Objectives: Mizoribine (MZR) with its high safety and low cost has been widely used in Asia. It has been questioned whether high or low dose of MZR could obtain the efficacy and safety similar to mycophenolate mofetil (MMF) following renal transplantation. This meta-analysis was done to compare the efficacy and safety of high-or low-dose MZR with MMF for immunosuppressive therapy in renal transplantation. Design and methods: Available data comparing MZR with MMF in renal transplant recipients were searched. Subgroup analysis was conducted according to the administration dosage of MZR. Trials were pooled using Meta-analysis software and confidence intervals were set at 95%. Results: Altogether 1149 Asian patients from 7 RCTs and 9 cohort studies were included. The efficacy of different MZR doses put on par with MMF, but the safety was better than MMF. Specifically, recipients taking MZR favor significantly fewer episodes of leucocytopenia [RR 0.40 (0.26, 0.60)], gastrointestinal disorder [RR 0.54 (0.40, 0.73)], CMV infection [RR 0.47 (0.34, 0.64)] and more favorable outcome of hepatic dysfunction, although the difference failed to reach a statistical significance [RR 0.67 (0.44, 1.00)]. Unfortunately, hyperuricemia was significantly obvious in MZR group [RR 1.96 (1.47, 2.61)]. Conclusions: MZR is an effective and safe immunosuppressive agent and high-dose MZR can be recommended as an alternative to MMF following adult renal transplantation in Asia, but hyperuricemia and liver damage should be closely monitored during the medication period. (C) 2014 The Canadian Society of Clinical Chemists. Published by Elsevier Inc.