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ROSIGLITAZONE Drug Record

  • Summary
  • Interactions
  • Claims
  • ROSIGLITAZONE chembl:CHEMBL121

    Alternate Names:

    AVANDAMET
    BRL-49653
    AVANDIA
    TDZ-01
    ROSIGLITAZONE
    AVANDARYL
    ROSIGLIZOLE
    5-((4-(2-(METHYL-2-PYRIDINYLAMINO)ETHOXY)PHENYL)METHYL)-2,4-THIAZOLIDINEDIONE
    ROSIGLITAZONUM
    ROSIGLITAZONA
    (±)-5-[P-[2-(METHYL-2-PYRIDYLAMINO)ETHOXY]BENZYL]-2,4-THIAZOLIDINEDIONE
    ROSIGLITAZON
    AVANDIA®
    (RS)-5-{4-[2-(METHYL-2-PYRIDYLAMINO)ETHOXY]BENZYL}-2,4-THIAZOLIDINEDION
    chemidplus:122320-73-4
    drugbank:00412
    rxcui:84108
    pubchem.compound:77999
    chembl:CHEMBL121

    Drug Info:

    Drug Class hypoglycemic agents
    Year of Approval 1999
    Drug Indications for treatment of Alzheimer's disease,antidiabetic
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antidiabetic
    (2 More Sources)

    Publications:

    Piemontese L et al., 2015, Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175., Eur J Med Chem
    Choi J et al., 2010, 1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists., Bioorg Med Chem
    Xiao B et al., 2012, Design and synthesis of marine fungal phthalide derivatives as PPAR-γ agonists., Bioorg Med Chem
    Gathiaka S et al., 2013, Design, development and evaluation of novel dual PPARδ/PPARγ agonists., Bioorg Med Chem Lett
    Kharbanda C et al., 2014, Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents., Bioorg Med Chem Lett
    Nazreen S et al., 2014, Thiazolidine-2,4-diones derivatives as PPAR-γ agonists: synthesis, molecular docking, in vitro and in vivo antidiabetic activity with hepatotoxicity risk evaluation and effect on PPAR-γ gene expression., Bioorg Med Chem Lett
    Festa C et al., 2012, Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor γ., J Med Chem
    Usui S et al., 2005, Design, synthesis, and biological activity of novel PPARgamma ligands based on rosiglitazone and 15d-PGJ2., Bioorg Med Chem Lett
    Kharbanda C et al., 2015, Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect., Bioorg Med Chem Lett
    Liu W et al., 2011, Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators., J Med Chem
    Gorczynski MJ et al., 2009, Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation., J Med Chem
    MacDonald ML et al., 2006, Identifying off-target effects and hidden phenotypes of drugs in human cells., Nat Chem Biol
    Kameda et al., 2000, [Rosiglitazone (BRL-49653)]., Nippon Rinsho
    Rieusset et al., 1999, Regulation of gene expression by activation of the peroxisome proliferator-activated receptor gamma with rosiglitazone (BRL 49653) in human adipocytes., Biochem. Biophys. Res. Commun.
    Johnson et al., 2000, Ligand-induced stabilization of PPARgamma monitored by NMR spectroscopy: implications for nuclear receptor activation., J. Mol. Biol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Su et al., 1999, Use of a PPAR gamma-specific monoclonal antibody to demonstrate thiazolidinediones induce PPAR gamma receptor expression in vitro., Hybridoma
    Camp et al., 2000, Differential activation of peroxisome proliferator-activated receptor-gamma by troglitazone and rosiglitazone., Diabetes
    Geng et al., 2006, Effect of peroxisome proliferator-activated receptor gamma ligand. Rosiglitazone on left ventricular remodeling in rats with myocardial infarction., Int. J. Cardiol.
    Dawed AY et al., 2016, CYP2C8 and SLCO1B1 Variants and Therapeutic Response to Thiazolidinediones in Patients With Type 2 Diabetes., Diabetes Care
    Yeow et al., 2001, Inhibition of myogenesis enables adipogenic trans-differentiation in the C2C12 myogenic cell line., FEBS Lett.
    Marx et al., 2003, Effect of rosiglitazone treatment on soluble CD40L in patients with type 2 diabetes and coronary artery disease., Circulation
    Wang et al., 2006, Insulin resistance accelerates muscle protein degradation: Activation of the ubiquitin-proteasome pathway by defects in muscle cell signaling., Endocrinology
    Sanguino et al., 2005, Different response of senescent female Sprague-Dawley rats to gemfibrozil and rosiglitazone administration., Exp. Gerontol.
    Kang ES et al., 2008, LPIN1 genetic variation is associated with rosiglitazone response in type 2 diabetic patients., Mol Genet Metab
    Bachmakov et al., 2008, Interaction of oral antidiabetic drugs with hepatic uptake transporters: focus on organic anion transporting polypeptides and organic cation transporter 1., Diabetes
    Kang ES et al., 2006, The 11482G >A polymorphism in the perilipin gene is associated with weight gain with rosiglitazone treatment in type 2 diabetes., Diabetes Care
    Chen M et al., 2014, Association of PAX4 genetic variants with oral antidiabetic drugs efficacy in Chinese type 2 diabetes patients., Pharmacogenomics J
    Risérus et al., 2005, Rosiglitazone increases indexes of stearoyl-CoA desaturase activity in humans: link to insulin sensitization and the role of dominant-negative mutation in peroxisome proliferator-activated receptor-gamma., Diabetes
    Kramer et al., 2001, Insulin-sensitizing effect of rosiglitazone (BRL-49653) by regulation of glucose transporters in muscle and fat of Zucker rats., Metab. Clin. Exp.
    Wang et al., 1997, Increased feeding in fatty Zucker rats by the thiazolidinedione BRL 49653 (rosiglitazone) and the possible involvement of leptin and hypothalamic neuropeptide Y., Br. J. Pharmacol.
    Cannavò et al., 2004, Baseline and CRH-stimulated ACTH and cortisol levels after administration of the peroxisome proliferator-activated receptor-gamma ligand, rosiglitazone, in Cushing's disease., J. Endocrinol. Invest.
    Hernandez-Trujillo et al., 2008, Rosiglitazone but not losartan prevents Nrf-2 dependent CD36 gene expression up-regulation in an in vivo atherosclerosis model., Cardiovasc Diabetol
    St-Pierre et al., 2004, Rosiglitazone increases extravasation of macromolecules and endothelial nitric oxide synthase in skeletal muscles of the fructose-fed rat model., Biochem. Pharmacol.
    Elias et al., 2006, Enhanced radioiodine uptake in a patient with poorly differentiated papillary thyroid cancer after treatment with rosiglitazone., Clin Nucl Med
    Philips et al., 2004, Effect of peroxisome proliferator-activated receptor gamma agonist, rosiglitazone, on dedifferentiated thyroid cancers., Nucl Med Commun
    Yang et al., 2005, Serum retinol binding protein 4 contributes to insulin resistance in obesity and type 2 diabetes., Nature
    Kirchheiner J et al., 2006, Pharmacokinetics and pharmacodynamics of rosiglitazone in relation to CYP2C8 genotype., Clin Pharmacol Ther
    Stage TB et al., 2013, The role of genetic variants in CYP2C8, LPIN1, PPARGC1A and PPARγ on the trough steady-state plasma concentrations of rosiglitazone and on glycosylated haemoglobin A1c in type 2 diabetes., Pharmacogenet Genomics
  • ROSIGLITAZONE   LPIN1

    Interaction Score: 5.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18693052


    Sources:
    PharmGKB

  • ROSIGLITAZONE   RBP4

    Interaction Score: 2.69

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16034410


    Sources:
    NCI

  • ROSIGLITAZONE   CRH

    Interaction Score: 2.69

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15279069


    Sources:
    NCI

  • ROSIGLITAZONE   PAX4

    Interaction Score: 2.69

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24752311


    Sources:
    PharmGKB

  • ROSIGLITAZONE   NPY

    Interaction Score: 1.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9421288


    Sources:
    NCI

  • ROSIGLITAZONE   SCD

    Interaction Score: 1.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15855323


    Sources:
    NCI

  • ROSIGLITAZONE   MAP2K3

    Interaction Score: 0.9

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11591391


    Sources:
    NCI

  • ROSIGLITAZONE   AGTR2

    Interaction Score: 0.9

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16891009


    Sources:
    NCI

  • ROSIGLITAZONE   PLIN1

    Interaction Score: 0.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16732015


    Sources:
    PharmGKB

  • ROSIGLITAZONE   SLC2A1

    Interaction Score: 0.49

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11699047


    Sources:
    NCI

  • ROSIGLITAZONE   CD40LG

    Interaction Score: 0.49

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12695287


    Sources:
    NCI

  • ROSIGLITAZONE   PPARG

    Interaction Score: 0.47

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name rosiglitazone + glimepiride,Avandaryl
    Novel drug target Established target
    Trial Name rosiglitazone maleate + metformin HCl,Ava/

    PMIDs:
    25497132 21030263 22819190 23273519 25442322 24890090 22934537 15745794 26384286 22070604 19719236 16680159 10707565 10548525 10764590 11752352 10475242 10871190


    Sources:
    DTC TdgClinicalTrial TEND

  • ROSIGLITAZONE   TG

    Interaction Score: 0.45

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16921272 15640776


    Sources:
    NCI

  • ROSIGLITAZONE   CYP2C8

    Interaction Score: 0.43

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27271184 17178266 23426382


    Sources:
    PharmGKB

  • ROSIGLITAZONE   HNF4A

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15998575


    Sources:
    NCI

  • ROSIGLITAZONE   SLCO2B1

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18314419


    Sources:
    NCI

  • ROSIGLITAZONE   NOS1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15130775


    Sources:
    NCI

  • ROSIGLITAZONE   SLCO1B1

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27271184


    Sources:
    PharmGKB

  • ROSIGLITAZONE   PIK3CG

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16777975


    Sources:
    NCI

  • ROSIGLITAZONE   NR1I2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ROSIGLITAZONE   NFE2L2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18302760


    Sources:
    NCI

  • ROSIGLITAZONE   HSD17B10

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ROSIGLITAZONE   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • TEND: ROSIGLITAZONE

    • Version: 01-August-2011

    Alternate Names:
    ROSIGLITAZONE Primary Drug Name

    Drug Info:
    Year of Approval 1999
    Drug Class hypoglycemic agents

    Publications:

  • TdgClinicalTrial: ROSIGLITAZONE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antidiabetic
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • NCI: ROSIGLITAZONE

    • Version: 14-September-2017

    Alternate Names:
    C2583 NCI drug code

    Drug Info:

    Publications:
    Geng et al., 2006, Effect of peroxisome proliferator-activated receptor gamma ligand. Rosiglitazone on left ventricular remodeling in rats with myocardial infarction., Int. J. Cardiol.
    Risérus et al., 2005, Rosiglitazone increases indexes of stearoyl-CoA desaturase activity in humans: link to insulin sensitization and the role of dominant-negative mutation in peroxisome proliferator-activated receptor-gamma., Diabetes
    Cannavò et al., 2004, Baseline and CRH-stimulated ACTH and cortisol levels after administration of the peroxisome proliferator-activated receptor-gamma ligand, rosiglitazone, in Cushing's disease., J. Endocrinol. Invest.

  • DTC: ROSIGLITAZONE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL121 ChEMBL Drug ID

    Drug Info:

    Publications:
    Xiao B et al., 2012, Design and synthesis of marine fungal phthalide derivatives as PPAR-γ agonists., Bioorg Med Chem
    Festa C et al., 2012, Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor γ., J Med Chem
    Nazreen S et al., 2014, Thiazolidine-2,4-diones derivatives as PPAR-γ agonists: synthesis, molecular docking, in vitro and in vivo antidiabetic activity with hepatotoxicity risk evaluation and effect on PPAR-γ gene expression., Bioorg Med Chem Lett

  • PharmGKB: rosiglitazone

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Kang ES et al., 2006, The 11482G >A polymorphism in the perilipin gene is associated with weight gain with rosiglitazone treatment in type 2 diabetes., Diabetes Care
    Chen M et al., 2014, Association of PAX4 genetic variants with oral antidiabetic drugs efficacy in Chinese type 2 diabetes patients., Pharmacogenomics J
    Dawed AY et al., 2016, CYP2C8 and SLCO1B1 Variants and Therapeutic Response to Thiazolidinediones in Patients With Type 2 Diabetes., Diabetes Care

  • ChemblDrugs: chembl:CHEMBL121

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21