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Updated: Aug 6, 2026
08:38
Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
Published on: November 8, 2015
Extended-Release Tacrolimus Versus LifeCycle Pharma Tacrolimus in Kidney Transplant Recipients: A Switch Study
Nienke A Manson1, Emma H C van Schijndel1, Theodora S M Standaar1
1Department of Internal Medicine, Nephrology, Amsterdam University Medical Center, Amsterdam, the Netherlands.
Therapeutic Drug Monitoring
|July 20, 2026
Summary
Switching to LCP-tacrolimus (Envarsus) in kidney transplant patients requires a 30% lower dose than ER-tacrolimus (Advagraf) to maintain therapeutic levels. This switch showed similar safety and exposure, with improved monitoring in CYP3A5 expressors.
Area of Science:
- Nephrology
- Pharmacology
- Transplantation Medicine
Background:
- Tacrolimus is a vital immunosuppressant for kidney transplant recipients.
- Its narrow therapeutic index and variable absorption pose clinical challenges.
- Extended-release (ER-tacrolimus) and prolonged-release (LCP-tacrolimus) formulations aim to improve patient adherence and drug bioavailability.
Purpose of the Study:
- To evaluate the safety and efficacy of switching immunosuppression from ER-tacrolimus to LCP-tacrolimus in kidney transplant patients.
- To assess the required dose adjustment for LCP-tacrolimus to maintain therapeutic tacrolimus trough concentrations.
- To compare pharmacokinetics, adverse events, and patient preference between the two formulations.
Main Methods:
- An open-label, switch study design involving adult kidney transplant recipients.
- Patients were switched from ER-tacrolimus to LCP-tacrolimus, followed by a switch back to ER-tacrolimus.
- Primary endpoint: dose adjustment for therapeutic trough levels; secondary endpoints: safety, pill burden, patient preference, and pharmacokinetic parameters (C0, Cmax, AUC).
Main Results:
- A 30% lower dose of LCP-tacrolimus (6.0 mg) was needed to achieve therapeutic trough levels compared to ER-tacrolimus (8.5 mg).
- No significant differences were observed in pill burden, adverse effects, or overall drug exposure (AUC, Cmax).
- In CYP3A5 expressors, LCP-tacrolimus showed a stronger correlation between trough concentration (C0) and exposure (AUC), suggesting more reliable monitoring.
Conclusions:
- Switching to LCP-tacrolimus with a 30% dose reduction is effective in maintaining therapeutic tacrolimus levels in kidney transplant recipients.
- The conversion is associated with comparable safety, pill burden, and drug exposure profiles to ER-tacrolimus.
- LCP-tacrolimus may offer more reliable therapeutic drug monitoring, particularly in CYP3A5 expressors, though larger studies are needed.
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