Population pharmacokinetics and Bayesian estimation of tacrolimus exposure in Chinese liver transplant patients.

What is known and objectives Tacrolimus ( TAC) is widely used as part of immunosuppressive regimens. There is great interindividual variation on the disposition of TAC. The aim of this study was to develop a population pharmacokinetic ( PPK) model for Chinese liver transplant patients and evaluate g...

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Publicado en:Journal of Clinical Pharmacy & Therapeutics Vol. 42; no. 6; pp. 679 - 689
Autores principales: Chen, B., Shi, H.‐Q., Liu, X.‐X., Zhang, W.‐X., Lu, J.‐Q., Xu, B.‐M., Chen, H.
Formato: research tables/charts Journal Article
Publicado: Wiley-Blackwell Dec2017
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Dec2017
      vid: 42
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      pub: Wiley-Blackwell
      place: Malden, Massachusetts
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        10.1111/jcpt.12599
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        atl: Population pharmacokinetics and Bayesian estimation of tacrolimus exposure in Chinese liver transplant patients.
      aug:
        au:
          Chen, B.
          Shi, H.‐Q.
          Liu, X.‐X.
          Zhang, W.‐X.
          Lu, J.‐Q.
          Xu, B.‐M.
          Chen, H.
        affil: Department of Pharmacy, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai China
      sug:
        subj:
          Tacrolimus Pharmacokinetics
          Transplant Recipients
          Liver Transplantation China
          China
          Human
          Male
          Female
          Genotype
          Polymorphism, Genetic
          Male
          Female
      ab: What is known and objectives Tacrolimus ( TAC) is widely used as part of immunosuppressive regimens. There is great interindividual variation on the disposition of TAC. The aim of this study was to develop a population pharmacokinetic ( PPK) model for Chinese liver transplant patients and evaluate genetic polymorphism and other possible factors on the PK parameters. The exposure of TAC is to be estimated through Bayesian modelling. Methods A total of 47 sets of rich-time PK and 1234 conventional therapeutic drug monitoring ( TDM) data were collected from 125 Chinese liver transplant patients. The pathophysiological data of these patients were recorded. CYP3A5*3 and ABCB1 genotypes were determined for each patient. The PPK model for TAC was established by nonlinear mixed-effects modelling ( nonmem). The impact of pathophysiology and genotype on PPK parameters was evaluated. Bayesian estimators for the area under concentration-time curve ( AUC) of TAC were validated. Results A two-compartment model with lag time was found to be the most suitable model for the pooled full PK and TDM data for Chinese liver transplant patients. The CL/F, V2/F, Q/F, V3/F, Ka and lag time were 17.4±0.81 L/h, 165±44.1 L, 54.9±25.8L/h, 594±87.5 L, 0.51±0.095 L/h and 1.57±0.34 h. Post-operative day ( POD), creatinine clearance ( CLcr) and ABCB1 C3435T genotypes were found to have significant influences on CL/F ( P<.01). ABCB1 C3435T genotypes showed a significant correlation with V2/F ( P<.01). C0-C2 and C0-C2-C4 were shown to be suitable for the estimation of AUC in Chinese liver transplant patients. What is new and conclusion A PPK model for TAC was established successfully in Chinese liver transplant patients. POD, CLcr and ABCB1 C3435T genotypes were shown to have significant effects on CL/F. The AUC of TAC in Chinese liver transplant patients could be estimated through Bayesian modelling, based on which individualized immunosuppressive regimens can be designed.
      pubtype: Academic Journal
      doctype:
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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