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 …

Clearance in drug design: miniperspective

DA Smith, K Beaumont, TS Maurer… - Journal of Medicinal …, 2018 - ACS Publications
Due to its implications for both dose level and frequency, clearance rate is one of the most
important pharmacokinetic parameters to consider in the design of drug candidates …

The evolving role of drug metabolism in drug discovery and development

LG Yengi, L Leung, J Kao - Pharmaceutical research, 2007 - Springer
Drug metabolism in pharmaceutical research has traditionally focused on the well-defined
aspects of absorption, distribution, metabolism and excretion, commonly-referred to ADME …

Prediction of pharmacokinetics and drug–drug interactions when hepatic transporters are involved

R Li, HA Barton, MV Varma - Clinical pharmacokinetics, 2014 - Springer
Hepatobiliary transport mechanisms have been identified to play a significant role in
determining the systemic clearance for a number of widely prescribed drugs and an …

Use of clearance concepts and modeling techniques in the prediction of metabolic drug–drug interactions

K Ito, Y Sugiyama - Trends in pharmacological sciences, 2010 - cell.com
Quantitative prediction of the in vivo drug–drug interactions (DDIs) caused by metabolic
inhibition, one of the most common DDI mechanisms in clinical practice, has long been …

The application of physiologically based pharmacokinetic modeling to predict the role of drug transporters: scientific and regulatory perspectives

Y Pan, V Hsu, M Grimstein, L Zhang… - The Journal of …, 2016 - Wiley Online Library
Transporters play an important role in drug absorption, disposition, and drug action. The
evaluation of drug transporters requires a comprehensive understanding of transporter …

Predicting transporter mediated drug–drug interactions via static and dynamic physiologically based pharmacokinetic modeling: A comprehensive insight on where …

G Vijaywargi, S Kollipara, T Ahmed… - … & Drug Disposition, 2023 - Wiley Online Library
The greater utilization and acceptance of physiologically‐based pharmacokinetic (PBPK)
modeling to evaluate the potential metabolic drug–drug interactions is evident by the …

[HTML][HTML] Quantitative prediction of pharmacokinetic properties of drugs in humans: Recent advance in in vitro models to predict the impact of efflux transporters in the …

Y Hashimoto, K Michiba, K Maeda… - Journal of Pharmacological …, 2022 - Elsevier
Efflux transport systems are essential to suppress the absorption of xenobiotics from the
intestinal lumen and protect the critical tissues at the blood-tissue barriers, such as the blood …

Quantitative prediction of in vivo drug clearance and drug interactions from in vitro data on metabolism, together with binding and transport

K Ito, T Iwatsubo, S Kanamitsu… - Annual Review of …, 1998 - annualreviews.org
▪ Abstract It is of great importance to predict in vivo pharmacokinetics in humans based on in
vitro data. We summarize recent findings of the quantitative prediction of the hepatic …

Intestinal and blood–brain drug transport: beyond involvement of a single transport function

H Lennernäs, E Lundgren - Drug Discovery Today: Technologies, 2004 - Elsevier
It is considered that an increased understanding of drug transport in the intestine, liver,
kidney and blood–brain barrier is vital to the successful development of new and effective …