Title : In vivo CYP3A4 activity, CYP3A5 genotype, and hematocrit predict tacrolimus dose requirements and clearance in renal transplant patients.

Pub. Date : 2012 Sep

PMID : 22871995






6 Functional Relationships(s)
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1 In vivo CYP3A4 activity, CYP3A5 genotype, and hematocrit predict tacrolimus dose requirements and clearance in renal transplant patients. Tacrolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Tacrolimus is metabolized by CYP3A4 and CYP3A5 and is characterized by a narrow therapeutic index and highly variable pharmacokinetics. Tacrolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 In vivo CYP3A4 activity and CYP3A5 genotype explain 56-59% of variability in tacrolimus dose requirements and clearance, contributing ~25 and 30%, respectively. Tacrolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 These data indicate that CYP3A4- and CYP3A5-mediated tacrolimus metabolisms are major determinants of tacrolimus disposition in vivo and explain a substantial part of the clinically observed high interindividual variability in tacrolimus pharmacokinetics. Tacrolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens
5 These data indicate that CYP3A4- and CYP3A5-mediated tacrolimus metabolisms are major determinants of tacrolimus disposition in vivo and explain a substantial part of the clinically observed high interindividual variability in tacrolimus pharmacokinetics. Tacrolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens
6 These data indicate that CYP3A4- and CYP3A5-mediated tacrolimus metabolisms are major determinants of tacrolimus disposition in vivo and explain a substantial part of the clinically observed high interindividual variability in tacrolimus pharmacokinetics. Tacrolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens