Update on the Use of Tacrolimus in Pediatrics

Kristi Higgins, PharmD


Pediatr Pharm. 2018;24(12) 

In This Article

Abstract and Introduction


Tacrolimus is one of the most widely used immunosuppressive agents following solid organ transplantation. Tacrolimus is a macrolide isolated from the soil bacterium Streptomyces tsukubaensis.[1] It exerts its effect by binding to the receptor FK binding protein, inhibiting the phosphatase activity of calcineurin. This interferes with the transcription of cytokines required for the activation and proliferation of T lymphocytes.[2,3] Prograf ® (tacrolimus) was first approved for use by the Food and Drug Administration (FDA) in 1994 for prophylaxis of organ rejection in patients receiving allogenic liver transplants. This approval was expanded in 2006 to include heart transplant recipients, and later in 2009 to include kidney transplant recipients.

In 2013 an extended release formulation, Astagraf XL™, was FDA approved for the prophylaxis of organ rejection in adult kidney transplant patients when used in combination with other immunosuppressant medications. Later, in 2015, Envarsus XR® was approved by the FDA for prophylaxis of organ rejection in adult kidney transplant patients converted from tacrolimus immediate release formulation in combination with other immunosuppressants. Due to the variety of available dosage forms, emerging data on optimal dosing, and novel uses for tacrolimus, this issue provides an update for clinicians who care for patients treated with tacrolimus.