[HTML][HTML] Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes

JWH Leow, Y Gu, ECY Chan - European Journal of Pharmaceutical …, 2023 - Elsevier
Abstract Cardiac cytochrome P450 2J2 (CYP2J2) metabolizes endogenous polyunsaturated
fatty acid, arachidonic acid (AA), to bioactive regioisomeric epoxyeicosatrienoic acid (EET) …

In vitro studies on flubromazolam metabolism and detection of its metabolites in authentic forensic samples

C Noble, M Mardal, N Bjerre Holm… - Drug testing and …, 2017 - Wiley Online Library
Flubromazolam is a triazole benzodiazepine with high potency and long‐lasting central
nervous system depressant effects; however, limited data about its pharmacokinetics are …

[HTML][HTML] In Vitro Drug Metabolism Studies Using Human Liver Microsomes

SNR Gajula, SA Vora, AG Dikundwar… - … Forms-Innovation and …, 2022 - intechopen.com
Metabolism of most pharmaceutical drugs occurs in the liver. In drug metabolism, enzymes
convert drugs to highly water-soluble metabolites to facilitate excretion from the body. Thus …

Understanding Cytochrome P450 Enzyme Substrate Inhibition and Prospects for Elimination Strategies

Y Zhang, G Zhang, T Wang, Y Chen, J Wang… - …, 2024 - Wiley Online Library
Abstract Cytochrome P450 (CYP450) enzymes, which are widely distributed and pivotal in
various biochemical reactions, catalyze diverse processes such as hydroxylation …

Atypical kinetics of cytochrome P450 enzymes in pharmacology and toxicology

JWH Leow, LWT Tang, ECY Chan - Advances in Pharmacology, 2022 - Elsevier
Atypical kinetics are observed in metabolic reactions catalyzed by cytochrome P450
enzymes (P450). Yet, this phenomenon is regarded as experimental artifacts in some …

Evaluation of an in-capillary approach for performing quantitative cytochrome P450 activity studies

R Curcio, R Nicoli, S Rudaz, JL Veuthey - Analytical and bioanalytical …, 2010 - Springer
An automated in-capillary assay requiring very small quantities of reagents was developed
for performing in vitro cytochrome P450 (CYP450) drug metabolism studies. The approach is …

In vitro inhibition of cytochrome P450 3A4 by Aronia melanocarpa constituents

M Bräunlich, H Christensen, S Johannesen… - Planta …, 2013 - thieme-connect.com
Extracts, subfractions, isolated anthocyanins and procyanidins, and two phenolic acids from
aronia [Aronia melanocarpa] were investigated for their CYP3A4 inhibitory effects, using …

CYP3A5-mediated metabolism of midazolam in recombinant systems is highly sensitive to NADPH-cytochrome P450 reductase activity

H Christensen, AL Hestad, E Molden, L Mathiesen - Xenobiotica, 2011 - Taylor & Francis
Data from in vitro drug metabolism studies with recombinant enzyme systems are frequently
used to predict human drug metabolism in vivo. However, for the CYP3A probe substrate …

Mechanism of Action of Panaxytriol on Midazolam 1′-Hydroxylation and 4-Hydroxylation Mediated by CYP3A in Liver Microsomes and Rat Primary Hepatocytes

F He, W Zhang, C Zeng, C Xia, Y Xiong… - Biological and …, 2015 - jstage.jst.go.jp
In our previous study, panaxytriol (PXT) was shown to enhance midazolam (MDZ) 1′-
hydroxylation significantly but to inhibit MDZ 4-hydroxylation. To explore the underlying …

Variability in human in vitro enzyme kinetics

CR Gibson, YH Wang, N Varkhede, B Ma - Enzyme Kinetics in Drug …, 2021 - Springer
There are many factors which are known to cause variability in human in vitro enzyme
kinetic data. Factors such as the source of enzyme and how it was prepared, the genetics …