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 …
tools for the assessment of clearance. Complexity of data analysis and modelling of …
Prediction of drug clearance from enzyme and transporter kinetics
PR Kulkarni, AS Youssef, AA Argikar - Enzyme Kinetics in Drug …, 2021 - Springer
Accurate estimation of in vivo clearance in human is pivotal to determine the dose and
dosing regimen for drug development. In vitro–in vivo extrapolation (IVIVE) has been …
dosing regimen for drug development. In vitro–in vivo extrapolation (IVIVE) has been …
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 …
have been recognized to play an important role in the disposition of various drugs. These …
Human clearance prediction: shifting the paradigm
T Lavé, K Chapman, P Goldsmith… - Expert opinion on drug …, 2009 - Taylor & Francis
There is a growing momentum to use in vitro methods, nestled in in silico physiologically
based pharmacokinetic models as the primary source of prediction of human clearance. This …
based pharmacokinetic models as the primary source of prediction of human clearance. This …
Transporter–enzyme interplay and the hepatic drug clearance: what have we learned so far?
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 …
clearance and elimination of drugs. Areas covered: This review provides an overview of the …
Absolute abundance and function of intestinal drug transporters: a prerequisite for fully mechanistic in vitro–in vivo extrapolation of oral drug absorption
MD Harwood, S Neuhoff, GL Carlson… - … & drug disposition, 2013 - Wiley Online Library
The use of whole body physiological‐based pharmacokinetic (PBPK) models linked with in
vitro‐in vivo extrapolation (IVIVE) of kinetic parameters from laboratory experiments, has …
vitro‐in vivo extrapolation (IVIVE) of kinetic parameters from laboratory experiments, has …
Predicting human hepatic clearance from in vitro drug metabolism and transport data: a scientific and pharmaceutical perspective for assessing drug–drug …
G Camenisch, K Umehara - Biopharmaceutics & drug …, 2012 - Wiley Online Library
Objectives Membrane transporters and metabolism are major determinants of the
hepatobiliary elimination of drugs. This work investigates several key questions for drug …
hepatobiliary elimination of drugs. This work investigates several key questions for drug …
Simultaneous assessment in vitro of transporter and metabolic processes in hepatic drug clearance: use of a media loss approach
Hepatocyte drug depletion-time assays are well established for determination of metabolic
clearance in vitro. The present study focuses on the refinement and evaluation of a “media …
clearance in vitro. The present study focuses on the refinement and evaluation of a “media …
Model-based approaches to predict drug–drug interactions associated with hepatic uptake transporters: preclinical, clinical and beyond
Introduction: Membrane transporters have been recognized to play a key role in determining
the absorption, distribution and elimination processes of drugs. The organic anion …
the absorption, distribution and elimination processes of drugs. The organic anion …
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 …
selection of small molecule drug candidates within the pharmaceutical industry. The …