Search Results - "Thummel, KE"
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EVIDENCE OF SIGNIFICANT CONTRIBUTION FROM CYP3A5 TO HEPATIC DRUG METABOLISM
Published in Drug metabolism and disposition (01-12-2004)“…CYP3A4 and CYP3A5 exhibit significant overlap in substrate specificity but can differ in product regioselectivity and formation activity. To further explore…”
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2
Clinical Pharmacogenetics Implementation Consortium (CPIC) Guidelines for CYP3A5 Genotype and Tacrolimus Dosing
Published in Clinical pharmacology and therapeutics (01-07-2015)“…Tacrolimus is the mainstay immunosuppressant drug used after solid organ and hematopoietic stem cell transplantation. Individuals who express CYP3A5 (extensive…”
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3
Enzyme-catalyzed processes of first-pass hepatic and intestinal drug extraction
Published in Advanced drug delivery reviews (15-09-1997)“…Oral bioavailability of pharmacologically effective drugs is often limited by first-pass biotransformation. In humans, both hepatic and intestinal enzymes can…”
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Fentanyl Metabolism by Human Hepatic and Intestinal Cytochrome P450 3A4: Implications for Interindividual Variability in Disposition, Efficacy, and Drug Interactions
Published in Drug metabolism and disposition (01-09-1997)“…The synthetic opioid fentanyl undergoes extensive metabolism in humans. Systemic elimination occurs primarily by hepatic metabolism. When administered as a…”
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Effects of Pregnancy on CYP3A and P-glycoprotein Activities as Measured by Disposition of Midazolam and Digoxin: A University of Washington Specialized Center of Research Study
Published in Clinical pharmacology and therapeutics (01-08-2008)“…The objectives of the study were to evaluate the effects of pregnancy on CYP3A and P‐glycoprotein (P‐gp) activities, as measured by disposition of midazolam…”
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Ethanol and production of the hepatotoxic metabolite of acetaminophen in healthy adults
Published in Clinical pharmacology and therapeutics (01-06-2000)“…Background Recent case reports suggest that consumption of ethanol may increase the risk of liver injury induced by acetaminophen (INN, paracetamol). However,…”
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Assessment of the Impact of Renal Impairment on Systemic Exposure of New Molecular Entities: Evaluation of Recent New Drug Applications
Published in Clinical pharmacology and therapeutics (01-03-2009)“…The US Food and Drug Administration (FDA) is currently developing a guidance for industry to replace a previous guidance, “Pharmacokinetics in Patients With…”
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Comparison of CYP2D6 content and metoprolol oxidation between microsomes isolated from human livers and small intestines
Published in Pharmaceutical research (01-08-1999)“…To assess the role of intestinal CYP2D6 in oral first-pass drug clearance by comparing the enzyme content and catalytic activity of a prototype CYP2D6…”
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Human liver microsomal enflurane defluorination catalyzed by cytochrome P-450 2E1
Published in Drug metabolism and disposition (01-03-1993)“…The volatile anesthetic agent enflurane undergoes oxidative metabolism in human liver, yielding both inorganic and organic fluoride metabolites. Numerous…”
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10
Effect of VKORC1 Haplotypes on Transcriptional Regulation and Warfarin Dose
Published in The New England journal of medicine (02-06-2005)“…The gene encoding vitamin K epoxide reductase complex 1 ( VKORC1 ) is the target of warfarin, and a variant of the gene may be associated with variations in…”
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Genetic contribution to variable human CYP3A-mediated metabolism
Published in Advanced drug delivery reviews (18-11-2002)“…The human CYP3A subfamily plays a dominant role in the metabolic elimination of more drugs than any other biotransformation enzyme. CYP3A enzyme is localized…”
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Human UGT1A4 and UGT1A3 Conjugate 25-Hydroxyvitamin D3: Metabolite Structure, Kinetics, Inducibility, and Interindividual Variability
Published in Endocrinology (Philadelphia) (01-06-2014)“…25-Hydroxyvitamin D3 (25OHD3) is used as a clinical biomarker for assessment of vitamin D status. Blood levels of 25OHD3 represent a balance between its…”
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13
Evaluation of 6β‐Hydroxycortisol, 6β‐Hydroxycortisone, and a Combination of the Two as Endogenous Probes for Inhibition of CYP3A4 In Vivo
Published in Clinical pharmacology and therapeutics (01-06-2011)“…An endogenous probe for CYP3A activity would be useful for early identification of in vivo cytochrome P450 (CYP) 3A4 inhibitors. The aim of this study was to…”
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EFFECT OF CYP3A5 POLYMORPHISM ON TACROLIMUS METABOLIC CLEARANCE IN VITRO
Published in Drug metabolism and disposition (01-05-2006)“…Previous investigations of solid organ transplant patients treated with tacrolimus showed that individuals carrying a CYP3A5*1 allele have lower dose-adjusted…”
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15
Genetic Risk Factors for Major Bleeding in Patients Treated With Warfarin in a Community Setting
Published in Clinical pharmacology and therapeutics (01-06-2014)“…The influence of warfarin pharmacogenomics on major bleeding risk has been little studied in long‐term users and non–specialist care settings. We conducted a…”
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In vitro and in vivo drug interactions involving human CYP3A
Published in Annual review of pharmacology and toxicology (01-01-1998)“…Cytochrome P4503A (CYP3A) is importantly involved in the metabolism of many chemically diverse drugs administered to humans. Moreover, its localization in high…”
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ROLE OF ITRACONAZOLE METABOLITES IN CYP3A4 INHIBITION
Published in Drug metabolism and disposition (01-10-2004)“…Itraconazole (ITZ) is a potent inhibitor of CYP3A in vivo. However, unbound plasma concentrations of ITZ are much lower than its reported in vitro K i , and no…”
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Accurate Prediction of Dose‐Dependent CYP3A4 Inhibition by Itraconazole and Its Metabolites From In Vitro Inhibition Data
Published in Clinical pharmacology and therapeutics (01-10-2010)“…Inhibitory drug metabolites may contribute to drug–drug interactions (DDIs). The aim of this study was to determine the importance of inhibitory metabolites of…”
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Co-regulation of CYP3A4 and CYP3A5 and contribution to hepatic and intestinal midazolam metabolism
Published in Molecular pharmacology (01-07-2002)“…We recently demonstrated that a variant allele of CYP3A5 (CYP3A5*3) confers low CYP3A5 expression as a result of improper mRNA splicing. In this study, we…”
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Ethical Issues in Developing Pharmacogenetic Research Partnerships With American Indigenous Communities
Published in Clinical pharmacology and therapeutics (01-03-2011)“…Pharmacogenetic research offers the potential to improve the safety and efficacy of drug prescribing. Assuring that the benefits of this research reach…”
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