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Pharmacokinetics and Pharmacodynamics of Mycophenolic Acid After Enteric-Coated Mycophenolate Versus Mycophenolate Mofetil in Patients With Progressive IgA Nephritis

From the University Hospital Ulm, Division of Nephrology, Ulm, Germany (Dr Czock, Dr Rasche, Dr Carius, Dr Keller); Department of Nephrology (Dr Glander, Dr Budde) and Department of Clinical Pharmacology (Dr Bauer), Charite University Hospital, Berlin, Germany; and University of Saarland Hospital, Institute of Medical Microbiology and Hygiene, Homburg/Saar, Germany (Dr von Müller).

Mycophenolic acid can be administered orally using mycophenolate mofetil or enteric-coated mycophenolate. In renal transplant patients on immunosuppressant combination therapy, the overall mycophenolic acid exposure after oral dosing with mycophenolate mofetil and enteric-coated mycophenolate is similar. This study compared pharmacokinetics and pharmacodynamics of mycophenolic acid after equivalent doses of enteric-coated mycophenolate (360 mg twice daily) or mycophenolate mofetil (500 mg twice daily) in 7 patients with progressive IgA nephritis (glomerular filtration rate 20-35 mL/min) using a randomized crossover design. The pharmacokinetics of mycophenolic acid concentrations and pharmacodynamics (using inosine 5'-monophosphate dehydrogenase activity as a bio-marker) were sequentially monitored for 12 hours. After enteric-coated mycophenolate treatment, the mycophenolic acid peak concentration (C_max = 12.8 vs 6.0 µg/mL, P < .05) and the overall exposure were significantly higher (AUC = 60.9 vs 40.7 µg·h/mL, P < .05), and the apparent clearance was significantly lower (CL/F = 7.9 vs 10.7 L/h, P < .05) as compared to that after mycophenolate mofetil. Paradoxically, inosine 5'-monophosphate dehydrogenase activity was not significantly different. In conclusion, the steady-state mycophenolic acid exposure was higher during treatment with enteric-coated mycophenolate as compared to mycophenolate mofetil, which might be explained by more extensive enterohepatic recycling of mycophenolic acid after administration of enteric-coated mycophenolate, whereas inosine 5'-monophosphate dehydrogenase suppression was not different.

Key Words: Pharmacokinetics • pharmacodynamics • mycophenolate mofetil • enteric-coated mycophenolate • IgA nephropathy

Address for correspondence: Frieder Keller, University Hospital Ulm, Medical Department I, Division of Nephrology, Robert-Koch-Str. 8, 89070 Ulm, Germany; e-mail: frieder.keller{at}uni-ulm.de.

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