Enteric-coated mycophenolate sodium provides higher mycophenolic acid predose levels compared with mycophenolate mofetil: implications for therapeutic drug monitoring. 2007

Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
Department of Nephrology, University Hospital Charité, Berlin, Germany. klemens.budde@charite.de

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.

UI MeSH Term Description Entries
D007166 Immunosuppressive Agents Agents that suppress immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-CELLS or by inhibiting the activation of HELPER CELLS. While immunosuppression has been brought about in the past primarily to prevent rejection of transplanted organs, new applications involving mediation of the effects of INTERLEUKINS and other CYTOKINES are emerging. Immunosuppressant,Immunosuppressive Agent,Immunosuppressants,Agent, Immunosuppressive,Agents, Immunosuppressive
D009173 Mycophenolic Acid Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION. Cellcept,Mycophenolate Mofetil,Mycophenolate Mofetil Hydrochloride,Mycophenolate Sodium,Mycophenolic Acid Morpholinoethyl Ester,Myfortic,RS 61443,RS-61443,Sodium Mycophenolate,Mofetil Hydrochloride, Mycophenolate,Mofetil, Mycophenolate,Mycophenolate, Sodium,RS61443
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000903 Antibiotics, Antineoplastic Chemical substances, produced by microorganisms, inhibiting or preventing the proliferation of neoplasms. Antineoplastic Antibiotics,Cytotoxic Antibiotics,Antibiotics, Cytotoxic
D013608 Tablets, Enteric-Coated Tablets coated with material that delays release of the medication until after they leave the stomach. (Dorland, 28th ed) Enteric-Coated Tablets,Tablets, Enteric Coated
D016032 Randomized Controlled Trials as Topic Works about clinical trials that involve at least one test treatment and one control treatment, concurrent enrollment and follow-up of the test- and control-treated groups, and in which the treatments to be administered are selected by a random process, such as the use of a random-numbers table. Clinical Trials, Randomized,Controlled Clinical Trials, Randomized,Trials, Randomized Clinical
D016903 Drug Monitoring The process of observing, recording, or detecting the effects of a chemical substance administered to an individual therapeutically or diagnostically. Monitoring, Drug,Therapeutic Drug Monitoring,Drug Monitoring, Therapeutic,Monitoring, Therapeutic Drug
D019540 Area Under Curve A statistical means of summarizing information from a series of measurements on one individual. It is frequently used in clinical pharmacology where the AUC from serum levels can be interpreted as the total uptake of whatever has been administered. As a plot of the concentration of a drug against time, after a single dose of medicine, producing a standard shape curve, it is a means of comparing the bioavailability of the same drug made by different companies. (From Winslade, Dictionary of Clinical Research, 1992) AUC,Area Under Curves,Curve, Area Under,Curves, Area Under,Under Curve, Area,Under Curves, Area

Related Publications

Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
January 2005, Drugs,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
April 2010, Expert opinion on pharmacotherapy,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
January 2007, Clinical transplantation,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
April 2005, Clinical transplantation,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
March 2005, Transplantation proceedings,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
March 2011, Clinical journal of the American Society of Nephrology : CJASN,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
September 2007, Transplantation proceedings,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
May 2008, Transplantation proceedings,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
October 2006, Transplantation proceedings,
Klemens Budde, and Helio Tedesco-Silva, and Jose Medina Pestana, and Petra Glander, and Hans-H Neumayer, and Claudia Rosso Felipe, and Paula Pinheiro Machado, and Romain Sechaud, and Robert Schmouder
December 2002, Transplantation proceedings,
Copied contents to your clipboard!