In vitro-to-in vivo predictions of drug–drug interactions involving multiple reversible inhibitors

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Expert Opinion on Drug Metabolism & Toxicology

• Publication date

  2012-03-21

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1517/17425255.2012.667801PMID 22384784
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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• Qualitative Analysis of the Role of Metabolites in Inhibitory Drug‐Drug Interactions: literature evaluation based on the Metabolism and Transport Drug Interaction Database

  2009influential reference
• Predicting drug-drug interactions from in vitro drug metabolism data: challenges and recent advances.

  2009cited by this paper
• Multiple Inhibition Mechanisms and Prediction of Drug–Drug Interactions: Status of Metabolism and Transporter Models as Exemplified by Gemfibrozil–Drug Interactions

  2008cited by this paper
• The Influence of CYP3A5 Expression on the Extent of Hepatic CYP3A Inhibition Is Substrate-Dependent: An in Vitro-in Vivo Evaluation

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• An in Vitro Mechanistic Study to Elucidate the Desipramine/Bupropion Clinical Drug-Drug Interaction

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• Comparison of different approaches to predict metabolic drug–drug interactions

  2007cited by this paper
• Mechanism-Based Inactivation of Human Cytochrome P450 Enzymes and the Prediction of Drug-Drug Interactions

  2007cited by this paper
• Inhibitory Effects of Neurotransmitters and Steroids on Human CYP2A6

  2007cited by this paper
• CYP2C9 Inhibition: Impact of Probe Selection and Pharmacogenetics on in Vitro Inhibition Profiles

  2006influential reference
• STOCHASTIC PREDICTION OF CYP3A-MEDIATED INHIBITION OF MIDAZOLAM CLEARANCE BY KETOCONAZOLE

  2006cited by this paper
• INTERACTIONS OF TWO MAJOR METABOLITES OF PRASUGREL, A THIENOPYRIDINE ANTIPLATELET AGENT, WITH THE CYTOCHROMES P450

  2006cited by this paper
• In vitro cytochrome P450 inhibition data and the prediction of drug‐drug interactions: Qualitative relationships, quantitative predictions, and the rank‐order approach

  2005cited by this paper
• Prediction of in vivo drug-drug interactions from in vitro data: impact of incorporating parallel pathways of drug elimination and inhibitor absorption rate constant.

  2005cited by this paper
• IMPACT OF PARALLEL PATHWAYS OF DRUG ELIMINATION AND MULTIPLE CYTOCHROME P450 INVOLVEMENT ON DRUG-DRUG INTERACTIONS: CYP2D6 PARADIGM

  2005cited by this paper
• 'In silico' simulations to assess the 'in vivo' consequences of 'in vitro' metabolic drug-drug interactions.

  2004cited by this paper
• Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities.

  2004influential reference
• The effect of cimetidine on dextromethorphan O-demethylase activity of human liver microsomes and recombinant CYP2D6.

  2004cited by this paper
• EVIDENCE OF SIGNIFICANT CONTRIBUTION FROM CYP3A5 TO HEPATIC DRUG METABOLISM

  2004cited by this paper
• ROLE OF ITRACONAZOLE METABOLITES IN CYP3A4 INHIBITION

  2004cited by this paper
• Atomoxetine Hydrochloride: Clinical Drug-Drug Interaction Prediction and Outcome

  2004cited by this paper
• An evaluation of the in vitro metabolism data for predicting the clearance and drug-drug interaction potential of CYP2C9 substrates.

  2004cited by this paper
• Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites.

  2004cited by this paper
• Differences in the inhibition of cytochromes P450 3A4 and 3A5 by metabolite-inhibitor complex-forming drugs.

  2004cited by this paper
• A pharmacokinetic study comparing single and repeated oral doses of 20 mg and 40 mg omeprazole and its two optical isomers, S-omeprazole (esomeprazole) and R-omeprazole, in healthy subjects

  2004cited by this paper
• Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir.

  2003cited by this paper
• In vitro inhibitory effect of 1-aminobenzotriazole on drug oxidations catalyzed by human cytochrome P450 enzymes: a comparison with SKF-525A and ketoconazole.

  2003cited by this paper
• Impact of nonspecific binding to microsomes and phospholipid on the inhibition of cytochrome P4502D6: implications for relating in vitro inhibition data to in vivo drug interactions.

  2003cited by this paper
• Multisite kinetic analysis of interactions between prototypical CYP3A4 subgroup substrates: midazolam, testosterone, and nifedipine.

  2003cited by this paper
• Effects of gemfibrozil, itraconazole, and their combination on the pharmacokinetics and pharmacodynamics of repaglinide: potentially hazardous interaction between gemfibrozil and repaglinide

  2003cited by this paper
• Drug metabolism and drug interactions: application and clinical value of in vitro models.

  2003cited by this paper
• Plasma Concentrations of the Enantiomers of Fluoxetine and Norfluoxetine: Sources of Variability and Preliminary Observations on Relations With Clinical Response

  2002cited by this paper
• Interactions Between Antiretroviral Drugs and Drugs Used for the Therapy of the Metabolic Complications Encountered During HIV Infection

  2002cited by this paper
• Isoniazid is a mechanism-based inhibitor of cytochrome P450 1A2, 2A6, 2C19 and 3A4 isoforms in human liver microsomes

  2001cited by this paper
• Fluvoxamine‐theophylline interaction: Gap between in vitro and in vivo inhibition constants toward cytochrome P4501A2

  2001cited by this paper
• Fluvoxamine-theophylline interaction

  2001cited by this paper
• A novel testosterone 6 beta-hydroxylase activity assay for the study of CYP3A-mediated metabolism, inhibition, and induction in vitro.

  2001cited by this paper
• Inhibition of Cytochrome P450 (CYP450) Isoforms by Isoniazid: Potent Inhibition of CYP2C19 and CYP3A

  2001cited by this paper
• Inhibition of drug metabolism in human liver microsomes by nizatidine, cimetidine and omeprazole

  2001cited by this paper
• Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s.

  2001cited by this paper
• Potent inhibition of CYP2D6 by haloperidol metabolites: stereoselective inhibition by reduced haloperidol.

  2001cited by this paper
• 5-hydroxylation of omeprazole by human liver microsomal fractions from Chinese populations related to CYP2C19 gene dose and individual ethnicity.

  2000cited by this paper
• Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.

  2000cited by this paper
• In vitro inhibition of the cytochrome P450 (CYP450) system by the antiplatelet drug ticlopidine: potent effect on CYP2C19 and CYP2D6.

  2000cited by this paper
• In vitro inhibitory effects of troglitazone and its metabolites on drug oxidation activities of human cytochrome P450 enzymes: comparison with pioglitazone and rosiglitazone.

  2000cited by this paper
• Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug–drug interactions

  2000cited by this paper
• Inhibitory effects of amiodarone and its N-deethylated metabolite on human cytochrome P450 activities: prediction of in vivo drug interactions.

  2000cited by this paper
• Quantitative Prediction of In Vivo Drug-Drug Interactions from In Vitro Data Based on Physiological Pharmacokinetics: Use of Maximum Unbound Concentration of Inhibitor at the Inlet to the Liver

  2000cited by this paper
• Midazolam and triazolam biotransformation in mouse and human liver microsomes: relative contribution of CYP3A and CYP2C isoforms.

  2000cited by this paper
• Pharmacokinetic interaction between warfarin and a uricosuric agent, bucolome: application of In vitro approaches to predicting In vivo reduction of (S)-warfarin clearance.

  1999cited by this paper
• Inhibitory effects of azelastine and its metabolites on drug oxidation catalyzed by human cytochrome P-450 enzymes.

  1999cited by this paper
• Midazolam alpha-hydroxylation by human liver microsomes in vitro: inhibition by calcium channel blockers, itraconazole and ketoconazole.

  1999cited by this paper
• The 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor fluvastatin: effect on human cytochrome P-450 and implications for metabolic drug interactions.

  1999cited by this paper
• Effect of antipsychotic drugs on human liver cytochrome P-450 (CYP) isoforms in vitro: preferential inhibition of CYP2D6.

  1999cited by this paper
• Inhibition of cytochrome P-450 3A (CYP3A) in human intestinal and liver microsomes: comparison of Ki values and impact of CYP3A5 expression.

  1999cited by this paper
• The oxidative metabolism of metoprolol in human liver microsomes: inhibition by the selective serotonin reuptake inhibitors

  1998cited by this paper
• Terfenadine-antidepressant interactions: an in vitro inhibition study using human liver microsomes.

  1998cited by this paper
• Inhibition of S-warfarin metabolism by nonsteroidal antiinflammatory drugs in human liver microsomes in vitro.

  1998cited by this paper
• Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents.

  1998cited by this paper
• Characterization of the selectivity and mechanism of human cytochrome P450 inhibition by the human immunodeficiency virus-protease inhibitor nelfinavir mesylate.

  1998cited by this paper
• Biochemistry by numbers: simulation of biochemical pathways with Gepasi 3.

  1997cited by this paper
• Inhibition of coumarin 7-hydroxylase activity in human liver microsomes.

  1997cited by this paper
• Human liver cytochrome P450 enzymes involved in the 7-hydroxylation of R- and S-warfarin enantiomers.

  1997cited by this paper
• In vitro comparative inhibition profiles of major human drug metabolising cytochrome P450 isozymes (CYP2C9, CYP2D6 and CYP3A4) by HMG-CoA reductase inhibitors

  1996cited by this paper
• Interaction of human liver cytochromes P450 in vitro with LY307640, a gastric proton pump inhibitor.

  1996cited by this paper
• Inhibition of terfenadine metabolism in vitro by azole antifungal agents and by selective serotonin reuptake inhibitor antidepressants: relation to pharmacokinetic interactions in vivo.

  1996cited by this paper
• Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalyzed by human liver microsomes.

  1996cited by this paper
• Midazolam Hydroxylation by Human Liver Microsomes In Vitro: Inhibition by Fluoxetine, Norfluoxetine, and by Azole Antifungal Agents

  1996cited by this paper
• In vitro interaction of the antipsychotic agent olanzapine with human cytochromes P450 CYP2C9, CYP2C19, CYP2D6 and CYP3A.

  1996cited by this paper
• Phenacetin O-deethylation by human liver microsomes in vitro: inhibition by chemical probes, SSRI antidepressants, nefazodone and venlafaxine

  1996cited by this paper
• Inhibition of Human Cytochrome P450‐3A Isoforms by Fluoxetine and Norfluoxetine: In Vitro and In Vivo Studies

  1996cited by this paper
• Role of cytochrome P450 3A4 in human metabolism of MK-639, a potent human immunodeficiency virus protease inhibitor.

  1996cited by this paper
• Effect of Dirithromycin on Human CYP3A In Vitro and on Pharmacokinetics and Pharmacodynamics of Terfenadine In Vivo

  1996cited by this paper
• Inhibition of (S)-warfarin metabolism by sulfinpyrazone and its metabolites.

  1995cited by this paper
• Effect of fluoxetine, norfluoxetine, sertraline and desmethyl sertraline on human CYP3A catalyzed 1'-hydroxy midazolam formation in vitro.

  1995cited by this paper
• The effects of selective serotonin reuptake inhibitors and their metabolites on S-mephenytoin 4'-hydroxylase activity in human liver microsomes.

  1995cited by this paper
• Selective serotonin reuptake inhibitors and theophylline metabolism in human liver microsomes: potent inhibition by fluvoxamine.

  1995cited by this paper
• Metabolic interactions of methoxsalen and coumarin in humans and mice.

  1994cited by this paper
• Interaction of the enantiomers of fluoxetine and norfluoxetine with human liver cytochromes P450.

  1993cited by this paper
• Quantification and mechanism of the fluoxetine and tricyclic antidepressant interaction

  1992cited by this paper
• Metabolic enantiomeric interactions: the inhibition of human (S)-warfarin-7-hydroxylase by (R)-warfarin.

  1991cited by this paper
• Clinical pharmacokinetics : concepts and applications

  1989cited by this paper
• In vitro inhibition studies of tolbutamide hydroxylase activity of human liver microsomes by azoles, sulphonamides and quinolines.

  1988cited by this paper
• Tolbutamide 4-hydroxylase activity of human liver microsomes: effect of inhibitors.

  1987cited by this paper
• Prediction of hepatic extraction ratio from in vitro measurement of intrinsic clearance.

  1977cited by this paper
• Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady-State Enzyme Systems

  1975influential reference

• Role of metabolites in drug-drug interactions.

  2025cites this paper
• Drug-drug interaction potentials of tucatinib inhibition of human UDP-glucuronosyltransferases.

  2023cites this paper
• Inhibition of human UDP-glucuronosyltransferase enzyme by ripretinib: Implications for drug-drug interactions.

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  2021cites this paper
• Inhibition and induction of CYP enzymes in humans: an update

  2020cites this paper
• In vitro characterization and in vitro to in vivo predictions of drug-drug interactions

  2020cites this paper
• Abemaciclib Inhibits Renal Tubular Secretion Without Changing Glomerular Filtration Rate

  2018cites this paper
• Accurate Estimation of In Vivo Inhibition Constants of Inhibitors and Fraction Metabolized of Substrates with Physiologically Based Pharmacokinetic Drug–Drug Interaction Models Incorporating Parent Drugs and Metabolites of Substrates with Cluster Newton Method

  2018cites this paper
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  2017cites this paper
• An S‐warfarin and AZD1981 interaction: in vitro and clinical pilot data suggest the N‐deacetylated amino acid metabolite as the primary perpetrator

  2017cites this paper
• Pharmacokinetics and Physiologically Based Pharmacokinetic Modeling of Xenobiotic Disposition in Special Populations

  2017cites this paper
• In vitro to in vivo extrapolation of the complex drug‐drug interaction of bupropion and its metabolites with CYP2D6; simultaneous reversible inhibition and CYP2D6 downregulation

  2017cites this paper
• Application of Static Models to Predict Midazolam Clinical Interactions in the Presence of Single or Multiple Hepatitis C Virus Drugs

  2016cites this paper
• Enantioselective inhibition of Cytochrome P450-mediated drug metabolism by a novel antithrombotic agent, S002-333: Major effect on CYP2B6.

  2016cites this paper
• Chiral Plasma Pharmacokinetics and Urinary Excretion of Bupropion and Metabolites in Healthy Volunteers

  2016influential citation
• Integrated approach to structure-based enzymatic drug design: molecular modeling, spectroscopy, and experimental bioactivity.

  2014cites this paper
• Effects of cytochrome P450 enzyme inhibitors and inducers on the metabolism of S-ketamine

  2013cites this paper
• The evolution of our understanding of endo-xenobiotic crosstalk and cytochrome P450 regulation and the therapeutic implications

  2013cites this paper
• ATP-Binding-Cassette Transporters in Biliary Efflux and Drug-Induced Liver Injury

  2013influential citation
• Prediction of in vivo metabolite disposition and complex metabolite-dependent drug-drug interactions

  2013cites this paper
• Special Section on Prediction of Human Pharmacokinetic Parameters from In Vitro Systems Stereoselective Inhibition of CYP2C19 and CYP3A4 by Fluoxetine and Its Metabolite: Implications for Risk Assessment of Multiple Time-Dependent Inhibitor Systems s

  2013cites this paper
• Stereoselective Inhibition of CYP2C19 and CYP3A4 by Fluoxetine and Its Metabolite: Implications for Risk Assessment of Multiple Time-Dependent Inhibitor Systems

  2013cites this paper
• Special Section on Prediction of Human Pharmacokinetic Parameters from In Vitro Systems Stereoselective Inhibition of CYP2C19 and CYP3A4 by Fluoxetine and Its Metabolite: Implications for Risk Assessment of Multiple Time- Dependent Inhibitor Systems s

  2013cites this paper
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  2012influential citation