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Pharmacokinetics of enteric-coated mycophenolate sodium in stable liver transplant recipients

Theodore W Perry1, Uwe Christians, James F Trotter

  • 1Division of Gastroenterology/Hepatology, Department of Anesthesiology, University of Colorado Health Sciences Center, Denver, CO 80262, USA.

Clinical Transplantation
|May 10, 2007
PubMed
Abstract

Insights

Enteric-coated mycophenolate sodium (EC-MPS) shows significant pharmacokinetic variability in liver transplant recipients. This wide variation suggests that therapeutic drug monitoring for EC-MPS may not be consistently useful in this patient population.

Area of Science:

  • Pharmacology
  • Transplantation Medicine
  • Drug Metabolism

Background:

  • Mycophenolate mofetil (MMF) is a key immunosuppressant post-liver transplant.
  • Enteric-coated mycophenolate sodium (EC-MPS) was developed to reduce MMF's gastrointestinal side effects.
  • Understanding EC-MPS pharmacokinetics is crucial for optimizing immunosuppression.

Purpose of the Study:

  • To characterize the pharmacokinetic profile of EC-MPS in stable liver transplant recipients.
  • To assess the variability of key pharmacokinetic parameters after a single EC-MPS dose.
  • To evaluate the potential utility of therapeutic drug monitoring for EC-MPS.

Main Methods:

  • A single 720 mg dose of EC-MPS was administered to stable liver transplant recipients (>1 year post-transplant).
  • Blood levels of mycophenolic acid (MPA) were measured at frequent intervals.
  • A validated LC-MS/MS assay was used for MPA quantification.

Main Results:

  • Pharmacokinetic parameters including half-life, time to maximum concentration (tmax), and area under the curve (AUC) exhibited substantial inter-individual variability.
  • Trough concentrations (C12h) showed a wide range (0-9.2 microg/mL).
  • No significant differences in pharmacokinetics were observed based on gender, hepatitis C status, or concomitant immunosuppressants (tacrolimus vs. cyclosporine).

Conclusions:

  • Stable liver transplant recipients demonstrate significant inter-individual variability in EC-MPS pharmacokinetics.
  • The wide variability in pharmacokinetic parameters suggests limited utility for routine therapeutic drug monitoring of EC-MPS.
  • Further research may be needed to refine dosing strategies or identify patient subgroups benefiting from monitoring.

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