Breast cancer (BC) is the most common malignant tumor in women. In recent years, research data shows that early diagnosis and treatment can significantly reduce the mortality of patients with cancer. Positron mission computed tomography (PET/CT) is a noninvasive and systemic imaging method which integrates function and anatomy, and plays an important role in the clinical staging and guiding treatment of BC. _¹⁸F-fluorodeoxyglucose (_¹⁸F-FDG) is the most widely used imaging agent, because of non-specificity, its application in BC patients is limited to some extent. Therefore, for the past few years, there are more researches on the specific receptor imaging agents for BC patients. This paper reviews the development and clinical application of new molecular targeted positron drugs in PET imaging of breast cancer.