Allometric scaling of pharmacokinetic parameters in drug discovery: Can human CL, Vss and t1/2 be predicted fromin-vivo rat data?

@article{Caldwell2004AllometricSO,
  title={Allometric scaling of pharmacokinetic parameters in drug discovery: Can human CL, Vss and t1/2 be predicted fromin-vivo rat data?},
  author={Gary W. Caldwell and John A. Masucci and Zhengyin Yan and William E Hageman},
  journal={European Journal of Drug Metabolism and Pharmacokinetics},
  year={2004},
  volume={29},
  pages={133-143}
}
In a drug discovery environment, reasonable go/no-go humanin-vivo pharmacokinetic (PK) decisions must be made in a timely manner with a minimum amount of animalin-vivo orin-vitro data. We have investigated the accuracy of thein-vivo correlation between rat and human for the prediction of the total systemic clearance (CL), the volume of distribution at steady state (Vss), and the half-life (t1/2) using simple allometric scaling techniques. We have shown, using a large diverse set of drugs, that… CONTINUE READING

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