DGIdb - ROSIGLITAZONE Drug Record

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:

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

ROSIGLITAZONE Drug Record

ROSIGLITAZONE chembl:CHEMBL121

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18693052

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16034410

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15279069

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24752311

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9421288

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15855323

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11591391

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16891009

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16732015

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11699047

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12695287

Sources: NCI

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16921272 15640776

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27271184 17178266 23426382

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15998575

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18314419

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15130775

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27271184

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16777975

Interaction Types & Directionality:

n/a

PMIDs:
18693052

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16034410

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15279069

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
24752311

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9421288

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15855323

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11591391

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16891009

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16732015

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
11699047

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12695287

Sources:
NCI

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

Interaction Types & Directionality:

n/a

PMIDs:
16921272 15640776

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
27271184 17178266 23426382

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15998575

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
18314419

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15130775

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
27271184

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16777975

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18302760

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Alternate Names:

ROSIGLITAZONE Primary Drug Name

Drug Info:

Year of Approval 1999

Drug Class hypoglycemic agents

Drug Info:

Drug Indications antidiabetic

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C2583 NCI drug code

Alternate Names:

CHEMBL121 ChEMBL Drug ID