Results 291 to 300 of about 61,480 (319)

Human variability in CYP3A4 metabolism and CYP3A4-related uncertainty factors for risk assessment

Food and Chemical Toxicology, 2003
CYP3A4 constitutes the major liver cytochrome P450 isoenzyme and is responsible for the oxidation of more than 50% of all known drugs. Human variability in kinetics for this pathway has been quantified using a database of 15 compounds metabolised extensively (>60%) by this CYP isoform in order to develop CYP3A4-related uncertainty factors for the risk ...
Dorne, J.L.C.M., Walton, K., Renwick, A.G.   +2 more
openaire   +3 more sources

Utility of CYP3A4 and PXR-CAR-CYP3A4/3A7 Transgenic Mouse Models To Assess the Magnitude of CYP3A4 Mediated Drug–Drug Interactions

Molecular Pharmaceutics, 2017
Species differences in the expression, activity, regulation, and substrate specificity of metabolizing enzymes preclude the use of animal models to predict clinical drug-drug interactions (DDIs). The objective of this work is to determine if the transgenic (Tg) Cyp3a-/-Tg-3A4Hep/Int and Nr1i2/Nr1i3-/--Cyp3a-/-Tg-PXR-CAR-3A4/3A7Hep/Int (PXR-CAR-CYP3A4 ...
Justin Q. Ly, Kirsten Messick, Ann Qin, Ryan H. Takahashi, Edna F. Choo   +4 more
openaire   +2 more sources

CYP3A4*22 Impairs the Elimination of Ticagrelor, But Has No Significant Effect on the Bioactivation of Clopidogrel or Prasugrel

Clinical pharmacology and therapy, 2018
CYP3A enzymes participate in the elimination of ticagrelor and the bioactivation of clopidogrel and prasugrel. We studied the effects of functional CYP3A genetic variants (CYP3A4*22; rs35599367 and CYP3A5*3; rs776746) on the pharmacokinetics and ...
M. Holmberg, A. Tornio, M. Paile-Hyvärinen, E. Tarkiainen, M. Neuvonen, P. Neuvonen, J. Backman, M. Niemi   +7 more
semanticscholar   +1 more source

CYP3A4: The Workhorse

2015
This chapter discusses the genetics, metabolic actions, substrates, inducers, and inhibitors of cytochrome P450 3A4.
Jennifer DeCou, Nathaniel Birgenheier, Randal O. Dull   +2 more
openaire   +1 more source

CYP3A4-based drug–drug interaction: CYP3A4 substrates’ pharmacokinetic properties and ketoconazole dose regimen effect

European Journal of Drug Metabolism and Pharmacokinetics, 2014
The aim of the study was to assess the magnitude of the CYP3A4 inhibitory effect of 2 dosing regimens of ketoconazole and the influence of the pharmacokinetic properties of the CYP3A4 substrate on the extent of the substrate exposure increase. For this purpose, a clinical study was conducted and PBPK modeling simulations were performed.
Xavier, Boulenc, Olivier, Nicolas, Stéphanie, Hermabessière, Isabelle, Zobouyan, Valérie, Martin, Yves, Donazzolo, Céline, Ollier   +6 more
openaire   +2 more sources

CYP3A4-mediated pharmacokinetic interactions in cancer therapy.

Current Drug Metabolism, 2015
Cytochromes P450 enzymes, especially CYP3A4, are responsible for metabolizing a broad range of anticancer drugs. Combination therapy is common in patients with cancer, which may cause potential drug drug interactions (DDIs) leading to increased risk of side-effects/toxicity or decreased effectiveness.
Dandan Tian, Zheyi Hu
semanticscholar   +5 more sources

Metabolic Activation of Benzodiazepines by CYP3A4

Drug Metabolism and Disposition, 2009
Cytochrome P450 3A4 is the predominant isoform in liver, and it metabolizes more than 50% of the clinical drugs commonly used. However, CYP3A4 is also responsible for metabolic activation of drugs, leading to liver injury. Benzodiazepines are widely used as hypnotics and sedatives for anxiety, but some of them induce liver injury in humans.
Katsuhiko, Mizuno, Miki, Katoh, Hirotoshi, Okumura, Nao, Nakagawa, Toru, Negishi, Takanori, Hashizume, Miki, Nakajima, Tsuyoshi, Yokoi   +7 more
openaire   +2 more sources

Lessons from the CYP3A4 Promoter

Molecular Pharmacology, 2004
There is considerable interest in determining the molecular basis for human variation in drug response. Investigations over the past 20 years have largely focused on identifying polymorphisms in genes that encode drug metabolism enzymes.
openaire   +2 more sources

Transport and Metabolic Characterization of Caco-2 Cells Expressing CYP3A4 and CYP3A4 Plus Oxidoreductase

Pharmaceutical Research, 1999
To further characterize CYP3A4-transfected Caco-2 cells with regard to morphological, transport, and metabolic properties, and to evaluate a different Caco-2 cell strain transfected with both CYP3A4 and oxidoreductase (OR).Transfected Caco-2 cells, Caco-2 TC7 cells, and wild-type Caco-2 cells grown onto Millicell were used.
M, Hu, Y, Li, C M, Davitt, S M, Huang, K, Thummel, B W, Penman, C L, Crespi   +6 more
openaire   +2 more sources

Genetic epidemiology of induced CYP3A4 activity

Pharmacogenetics and Genomics, 2011
The cytochrome P450 3A4 (CYP3A4) enzyme is implicated in the metabolism of more than 50% of all prescribed medications and its activity - including induced or inhibited activity - is deemed to be a crucial determinant of interindividual variability in drug disposition, poor therapeutic efficacy, and adverse response to medication.We used the classical ...
Rahmioglu, Nilufer, Heaton, James, Clement, Gail, Gill, Raj, Surdulescu, Gabriela, Zlobecka, Karolina, Hodgkiss, Dylan, Ma, Yongmin, Hider, Robert C., Smith, Norman W., Ahmadi, Kourosh R.   +10 more
openaire   +3 more sources