Abstract: Great progress has been achieved in breast cancer molecular imaging thanks to the rapid development of nuclear medicine equipment and novel imaging agents. The exploration of specific molecular targets is not only helpful in the diagnostic evaluation of breast cancer, but also promotes the blossom of radionuclide targeted therapy. Along with the continuous emergence of molecular targeted probes and improvement of molecular targeted technologies, radionuclide targeted imaging and therapy may eventually become promising approaches in the personalized therapy of breast cancer. This review summarizes the research progress of radionuclide targeted therapy of breast cancer mediated by receptor, antibody and gene, and briefly introduces the improvement strategies and development prospects in the theranostics of breast cancer.