Background: Tacrolimus (Tac, or FK506), a calcineurin inhibitor (CNI), is the first-line immunosuppressant
which consists of the footstone as immunosuppressive regimens in kidney transplantation. However, the drug
toxicity and the significant differences of pharmacokinetics (PK) and pharmacodynamics (PD) among individuals are
hidden troubles for clinical application. Recently, emerging evidences of Tac pharmacogenetics (PG) regarding drug
absorption, metabolism, disposition, excretion and response are discovered for better understanding of this drug.
Method: We reviewed the published articles regarding the Tac PG and its effects on PK and PD in kidney transplantation.
In addition, we summarized information on polygenic algorithms.
Results: The polymorphism of genes encoding metabolic enzymes and transporters related to Tac were largely investigated,
but the results were inconsistent. In addition to CYP3A4, CYP3A5 and P-gp (also known as ABCB1), single
nucleotide polymorphisms (SNPs) might also affect the PK and PD parameters of Tac.
Conclusion: The correlation between Tac PK, PD and PG is very complex. Although many factors need to be verified,
it is envisaged that thorough understanding of PG may assist clinicians to predict the optimal starting dosage,
help adjust the maintenance regimen, as well as identify high risk patients for adverse effects or drug inefficacy.