Page last updated: 2024-09-04

ezetimibe and sch 60663

ezetimibe has been researched along with sch 60663 in 18 studies

Compound Research Comparison

Studies
(ezetimibe)
Trials
(ezetimibe)
Recent Studies (post-2010)
(ezetimibe)
Studies
(sch 60663)
Trials
(sch 60663)
Recent Studies (post-2010) (sch 60663)
2,4845631,46523411

Protein Interaction Comparison

ProteinTaxonomyezetimibe (IC50)sch 60663 (IC50)
Niemann-Pick C1-like 1 proteinCanis lupus familiaris (dog)0.06
Niemann-Pick C1-like 1 proteinMacaca mulatta (Rhesus monkey)0.03
NPC1-like intracellular cholesterol transporter 1Rattus norvegicus (Norway rat)0.58
NPC1-like intracellular cholesterol transporter 1Homo sapiens (human)0.3

Research

Studies (18)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's1 (5.56)18.2507
2000's8 (44.44)29.6817
2010's8 (44.44)24.3611
2020's1 (5.56)2.80

Authors

AuthorsStudies
Davis, HR; Vaccaro, WD1
Altmann, SW; Browne, ME; Burnett, DA; Caplen, MA; Clader, JW; Davis, HR; Zhau, H1
Auerbach, B; Barton, T; Bousley, R; Cai, H; Davis, J; Esmaiel, N; Larsen, SD; Mertz, T; Mueller, SB; Olsen, K; Pfefferkorn, JA; Sorenson, R; Van Huis, C; Welch, K; Winters, T; Wolfram, TJ; Wu, C1
Canet, MJ; Cherrington, NJ; Fisher, CD; Hardwick, RN; Street, SM1
Alton, KB; Compton, DS; Davis, HR; Farley, C; Hoos, L; Sybertz, EJ; van Heek, M1
Affrime, M; Alton, KB; Cayen, MN; Chowdhury, S; Iannucci, R; Kosoglou, T; Maxwell, SE; Patrick, JE; Statkevich, P; Stauber, KL; Zhu, Y1
Achari, R; Burt, DA; Chira, T; Edeki, T; Gustavson, LE; Kelly, MT; Rieser, MJ; Schweitzer, SM; Yannicelli, HD1
Basha, SJ; Kumar, NV; Kumar, TR; Mullangi, R; Muzeeb, S; Naveed, SA; Rao, NP; Shashikumar, D; Srinivas, N; Srinivas, NR; Tiwari, NK1
Koll, C; Oswald, S; Siegmund, W1
de Waart, DR; Kunne, C; Oude Elferink, RP; Schinkel, AH; Vlaming, ML1
Lütjohann, D; May, K; Oswald, S; Rosin, J; Siegmund, W1
Bae, JW; Choi, CI; Chung, MW; Jang, CG; Lee, JH; Lee, SY1
Auge, D; Fahrmayr, C; Fromm, MF; König, J; Mieth, M1
Ban, MR; DeGorter, MK; Hegele, RA; Kim, RB; Schwarz, UI; Tirona, RG; Ziada, A1
Chiba, T; Kawagishi, H; Kimura, Y; Kioka, N; Matsuo, M; Sakurada, T; Ueda, K; Watanabe, R; Yamaguchi, K1
Guo, L; He, M; Jiang, J; Qiu, FR; Wang, MM1
Karalis, V; Soulele, K1
Kagatani, S; Nakagami, H; Sasagane, Y; Wada, S1

Trials

4 trial(s) available for ezetimibe and sch 60663

ArticleYear
Disposition of the selective cholesterol absorption inhibitor ezetimibe in healthy male subjects.
    Drug metabolism and disposition: the biological fate of chemicals, 2002, Volume: 30, Issue:4

    Topics: Adult; Anticholesteremic Agents; Area Under Curve; Azetidines; Biotransformation; Chromatography, Liquid; Enterohepatic Circulation; Ezetimibe; Feces; Humans; Male; Mass Spectrometry; Urine

2002
Evaluation of the potential for pharmacokinetic interaction between fenofibrate and ezetimibe: A phase I, open-label, multiple-dose, three-period crossover study in healthy subjects.
    Clinical therapeutics, 2006, Volume: 28, Issue:3

    Topics: Adult; Azetidines; Cross-Over Studies; Drug Interactions; Drug Therapy, Combination; Ezetimibe; Female; Fenofibrate; Glucuronides; Humans; Hypolipidemic Agents; Male; Middle Aged

2006
Simultaneous determination of ezetimibe and its glucuronide metabolite in human plasma by solid phase extraction and liquid chromatography-tandem mass spectrometry.
    Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2015, Apr-01, Volume: 986-987

    Topics: Azetidines; Chromatography, Liquid; Ezetimibe; Glucuronides; Humans; Linear Models; Male; Reproducibility of Results; Sensitivity and Specificity; Solid Phase Extraction; Tandem Mass Spectrometry

2015
Development of a joint population pharmacokinetic model of ezetimibe and its conjugated metabolite.
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2019, Feb-01, Volume: 128

    Topics: Adult; Azetidines; Drug Compounding; Ezetimibe; Glucuronides; Humans; Hypolipidemic Agents; Models, Biological

2019

Other Studies

14 other study(ies) available for ezetimibe and sch 60663

ArticleYear
Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: enhanced potency by modification of the sugar.
    Bioorganic & medicinal chemistry letters, 1998, Feb-03, Volume: 8, Issue:3

    Topics: Animals; Anticholesteremic Agents; Azetidines; Carbohydrates; Cholesterol; Chromatography, High Pressure Liquid; Cricetinae; Liver; Magnetic Resonance Spectroscopy; Mass Spectrometry; Molecular Structure; Structure-Activity Relationship

1998
Synthesis of fluorescent biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
    Bioorganic & medicinal chemistry letters, 2002, Feb-11, Volume: 12, Issue:3

    Topics: Animals; Anticholesteremic Agents; Azetidines; Catalysis; Cholesterol; Drug Design; Ezetimibe; Fluorescent Dyes; Intestinal Absorption; Male; Palladium; Rats; Rats, Sprague-Dawley; Stereoisomerism; Structure-Activity Relationship

2002
Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption.
    Bioorganic & medicinal chemistry letters, 2008, Jan-15, Volume: 18, Issue:2

    Topics: Animals; Cholesterol; Intestinal Absorption; Ligands; Membrane Transport Proteins; Microvilli; Oxazolidinones; Rats; X-Ray Diffraction

2008
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
    Drug metabolism and disposition: the biological fate of chemicals, 2012, Volume: 40, Issue:3

    Topics: Animals; Anticholesteremic Agents; Azetidines; Bile Acids and Salts; Biliary Tract; Biological Transport; Choline Deficiency; Diet; Ezetimibe; Fatty Liver; Glucuronosyltransferase; Intestinal Mucosa; Liver; Male; Membrane Transport Proteins; Methionine; Multidrug Resistance-Associated Proteins; Non-alcoholic Fatty Liver Disease; Rats; Rats, Sprague-Dawley

2012
Comparison of the activity and disposition of the novel cholesterol absorption inhibitor, SCH58235, and its glucuronide, SCH60663.
    British journal of pharmacology, 2000, Volume: 129, Issue:8

    Topics: Animals; Anticholesteremic Agents; Autoradiography; Azetidines; Bile; Bile Ducts; Catheterization; Cholesterol; Chromatography, High Pressure Liquid; Ezetimibe; Injections, Intravenous; Intestinal Absorption; Intestines; Male; Rats; Rats, Sprague-Dawley; Time Factors; Tritium

2000
Concurrent determination of ezetimibe and its phase-I and II metabolites by HPLC with UV detection: quantitative application to various in vitro metabolic stability studies and for qualitative estimation in bile.
    Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2007, Jun-15, Volume: 853, Issue:1-2

    Topics: Animals; Azetidines; Bile; Chromatography, High Pressure Liquid; Ezetimibe; Glucuronides; Male; Molecular Structure; Rats; Rats, Wistar; Reproducibility of Results; Spectrophotometry, Ultraviolet; Tandem Mass Spectrometry

2007
Disposition of the cholesterol absorption inhibitor ezetimibe in mdr1a/b (-/-) mice.
    Journal of pharmaceutical sciences, 2007, Volume: 96, Issue:12

    Topics: Administration, Oral; Animals; Anticholesteremic Agents; ATP Binding Cassette Transporter, Subfamily B; ATP-Binding Cassette Sub-Family B Member 4; ATP-Binding Cassette Transporters; Azetidines; Biological Availability; Biotransformation; Cholesterol; Ezetimibe; Feces; Glucuronides; Intestinal Absorption; Kidney; Male; Mice; Mice, Knockout; Tissue Distribution

2007
Complex pharmacokinetic behavior of ezetimibe depends on abcc2, abcc3, and abcg2.
    Drug metabolism and disposition: the biological fate of chemicals, 2009, Volume: 37, Issue:8

    Topics: Administration, Oral; Animals; Anticholesteremic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Azetidines; Biological Transport; Biotransformation; Cell Line; Enterohepatic Circulation; Estradiol; Ezetimibe; Glucuronides; Intestinal Absorption; Intestine, Small; Intubation, Gastrointestinal; Methotrexate; Mice; Mice, Knockout; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Transfection

2009
Synergistic influence of Abcb1 and Abcc2 on disposition and sterol lowering effects of ezetimibe in rats.
    Journal of pharmaceutical sciences, 2010, Volume: 99, Issue:1

    Topics: Animals; Anticholesteremic Agents; ATP Binding Cassette Transporter, Subfamily B; ATP-Binding Cassette Transporters; Azetidines; Cholesterol, Dietary; Cyclosporins; Ezetimibe; Feces; Glucuronides; Male; Metabolic Clearance Rate; Rats; Rats, Inbred Lew; Species Specificity; Sterols; Tissue Distribution

2010
Effects of UDP-glucuronosyltransferase polymorphisms on the pharmacokinetics of ezetimibe in healthy subjects.
    European journal of clinical pharmacology, 2011, Volume: 67, Issue:1

    Topics: Alleles; Anticholesteremic Agents; Area Under Curve; Azetidines; Ezetimibe; Female; Genotype; Glucuronides; Glucuronosyltransferase; Humans; Intestinal Mucosa; Intestines; Male; Polymorphism, Genetic

2011
Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells.
    British journal of pharmacology, 2012, Volume: 165, Issue:6

    Topics: Animals; Azetidines; Cell Line; Dogs; Etoposide; Ezetimibe; Glucuronides; Glucuronosyltransferase; HEK293 Cells; Humans; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Organic Anion Transport Protein 1; RNA, Messenger; Transfection

2012
Incremental lowering of low-density lipoprotein cholesterol with ezetimibe 20 mg vs 10 mg daily in patients receiving concomitant statin therapy.
    The Canadian journal of cardiology, 2013, Volume: 29, Issue:11

    Topics: Aged; Anticholesteremic Agents; Aspartate Aminotransferases; Azetidines; Cholesterol, LDL; Creatine Kinase; Dose-Response Relationship, Drug; Dyslipidemias; Ezetimibe; Female; Glucuronides; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Male; Middle Aged; Retrospective Studies

2013
Fomiroid A, a novel compound from the mushroom Fomitopsis nigra, inhibits NPC1L1-mediated cholesterol uptake via a mode of action distinct from that of ezetimibe.
    PloS one, 2014, Volume: 9, Issue:12

    Topics: Anticholesteremic Agents; Azetidines; Binding Sites; Binding, Competitive; Caco-2 Cells; Cholesterol; Coriolaceae; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Esterification; Ezetimibe; Glucuronides; HEK293 Cells; Humans; Lanosterol; Membrane Proteins; Membrane Transport Proteins; Molecular Structure

2014
Bioequivalence Study of Ezetimibe Tablets After a Single Oral Dose of 10 mg in Healthy Japanese Subjects Under Fasting Conditions.
    Clinical pharmacology in drug development, 2023, Volume: 12, Issue:7

    Topics: Administration, Oral; Drugs, Generic; East Asian People; Ezetimibe; Fasting; Healthy Volunteers; Humans; Male; Tablets; Therapeutic Equivalency

2023