Drugs behave as substrates, inhibitors and inducers of human cytochrome P450 3A4

SF Zhou - Current drug metabolism, 2008 - ingentaconnect.com
Human cytochrome P450 (CYP) 3A4 is the most abundant hepatic and intestinal phase I
enzyme that metabolizes approximately 50% marketed drugs. The crystal structure of bound …

Colchicine update: 2008

RA Terkeltaub - Seminars in arthritis and rheumatism, 2009 - Elsevier
OBJECTIVES: To review recent advances in the understanding of molecular mechanisms of
drug disposition and cellular mechanisms of action and targets of colchicine, and disease …

The utility of in vitro cytochrome P450 inhibition data in the prediction of drug-drug interactions

RS Obach, RL Walsky, K Venkatakrishnan… - … of Pharmacology and …, 2006 - ASPET
The accuracy of in vitro inhibition parameters in scaling to in vivo drug-drug interactions
(DDI) was examined for over 40 drugs using seven human P450-selective marker activities …

In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin …

D Zhang, TJ Chando, DW Everett, CJ Patten… - Drug Metabolism and …, 2005 - ASPET
Several human immunodeficiency virus (HIV) protease inhibitors, including atazanavir,
indinavir, lopinavir, nelfinavir, ritonavir, and saquinavir, were tested for their potential to …

Appropriate phenotyping procedures for drug metabolizing enzymes and transporters in humans and their simultaneous use in the “cocktail” approach

U Fuhr, A Jetter, J Kirchheiner - Clinical Pharmacology & …, 2007 - Wiley Online Library
Phenotyping for drug metabolizing enzymes and transporters is used to assess
quantitatively the effect of an intervention (eg, drug therapy, diet) or a condition (eg, genetic …

Mechanisms underlying food–drug interactions: inhibition of intestinal metabolism and transport

CS Won, NH Oberlies, MF Paine - Pharmacology & therapeutics, 2012 - Elsevier
Food–drug interaction studies are critical to evaluate appropriate dosing, timing, and
formulation of new drug candidates. These interactions often reflect prandial-associated …

Physiologically based mechanistic modelling to predict complex drug–drug interactions involving simultaneous competitive and time-dependent enzyme inhibition by …

KR Yeo, M Jamei, J Yang, GT Tucker… - European Journal of …, 2010 - Elsevier
AIM: To predict the magnitude of metabolic drug–drug interaction (mDDI) between triazolam
and diltiazem and its primary metabolite N-desmethyldiltiazem (MA). METHODS: Relevant in …

Molecular probes for human cytochrome P450 enzymes: Recent progress and future perspectives

J Wu, X Guan, Z Dai, R He, X Ding, L Yang… - Coordination Chemistry …, 2021 - Elsevier
The cytochrome P450 enzymes (P450s or CYPs) are a class of heme-containing
monooxygenases responsible for the oxidative metabolism of a wide range of endogenous …

Drugs as CYP3A probes, inducers, and inhibitors

YT Liu, HP Hao, CX Liu, GJ Wang… - Drug metabolism …, 2007 - Taylor & Francis
Human cytochrome P450 (CYP) 3A subfamily members (mainly CYP3A4 and CYP3A5)
mediate the metabolism of approximately half all marketed drugs and thus play a critical role …

Critique of the two-fold measure of prediction success for ratios: application for the assessment of drug-drug interactions

EJ Guest, L Aarons, JB Houston… - Drug metabolism and …, 2011 - ASPET
Current assessment of drug-drug interaction (DDI) prediction success is based on whether
predictions fall within a two-fold range of the observed data. This strategy results in a …