapies could effectively reduce the recurrence and improve the prognosis of breast cancer. In recent years, the application of new anti-HER-2 agents, such as pertuzumab, T-DM1, and pyrotinib, have further improved the survival of patients with HER2-positive breast cancer, and updated the guidelines for the treatment of breast cancer, making anti-HER-2 targeted therapy more accurate. This review described the latest development of targeted agents for HER-2-positive breast cancer.