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Updated: Aug 13, 2026

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
08:38

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS

Published on: November 8, 2015

Modified-release tacrolimus

Marie A Chisholm1, Matthew D Middleton

  • 1College of Pharmacy, University of Georgia, Augusta, GA 30912-2450, USA. Mchishol@mail.mcg.edu

The Annals of Pharmacotherapy
|February 2, 2006
PubMed
Abstract

Insights

Modified-release tacrolimus (MR-4) demonstrates pharmacokinetic, efficacy, and safety profiles comparable to standard tacrolimus. Once-daily MR-4 offers an advantage in preventing graft rejection, though further adherence studies are needed.

Area of Science:

  • Pharmacology and Transplantation Medicine
  • Immunosuppressive Therapy Research
  • Drug Formulation and Delivery Systems

Background:

  • Tacrolimus is a vital calcineurin inhibitor for preventing solid-organ graft rejection.
  • Current tacrolimus formulations require twice-daily dosing, potentially impacting patient adherence.
  • Modified-release formulations aim to improve dosing convenience and therapeutic outcomes.

Purpose of the Study:

  • To review and compare the pharmacokinetics, efficacy, and safety of modified-release tacrolimus (MR-4) against non-modified-release tacrolimus.
  • To assess the equivalence of MR-4 to standard tacrolimus in clinical trials.
  • To evaluate the potential benefits of MR-4's once-daily dosing regimen.

Main Methods:

  • Comprehensive literature search of PubMed/MEDLINE (1966-July 2005) using keywords: MR-4, tacrolimus, FK506, Prograf, transplantation, calcineurin inhibitors, immunosuppression.
  • Inclusion of English-language, published randomized clinical trials evaluating MR-4 and tacrolimus for graft rejection prevention.
  • Data extraction from identified publications, meeting abstracts, and manufacturer information.

Main Results:

  • MR-4 exhibits similar pharmacokinetic profiles to standard tacrolimus in healthy volunteers and transplant recipients (renal, liver).
  • Comparable efficacy and safety profiles were observed between MR-4 and standard tacrolimus.
  • A 1:1 conversion from twice-daily tacrolimus to once-daily MR-4 is considered safe, with similar target whole blood trough concentrations.

Conclusions:

  • Short-term clinical trials suggest MR-4 possesses similar efficacy and safety to tacrolimus.
  • The once-daily administration of MR-4 presents a dosing advantage for preventing graft rejection compared to existing calcineurin inhibitors.
  • Further adherence studies are required to evaluate the clinical and economic outcomes associated with MR-4.

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