Role of cytochrome P450 2C8 in drug metabolism and interactions
During the last 10-15 years, cytochrome P450 (CYP) 2C8 has emerged as an important drug-
metabolizing enzyme. CYP2C8 is highly expressed in human liver and is known to …
metabolizing enzyme. CYP2C8 is highly expressed in human liver and is known to …
A cocktail approach for assessing the in vitro activity of human cytochrome P450s: an overview of current methodologies
An assessment of cytochrome P450 (CYP) enzyme activity is essential for characterizing the
phase I metabolism of biological systems or to evaluate the inhibition/induction properties of …
phase I metabolism of biological systems or to evaluate the inhibition/induction properties of …
Exploration and application of a liver-on-a-chip device in combination with modelling and simulation for quantitative drug metabolism studies
L Docci, N Milani, T Ramp, AA Romeo, P Godoy… - Lab on a Chip, 2022 - pubs.rsc.org
Microphysiological systems (MPS) are complex and more physiologically realistic cellular in
vitro tools that aim to provide more relevant human in vitro data for quantitative prediction of …
vitro tools that aim to provide more relevant human in vitro data for quantitative prediction of …
Cyclosporine inhibition of hepatic and intestinal CYP3A4, uptake and efflux transporters: application of PBPK modeling in the assessment of drug-drug interaction …
M Gertz, CM Cartwright, MJ Hobbs… - Pharmaceutical …, 2013 - Springer
Purpose To apply physiologically-based pharmacokinetic (PBPK) modeling to investigate
the consequences of reduction in activity of hepatic and intestinal uptake and efflux …
the consequences of reduction in activity of hepatic and intestinal uptake and efflux …
Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes
K Menochet, KE Kenworthy, JB Houston… - Drug Metabolism and …, 2012 - ASPET
Interindividual variability in activity of uptake transporters is evident in vivo, yet limited data
exist in vitro, confounding in vitro-in vivo extrapolation. The uptake kinetics of seven organic …
exist in vitro, confounding in vitro-in vivo extrapolation. The uptake kinetics of seven organic …
Use of physiologically based pharmacokinetic modeling to evaluate the effect of chronic kidney disease on the disposition of hepatic CYP 2C8 and OATP 1B drug …
ML Tan, P Zhao, L Zhang, YF Ho… - Clinical …, 2019 - Wiley Online Library
Chronic kidney disease (CKD) differentially affects the pharmacokinetics (PK) of nonrenally
cleared drugs via certain pathways (eg, cytochrome P450 (CYP) 2D6); however, the effect …
cleared drugs via certain pathways (eg, cytochrome P450 (CYP) 2D6); however, the effect …
Prediction of pharmacokinetics and drug–drug interactions when hepatic transporters are involved
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 …
determining the systemic clearance for a number of widely prescribed drugs and an …
Mechanistic modeling to predict the transporter-and enzyme-mediated drug-drug interactions of repaglinide
Purpose Quantitative prediction of complex drug-drug interactions (DDIs) is challenging.
Repaglinide is mainly metabolized by cytochrome-P-450 (CYP) 2C8 and CYP3A4, and is …
Repaglinide is mainly metabolized by cytochrome-P-450 (CYP) 2C8 and CYP3A4, and is …
Dealing with the complex drug–drug interactions: towards mechanistic models
MV Varma, KS Pang, N Isoherranen… - … & drug disposition, 2015 - Wiley Online Library
Unmanageable severe adverse events caused by drug‐drug interactions (DDIs), leading to
market withdrawals or restrictions in the clinical usage, are increasingly avoided with the …
market withdrawals or restrictions in the clinical usage, are increasingly avoided with the …
Complex drug–drug–gene–disease interactions involving cytochromes P450: systematic review of published case reports and clinical perspectives
Drug pharmacokinetics (PK) is influenced by multiple intrinsic and extrinsic factors, among
which concomitant medications are responsible for drug–drug interactions (DDIs) that may …
which concomitant medications are responsible for drug–drug interactions (DDIs) that may …