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Open AccessReview

Interpretation of Non-Clinical Data for Prediction of Human Pharmacokinetic Parameters: In Vitro-In Vivo Extrapolation and Allometric Scaling

1
College of Pharmacy, CHA University, 335 Pangyo-ro, Bundang-gu, Seongnam-si, Gyeonggi-do 13488, Korea
2
College of Pharmacy, Chonnam National University, 77 Yongbong-ro, Buk-Gu, Gwangju 61186, Korea
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(4), 168; https://doi.org/10.3390/pharmaceutics11040168
Received: 31 January 2019 / Revised: 22 March 2019 / Accepted: 2 April 2019 / Published: 5 April 2019
Extrapolation of pharmacokinetic (PK) parameters from in vitro or in vivo animal to human is one of the main tasks in the drug development process. Translational approaches provide evidence for go or no-go decision-making during drug discovery and the development process, and the prediction of human PKs prior to the first-in-human clinical trials. In vitro-in vivo extrapolation and allometric scaling are the choice of method for projection to human situations. Although these methods are useful tools for the estimation of PK parameters, it is a challenge to apply these methods since underlying biochemical, mathematical, physiological, and background knowledge of PKs are required. In addition, it is difficult to select an appropriate methodology depending on the data available. Therefore, this review covers the principles of PK parameters pertaining to the clearance, volume of distribution, elimination half-life, absorption rate constant, and prediction method from the original idea to recently developed models in order to introduce optimal models for the prediction of PK parameters. View Full-Text
Keywords: pharmacokinetics; in vitro-in vivo extrapolation; allometric scaling; animal scale-up; translational approach; non-clinical study pharmacokinetics; in vitro-in vivo extrapolation; allometric scaling; animal scale-up; translational approach; non-clinical study
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MDPI and ACS Style

Choi, G.-W.; Lee, Y.-B.; Cho, H.-Y. Interpretation of Non-Clinical Data for Prediction of Human Pharmacokinetic Parameters: In Vitro-In Vivo Extrapolation and Allometric Scaling. Pharmaceutics 2019, 11, 168.

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