Mycophenolic acid metabolite profile in renal transplant patients receiving enteric-coated mycophenolate sodium or mycophenolate mofetil

Mycophenolic acid metabolite profile in renal transplant patients receiving enteric-coated mycophenolate sodium or mycophenolate mofetil

Autor Tedesco-Silva, H. Google Scholar
Bastien, M. C. Google Scholar
Choi, L. Google Scholar
Felipe, C. Google Scholar
Campestrini, J. Google Scholar
Picard, F. Google Scholar
Schmouder, R. Google Scholar
Instituição Universidade Federal de São Paulo (UNIFESP)
Resumo Mycophenolate mofetil (MMF), a prodrug of mycophenolic acid (MPA), is an effective immunosuppressive treatment in renal transplant recipients but is known to have gastrointestinal side effects. Enteric-coated mycophenolate sodium (EC-MPS; myfortic) is a new formulation for delivering MPA. This open-label, two-period, cross-over study was carried out to characterize the time course of MPA and its metabolites, mycophenolic acid glucuronide (MPAG) and acyl mycophenolic acid glucuronide (AcMPAG) in stable renal transplant patients (n = 40) after 28-day chronic dosing with EC-MPS (720 mg bid) or MMF (1000 mg bid). the relative abundance and exposure of all three compounds was also assessed. EC-MPS demonstrated the typical pharmacokinetic profile of an enteric-coated formulation with a delayed release of MPA compared with MMF (T-max 2.5 versus 1.0 hours, respectively). Consistent with a similar disposition of MPA, both EC-MPS and MMF treatments resulted in the same ratio of MPAG to MPA exposure, 23:1. Furthermore, comparison of the AUC of MPAG and AcMPAG for both treatments indicated that steady state MPAG exposure was 75 to 90 times that of AcMPAG, confirming MPAG as the predominant metabolite of MPA. AcMPAG has been identified as a possible active metabolite of MPA; the present study indicates that AcMPAG may contribute around 14% of the exposure to active drug after administration of MPA. Both EC-MPS and MMF treatments were well tolerated over the 1-month period of chronic treatment. in summary, consistent with its enteric-coated design, EC-MPS delays delivery of MPA, but results in similar exposure to that provided by MMF.
Idioma Inglês
Data de publicação 2005-03-01
Publicado em Transplantation Proceedings. New York: Elsevier B.V., v. 37, n. 2, p. 852-855, 2005.
ISSN 0041-1345 (Sherpa/Romeo, fator de impacto)
Publicador Elsevier B.V.
Extensão 852-855
Fonte http://dx.doi.org/10.1016/j.transproceed.2004.12.186
Direito de acesso Acesso restrito
Tipo Artigo
Web of Science WOS:000228568900106
Endereço permanente http://repositorio.unifesp.br/handle/11600/28185

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