Pharmacokinetic and metabolic investigations of mycophenolic acid in pediatric patients after renal transplantation: implications for therapeutic drug monitoring

The need for mycophenolic acid (MPA) monitoring is still under discussion. Key issues for the PK/PD relationships of this drug are: the role of metabolites, the usefulness of AUC versus predose levels, and the need to monitor the free concentration of MPA (f-MPA). Recent advances have revealed that,...

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Main Authors: Oellerich, Michael (Author) , Shipkova, Maria (Author) , Schütz, Ekkehard (Author) , Wieland, Eberhard (Author) , Weber, Lutz T. (Author) , Tönshoff, Burkhard (Author) , Armstrong, Victor W. (Author)
Format: Article (Journal)
Language:English
Published: February 2000
In: Therapeutic drug monitoring
Year: 2000, Volume: 22, Issue: 1, Pages: 20-26
ISSN:1536-3694
Online Access:Verlag, lizenzpflichtig, Volltext: https://journals.lww.com/drug-monitoring/Fulltext/2000/02000/Pharmacokinetic_and_Metabolic_Investigations_of.4.aspx
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Author Notes:Michael Oellerich, Maria Shipkova, Ekkehard Schütz, Eberhard Wieland, Lute Weber, Burkhard Tönshoff, Victor W. Armstrong

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520 |a The need for mycophenolic acid (MPA) monitoring is still under discussion. Key issues for the PK/PD relationships of this drug are: the role of metabolites, the usefulness of AUC versus predose levels, and the need to monitor the free concentration of MPA (f-MPA). Recent advances have revealed that, in addition to 7-O-MPAG, three additional MPA metabolites are present in the plasma of transplant recipients. One of these metabolites (M-2), identified as an acyl glucuronide of MPA, was found to inhibit IMPDH-II in vitro. This active metabolite was also found to cross-react in the Emit assay for MPA. In an ongoing multicenter study, the authors are evaluating the relevance of monitoring total (t-MPA) and free mycophenolic acid (f-MPA) in pediatric renal transplant recipients. 
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