Abstract: Immunosuppressants, which are commonly used for liver transplantation, mainly included calcineurin inhibitors, such as ciclosporin (CsA) and tacrolimus (FK506); glucocorticoid drugs, such as prednisone and prednisolone; cytotoxic drugs, such as azathioprine, mycophenolate mofetil and cyclophosphamide; mammalian target of rapamycin (mTOR) inhibitors, such as sirolimus and everolimus; antibody drugs, such as polyclonal or monoclonal antibodies and interleukin (IL)-2 receptor antibodies, etc. Although many categories of immunosuppressants are available, FK506 is the most commonly adopted in liver transplant recipients. However, FK506 can provoke significant adverse effects in the late stage of liver transplantation, especially severe infection and nephrotoxicity. Consequently, it is an urgent task and research hot spot to develop new immunosuppressants with strong immune tolerance and mild adverse effects in clinical practice. In this article, the research progress on immunosuppressants and the research and development status of new immunosuppressants for liver transplantation were reviewed.