Gut instincts: explorations in intestinal physiology and drug delivery

EL McConnell, HM Fadda, AW Basit - International journal of pharmaceutics, 2008 - Elsevier
We need to look beyond our gut instincts to use information on “simple” intestinal
physiological parameters as they have been presented to us in the past. Here we present a …

Xenobiotic-induced transcriptional regulation of xenobiotic metabolizing enzymes of the cytochrome P450 superfamily in human extrahepatic tissues

P Pavek, Z Dvorak - Current drug metabolism, 2008 - ingentaconnect.com
Numerous members of the cytochrome P450 (CYP) superfamily are induced after exposure
to a variety of xenobiotics in human liver. We have gained considerable mechanistic insights …

Does sex matter? The influence of gender on gastrointestinal physiology and drug delivery

AC Freire, AW Basit, R Choudhary, CW Piong… - International journal of …, 2011 - Elsevier
We all respond differently to drugs. Personalised medicine aims to improve efficacy and
reduce side effects, and efforts are being made to understand the physiological differences …

Impact of OATP1B1, MDR1, and CYP3A4 expression in liver and intestine on interpatient pharmacokinetic variability of atorvastatin in obese subjects

M Ulvestad, IB Skottheim, GS Jakobsen… - Clinical …, 2013 - Wiley Online Library
Individual variability in expression and function of organic anion‐transporting polypeptide
1B1 (OATP1B1), multidrug resistance protein 1 (MDR1), and/or cytochrome P450 3A4 …

Extrahepatic metabolism at the body's internal–external interfaces

U Gundert-Remy, U Bernauer, B Blömeke… - Drug metabolism …, 2014 - Taylor & Francis
In general, xenobiotic metabolizing enzymes (XMEs) are expressed in lower levels in the
extrahepatic tissues than in the liver, making the former less relevant for the clearance of …

From gut to kidney: transporting and metabolizing calcineurin-inhibitors in solid organ transplantation

N Knops, E Levtchenko, B van den Heuvel… - International journal of …, 2013 - Elsevier
Since their introduction circa 35 years ago, calcineurin-inhibitors (CNI) have become the
cornerstone of immunosuppressive therapy in solid organ transplantation. However, CNI's …

Update information on drug metabolism systems—2009, part II. Summary of information on the effects of diseases and environmental factors on human cytochrome …

S Rendic, FP Guengerich - Current drug metabolism, 2010 - ingentaconnect.com
The present paper is an update of the data on the effects of diseases and environmental
factors on the expression and/or activity of human cytochrome P450 (CYP) enzymes and …

Colonic treatments and targets: issues and opportunities

EL McConnell, F Liu, AW Basit - Journal of drug targeting, 2009 - Taylor & Francis
The colon provides a plethora of therapeutic opportunities. There are multiple disease
targets, drug molecules, and colon-specific delivery systems to be explored. Clinical studies …

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 …

A decade of improvements in quantification of gene expression and internal standard selection

O Thellin, B ElMoualij, E Heinen, W Zorzi - Biotechnology Advances, 2009 - Elsevier
Major improvements have been made in mRNA quantification and internal standard
selection over the last decade. Our aim in this paper is to present the main developments …