Class-specific relative genetic contribution for key antiretroviral drugs.

Objectives: Antiretroviral pharmacokinetics is defined by numerous factors affecting absorption, distribution, metabolism and elimination. Biological processes underpinning drug distribution are only partially characterized and multiple genetic factors generate cumulative or antagonistic interaction...

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Publicado en:Journal of Antimicrobial Chemotherapy (JAC) Vol. 70; no. 11; pp. 3074 - 3080
Autores principales: Siccardi, Marco, Olagunju, Adeniyi, Simiele, Marco, D'Avolio, Antonio, Calcagno, Andrea, Di Perri, Giovanni, Bonora, Stefano, Owen, Andrew
Formato: research Journal Article
Publicado: Oxford University Press / USA Nov2015
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Nov2015
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      pub: Oxford University Press / USA
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        atl: Class-specific relative genetic contribution for key antiretroviral drugs.
      aug:
        au:
          Siccardi, Marco
          Olagunju, Adeniyi
          Simiele, Marco
          D'Avolio, Antonio
          Calcagno, Andrea
          Di Perri, Giovanni
          Bonora, Stefano
          Owen, Andrew
        affil: Molecular and Clinical Pharmacology, Institute of Translational Medicine, University of Liverpool, Liverpool, UK
      sug:
        subj:
          Plasma
          Anti-Retroviral Agents Pharmacokinetics
          Pharmacogenetics Methods
          Aged, 80 and Over
          Female
          Anti-Retroviral Agents Administration and Dosage
          Middle Age
          Young Adult
          Retrospective Design
          Male
          Adult
          Aged
          Funding Source
          Human
          Aged, 80 & over
          Middle Aged: 45-64 years
          Adult: 19-44 years
          Aged: 65+ years
          Female
          Male
      ab: Objectives: Antiretroviral pharmacokinetics is defined by numerous factors affecting absorption, distribution, metabolism and elimination. Biological processes underpinning drug distribution are only partially characterized and multiple genetic factors generate cumulative or antagonistic interactions, which complicates the implementation of pharmacogenetic markers. The aim of this study was to assess the degree to which heredity influences pharmacokinetics through the quantification of the relative genetic contribution (rGC) for key antiretrovirals.Methods: A total of 407 patients receiving lopinavir/ritonavir, atazanavir/ritonavir, atazanavir, efavirenz, nevirapine, etravirine, maraviroc, tenofovir or raltegravir were included. Intra-patient variability (SDw) and inter-patient (SDb) variability were measured in patients with plasma concentrations available from more than two visits. The rGC was calculated using the following equation: 1 - (1 / F) where F = SDb(2) / SDw(2).Results: Mean (95% CI) rGC was calculated to be 0.81 (0.72-0.88) for efavirenz, 0.74 (0.61-0.84) for nevirapine, 0.67 (0.49-0.78) for etravirine, 0.65 (0.41-0.79) for tenofovir, 0.59 (0.38-0.74) for atazanavir, 0.47 (0.27-0.60) for atazanavir/ritonavir, 0.36 (0.01-0.48) for maraviroc, 0.15 (0.01-0.44) for lopinavir/ritonavir and 0 (0-0.33) for raltegravir.Conclusions: The rank order for genetic contribution to variability in plasma concentrations for the study drugs was efavirenz > nevirapine > etravirine > tenofovir > atazanavir > atazanavir/ritonavir > maraviroc > lopinavir/ritonavir > raltegravir, indicating that class-specific differences exist. The rGC strategy represents a useful tool to rationalize future investigations as drugs with higher rGC scores may represent better candidates for pharmacogenetic-pharmacokinetic studies.
      pubtype: Academic Journal
      doctype:
        research
        Journal Article
      ougenre: Article
    language: English
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