Navigating transporter sciences in pharmacokinetics characterization using the extended clearance classification system

AF El-Kattan, MVS Varma - Drug Metabolism and Disposition, 2018 - ASPET
Membrane transporters play an important role in the absorption, distribution, clearance, and
elimination of drugs. Supported by the pharmacokinetics data in human, several transporters …

Transporter–enzyme interplay and the hepatic drug clearance: what have we learned so far?

RV Alluri, R Li, MVS Varma - Expert opinion on drug metabolism & …, 2020 - Taylor & Francis
Introduction: Transporters and enzymes play an important role in absorption, distribution,
clearance and elimination of drugs. Areas covered: This review provides an overview of the …

Transporter‐enzyme interplay: deconvoluting effects of hepatic transporters and enzymes on drug disposition using static and dynamic mechanistic models

MV Varma, AF El‐Kattan - The Journal of Clinical …, 2016 - Wiley Online Library
A large body of evidence suggests hepatic uptake transporters, organic anion‐transporting
polypeptides (OATPs), are of high clinical relevance in determining the pharmacokinetics of …

Model-based approaches to predict drug–drug interactions associated with hepatic uptake transporters: preclinical, clinical and beyond

HA Barton, Y Lai, TC Goosen, HM Jones… - Expert opinion on …, 2013 - Taylor & Francis
Introduction: Membrane transporters have been recognized to play a key role in determining
the absorption, distribution and elimination processes of drugs. The organic anion …

Highlights from the American Association of Pharmaceutical Scientists/International Transporter Consortium Joint Workshop on drug transporters in absorption …

PT Ronaldson, B Bauer, AF El‐Kattan… - Clinical …, 2016 - Wiley Online Library
The American Association of Pharmaceutical Scientists/International Transporter
Consortium Joint Workshop on Drug Transporters in absorption, distribution, metabolism …

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 …

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 …

Transporter-mediated drug–drug interactions

F Müller, MF Fromm - Pharmacogenomics, 2011 - Taylor & Francis
Drug–drug interactions are a serious clinical issue. An important mechanism underlying
drug–drug interactions is induction or inhibition of drug transporters that mediate the cellular …

Recent advances in preclinical in vitro approaches towards quantitative prediction of hepatic clearance and drug-drug interactions involving organic anion …

Y Nozaki, S Izumi - Drug Metabolism and Pharmacokinetics, 2020 - Elsevier
Hepatic uptake mediated by organic anion transporting polypeptide (OATP) 1B1 and 1B3
can serve as a major elimination pathway for various anionic drugs and as a site of drug …

Evaluation of proposed in vivo probe substrates and inhibitors for phenotyping transporter activity in humans

JD Momper, SM Tsunoda, JD Ma - The Journal of Clinical …, 2016 - Wiley Online Library
Drug transporters are present in various tissues and have a significant role in drug
absorption, distribution, and elimination. The International Transporter Consortium has …