Abstract

Tacrolimus remains mainstay of immunosuppression in renal transplant recipients. Tacrolimus has narrow therapeutic window. Underdosing can precipitate rejection, whereas overdose may result in toxicity. CYP3A5 polymorphism can explain the inter individual variability in the tacrolimus pharmacokinetics. CYP3A5 expressers have faster tacrolimus metabolism as compared to nonexpressers. Using genotype-based tacrolimus dosing can help achieve therapeutic drug levels faster than weight-based dosing. However, differences in CYP3A5 expression have not translated into clinical outcomes in many studies. Further studies are needed to ascertain the role of CYP3A5 in tacrolimus toxicity. In this article, we reviewed the evidence pertaining to CYP3A5 polymorphism and its impact on tacrolimus pharmacokinetics and also their role in tacrolimus dose decision-making.

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