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 …

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 …

Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data

M Gertz, A Harrison, JB Houston, A Galetin - Drug Metabolism and …, 2010 - ASPET
Intestinal first-pass metabolism may contribute to low oral drug bioavailability and drug-drug
interactions, particularly for CYP3A substrates. The current analysis predicted intestinal …

Applications of human pharmacokinetic prediction in first-in-human dose estimation

P Zou, Y Yu, N Zheng, Y Yang, HJ Paholak, LX Yu… - The AAPS journal, 2012 - Springer
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 …

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 …

Contribution of intestinal cytochrome p450-mediated metabolism to drug-drug inhibition and induction interactions

A Galetin, M Gertz, JB Houston - Drug metabolism and …, 2010 - jstage.jst.go.jp
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 …

Altered bioavailability and pharmacokinetics in Crohn's disease: capturing systems parameters for PBPK to assist with predicting the fate of orally administered drugs

S Alrubia, J Mao, Y Chen, J Barber… - Clinical …, 2022 - Springer
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 …

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 …

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 …

Interplay of transporters and enzymes in drug and metabolite processing

KS Pang, HJ Maeng, J Fan - Molecular Pharmaceutics, 2009 - ACS Publications
This review highlights the “interplay” between enzymes and transporters, essential
components of eliminating organs for drug removal. The understanding of the interplay is …