Abstract

Enteric-coated mycophenolate sodium is an advanced formulation delivering mycophenolic acid (MPA), designed to improve MPA-related upper gastrointestinal adverse events by delaying MPA release until the small intestine. Objective: Two studies were undertaken to identify the absolute bioavailability and dose-proportionality of enteric-coated mycophenolate sodium in stable renal transplant patients receiving cyclosporine. Methods: Study 1: The mean MPA AUC0–t was shown to be greater after MPA infusion than after oral enteric-coated mycophenolate sodium (42.1 vs. 28.9 µg × h/ml). Mean absolute bioavailability was 0.71 ± 0.21 (SD). Study 2: The AUC0–t and Cmax for MPA were proportional to the dose of enteric-coated mycophenolate sodium, similarly mean AUC0–¥ and Cmax for MPA glucuronide were proportional to dose administered. Results and conclusions: In patients receiving cyclosporine the absolute bioavailability of MPA provided by enteric-coated mycophenolate sodium is equivalent to that provided by mycophenolate mofetil when administered in combination with cyclosporine, and exhibits dose-proportionality. Enteric-coated mycophenolate sodium was well tolerated from 180 – 2,160 mg with no serious adverse events reported.

Author Details

Authors

• W. Arns¹
• M. Gies¹
• L. Choi²
• W. Zhu²
• P. Cooper²
• C.-M. Yeh²
• P. Prasad²
• P. Graf²
• R. Schmouder²

Departments

• ¹ Kliniken der Stadt Köln gGmbH, Clinic Merheim, Medical Clinic I, Cologne, Germany, and
• ² Novartis Pharma Corp., Basle, Switzerland

Address

Dr. W. Arns
Kliniken der Stadt Köln gGmbH
Clinic Merheim, Medical Clinic I
Ostmerheimer Straße 200
51109 Cologne, Germany
Email: [email protected]

Citation