A critical perspective on 3D liver models for drug metabolism and toxicology studies

AS Serras, JS Rodrigues, M Cipriano… - Frontiers in cell and …, 2021 - frontiersin.org
The poor predictability of human liver toxicity is still causing high attrition rates of drug
candidates in the pharmaceutical industry at the non-clinical, clinical, and post-marketing …

Clinical significance of organic anion transporting polypeptides (OATPs) in drug disposition: their roles in hepatic clearance and intestinal absorption

Y Shitara, K Maeda, K Ikejiri, K Yoshida… - … & drug disposition, 2013 - Wiley Online Library
Organic anion transporting polypeptide (OATP) family transporters accept a number of drugs
and are increasingly being recognized as important factors in governing drug and …

Predicting clearance mechanism in drug discovery: extended clearance classification system (ECCS)

MV Varma, SJ Steyn, C Allerton, AF El-Kattan - Pharmaceutical research, 2015 - Springer
Early prediction of clearance mechanisms allows for the rapid progression of drug discovery
and development programs, and facilitates risk assessment of the pharmacokinetic …

Species differences in drug transporters and implications for translating preclinical findings to humans

X Chu, K Bleasby, R Evers - Expert opinion on drug metabolism & …, 2013 - Taylor & Francis
Introduction: Drug transporters play an important role in the absorption, distribution, and
excretion (ADE) of many drugs. In the last several years it has become increasingly clear …

Drug–drug interaction studies: regulatory guidance and an industry perspective

T Prueksaritanont, X Chu, C Gibson, D Cui, KL Yee… - The AAPS journal, 2013 - Springer
Recently, the US Food and Drug Administration and European Medicines Agency have
issued new guidance for industry on drug interaction studies, which outline comprehensive …

Intracellular drug concentrations and transporters: measurement, modeling, and implications for the liver

X Chu, K Korzekwa, R Elsby, K Fenner… - Clinical …, 2013 - Wiley Online Library
Intracellular concentrations of drugs and metabolites are often important determinants of
efficacy, toxicity, and drug interactions. Hepatic drug distribution can be affected by many …

ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport‐mediated PK and DDIs in humans

MJ Zamek‐Gliszczynski, CA Lee… - Clinical …, 2013 - Wiley Online Library
This white paper provides a critical analysis of methods for estimating transporter kinetics
and recommendations on proper parameter calculation in various experimental systems …

Understanding the critical disposition pathways of statins to assess drug–drug interaction risk during drug development: it's not just about OATP1B1

R Elsby, C Hilgendorf, K Fenner - Clinical Pharmacology & …, 2012 - Wiley Online Library
The use of statins is widespread across disease areas because many patients have
comorbidities. Given that these drugs have become common as comedications, it is …

Advancing Predictions of Tissue and Intracellular Drug Concentrations Using In Vitro, Imaging and Physiologically Based Pharmacokinetic Modeling Approaches

Y Guo, X Chu, NJ Parrott, KLR Brouwer… - Clinical …, 2018 - Wiley Online Library
This white paper examines recent progress, applications, and challenges in predicting
unbound and total tissue and intra/subcellular drug concentrations using in vitro and …

Rapid measurement of intracellular unbound drug concentrations

A Mateus, P Matsson, P Artursson - Molecular pharmaceutics, 2013 - ACS Publications
Intracellular unbound drug concentrations determine affinity to targets in the cell interior.
However, due to difficulties in measuring them, they are often overlooked in pharmacology …