Physiologically-based pharmacokinetics in drug development and regulatory science
M Rowland, C Peck, G Tucker - Annual review of pharmacology …, 2011 - annualreviews.org
The application of physiologically-based pharmacokinetic (PBPK) modeling is coming of
age in drug development and regulation, reflecting significant advances over the past 10 …
age in drug development and regulation, reflecting significant advances over the past 10 …
In vivo methods for drug absorption–comparative physiologies, model selection, correlations with in vitro methods (IVIVC), and applications for formulation/API …
E Sjögren, B Abrahamsson, P Augustijns… - European Journal of …, 2014 - Elsevier
This review summarizes the current knowledge on anatomy and physiology of the human
gastrointestinal tract in comparison with that of common laboratory animals (dog, pig, rat and …
gastrointestinal tract in comparison with that of common laboratory animals (dog, pig, rat and …
Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data
Intestinal first-pass metabolism may contribute to low oral drug bioavailability and drug-drug
interactions, particularly for CYP3A substrates. The current analysis predicted intestinal …
interactions, particularly for CYP3A substrates. The current analysis predicted intestinal …
Applications of human pharmacokinetic prediction in first-in-human dose estimation
Quantitative estimations of first-in-human (FIH) doses are critical for phase I clinical trials in
drug development. Human pharmacokinetic (PK) prediction methods have been developed …
drug development. Human pharmacokinetic (PK) prediction methods have been developed …
Absolute abundance and function of intestinal drug transporters: a prerequisite for fully mechanistic in vitro–in vivo extrapolation of oral drug absorption
MD Harwood, S Neuhoff, GL Carlson… - … & drug disposition, 2013 - Wiley Online Library
The use of whole body physiological‐based pharmacokinetic (PBPK) models linked with in
vitro‐in vivo extrapolation (IVIVE) of kinetic parameters from laboratory experiments, has …
vitro‐in vivo extrapolation (IVIVE) of kinetic parameters from laboratory experiments, has …
Contribution of intestinal cytochrome p450-mediated metabolism to drug-drug inhibition and induction interactions
Current drug-drug interaction (DDI) prediction models incorporate intestinal interaction as
the ratio of the intestinal availability in the presence and absence of an inhibitor/inducer …
the ratio of the intestinal availability in the presence and absence of an inhibitor/inducer …
Altered bioavailability and pharmacokinetics in Crohn's disease: capturing systems parameters for PBPK to assist with predicting the fate of orally administered drugs
Abstract Backgrond and Objective Crohn's disease (CD) is a chronic inflammatory bowel
disease that affects a wide age range. Hence, CD patients receive a variety of drugs over …
disease that affects a wide age range. Hence, CD patients receive a variety of drugs over …
Effect of variations in the amounts of P-glycoprotein (ABCB1), BCRP (ABCG2) and CYP3A4 along the human small intestine on PBPK models for predicting intestinal …
A Bruyere, X Decleves, F Bouzom, K Ball… - Molecular …, 2010 - ACS Publications
It is difficult to predict the first-pass effect in the human intestine due to a lack of scaling
factors for correlating in vitro and in vivo data. We have quantified cytochrome P450/3A4 …
factors for correlating in vitro and in vivo data. We have quantified cytochrome P450/3A4 …
Dealing with the complex drug–drug interactions: towards mechanistic models
MV Varma, KS Pang, N Isoherranen… - … & drug disposition, 2015 - Wiley Online Library
Unmanageable severe adverse events caused by drug‐drug interactions (DDIs), leading to
market withdrawals or restrictions in the clinical usage, are increasingly avoided with the …
market withdrawals or restrictions in the clinical usage, are increasingly avoided with the …
Interplay of transporters and enzymes in drug and metabolite processing
This review highlights the “interplay” between enzymes and transporters, essential
components of eliminating organs for drug removal. The understanding of the interplay is …
components of eliminating organs for drug removal. The understanding of the interplay is …