Computational approaches to modeling drug transporters
Computational modeling has advanced our understanding of drug absorption, tissue
distribution, excretion and toxicity profiles by providing both direct and indirect knowledge of …
distribution, excretion and toxicity profiles by providing both direct and indirect knowledge of …
The evolution of the OATP hepatic uptake transport protein family in DMPK sciences: from obscure liver transporters to key determinants of hepatobiliary clearance
KS Fenner, HM Jones, M Ullah, S Kempshall… - Xenobiotica, 2012 - Taylor & Francis
Over the last two decades the impact on drug pharmacokinetics of the organic anion
transporting polypeptides (OATPs: OATP-1B1, 1B3 and 2B1), expressed on the sinusoidal …
transporting polypeptides (OATPs: OATP-1B1, 1B3 and 2B1), expressed on the sinusoidal …
Transport vs. metabolism: what determines the pharmacokinetics and pharmacodynamics of drugs? Insights from the extended clearance model
G Patilea‐Vrana, JD Unadkat - Clinical Pharmacology & …, 2016 - Wiley Online Library
The well‐stirred hepatic clearance model (WSHM) has been expanded to include drug
transporters (ie, extended clearance model [ECM]). However, the consequences of this …
transporters (ie, extended clearance model [ECM]). However, the consequences of this …
Identification and evaluation of clinical substrates of organic anion transporting polypeptides 1B1 and 1B3
SJ McFeely, TK Ritchie, J Yu… - Clinical and …, 2019 - Wiley Online Library
Organic anion transporting polypeptides (OATPs) 1B1 and 1B3 facilitate the uptake of drugs
and endogenous compounds into the liver. In recent years, the impact of these transporters …
and endogenous compounds into the liver. In recent years, the impact of these transporters …
[HTML][HTML] A mechanistic framework for in vitro–in vivo extrapolation of liver membrane transporters: prediction of drug–drug interaction between rosuvastatin and …
Abstract Background and Objectives The interplay between liver metabolising enzymes and
transporters is a complex process involving system-related parameters such as liver blood …
transporters is a complex process involving system-related parameters such as liver blood …
PBPK modeling of intestinal and liver enzymes and transporters in drug absorption and sequential metabolism
Experimental strategies have long been applied for in vitro or in vivo evaluation of the effect
of transporters and/or enzymes on the bioavailability. However, the lack of specific inhibitors …
of transporters and/or enzymes on the bioavailability. However, the lack of specific inhibitors …
Overcoming the shortcomings of the extended-clearance concept: a framework for developing a physiologically-based pharmacokinetic (PBPK) model to select drug …
Introduction: Human pharmacokinetic (PK) prediction can be a significant challenge to drug
candidates undergoing transporter-mediated clearance, when only animal data and in vitro …
candidates undergoing transporter-mediated clearance, when only animal data and in vitro …
Hepatic and intestinal drug transporters: prediction of pharmacokinetic effects caused by drug-drug interactions and genetic polymorphisms
Recent studies of membrane transporters have revealed their importance in determining the
pharmacokinetics of transporter substrates. When drug-drug interactions (DDIs) or genetic …
pharmacokinetics of transporter substrates. When drug-drug interactions (DDIs) or genetic …
The presence of a transporter-induced protein binding shift: a new explanation for protein-facilitated uptake and improvement for in vitro-in vivo extrapolation
CM Bowman, H Okochi, LZ Benet - Drug Metabolism and Disposition, 2019 - ASPET
Accurately predicting hepatic clearance is an integral part of the drug-development process,
and yet current in vitro to in vivo (IVIVE) extrapolation methods yield poor predictions …
and yet current in vitro to in vivo (IVIVE) extrapolation methods yield poor predictions …
In vitro evidence for the role of OATP and OCT uptake transporters in drug–drug interactions
Background: Transport proteins, for example the drug export pump P-glycoprotein, are
important for the absorption, distribution and excretion of drugs. Inhibition and induction of P …
important for the absorption, distribution and excretion of drugs. Inhibition and induction of P …