Predicting Drug Extraction in the Human Gut Wall: Assessing Contributions from Drug Metabolizing Enzymes and Transporter Proteins using Preclinical Models

Physiologically based pharmacokinetic modeling in drug discovery and development: A pharmaceutical industry perspective

(2015) HM Jones et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Interplay of Drug-Metabolizing Enzymes and Transporters in Drug Absorption and Disposition

(2015) Shaojun Shi et al.   CURRENT DRUG METABOLISM

Prediction of hepatic and intestinal glucuronidation using in vitro–in vivo extrapolation

(2015) Yoichi Naritomi et al.   Drug Metabolism and Pharmacokinetics

Transgenic mice and metabolomics for study of hepatic xenobiotic metabolism and toxicity

(2015) Frank J Gonzalez et al.   Expert Opinion on Drug Metabolism & Toxicology

In situ perfusion in rodents to explore intestinal drug absorption: Challenges and opportunities

(2015) Jef Stappaerts et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

Intestinal transporters: enhanced absorption through P-glycoprotein-related drug interactions

(2014) Parvin Zakeri-Milani et al.   Expert Opinion on Drug Metabolism & Toxicology

Quantitative ADME Proteomics – CYP and UGT Enzymes in the Beagle Dog Liver and Intestine

(2014) Aki T. Heikkinen et al.   PHARMACEUTICAL RESEARCH

Immunochemical detection of cytochrome P450 enzymes in small intestine microsomes of male and female untreated juvenile cynomolgus monkeys

(2014) Shotaro Uehara et al.   XENOBIOTICA

Mass Spectrometry-Based Targeted Proteomics as a Tool to Elucidate the Expression and Function of Intestinal Drug Transporters

(2013) Stefan Oswald et al.   AAPS Journal

Combining the ‘bottom up’ and ‘top down’ approaches in pharmacokinetic modelling: fitting PBPK models to observed clinical data

(2013) Nikolaos Tsamandouras et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Evaluation of Various Static In Vitro–In Vivo Extrapolation Models for Risk Assessment of the CYP3A Inhibition Potential of an Investigational Drug

(2013) Md L T Vieira et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Genetically modified mouse models for oral drug absorption and disposition

(2013) Seng Chuan Tang et al.   CURRENT OPINION IN PHARMACOLOGY

Quantitative Prediction of Glucuronidation in Humans Using the In Vitro- In Vivo Extrapolation Approach

(2013) Baojian Wu et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

In silico predictions of gastrointestinal drug absorption in pharmaceutical product development: Application of the mechanistic absorption model GI-Sim

(2013) Erik Sjögren et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Animal versus human oral drug bioavailability: Do they correlate?

(2013) Helen Musther et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

In vitro models for the prediction of in vivo performance of oral dosage forms

(2013) Edmund S. Kostewicz et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

LC–MS/MS-based quantification of clinically relevant intestinal uptake and efflux transporter proteins

(2013) C. Gröer et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

In Vitro to in Vivo Extrapolation and Physiologically Based Modeling of Cytochrome P450 Mediated Metabolism in Beagle Dog Gut Wall and Liver

(2013) Aki T. Heikkinen et al.   MOLECULAR PHARMACEUTICS

Species differences in intestinal glucuronidation activities between humans, rats, dogs and monkeys

(2013) Takako Furukawa et al.   XENOBIOTICA

Rat poorly predicts the combined non-absorbed and presystemically metabolized fractions in the human

(2013) Tjerk Bueters et al.   XENOBIOTICA

Genetically humanized mouse models of drug metabolizing enzymes and transporters and their applications

(2013) Nico Scheer et al.   XENOBIOTICA

Comparison of intestinal metabolism of CYP3A substrates between rats and humans: application of portal–systemic concentration difference method

(2013) Keitaro Kadono et al.   XENOBIOTICA

Species differences in hepatic and intestinal metabolic activities for 43 human cytochrome P450 substrates between humans and rats or dogs

(2013) Haruka Nishimuta et al.   XENOBIOTICA

Intestinal drug transporters: An overview

(2012) Margarida Estudante et al.   ADVANCED DRUG DELIVERY REVIEWS

Hepatic and Intestinal Drug Transporters: Prediction of Pharmacokinetic Effects Caused by Drug-Drug Interactions and Genetic Polymorphisms

(2012) Kenta Yoshida et al.   Annual Review of Pharmacology and Toxicology

Absolute abundance and function of intestinal drug transporters: a prerequisite for fully mechanisticin vitro-in vivoextrapolation of oral drug absorption

(2012) M. D. Harwood et al.   BIOPHARMACEUTICS & DRUG DISPOSITION

Why We Need Proper PBPK Models to Examine Intestine and Liver Oral Drug Absorption

(2012) Edwin C.Y. Chow et al.   CURRENT DRUG METABOLISM

In Vitro Methods to Study the Interplay of Drug Metabolism and Efflux in the Intestine

(2012) Sanna Siissalo et al.   CURRENT DRUG METABOLISM

Precision-cut Intestinal Slices as In Vitro Tool for Studies on Drug Metabolism

(2012) Geny M.M. Groothuis et al.   CURRENT DRUG METABOLISM

The right compound in the right assay at the right time: an integrated discovery DMPK strategy

(2012) Peter Ballard et al.   DRUG METABOLISM REVIEWS

Application of PBPK modeling to predict human intestinal metabolism of CYP3A substrates – An evaluation and case study using GastroPlus™

(2012) Aki T. Heikkinen et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Comprehensive study on regional human intestinal permeability and prediction of fraction absorbed of drugs using the Ussing chamber technique

(2012) Åsa Sjöberg et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

In Silico Modeling for the Nonlinear Absorption Kinetics of UK-343,664: A P-gp and CYP3A4 Substrate

(2012) Bilal S. Abuasal et al.   MOLECULAR PHARMACEUTICS

Mass Spectrometry-Based Quantification of CYP Enzymes to Establish In Vitro/In Vivo Scaling Factors for Intestinal and Hepatic Metabolism in Beagle Dog

(2012) Aki T. Heikkinen et al.   PHARMACEUTICAL RESEARCH

Method for predicting human intestinal first-pass metabolism of UGT substrate compounds

(2012) Takako Furukawa et al.   XENOBIOTICA

Quantification of Human Uridine-Diphosphate Glucuronosyl Transferase 1A Isoforms in Liver, Intestine, and Kidney Using Nanobore Liquid Chromatography–Tandem Mass Spectrometry

(2011) David E. Harbourt et al.   ANALYTICAL CHEMISTRY

Absolute immunoquantification of the expression of ABC transporters P-glycoprotein, breast cancer resistance protein and multidrug resistance-associated protein 2 in human liver and duodenum

(2011) Theodora G.H.A. Tucker et al.   BIOCHEMICAL PHARMACOLOGY

PBPK Modeling of Intestinal and Liver Enzymes and Transporters in Drug Absorption and Sequential Metabolism

(2011) Jianghong Fan et al.   CURRENT DRUG METABOLISM

Interplay of Metabolism and Transport in Determining Oral Drug Absorption and Gut Wall Metabolism: A Simulation Assessment Using the “Advanced Dissolution, Absorption, Metabolism (ADAM)” Model

(2011) A. S. Darwich et al.   CURRENT DRUG METABOLISM

Humanized Transgenic Mouse Models for Drug Metabolism and Pharmacokinetic Research

(2011) Hong-Wu Shen et al.   CURRENT DRUG METABOLISM

In Silico, In Vitro and In Situ Models to Assess Interplay Between CYP3A and P-gp

(2011) Daniel R. Mudra et al.   CURRENT DRUG METABOLISM

Characterization of the Expression and Activity of Carboxylesterases 1 and 2 from the Beagle Dog, Cynomolgus Monkey, and Human

(2011) E. T. Williams et al.   DRUG METABOLISM AND DISPOSITION

Physiologically Based Pharmacokinetic Modeling of Intestinal First-Pass Metabolism of CYP3A Substrates with High Intestinal Extraction

(2011) M. Gertz et al.   DRUG METABOLISM AND DISPOSITION

Inhibitory Effect of Zinc on the Absorption of JBP485 via the Gastrointestinal Oligopeptide Transporter (PEPT1) in Rats

(2011) Qi Miao et al.   Drug Metabolism and Pharmacokinetics

Species Differences in Intestinal Metabolic Activities of Cytochrome P450 isoforms between Cynomolgus Monkeys and Humans

(2011) Haruka Nishimuta et al.   Drug Metabolism and Pharmacokinetics

Prediction of the Intestinal First-pass Metabolism of CYP3A and UGT Substrates in Humans from in vitro Data

(2011) Haruka Nishimuta et al.   Drug Metabolism and Pharmacokinetics

Quantitative Prediction of Intestinal Glucuronidation of Drugs in Rats Using In Vitro Metabolic Clearance Data

(2011) Takako Furukawa et al.   Drug Metabolism and Pharmacokinetics

In vitroandin vivosmall intestinal metabolism of CYP3A and UGT substrates in preclinical animals species and humans: species differences

(2011) Hiroshi Komura et al.   DRUG METABOLISM REVIEWS

Evolution of a detailed physiological model to simulate the gastrointestinal transit and absorption process in humans, Part 1: Oral solutions

(2011) Kirstin Thelen et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Transporter-mediated drug–drug interactions

(2011) Fabian Müller et al.   PHARMACOGENOMICS

A Critical Analysis of the Interplay between Cytochrome P450 3A and P-Glycoprotein: Recent Insights from Knockout and Transgenic Mice

(2011) R. A. B. van Waterschoot et al.   PHARMACOLOGICAL REVIEWS

Investigation of the Intestinal Permeability and First-Pass Metabolism of Drugs in Cynomolgus Monkeys Using Single-Pass Intestinal Perfusion

(2010) Masayuki Takahashi et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir

(2010) RAB van Waterschoot et al.   BRITISH JOURNAL OF PHARMACOLOGY

Grapefruit Juice Greatly Reduces the Plasma Concentrations of the OATP2B1 and CYP3A4 Substrate Aliskiren

(2010) T Tapaninen et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Contribution of Rat Pulmonary Metabolism to the Elimination of Lidocaine, Midazolam, and Nifedipine

(2010) M. Aoki et al.   DRUG METABOLISM AND DISPOSITION

Quantitative Prediction of Intestinal Metabolism in Humans from a Simplified Intestinal Availability Model and Empirical Scaling Factor

(2010) K. Kadono et al.   DRUG METABOLISM AND DISPOSITION

Prediction of Human Intestinal First-Pass Metabolism of 25 CYP3A Substrates from In Vitro Clearance and Permeability Data

(2010) M. Gertz et al.   DRUG METABOLISM AND DISPOSITION

Contribution of Intestinal Cytochrome P450-Mediated Metabolism to Drug-Drug Inhibition and Induction Interactions

(2010) Aleksandra Galetin et al.   Drug Metabolism and Pharmacokinetics

Gene expression of carnitine organic cation transporters 1 and 2 (OCTN) is downregulated in patients with ulcerative colitis

(2010) Jesús K. Yamamoto-Furusho et al.   INFLAMMATORY BOWEL DISEASES

Cytochrome P450-mediated metabolism in the human gut wall

(2010) Kirstin Thelen et al.   JOURNAL OF PHARMACY AND PHARMACOLOGY

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 First Pass

(2010) Arnaud Bruyère et al.   MOLECULAR PHARMACEUTICS

Preparation and incubation of precision-cut liver and intestinal slices for application in drug metabolism and toxicity studies

(2010) Inge A M de Graaf et al.   Nature Protocols

Physiological Modeling to Understand the Impact of Enzymes and Transporters on Drug and Metabolite Data and Bioavailability Estimates

(2010) Huadong Sun et al.   PHARMACEUTICAL RESEARCH

Evaluation of the human prediction of clearance from hepatocyte and microsome intrinsic clearance for 52 drug compounds

(2010) A.-K. Sohlenius-Sternbeck et al.   XENOBIOTICA

INTESTINAL PERFUSION WITH MESENTERIC BLOOD SAMPLING IN WILD-TYPE AND KNOCKOUT MICE: Evaluation of a Novel Tool in Biopharmaceutical Drug Profiling

(2009) R. Mols et al.   DRUG METABOLISM AND DISPOSITION

A Comparison of Pharmacokinetics between Humans and Monkeys

(2009) T. Akabane et al.   DRUG METABOLISM AND DISPOSITION

Inhibition and Stimulation of Intestinal and Hepatic CYP3A Activity: Studies in Humanized CYP3A4 Transgenic Mice Using Triazolam

(2009) R. A. B. van Waterschoot et al.   DRUG METABOLISM AND DISPOSITION

Comparison of Different Algorithms for Predicting Clinical Drug-Drug Interactions, Based on the Use of CYP3A4 in Vitro Data: Predictions of Compounds as Precipitants of Interaction

(2009) O. A. Fahmi et al.   DRUG METABOLISM AND DISPOSITION

Quantitative Evaluation of the Expression and Activity of Five Major Sulfotransferases (SULTs) in Human Tissues: The SULT "Pie"

(2009) Z. Riches et al.   DRUG METABOLISM AND DISPOSITION

A Framework for Assessing Inter-individual Variability in Pharmacokinetics Using Virtual Human Populations and Integrating General Knowledge of Physical Chemistry, Biology, Anatomy, Physiology and Genetics: A Tale of ‘Bottom-Up’ vs ‘Top-Down’ Recognition of Covariates

(2009) Masoud Jamei et al.   Drug Metabolism and Pharmacokinetics

The Drug Transporter−Metabolism Alliance: Uncovering and Defining the Interplay

(2009) Leslie Z. Benet   MOLECULAR PHARMACEUTICS

Relative Importance of Intestinal and Hepatic Glucuronidation—Impact on the Prediction of Drug Clearance

(2009) Helen E. Cubitt et al.   PHARMACEUTICAL RESEARCH

Development of an optimized procedure for the preparation of rat intestinal microsomes: comparison of hepatic and intestinal microsomal cytochrome P450 enzyme activities in two rat strains

(2009) A. Bruyère et al.   XENOBIOTICA

Identification of Intestinal Loss of a Drug through Physiologically Based Pharmacokinetic??Simulation of Plasma??Concentration-Time Profiles

(2008) Sheila Annie Peters   CLINICAL PHARMACOKINETICS

Evaluation of a Generic Physiologically Based Pharmacokinetic Model for Lineshape Analysis

(2008) Sheila Annie Peters   CLINICAL PHARMACOKINETICS

Applications and Limitations of Genetically Modified Mouse Models in Drug Discovery and Development

(2008) Jiunn Lin   CURRENT DRUG METABOLISM

Grapefruit Juice-Drug Interaction Studies as a Method to Assess the Extent of Intestinal Availability: Utility and Limitations

(2008) Michael Gertz et al.   CURRENT DRUG METABOLISM

A Combined Model for Predicting CYP3A4 Clinical Net Drug-Drug Interaction Based on CYP3A4 Inhibition, Inactivation, and Induction Determined in Vitro

(2008) O. A. Fahmi et al.   DRUG METABOLISM AND DISPOSITION

Characterization of Cytochrome P450 Protein Expression along the Entire Length of the Intestine of Male and Female Rats

(2008) D. Mitschke et al.   DRUG METABOLISM AND DISPOSITION

Potential role of intestinal first-pass metabolism in the prediction of drug–drug interactions

(2008) Aleksandra Galetin et al.   Expert Opinion on Drug Metabolism & Toxicology

Intestinal efflux transporters and drug absorption

(2008) Teruo Murakami et al.   Expert Opinion on Drug Metabolism & Toxicology

Humanized Mouse Lines and Their Application for Prediction of Human Drug Metabolism and Toxicological Risk Assessment

(2008) C. Cheung et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Applications of Physiologically Based Absorption Models in Drug Discovery and Development

(2008) Neil Parrott et al.   MOLECULAR PHARMACEUTICS

Species Differences in In Vitro and In Vivo Small Intestinal Metabolism of CYP3A Substrates

(2007) Hiroshi Komura et al.   JOURNAL OF PHARMACEUTICAL SCIENCES