In vitro and in vivo approaches to characterize transporter-mediated disposition in drug discovery

B Feng, MV Varma, C Costales, H Zhang… - Expert opinion on drug …, 2014 - Taylor & Francis
Introduction: It is becoming increasingly evident that transporters play an important role in
the absorption, distribution and elimination of many drugs. Different approaches have been …

Physiologically-based pharmacokinetic (PBPK) modelling of transporter mediated drug absorption, clearance and drug-drug interactions

KS Taskar, I Harada, RV Alluri - Current Drug Metabolism, 2021 - ingentaconnect.com
Membrane transporters play an important role in intestinal absorption, distribution and
clearance of drugs. Additionally transporters along with enzymes regulate tissue exposures …

Understanding the transport properties of metabolites: case studies and considerations for drug development

MJ Zamek-Gliszczynski, X Chu, JW Polli… - Drug Metabolism and …, 2014 - ASPET
Recent analyses demonstrated that metabolites are unlikely to contribute significantly to
clinical inhibition of cytochrome P450 (P450)–mediated drug metabolism, and that only∼ …

Impact of hepatic uptake transporters on pharmacokinetics and drug− drug interactions: use of assays and models for decision making in the pharmaceutical industry

MG Soars, PJH Webborn, RJ Riley - Molecular pharmaceutics, 2009 - ACS Publications
The ability to predict hepatic metabolic clearance is a key component in the design and
selection of small molecule drug candidates within the pharmaceutical industry. The …

New strategies to address drug-drug interactions involving OATPs.

A Poirier, C Funk, T Lave, J Noe - Current opinion in drug discovery …, 2007 - europepmc.org
Pharmacokinetic drug-drug interactions (DDIs) are a major concern in drug development.
Drug transport, along with drug metabolism via cytochrome P450s (CYPs), is increasingly …

Studying the right transporter at the right time: an in vitro strategy for assessing drug-drug interaction risk during drug discovery and development

R Elsby, H Atkinson, P Butler… - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Transporters are significant in dictating drug pharmacokinetics, thus inhibition of
transporter function can alter drug concentrations resulting in drug-drug interactions (DDIs) …

Organic anion transporter 2–mediated hepatic uptake contributes to the clearance of high-permeability–low-molecular-weight acid and zwitterion drugs: evaluation …

E Kimoto, S Mathialagan, L Tylaska, M Niosi… - … of Pharmacology and …, 2018 - ASPET
High-permeability–low-molecular-weight acids/zwitterions [ie, extended clearance
classification system class 1A (ECCS 1A) drugs] are considered to be cleared by …

Current understanding of hepatic and intestinal OATP-mediated drug–drug interactions

A Koenen, HK Kroemer, M Grube… - Expert review of …, 2011 - Taylor & Francis
At present, many patients are medicated with various drugs, which are, at the same time,
associated with an increased risk of drug–drug interactions (DDIs). Detailed analysis of …

Predicting human hepatic clearance from in vitro drug metabolism and transport data: a scientific and pharmaceutical perspective for assessing drug–drug …

G Camenisch, K Umehara - Biopharmaceutics & drug …, 2012 - Wiley Online Library
Objectives Membrane transporters and metabolism are major determinants of the
hepatobiliary elimination of drugs. This work investigates several key questions for drug …

Biomarkers for in vivo assessment of transporter function

F Müller, A Sharma, J König, MF Fromm - Pharmacological Reviews, 2018 - ASPET
Drug–drug interactions are a major concern not only during clinical practice, but also in drug
development. Due to limitations of in vitro–in vivo predictions of transporter-mediated drug …