[HTML][HTML] Preclinical experimental models of drug metabolism and disposition in drug discovery and development

D Zhang, G Luo, X Ding, C Lu - Acta Pharmaceutica Sinica B, 2012 - Elsevier
Drug discovery and development involve the utilization of in vitro and in vivo experimental
models. Different models, ranging from test tube experiments to cell cultures, animals …

The HepaRG cell line: a unique in vitro tool for understanding drug metabolism and toxicology in human

TB Andersson, KP Kanebratt… - Expert opinion on drug …, 2012 - Taylor & Francis
Introduction: HepaRG is a unique cell line showing a great plasticity, which differentiates to
both canaliculae-like and hepatocyte-like cells. The long-term stability of key cell functions …

Optimization of the HepaRG cell model for drug metabolism and toxicity studies

S Anthérieu, C Chesné, R Li, C Guguen-Guillouzo… - Toxicology in Vitro, 2012 - Elsevier
The HepaRG cell line is the first human cell line able to differentiate in vitro into mature
hepatocyte-like cells. Our main objective within the framework of the EEC-LIINTOP project …

Prediction of Human Metabolic Clearance from In Vitro Systems: Retrospective Analysis and Prospective View

D Hallifax, JA Foster, JB Houston - Pharmaceutical research, 2010 - Springer
Purpose To provide a definitive assessment of prediction of in vivo CL int from human liver in
vitro systems for assessment of typical underprediction. Methods A database of published …

[HTML][HTML] Strategies for immortalization of primary hepatocytes

E Ramboer, B De Craene, J De Kock, T Vanhaecke… - Journal of …, 2014 - Elsevier
The liver has the unique capacity to regenerate in response to a damaging event. Liver
regeneration is hereby largely driven by hepatocyte proliferation, which in turn relies on cell …

Through a glass, darkly? HepaRG and HepG2 cells as models of human phase I drug metabolism

LA Stanley, CR Wolf - Drug Metabolism Reviews, 2022 - Taylor & Francis
The pharmacokinetic and safety assessment of drug candidates is becoming increasingly
dependent upon in vitro models of hepatic metabolism and toxicity. Predominant among …

Activation of pregnane X receptor (PXR) and constitutive androstane receptor (CAR) by herbal medicines

TKH Chang - The AAPS journal, 2009 - Springer
Pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are transcription
factors that control the expression of a broad array of genes involved not only in transcellular …

A Review of CYP-Mediated Drug Interactions: Mechanisms and In Vitro Drug-Drug Interaction Assessment

J Lee, JL Beers, RM Geffert, KD Jackson - Biomolecules, 2024 - mdpi.com
Drug metabolism is a major determinant of drug concentrations in the body. Drug-drug
interactions (DDIs) caused by the co-administration of multiple drugs can lead to alteration in …

Stem cell-derived hepatocytes and their use in toxicology

C Guguen-Guillouzo, A Corlu, A Guillouzo - Toxicology, 2010 - Elsevier
Better prediction of safety risk and understanding of mechanism of action of drug candidates
remain a major challenge in order to prevent late stage attrition. Continuous efforts are made …

[引用][C] In vitro evaluation of potential drug-drug interactions with ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics

D Zhou, TB Andersson, SW Grimm - Drug metabolism and disposition, 2011 - ASPET