Abstract: OBJECTIVE To introduce the progress of specific human prolactin receptor antagonist G129R-hPRL in breast cancer therapy research. METHODS Review the function, mechanism, advantages and disadvantages, improvements, the application and the prospect of the prolactin receptor antagonist G129R-hPRL in therapy of breast tumor through searching and summarizing relevant literatures. RESULTS G129R-hPRL can inhibit proliferation, mediate apoptosis of breast cancer cell and play the role of anti-breast cancer by competitively antagonize endogenous prolactin. G129R-hPRL-based multi-functional fusion protein, as well as combination G129R-hPRL with other anti-tumor component also shows a stronger tumor suppressor effect. CONCLUSION G129R-hPRL is expected to be an ideal drug in treatment and prevention of breast cancer.