Evaluation of the Pharmacokinetics of Felcisetrag (TAK‐954), a 5‐HT4 Receptor Agonist, in the Presence and Absence of Itraconazole, a Potent CYP3A4 Inhibitor
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DOI: 10.1002/cpdd.1046
Abstract: The 5‐hydroxytryptamine type‐4 receptor agonist felcisetrag (TAK‐954) is being investigated for improving gastrointestinal motility in postoperative gastrointestinal dysfunction. Polypharmacy often occurs in this setting, and as in vitro data indicate, felcisetrag is primarily metabolized by… read more here.
Keywords: tak 954; cyp3a4; period; felcisetrag tak ... See more keywords
Prediction of the Impact of Cytochrome P450 2C9 Genotypes on the Drug–Drug Interaction Potential of Siponimod With Physiologically‐Based Pharmacokinetic Modeling: A Comprehensive Approach for Drug Label Recommendations
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DOI: 10.1002/cpt.1547
Abstract: We predicted the drug–drug interaction (DDI) potential of siponimod in presence of cytochrome P450 (CYP)2C9/CYP3A4 inhibitors/inducers in subjects with different CYP2C9 genotypes by physiologically‐based pharmacokinetic (PK) modeling. The model was established using in vitro and… read more here.
Keywords: siponimod; drug interaction; potential siponimod; drug ... See more keywords
An in vitro system for measuring genotoxicity mediated by human CYP3A4 in Saccharomyces cerevisiae
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DOI: 10.1002/em.22093
Abstract: P450 activity is required to metabolically activate many chemical carcinogens, rendering them highly genotoxic. CYP3A4 is the most abundantly expressed P450 enzyme in the liver, accounting for most drug metabolism and constituting 50% of all… read more here.
Keywords: saccharomyces cerevisiae; genotoxicity; human cyp3a4; yeast ... See more keywords
Use of Physiologically Based Pharmacokinetic Modeling to Evaluate the Impact of Chronic Kidney Disease on CYP3A4‐Mediated Metabolism of Saxagliptin
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DOI: 10.1002/jcph.2043
Abstract: We characterized the impact of chronic kidney disease (CKD) on the cytochrome P450 (CYP) 3A4–mediated metabolism of saxagliptin to its metabolite, 5‐hydroxysaxagliptin, using a physiologically based pharmacokinetic (PBPK) model. A PBPK model of saxagliptin and… read more here.
Keywords: metabolism saxagliptin; cyp3a4 activity; cyp3a4; impact ... See more keywords
Effect of panaxytriol on cytochrome P450 3A4 via the pregnane X receptor regulatory pathway
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DOI: 10.1002/ptr.6290
Abstract: Panaxytriol (PXT) is one of the major effective components of red ginseng and Shenmai injection. The present study aimed to explore the effect of PXT on cytochrome P450 3A4 (CYP3A4) based on the pregnane X… read more here.
Keywords: regulatory pathway; cyp3a4; hepg2 cells; hepg2 ... See more keywords
Interaction potential of the dual orexin receptor antagonist ACT-541468 with CYP3A4 and food: results from two interaction studies
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DOI: 10.1007/s00228-018-2559-5
Abstract: PurposeACT-541468 is a novel dual orexin receptor antagonist (DORA) under development for the treatment of insomnia. In vitro studies suggested a significant role of CYP3A4 in ACT-541468 metabolism and an impact on CYP3A4 activity.MethodsSubsequently, two… read more here.
Keywords: act; act 541468; dual orexin; interaction ... See more keywords
In vitro and clinical investigations to determine the drug-drug interaction potential of entrectinib, a small molecule inhibitor of neurotrophic tyrosine receptor kinase (NTRK)
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DOI: 10.1007/s10637-021-01156-9
Abstract: Background Entrectinib is a CNS-active, potent inhibitor of tyrosine receptor kinases A/B/C, ROS1 and anaplastic lymphoma kinase approved for use in patients with solid tumors. We describe the in vitro and clinical studies investigating potential… read more here.
Keywords: inhibitor; entrectinib; vitro clinical; drug ... See more keywords
Genotyping and phenotyping CYP3A4\CYP3A5: no association with antiplatelet effect of clopidogrel
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DOI: 10.1007/s11033-019-04871-y
Abstract: The objective of this study was to determine the impact of polymorphism of CYP3A subfamily isoenzymes (allelic variants of CYP3A4*22 and CYP3A5*3) on the efficacy clopidogrel in patients with an acute coronary syndrome (ACS), who… read more here.
Keywords: clopidogrel; cyp3a4 cyp3a5; phenotyping cyp3a4; antiplatelet effect ... See more keywords
Effects of diltiazem, a moderate inhibitor of CYP3A4, on the pharmacokinetics of tamsulosin in different CYP2D6 genotypes
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DOI: 10.1007/s12272-018-1030-6
Abstract: Tamsulosin, a selective antagonist of the α1-adrenoceptor, is primarily metabolized by CYP3A4 and CYP2D6, and tamsulosin exposure is significantly increased according to the genetic polymorphism of CYP2D6. In this study, we investigated the effects of… read more here.
Keywords: different cyp2d6; tamsulosin; cyp2d6 genotypes; cyp3a4 ... See more keywords
A New CYP3A5*3 and CYP3A4*22 Cluster Influencing Tacrolimus Target Concentrations: A Population Approach
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DOI: 10.1007/s40262-016-0491-3
Abstract: BackgroundSingle nucleotide polymorphisms (SNPs) in the CYP3A5 and CYP3A4 genes have been reported to be an important cause of variability in the pharmacokinetics of tacrolimus in renal transplant patients. The aim of this study was… read more here.
Keywords: cyp3a4; model; renal transplant; cyp3a5 cyp3a4 ... See more keywords
Levomepromazine and clozapine induce the main human cytochrome P450 drug metabolizing enzyme CYP3A4
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DOI: 10.1007/s43440-020-00157-4
Abstract: Background Cytochrome P450 (CYP) enzymes are involved in the metabolism of many important endogenous substrates (steroids, melatonin), drugs and toxic xenobiotics. Their induction accelerates drug metabolism and elimination. The present study aimed at examining the… read more here.
Keywords: clozapine induce; clozapine; cyp3a4; levomepromazine clozapine ... See more keywords