Title : Impact of Pharmacogenetics on Intravenous Tacrolimus Exposure and Conversions to Oral Therapy.

Pub. Date : 2022 Jan

PMID : 34583027






5 Functional Relationships(s)
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1 BACKGROUND: CYP3A5 and CYP3A4 are the predominant enzymes responsible for tacrolimus metabolism, however only a proportion of the population expresses CYP3A5 secondary to genetic variation. Tacrolimus cytochrome P450 family 3 subfamily A member 5 Homo sapiens
2 CYP3A5 is expressed in both the intestine and the liver and has been shown to impact both oral tacrolimus bioavailability and metabolism. Tacrolimus cytochrome P450 family 3 subfamily A member 5 Homo sapiens
3 OBJECTIVE: The objective of this study was to evaluate the impact of CYP3A5 genotype as well as other pharmacogenes on IV tacrolimus exposure to determine whether the current genotype-guided dosing recommendations are appropriate for this formulation. Tacrolimus cytochrome P450 family 3 subfamily A member 5 Homo sapiens
4 Additionally, this study aimed to investigate dose conversion requirements among CYP3A5 genotypes when converting from IV to PO tacrolimus. Tacrolimus cytochrome P450 family 3 subfamily A member 5 Homo sapiens
5 RESULTS: CYP3A5 and CYP3A4 genotypes were significantly associated with the IV C/D with CYP3A5 expressers having 20% lower and CYP3A4 rapid metabolizers having 20% lower tacrolimus exposure. Tacrolimus cytochrome P450 family 3 subfamily A member 5 Homo sapiens