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 …

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 …

Application of model-based approaches to evaluate hepatic transporter-mediated drug clearance: in vitro, in vivo, and in vitro-in vivo extrapolation

Z Liu, K Liu - Current drug metabolism, 2016 - ingentaconnect.com
Background: Hepatic transporters, including efflux transporters and uptake transporters,
have been recognized to play an important role in the disposition of various drugs. These …

[HTML][HTML] Transport− Metabolism Interplay

L Salphati - Molecular pharmaceutics, 2009 - ACS Publications
The hypothesis that cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp) played
complementary roles in drug absorption and disposition was first proposed 15 years ago. 1 …

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 …

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 …

Rationalizing underprediction of drug clearance from enzyme and transporter kinetic data: from in vitro tools to mechanistic modeling

A Galetin - Enzyme kinetics in drug metabolism: fundamentals and …, 2014 - Springer
Over the years, there has been an increase in the number and quality of available in vitro
tools for the assessment of clearance. Complexity of data analysis and modelling of …

Hepatic transporter‐mediated pharmacokinetic drug–drug interactions: Recent studies and regulatory recommendations

N Izat, S Sahin - Biopharmaceutics & Drug Disposition, 2021 - Wiley Online Library
Transporter‐mediated drug–drug interactions are one of the major mechanisms in
pharmacokinetic‐based drug interactions and correspondingly affecting drugs' safety and …

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 …

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 …