Extended-release tacrolimus tablets for preventing organ transplant rejection

Timothy A. Horwedel, Daniel C. Brennan

Research output: Contribution to journalArticlepeer-review


Introduction: Tacrolimus has been used for prophylaxis of organ rejection since 1994, and has become a mainstay of immunosuppressive therapy. Tacrolimus XR tablets were released in the U.S. in 2015 and offer greater bioavailability and less variability in daily exposure as compared to other available tacrolimus formulations. These pharmacokinetic differences may offer transplant recipients several unique advantages, including potential for more predictable immunosuppression. Areas covered: Tacrolimus XR is discussed in the kidney transplant population, as these present the largest population in which it has been studied and demonstrates the key differences compared to other formulations. Several key studies are analyzed to determine key patients that will benefit from these more predictable kinetics. Additionally, tacrolimus XR may offer benefit for patients experiencing neurotoxicity. Here we review the potential mechanisms for this adverse effect, as well as available literature regarding management of neurotoxicity with tacrolimus XR. Expertopinion: Tacrolimus XR offers a significant advantage to transplant recipients due to its increased bioavailability and slower absorption, which leads to less concentration variability over a dosing interval. Several key populations, including black patients, older patients, non-adherent patients, and those with tremor may see benefits. Further research is necessary to better understand the role that Tacrolimus XR will fill in transplantation.

Original languageEnglish (US)
Pages (from-to)1079-1086
Number of pages8
JournalExpert Opinion on Orphan Drugs
Issue number10
StatePublished - Oct 2 2016
Externally publishedYes


  • Tacrolimus
  • immunosuppression
  • pharmacogenomics
  • pharmacokinetics
  • transplantation

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
  • Health Policy
  • Pharmacology (medical)


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