Abstract: Abnormally activation of phosphatidylinositol-3-kinase (PI3K)-protein kinase B (Akt/PKB)-mammalian target of rapamycin (mTOR) signaling pathway in breast cancer can induce proliferation and differentiation of breast cancer cells. At present, molecular targeted therapy for this pathway has become a hot spot in the cancer research field, and some Akt inhibitors have entered in clinical trials of breast cancer. Akt inhibitors include broad-spectrum Akt inhibitors, selective Akt inhibitors and PI3K/Akt dual inhibitors. This article summarizes the research progress of Akt molecular targeting inhibitors in the treatment of breast cancer, in order to provide evidences for further research.