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Physiologically based pharmacokinetics (PBPK)

Pascal Espié, Dominique Tytgat, Maria-Laura Sargentini-Maier, Italo Poggesi and Jean-Baptiste Watelet UGent (2009) DRUG METABOLISM REVIEWS. 41(3). p.391-407
abstract
Allometric scaling is widely used to predict human pharmacokinetic parameters from preclinical species, and many different approaches have been proposed over the years to improve its predictive performance. Nevertheless, prediction errors are commonly observed in the practical application of simple allometry, for example, in cases where the hepatic metabolic clearance is mainly determined by enzyme activities, which do not scale allometrically across species. Therefore, if good correlation was noted for some drugs, poor correlation was observed for others, highlighting the need for other conceptual approaches. Physiologically based pharmacokinetic (PBPK) models are now a well-established approach to conduct extrapolations across species and to generate simulations of pharmacokinetic profiles under various physiological conditions. While conventional pharmacokinetic models are defined by drug-related data themselves, PBPK models have richer information content and integrate information from various sources, including drug-dependent, physiological, and biological parameters as they vary in between species, subjects, or with age and disease state. Therefore, the biological and mechanistic bases of PBPK models allow the extrapolation of the kinetic behavior of drugs with regard to dose, route, and species. In addition, by providing a link between tissue concentrations and toxicological or pharmacological effects, PBPK modeling represents a framework for mechanistic pharmacokinetic-pharmacodynamic models.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (review)
publication status
published
subject
keyword
Physiologically based pharmacokinetic, interspecies extrapolation, physiology, discovery, development, population, IN-VITRO DATA, PLASMA PARTITION-COEFFICIENTS, HEPATIC METABOLIC-CLEARANCE, VIVO DRUG CLEARANCE, QUANTITATIVE PREDICTION, TISSUE DISTRIBUTION, INTESTINAL-ABSORPTION, CANDIDATE SELECTION, XENOBIOTIC LEVELS, RISK-ASSESSMENT, allometry, human prediction, pharmacokinetic/pharmacodynamic
journal title
DRUG METABOLISM REVIEWS
Drug Metab. Rev.
volume
41
issue
3
pages
391 - 407
Web of Science type
Review
Web of Science id
000269410900005
JCR category
PHARMACOLOGY & PHARMACY
JCR impact factor
5.439 (2009)
JCR rank
15/236 (2009)
JCR quartile
1 (2009)
ISSN
0360-2532
DOI
10.1080/10837450902891360
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
4324902
handle
http://hdl.handle.net/1854/LU-4324902
date created
2014-03-07 09:35:51
date last changed
2016-12-19 15:43:43
@article{4324902,
  abstract     = {Allometric scaling is widely used to predict human pharmacokinetic parameters from preclinical species, and many different approaches have been proposed over the years to improve its predictive performance. Nevertheless, prediction errors are commonly observed in the practical application of simple allometry, for example, in cases where the hepatic metabolic clearance is mainly determined by enzyme activities, which do not scale allometrically across species. Therefore, if good correlation was noted for some drugs, poor correlation was observed for others, highlighting the need for other conceptual approaches. Physiologically based pharmacokinetic (PBPK) models are now a well-established approach to conduct extrapolations across species and to generate simulations of pharmacokinetic profiles under various physiological conditions. While conventional pharmacokinetic models are defined by drug-related data themselves, PBPK models have richer information content and integrate information from various sources, including drug-dependent, physiological, and biological parameters as they vary in between species, subjects, or with age and disease state. Therefore, the biological and mechanistic bases of PBPK models allow the extrapolation of the kinetic behavior of drugs with regard to dose, route, and species. In addition, by providing a link between tissue concentrations and toxicological or pharmacological effects, PBPK modeling represents a framework for mechanistic pharmacokinetic-pharmacodynamic models.},
  author       = {Espi{\'e}, Pascal and Tytgat, Dominique and Sargentini-Maier, Maria-Laura and Poggesi, Italo and Watelet, Jean-Baptiste},
  issn         = {0360-2532},
  journal      = {DRUG METABOLISM REVIEWS},
  keyword      = {Physiologically based pharmacokinetic,interspecies extrapolation,physiology,discovery,development,population,IN-VITRO DATA,PLASMA PARTITION-COEFFICIENTS,HEPATIC METABOLIC-CLEARANCE,VIVO DRUG CLEARANCE,QUANTITATIVE PREDICTION,TISSUE DISTRIBUTION,INTESTINAL-ABSORPTION,CANDIDATE SELECTION,XENOBIOTIC LEVELS,RISK-ASSESSMENT,allometry,human prediction,pharmacokinetic/pharmacodynamic},
  language     = {eng},
  number       = {3},
  pages        = {391--407},
  title        = {Physiologically based pharmacokinetics (PBPK)},
  url          = {http://dx.doi.org/10.1080/10837450902891360},
  volume       = {41},
  year         = {2009},
}

Chicago
Espié, Pascal, Dominique Tytgat, Maria-Laura Sargentini-Maier, Italo Poggesi, and Jean-Baptiste Watelet. 2009. “Physiologically Based Pharmacokinetics (PBPK).” Drug Metabolism Reviews 41 (3): 391–407.
APA
Espié, P., Tytgat, D., Sargentini-Maier, M.-L., Poggesi, I., & Watelet, J.-B. (2009). Physiologically based pharmacokinetics (PBPK). DRUG METABOLISM REVIEWS, 41(3), 391–407.
Vancouver
1.
Espié P, Tytgat D, Sargentini-Maier M-L, Poggesi I, Watelet J-B. Physiologically based pharmacokinetics (PBPK). DRUG METABOLISM REVIEWS. 2009;41(3):391–407.
MLA
Espié, Pascal, Dominique Tytgat, Maria-Laura Sargentini-Maier, et al. “Physiologically Based Pharmacokinetics (PBPK).” DRUG METABOLISM REVIEWS 41.3 (2009): 391–407. Print.