Limited sampling strategy and population pharmacokinetic model of mycophenolic acid in pediatric patients with systemic lupus erythematosus: application of a double gamma absorption model with SAEM algorithm.

Introduction: Mycophenolic acid (MPA), the active metabolite of mycophenolate mofetil (MMF), is widely used in the treatment of systemic lupus erythematosus (SLE). It has been shown that its therapeutic drug monitoring based on the area under the curve (AUC) improves treatment efficacy. MPA exhibits...

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Published in:European Journal of Clinical Pharmacology Vol. 80; no. 1; pp. 83 - 93
Main Authors: Koloskoff, Kévin, Benito, Sylvain, Chambon, Lucie, Dayan, Frédéric, Marquet, Pierre, Jacqz-Aigrain, Evelyne, Woillard, Jean-Baptiste
Format: equations & formulas research tables/charts Journal Article
Published: Springer Nature Jan2024
Online Access:View this record in EBSCOhost
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      dt: Jan2024
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      pub: Springer Nature
      place: New York, New York
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        10.1007/s00228-023-03587-0
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        atl: Limited sampling strategy and population pharmacokinetic model of mycophenolic acid in pediatric patients with systemic lupus erythematosus: application of a double gamma absorption model with SAEM algorithm.
      aug:
        au:
          Koloskoff, Kévin
          Benito, Sylvain
          Chambon, Lucie
          Dayan, Frédéric
          Marquet, Pierre
          Jacqz-Aigrain, Evelyne
          Woillard, Jean-Baptiste
        affil: INSERM, University of Limoges, CHU Limoges, P&T, U1248, Limoges, France
      sug:
        subj:
          Lupus Erythematosus, Systemic Drug Therapy
          Mycophenolate Mofetil Pharmacokinetics
          Mycophenolic Acid Pharmacokinetics
          Absorption
          Sampling Methods
          Strategic Planning
          Models, Theoretical
          Algorithms
          Human
          Child
          Descriptive Statistics
          Program Implementation
          Comparative Studies
          Adolescence
          Mycophenolate Mofetil Administration and Dosage
          Dosage Calculation
          Population Characteristics
          Funding Source
          Child: 6-12 years
          Adolescent: 13-18 years
      ab: Introduction: Mycophenolic acid (MPA), the active metabolite of mycophenolate mofetil (MMF), is widely used in the treatment of systemic lupus erythematosus (SLE). It has been shown that its therapeutic drug monitoring based on the area under the curve (AUC) improves treatment efficacy. MPA exhibits a complex bimodal absorption, and a double gamma distribution model has been already proposed in the past to accurately describe this phenomenon. These previous population pharmacokinetics models (POPPK) have been developed using iterative two stage Bayesian (IT2B) or non-parametric adaptive grid (NPAG) methods. However, non-linear mixed effect (NLME) approaches based on stochastic approximation expectation–maximization (SAEM) algorithms have never been published so far for this particular model. The objectives of this study were (i) to implement the double absorption gamma model in Monolix, (ii) to compare different absorption models to describe the pharmacokinetics of MMF, and (iii) to develop a limited sampling strategy (LSS) to estimate AUC in pediatric SLE patients. Material and methods: A data splitting of full pharmacokinetic profiles sampled in 67 children extracted either from the expert system ISBA (n = 34) or the hospital Saint Louis (n = 33) was performed into train (75%) and test (25%) sets. A POPPK was developed for MPA in the train set using a NLME and the SAEM algorithm and different absorption models were implemented and compared (first order, transit, or simple and double gamma). The best limited sampling strategy was then determined in the test set using a maximum-a-posteriori Bayesian method to estimate individual PK parameters and AUC based on three blood samples compared to the reference AUC calculated using the trapezoidal rule applied on all samples and performances were assessed in the test set. Results: Mean patient age and dose was 13 years old (5–18) and 18.1 mg/kg (7.9–47.6), respectively. MPA concentrations (764) from 107 occasions were included in the analysis. A double gamma absorption with a first-order elimination from the central compartment best fitted the data. The optimal LSS with samples at 30 min, 2 h, and 3 h post-dose exhibited good performances in the test set (mean bias − 0.32% and RMSE 21.0%). Conclusion: The POPPK developed in this study adequately estimated the MPA AUC in pediatric patients with SLE based on three samples. The double absorption gamma model developed with the SAEM algorithm showed very accurate fit and reduced computation time.
      pubtype: Academic Journal
      doctype:
        equations & formulas
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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