Abstract: Patients with HER-2-positive advanced breast cancer were associated with poor prognosis. Meanwhile, HER- 2-targeted ther -apy has dramatically improved survival and prognosis among breast cancer patients. Over the years, multiple HER- 2- targeting drugs stepped into clinical practice, and the targeted agents are now considered as the standard of care in the first-line setting and beyond. This review basically summarizes the importance of HER-2-targeted therapy, the significance of the clinical trial results, and the clinical practice guidelines for the management of patients with HER- 2-positive advanced breast cancer.