Tacrolimus: An Updated Review on Pharmacological, Pharmacodynamic, Pharmacokinetic Profile and Pharmacogenomics

Tacrolimus is a commonly prescribed immunosuppressant medication for prevention of organ transplant rejection. After organ transplantation, most of the patients are discharged and prescribed with tacrolimus medication due its high immunosuppressive efficacy. Although, tacrolimus is a go-to medication for the organ transplantation, it comes with numerous challenges such as narrow therapeutic index, high intra and interpatient variability in pharmacokinetics and the associated adverse effects. Therefore, it creates major difficulties for the clinicians by making the regular therapeutic drug monitoring and dose adjustment necessary. This review highlights various aspects including pharmacokinetics, food and drug interactions and genetics which are critical to understand the risk factors associated with tacrolimus and the measures required to overcome them. In particular, the information on human pharmacokinetics of tacrolimus would assist in further dose optimization with the defined pharmacokinetic-pharmacodynamic relationship.