gemfibrozil and gemfibrozil 1-o-acylglucuronide

gemfibrozil has been researched along with gemfibrozil 1-o-acylglucuronide in 17 studies

Research

Studies (17)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's4 (23.53)18.2507
2000's7 (41.18)29.6817
2010's6 (35.29)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Ballard, TE; Henderson, JL; Kalgutkar, AS; Obach, RS; Orr, ST; Ripp, SL; Scott, DO; Sun, H1
Dalvie, D; Fu, Y; Khojasteh, SC; Ma, Y; Zhang, D1
Fairchild, BA; Sallustio, BC1
Evans, AM; Fairchild, BA; Nation, RL; Sallustio, BC; Shanahan, K1
Fairchild, BA; Pannall, PR; Sallustio, BC1
Evans, AM; Nation, RL; Sabordo, L; Sallustio, BC2
Charman, WN; Prankerd, RJ; Scanlon, MJ; Shackleford, DM1
Brogan, LR; Evans, AM; Lucas, AN; Milne, RW; Nation, RL; Shackleford, DM1
Gipson, AE; Holsapple, J; Li, W; Ogilvie, BW; Parkinson, A; Rodrigues, AD; Toren, P; Zhang, D1
Backman, JT; Kalliokoski, A; Laitila, J; Neuvonen, M; Neuvonen, PJ; Niemi, M; Tornio, A1
Allen, A; Baer, BR; DeLisle, RK1
Backman, JT; Honkalammi, J; Kurkinen, KJ; Neuvonen, M; Neuvonen, PJ; Niemi, M; Tornio, A1
Backman, JT; Karonen, T; Neuvonen, PJ1
Backman, JT; Honkalammi, J; Neuvonen, PJ; Niemi, M1
Backman, JT; Neuvonen, PJ; Niemi, M; Tornio, A1
Dai, M; Lin, H; Lin, J; Liu, A; Luo, M; Xie, M; Yang, J1

Reviews

3 review(s) available for gemfibrozil and gemfibrozil 1-o-acylglucuronide

ArticleYear
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
    Journal of medicinal chemistry, 2012, Jun-14, Volume: 55, Issue:11

    Topics: Animals; Apoproteins; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Discovery; Drug Interactions; Heme; Humans; Models, Biological; Pharmacokinetics; Structure-Activity Relationship; Time Factors

2012
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).
    Journal of medicinal chemistry, 2017, 11-09, Volume: 60, Issue:21

    Topics: Anions; Binding Sites; Cytochrome P-450 CYP2C8; Drug Interactions; Glucuronides; Humans; Ligands

2017
Role of gemfibrozil as an inhibitor of CYP2C8 and membrane transporters.
    Expert opinion on drug metabolism & toxicology, 2017, Volume: 13, Issue:1

    Topics: Cytochrome P-450 CYP2C8; Cytochrome P-450 CYP2C8 Inhibitors; Drug Interactions; Gemfibrozil; Glucuronates; Humans; Hypolipidemic Agents; Membrane Transport Proteins

2017

Trials

5 trial(s) available for gemfibrozil and gemfibrozil 1-o-acylglucuronide

ArticleYear
The effect of gemfibrozil on repaglinide pharmacokinetics persists for at least 12 h after the dose: evidence for mechanism-based inhibition of CYP2C8 in vivo.
    Clinical pharmacology and therapeutics, 2008, Volume: 84, Issue:3

    Topics: Adult; Area Under Curve; Aryl Hydrocarbon Hydroxylases; Blood Glucose; Carbamates; Cytochrome P-450 CYP2C8; Drug Interactions; Female; Gemfibrozil; Glucuronates; Half-Life; Humans; Hypoglycemic Agents; Hypolipidemic Agents; Male; Piperidines

2008
CYP2C8 activity recovers within 96 hours after gemfibrozil dosing: estimation of CYP2C8 half-life using repaglinide as an in vivo probe.
    Drug metabolism and disposition: the biological fate of chemicals, 2009, Volume: 37, Issue:12

    Topics: Administration, Oral; Area Under Curve; Aryl Hydrocarbon Hydroxylases; Biotransformation; Blood Glucose; Carbamates; Cross-Over Studies; Cytochrome P-450 CYP2C8; Drug Interactions; Enzyme Inhibitors; Female; Gemfibrozil; Genotype; Glucuronates; Half-Life; Humans; Hypoglycemic Agents; Hypolipidemic Agents; Liver-Specific Organic Anion Transporter 1; Male; Models, Biological; Molecular Probes; Organic Anion Transporters; Phenotype; Piperidines; Young Adult

2009
The CYP2C8 inhibitor gemfibrozil does not affect the pharmacokinetics of zafirlukast.
    European journal of clinical pharmacology, 2011, Volume: 67, Issue:2

    Topics: Adult; Aryl Hydrocarbon Hydroxylases; Cross-Over Studies; Cytochrome P-450 CYP2C8; Drug Interactions; Female; Gemfibrozil; Glucuronates; Humans; Indoles; Male; Phenylcarbamates; Sulfonamides; Tosyl Compounds; Young Adult

2011
Mechanism-based inactivation of CYP2C8 by gemfibrozil occurs rapidly in humans.
    Clinical pharmacology and therapeutics, 2011, Volume: 89, Issue:4

    Topics: Adult; Area Under Curve; Aryl Hydrocarbon Hydroxylases; Carbamates; Cross-Over Studies; Cytochrome P-450 CYP2C8; Female; Gemfibrozil; Glucuronates; Humans; Hypoglycemic Agents; Male; Piperidines; Time Factors

2011
Species-related exposure of phase II metabolite gemfibrozil 1-O-β-glucuronide between human and mice: A net induction of mouse P450 activity was revealed.
    Biopharmaceutics & drug disposition, 2017, Volume: 38, Issue:9

    Topics: Adult; Animals; Cytochrome P-450 Enzyme Inducers; Cytochrome P-450 Enzyme System; Drug Interactions; Gemfibrozil; Glucuronates; Humans; Hypolipidemic Agents; Liver; Male; Mice; Species Specificity; Time Factors; Young Adult

2017

Other Studies

9 other study(ies) available for gemfibrozil and gemfibrozil 1-o-acylglucuronide

ArticleYear
Biosynthesis, characterisation and direct high-performance liquid chromatographic analysis of gemfibrozil 1-O-beta-acylglucuronide.
    Journal of chromatography. B, Biomedical applications, 1995, Mar-24, Volume: 665, Issue:2

    Topics: Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Drug Stability; Gemfibrozil; Glucuronates; Humans; Hydrogen-Ion Concentration; Magnetic Resonance Spectroscopy; Mass Spectrometry; Quality Control

1995
Disposition of gemfibrozil and gemfibrozil acyl glucuronide in the rat isolated perfused liver.
    Drug metabolism and disposition: the biological fate of chemicals, 1996, Volume: 24, Issue:9

    Topics: Animals; Bile; Gemfibrozil; Glucuronates; Hypolipidemic Agents; In Vitro Techniques; Kinetics; Liver; Male; Perfusion; Rats; Rats, Sprague-Dawley

1996
Interaction of human serum albumin with the electrophilic metabolite 1-O-gemfibrozil-beta-D-glucuronide.
    Drug metabolism and disposition: the biological fate of chemicals, 1997, Volume: 25, Issue:1

    Topics: Diazepam; Gemfibrozil; Glucuronates; Half-Life; Humans; Hydrogen-Ion Concentration; Hypolipidemic Agents; Male; Oxyphenbutazone; Pilot Projects; Protein Binding; Serum Albumin; Time Factors

1997
Hepatic disposition of the acyl glucuronide1-O-gemfibrozil-beta-D-glucuronide: effects of dibromosulfophthalein on membrane transport and aglycone formation.
    The Journal of pharmacology and experimental therapeutics, 1999, Volume: 288, Issue:2

    Topics: Animals; Biological Transport; Cell Membrane; Female; Gemfibrozil; Glucuronates; Hypolipidemic Agents; Liver; Male; Perfusion; Protein Binding; Rats; Rats, Sprague-Dawley; Sulfobromophthalein

1999
Hepatic disposition of the acyl glucuronide 1-O-gemfibrozil-beta-D-glucuronide: effects of clofibric acid, acetaminophen, and acetaminophen glucuronide.
    The Journal of pharmacology and experimental therapeutics, 2000, Volume: 295, Issue:1

    Topics: Acetaminophen; Animals; Biological Transport; Clofibric Acid; Gemfibrozil; Glucuronates; Liver; Male; Perfusion; Rats; Rats, Sprague-Dawley

2000
Self-micellization of gemfibrozil 1-O-beta acyl glucuronide in aqueous solution.
    Pharmaceutical research, 2003, Volume: 20, Issue:3

    Topics: Calorimetry; Chemistry, Pharmaceutical; Drug Compounding; Gemfibrozil; Glucuronates; Hydrogen-Ion Concentration; Magnetic Resonance Spectroscopy; Micelles; Pharmaceutical Solutions; Surface Tension; Water

2003
The effects of the phytoestrogenic isoflavone genistein on the hepatic disposition of preformed and hepatically generated gemfibrozil 1-O-acyl glucuronide in the isolated perfused rat liver.
    The Journal of pharmacy and pharmacology, 2003, Volume: 55, Issue:10

    Topics: Animals; Chemotherapy, Cancer, Regional Perfusion; Drug Interactions; Enzyme Inhibitors; Gemfibrozil; Genistein; Glucuronates; Kinetics; Liver; Male; Organ Culture Techniques; Rats; Rats, Sprague-Dawley

2003
Glucuronidation converts gemfibrozil to a potent, metabolism-dependent inhibitor of CYP2C8: implications for drug-drug interactions.
    Drug metabolism and disposition: the biological fate of chemicals, 2006, Volume: 34, Issue:1

    Topics: Alamethicin; Aryl Hydrocarbon Hydroxylases; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP2C8; Dose-Response Relationship, Drug; Drug Interactions; Gemfibrozil; Glucuronates; Glucuronides; Humans; Hypolipidemic Agents; Mass Spectrometry; Microsomes, Liver; Uridine Diphosphate Glucuronic Acid

2006
Benzylic oxidation of gemfibrozil-1-O-beta-glucuronide by P450 2C8 leads to heme alkylation and irreversible inhibition.
    Chemical research in toxicology, 2009, Volume: 22, Issue:7

    Topics: Alkylation; Aryl Hydrocarbon Hydroxylases; Catalytic Domain; Chromatography, High Pressure Liquid; Computer Simulation; Cytochrome P-450 CYP2C8; Gemfibrozil; Glucuronates; Heme; Humans; Hypolipidemic Agents; Mass Spectrometry; Oxidation-Reduction; Recombinant Proteins

2009