Tacrolimus: Does direct glucuronidation matter? An analytical and pharmacological perspective

Abstract : Tacrolimus, the gold standard of immunosuppressive treatment indicated to prevent graft rejection in solid organ recipients, is extensively metabolized. While impact of phase I metabolism on the drug pharmacokinetics has been widely discussed, little is known on its glucuronidation mediated by uridine diphosphate glucuronyltransferases (UGT). The impact of glucuronidation in the field of therapeutic drug monitoring might be underestimated mainly because glucuronide metabolite is presumed to be a non-active and short half-life drug. As part of an on-going pharmacokinetic study conducted in our center (CYPTAC’H, NCT01388387) we performed extensive kinetic profiles of tacrolimus whole-blood concentrations in liver transplant recipient patients.
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C. Tron, A. Petitcollin, M.-C. Verdier, M. Rayar, J.-M. Beaurepaire, et al.. Tacrolimus: Does direct glucuronidation matter? An analytical and pharmacological perspective. Pharmacological Research, Elsevier, 2017, 124, pp.164-166. ⟨10.1016/j.phrs.2017.03.027⟩. ⟨hal-01614704⟩

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