title: Enteric-coated mycophenolate sodium provides higher mycophenolic acid predose levels compared with mycophenolate mofetil: implications for therapeutic drug monitoring.
abstract: The delayed release of mycophenolic acid (MPA) from enteric-coated mycophenolate sodium (EC-MPS) may lead to different MPA predose (C0) levels compared with mycophenolate mofetil (MMF). A post hoc analysis was performed on MPA morning predose values assessed in 88 maintenance renal transplant patients from three studies converted from MMF (1000 mg twice a day) to equimolar EC-MPS (720 mg twice a day) or vice versa, both in combination with cyclosporine. The median MPA predose level was approximately 30% higher when patients received EC-MPS (2.40 microg/mL; range, 0.49-39.30 microg/mL) compared with MMF (1.83 microg/mL; range, <0.1-12.80 microg/mL). Rare cases (3.0%) of high MPA C0 levels 15 microg/mL or greater were observed with EC-MPS consistent with a very prolonged release of MPA from this formulation. Both EC-MPS and MMF exhibited a poor correlation between MPA C0 levels and exposure as assessed by MPA area under the curve. Physicians targeting a certain MPA predose level have to be aware of the higher morning C0 levels with EC-MPS, whereas the overall MPA exposure is not different to MMF.
authors.affiliation: Department of Nephrology, University Hospital Charité, Berlin, Germany. klemens.budde@charite.de
authors.forename: Klemens
authors.initials: K
authors.lastname: Budde
authors.forename: Helio
authors.initials: H
authors.lastname: Tedesco-Silva
authors.forename: Jose Medina
authors.initials: JM
authors.lastname: Pestana
authors.forename: Petra
authors.initials: P
authors.lastname: Glander
authors.forename: Hans-H
authors.initials: HH
authors.lastname: Neumayer
authors.forename: Claudia Rosso
authors.initials: CR
authors.lastname: Felipe
authors.forename: Paula Pinheiro
authors.initials: PP
authors.lastname: Machado
authors.forename: Romain
authors.initials: R
authors.lastname: Sechaud
authors.forename: Robert
authors.initials: R
authors.lastname: Schmouder
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000493:pharmacokinetics*; D019540:Area Under Curve; D003692:Delayed-Action Preparations / Q000493:pharmacokinetics; D016903:Drug Monitoring / Q000379:methods*; D006801:Humans; D007166:Immunosuppressive Agents / Q000493:pharmacokinetics*; D009173:Mycophenolic Acid / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D016032:Randomized Controlled Trials as Topic; D013608:Tablets, Enteric-Coated
chemical_list: D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D007166:Immunosuppressive Agents; D013608:Tablets, Enteric-Coated; D009173:Mycophenolic Acid