Prediction of phase I single-dose pharmacokinetics using recombinant cytochromes P450 and physiologically based modelling
CR Gibson, A Bergman, P Lu, F Kesisoglou… - Xenobiotica, 2009 - Taylor & Francis
Ten compounds from the Merck Research Laboratories pipeline were selected to evaluate
the utility of using intrinsic clearance derived from recombinantly expressed cytochromes …
the utility of using intrinsic clearance derived from recombinantly expressed cytochromes …
Evaluation of recombinant cytochrome P450 enzymes as an in vitro system for metabolic clearance predictions
RA Stringer, C Strain-Damerell, P Nicklin… - Drug Metabolism and …, 2009 - ASPET
The aim of this study was to explore the potential of recombinant cytochrome P450 (P450)
enzymes for human metabolic clearance prediction. The relative abundance and relative …
enzymes for human metabolic clearance prediction. The relative abundance and relative …
Predicting the effect of cytochrome P450 inhibitors on substrate drugs: analysis of physiologically based pharmacokinetic modeling submissions to the US Food and …
Abstract Background and Objective The US Food and Drug Administration (FDA) has seen a
recent increase in the application of physiologically based pharmacokinetic (PBPK) …
recent increase in the application of physiologically based pharmacokinetic (PBPK) …
Studying cytochrome P450 kinetics in drug metabolism
MA Kramer, TS Tracy - Expert opinion on drug metabolism & …, 2008 - Taylor & Francis
Background: Determination of cytochrome P450 enzyme-mediated kinetics in vitro can be
useful for predicting drug dosing and clearance in humans. Expressed P450s, human liver …
useful for predicting drug dosing and clearance in humans. Expressed P450s, human liver …
In Vitro Evaluation of Reversible and Irreversible Cytochrome P450 Inhibition: Current Status on Methodologies and their Utility for Predicting Drug–Drug Interactions
S Fowler, H Zhang - The AAPS journal, 2008 - Springer
It is widely accepted that today's practice of polypharmacy inevitably increases the incidence
of drug–drug interactions (DDIs). Serious DDI is a major liability for any new chemical entity …
of drug–drug interactions (DDIs). Serious DDI is a major liability for any new chemical entity …
Complex cytochrome P450 kinetics due to multisubstrate binding and sequential metabolism. part 2. modeling of experimental data
EM Paragas, Z Wang, K Korzekwa, S Nagar - Drug Metabolism and …, 2021 - ASPET
Three CYP3A4 substrates, midazolam, ticlopidine, and diazepam, display non–Michaelis-
Menten kinetics, form multiple primary metabolites, and are sequentially metabolized to …
Menten kinetics, form multiple primary metabolites, and are sequentially metabolized to …
Human plasma concentrations of five cytochrome P450 probes extrapolated from pharmacokinetics in dogs and minipigs using physiologically based pharmacokinetic …
S Shida, H Yamazaki - Xenobiotica, 2016 - Taylor & Francis
The pharmacokinetics of cytochrome P450 probes in humans can be extrapolated from
corresponding data in cynomolgus monkeys using simplified physiologically based …
corresponding data in cynomolgus monkeys using simplified physiologically based …
Integrated in vitro analysis for the in vivo prediction of cytochrome P450-mediated drug-drug interactions
DF McGinnity, NJ Waters, J Tucker, RJ Riley - Drug metabolism and …, 2008 - ASPET
Unbound IC50 (IC50, u) values of 15 drugs were determined in eight recombinantly
expressed human cytochromes P450 (P450s) and human hepatocytes, and the data were …
expressed human cytochromes P450 (P450s) and human hepatocytes, and the data were …
Projections of Drug-Drug Interactions Caused by Time-Dependent Inhibitors of Cytochrome P450 1A2, 2B6, 2C8, 2C9, 2C19, and 2D6 Using In Vitro Data in Static and …
E Tseng, J Lin, TJ Strelevitz, E DaSilva… - Drug Metabolism and …, 2024 - ASPET
In vitro time-dependent inhibition (TDI) kinetic parameters for cytochrome P450 (P450) 1A2,
2B6, 2C8, 2C9, 2C19, and 2D6 were determined in pooled human liver microsomes for 19 …
2B6, 2C8, 2C9, 2C19, and 2D6 were determined in pooled human liver microsomes for 19 …
Using Simcyp to project human oral pharmacokinetic variability in early drug research to mitigate mechanism‐based adverse events
CL Shaffer, RJ Scialis, H Rong… - … & drug disposition, 2012 - Wiley Online Library
ABSTRACT Positive allosteric modulators ('potentiators') of the α‐amino‐3‐hydroxy‐5‐
methyl‐4‐isoxazolepropionic acid receptor (AMPAR) have been shown to display a …
methyl‐4‐isoxazolepropionic acid receptor (AMPAR) have been shown to display a …