Tacrolimus Prolonged Release (Envarsus®): A Review of Its Use in Kidney and Liver Transplant Recipients

Tacrolimus prolonged release (Envarsus (R); henceforth referred to as tacrolimus PR) is a new, once-daily, prolonged-release tacrolimus formulation, utilizing a drug delivery technology designed to enhance the bioavailability of drugs with low water solubility by creating a solid solution of the drug. This article reviews the pharmacological properties of tacrolimus PR and its clinical efficacy and tolerability in adult kidney and liver transplant recipients. In phase III trials, tacrolimus PR was noninferior to tacrolimus immediate release (IR; twice daily) in both de novo and stable, previously treated kidney transplant recipients, and had a similar tolerability profile. Preliminary efficacy data from phase II trials in de novo and stable, previously treated liver transplant recipients imply that tacrolimus PR is effective in these patient groups; however, more data would be of interest. Pharmacokinetic analyses demonstrated that tacrolimus PR is associated with a higher bioavailability, reduced peak-trough concentration fluctuation ratio, lower mean values for percentage degree of fluctuation and percentage degree of swing, and a longer time to maximum concentration than tacrolimus IR. Tacrolimus PR is a promising addition to the treatment options available for kidney and liver transplant recipients.