The area under the concentration time curve (AUC) for oral tacrolimus (FK) may provide a more precise model for FK monitoring after renal transplantation. The purpose of this study is to identify a simple, cost-effective method for predicting FK AUG. FK concentrations were measured at 0, 1,2, 4, 6, 8, and 12 hours after the morning dose. The predicted AUCs (AUC(p)s) derived from regression equations were used to estimate the actual 12-hour AUCs (AUC(12)S) The relationship between AUG, and AUC(12) was validated by determining the coefficient of multiple determination (Re), percentage of prediction error (PE%), and percentage of absolute prediction error (APE%). Eighteen stable Oriental renal transplant recipients (9 men, 9 women) with a mean age of 42.6 +/- 6 years and mean body weight of 62.7 +/- 10 kg were recruited for the study. The FK AUC(12) trough, P-hour, and 4-hour concentrations were 125 +/- 24 h ng/mL (range, 87.7 to 181.9 h ng/mL), 6 1: 1.3 ng/mL, 18.1 +/- 4.7 ng/mL, and 11 +/- 2.4 ng/mL, respectively. Trough FK concentration did not have a significant correlation with AUC(12) (r = 0.34; P = 0.17). AUC(p) obtained by a two-time point regression equation using P-hour (C2) and 4-hour (C4) FK concentrations: (AUCp = 16.2 + 2.4(*)C2 +/- 5.9(*)C4) obtained an R-2, PE%, and APE% of 0.93, -0.2X +/- 5.2% (range, -13% to 9.3%), and 3.6% +/- 3.7% (range, 0.02% to 13%), respectively. We conclude that a two-point sampling method using C2 and C4 may be a more cost-effective FK monitoring strategy than morning FK trough levels in transplant recipients. (C) 2000 by the National Kidney Foundation, Inc.