Population pharmacokinetics of mycophenolic acid in adult kidney transplant patients under prednisone and tacrolimus regimen
Article
-
- Overview
-
- Research
-
- Identity
-
- Additional Document Info
-
- View All
-
Overview
abstract
-
Mycophenolate mofetil (MMF) is typically used in combination with prednisone and tacrolimus to avoid graft rejection in kidney transplant patients. The aim of this study was to develop and validate a population pharmacokinetic model of mycophenolic acid (MPA) in kidney transplant patients to investigate the influence of clinical and genetic covariates and to propose a dosage regimen based on the final model. Adult kidney transplant patients (>18 years old) receiving combination of MMF, prednisone and tacrolimus regimen were included. The population pharmacokinetic model was built using a two-compartment model and First Order Conditional Estimation method with Interaction (FOCEI though NONMEM v.7.4.). A total of 343 MPA concentrations at steady state from 77 kidney transplant patients were included in the analysis. MPA CL/F, V1/F, Q/F, V2/F, and Ka were 12.4 L/h, 45.6 L, 29.9 L/h, 658 L, and 1.67 h−1, respectively. It was found that CL/F increases with serum creatinine and uric acid levels and V1/F is modified by blood urea nitrogen and the UGT1A9 genotype. In the final model the interindividual variabilities associated to CL/F and V1/F were 56.5%25 and 105.8%25, respectively. The residual variability was 41.8%25. Evaluation by bootstrapping showed that the final model was stable. The predictive performance was evaluated by goodness-of-fit plots and visual predictive check. Dosage regimens for MMF were proposed based on the final model and would be appropriate for a prospective evaluation. In conclusion, it was building a population pharmacokinetic model for MPA in kidney transplant patients, which include clinical and genetic covariates. © 2020 Elsevier B.V.
publication date
funding provided via
published in
Research
keywords
-
Kidney transplant; Mycophenolate acid; Mycophenolate mofetil; Population pharmacokinetics creatinine; genomic DNA; glucuronosyltransferase 1A9; mycophenolate mofetil; mycophenolic acid; prednisone; prescription drug; tacrolimus; uric acid; absorption rate constant; adult; aged; area under the curve; Article; bootstrapping; central volume of distribution; compartment model; concentration at steady-state; creatinine blood level; drug clearance; drug dose regimen; evaluation study; female; genetic association; genotype; graft recipient; human; immunosuppressive treatment; intercompartmental clearance; kidney graft rejection; kidney transplantation; major clinical study; male; observational study; oral clearance; peripheral volume of distribution; pharmacogenetics; pharmacokinetic parameters; predictive value; prescription; priority journal; prospective study; single nucleotide polymorphism; trough concentration; urea nitrogen blood level; uric acid blood level; validation study
Identity
Digital Object Identifier (DOI)
PubMed ID
Additional Document Info
start page
end page
volume