Related Experiment Video
Updated: Mar 20, 2026

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
Published on: November 8, 2015
Pharmacokinetics of prolonged-release tacrolimus and implications for use in solid organ transplant recipients
Maria G Tanzi1, Nasrullah Undre2, James Keirns1
1Astellas Pharma Global Development, Northbrook, IL, USA.
Abstract:
Prolonged-release tacrolimus was developed as a once-daily formulation with ethylcellulose as the excipient, resulting in slower release and reduction in peak concentration (Cmax ) for a given dose compared with immediate-release tacrolimus, which is administered twice daily. This manuscript reviews pharmacokinetic information on prolonged-release tacrolimus in healthy subjects, in transplant recipients converted from immediate-release tacrolimus, and in de novo kidney and liver transplant recipients. As with the immediate-release formulation, prolonged-release tacrolimus shows a strong correlation between trough concentration (Cmin ) and area under the 24-hour time-concentration curve (AUC24 ), indicating that trough whole blood concentrations provide an accurate measure of drug exposure. We present the pharmacokinetic similarities and differences between the two formulations, so that prescribing physicians will have a better understanding of therapeutic drug monitoring in patients receiving prolonged-release tacrolimus.
More Related Videos
Related Concept Videos
Drug Accumulation During Multiple Dosing: Intermittent IV Infusions
Kidney Transplant II: Surgical Procedure
Pharmacokinetic–Pharmacodynamic Relationship: Influence of Elimination Half-Life on Effect Duration
Pharmacokinetics in Pediatric Patients: Drug Excretion
Pharmacokinetic–Pharmacodynamic Relationship: Duration of Dose-Effect Relationship
Kidney Transplant I: Introduction

