Profiling of absorption of cyclosporine (CsA) microemulsion is a concept in therapeutic drug monitoring (TDM) designed to optimize the clinical benefits of the drug in transplant recipients. A single blood concentration at 2 h (C(2)) after CsA microemulsion administration in kidney transplant recipients accurately predicts graft outcome. An international guidelines has recommended the target C(2) over time-course post-transplantation. We determined whether this recommendation is appropriate for our patients who are Asian ethnic. The clinical data of these C(2) monitoring kidney transplant recipients were compared with the historical cohort of microemulsion CsA trough (C(0)) level monitoring during the first 24-month post-transplantation. The inclusion and exclusion criteria were applied for both C(2) and C(0) cohorts. The mean target C(2) concentrations at 1, 3, 6, and 12-month post-transplantation were achieved in the C(2) cohort as the international guildlines. At 3-month post-transplantation, patients who had C(2) concentrations over 1500 ng/mL had higher serum creatinine as compared with those who had C(2) levels <1300 ng/mL (2.23 +/- 0.8 vs. 1.44 +/- 0.38 mg/dL: p = 0.01). Also, at 6-month post-transplantation, patients who had C(2) concentrations over 1300 ng/mL had higher serum creatinine (1.96 +/- 0.29 vs. 1.37 +/- 0.34 mg/dL: p < 0.01) as compared with those who had C(2) levels <1100 ng/mL. There was no statistical difference of acute rejection episodes between the two cohorts. The international consensus for C(2) concentraion may be too high for Asian ethnic kidney transplant recipients. The data from this study indicated lower than recommended C(2) concentraion as an appropriate C(2) target concentraion.