Update on the clinical utility of once-daily tacrolimus in the management of transplantation.

16 Stifft et al reported that patients with CYP3A5*1/*3 genotype had a greater decrease in intrapatient variability after conversion to once-daily tacrolimus compared to patients with CYP3A5*3/*3 genotype, although the differences did not reach statistical significance. 14 In a PK study on 97 Japanese kidney transplant recipients, absolute bioavailability was noted to be lower in CYP3A5*1 genotype patients compared to those with the CYP3A5*3/*3 genotype, while relative bioavailability was lower in patients on once-daily tacrolimus compared to those on twice-daily tacrolimus, regardless of CYP3A5 genotype. 16 In a similar study among Taiwanese kidney transplant recipients, 17 PK assessment was performed in 71 patients with high-expressive genotype (CYP3A5*1/*1 or CYP3A5*1/*3) and 79 patients with low-expressive genotype (CYP3A5*3/*3).

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