Prediction of pharmacokinetic drug-drug interactions using human hepatocyte suspension in plasma and cytochrome P450 phenotypic data. III. In vitro-in vivo correlation with fluconazole.

@article{Lu2008PredictionOP,
  title={Prediction of pharmacokinetic drug-drug interactions using human hepatocyte suspension in plasma and cytochrome P450 phenotypic data. III. In vitro-in vivo correlation with fluconazole.},
  author={Chuang Tai Lu and Cicely Berg and Shimoga R. Prakash and Frank W. H. Lee and Suresh K. Balani},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2008},
  volume={36 7},
  pages={
          1261-6
        }
}
Whereas ketoconazole is often used to study the worst-case scenario for clinical pharmacokinetic drug-drug interactions (DDIs) for drugs that are primarily metabolized by CYP3A4, fluconazole is considered to be a moderate inhibitor of CYP3A4, providing assessment of the moderate-case scenario of CYP3A-based DDIs. Fluconazole is also a moderate inhibitor of CYP2C9 and CYP2C19. For predicting clinical DDIs using conventional approaches, determining the in vivo inhibitor concentration at the… CONTINUE READING
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