Results 171 to 180 of about 76,948 (211)

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

Effect of Mibefradil on CYP3A4 In Vivo

The Journal of Clinical Pharmacology, 2003
Mibefradil, a calcium channel blocker, was removed from the market because of adverse drug interactions with coadministered CYP3A4 substrates. This study examined the effect of mibefradil on the activity of hepatic and intestinal CYP3A4 in vivo, employing the erythromycin breath test (EBT) and oral midazolam pharmacokinetics.
Maria L, Veronese, Lisa P, Gillen, Ellen P, Dorval, Walter W, Hauck, Scott A, Waldman, Howard E, Greenberg   +5 more
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Pioglitazone: Effect on CYP3A4 Activity

The Journal of Clinical Pharmacology, 2002
Clinical studies demonstrate CYP3A4 enzyme induction with troglitazone, a thiazolidinedione derivative structurally related to pioglitazone. The objective of this prospective, open‐label study conducted in healthy volunteers was to evaluate the influence of multiple‐dose pioglitazone therapy on the urinary excretion ratio of 6‐β‐hydroxycortisol to ...
Sandra N, Nowak, David J, Edwards, Anthony, Clarke, Gail D, Anderson, Linda A, Jaber   +4 more
openaire   +2 more sources

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

Functional Gene Variants of CYP3A4

Clinical Pharmacology & Therapeutics, 2014
Cytochrome P450 3A4 (CYP3A4) is involved in the metabolism of more drugs in clinical use than any other foreign compound-metabolizing enzyme in humans. Recently, increasing evidence has been found showing that variants in the CYP3A4 gene have functional significance and--in rare cases--lead to loss of activity, implying tremendous consequences for ...
A N, Werk, I, Cascorbi
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CYP3A4*16 and CYP3A4*18 Alleles Found in East Asians Exhibit Differential Catalytic Activities for Seven CYP3A4 Substrate Drugs

Drug Metabolism and Disposition, 2010
CYP3A4, the major form of cytochrome P450 (P450) expressed in the adult human liver, is involved in the metabolism of approximately 50% of commonly prescribed drugs. Several genetic polymorphisms in CYP3A4 are known to affect its catalytic activity and to contribute in part to interindividual differences in the pharmacokinetics and pharmacodynamics of ...
Keiko, Maekawa, Noriko, Harakawa, Takuya, Yoshimura, Su-Ryang, Kim, Yoshiyuki, Fujimura, Fumika, Aohara, Kimie, Sai, Noriko, Katori, Masahiro, Tohkin, Mikihiko, Naito, Ryuichi, Hasegawa, Haruhiro, Okuda, Jun-ichi, Sawada, Takuro, Niwa, Yoshiro, Saito   +14 more
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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

CYP3A4 variant alleles in white individuals with low CYP3A4 enzyme activity

Clinical Pharmacology & Therapeutics, 2002
ObjectiveOur objective was to evaluate the presence of CYP3A4 gene variants in white individualswith low CYP3A4 enzyme activity.MethodsPersons with extremely low enzyme activity, either in vitro or in vivo, were selected in a panel of 97 healthy subjects. Genetic analyses for CYP3A4 variant alleles present in white subjects, including CYP3A4*1B, CYP3A4*
Elena, García-Martín, Carmen, Martínez, Rosa M, Pizarro, Francisco J, García-Gamito, Harriet, Gullsten, Hannu, Raunio, José A G, Agúndez   +6 more
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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

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.
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