DGIdb - PIOGLITAZONE Drug Record

PIOGLITAZONE chembl:CHEMBL595 Approved

Alternate Names:

DUETACT
U-72107
ACTOS
AD-4833
PIOGLITAZONE
(+-)-5-((4-(2-(5-ETHYL-2-PYRIDINYL)ETHOXY)PHENYL)METHYL)-2,4-THIAZOLIDINEDIONE
PIOGLITAZONA
U-72107A
5-{4-[2-(5-ETHYLPYRIDIN-2-YL)ETHOXY]BENZYL}-1,3-THIAZOLIDINE-2,4-DIONE
XAB907
ZACTOS
PIOGLITAZONUM
chemidplus:111025-46-8
drugbank:01132
pubchem.compound:4829
rxcui:33738
chembl:CHEMBL595

Drug Info:

Year of Approval	1999
Drug Class	hypoglycemic agents
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antidiabetic

(4 More Sources)

Publications:

Kajosaari et al., 2006, Pioglitazone, an in vitro inhibitor of CYP2C8 and CYP3A4, does not increase the plasma concentrations of the CYP2C8 and CYP3A4 substrate repaglinide., Eur. J. Clin. Pharmacol.
Stuart et al., 2007, Overexpression of GLUT5 in diabetic muscle is reversed by pioglitazone., Diabetes Care
Blüher M et al., 2003, Analysis of the relationship between the Pro12Ala variant in the PPAR-gamma2 gene and the response rate to therapy with pioglitazone in patients with type 2 diabetes., Diabetes Care
Choi J et al., 2010, 1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists., Bioorg 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
Usui S et al., 2005, Design, synthesis, and biological activity of novel PPARgamma ligands based on rosiglitazone and 15d-PGJ2., Bioorg Med Chem Lett
MacDonald ML et al., 2006, Identifying off-target effects and hidden phenotypes of drugs in human cells., Nat Chem Biol
Sugii et al., 2009, PPARgamma activation in adipocytes is sufficient for systemic insulin sensitization., Proc. Natl. Acad. Sci. U.S.A.
Spiegelman, 1998, PPAR-gamma: adipogenic regulator and thiazolidinedione receptor., Diabetes
Willson et al., 1996, The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones., J. Med. Chem.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Miyazaki et al., 2004, Effect of pioglitazone on circulating adipocytokine levels and insulin sensitivity in type 2 diabetic patients., J. Clin. Endocrinol. Metab.
Lehmann et al., 1995, An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma)., J. Biol. Chem.
Otto et al., 2006, Increase in adiponectin levels during pioglitazone therapy in relation to glucose control, insulin resistance as well as ghrelin and resistin levels., J. Endocrinol. Invest.
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
Konturek et al., 2003, Pioglitazone, a specific ligand of peroxisome proliferator-activated receptor-gamma, accelerates gastric ulcer healing in rat., Eur. J. Pharmacol.
Yin SJ et al., 2017, Effects of functional CYP2C8,CYP2C9,CYP3A5,and ABCB1 genetic variants on the pharmacokinetics of insulin sensitizer pioglitazone in Chinese Han individuals., Pharmacogenet Genomics
Jia et al., 2007, [Effects of pioglitazone on the morphology and the expression of connective tissue growth factor of transforming growth factor beta-induced rat hepatic stellate cells in vitro]., Zhonghua Gan Zang Bing Za Zhi
Wang et al., 2006, [Effects of pioglitazone on MKP-1 and TSP-1 expression in early stages of diabetic retinopathy induced by streptozotocin]., Zhejiang Da Xue Xue Bao Yi Xue Ban
Kiaei et al., 2005, Peroxisome proliferator-activated receptor-gamma agonist extends survival in transgenic mouse model of amyotrophic lateral sclerosis., Exp. Neurol.

PIOGLITAZONE THBS1

Interaction Score: 1.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17063547

Sources:
NCI
PIOGLITAZONE ADIPOQ

Interaction Score: 0.8

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PIOGLITAZONE PTPRD

Interaction Score: 0.8

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PIOGLITAZONE SLC2A1

Interaction Score: 0.72

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17251278

Sources:
NCI
PIOGLITAZONE GHRL

Interaction Score: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16682836

Sources:
NCI
PIOGLITAZONE PPARG

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12610044 21030263 24890090 15745794 16680159 20018750 9568680 8576907 11752352 15356026 7768881

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology PharmGKB TTD
PIOGLITAZONE TRPM3

Interaction Score: 0.36

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Details of Interaction independent of PPAR-γ

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PIOGLITAZONE GFAP

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15649489

Sources:
NCI
PIOGLITAZONE HSPA4

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12871756

Sources:
NCI
PIOGLITAZONE TGFB1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17407709

Sources:
NCI
PIOGLITAZONE CYP3A5

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
PIOGLITAZONE G6PD

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PIOGLITAZONE NR1I2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PIOGLITAZONE YES1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PIOGLITAZONE CYP2C9

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28099407

Sources:
PharmGKB
PIOGLITAZONE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16447051

Sources:
NCI

TEND: PIOGLITAZONE
- Version: 01-August-2011
Alternate Names:

PIOGLITAZONE Primary Drug Name

Drug Info:

Drug Class hypoglycemic agents

Year of Approval 1999

Publications:
TdgClinicalTrial: PIOGLITAZONE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antidiabetic

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: PIOGLITAZONE

Version: 14-September-2017

Alternate Names:

C29367 NCI drug code

Drug Info:

Publications:

Otto et al., 2006, Increase in adiponectin levels during pioglitazone therapy in relation to glucose control, insulin resistance as well as ghrelin and resistin levels., J. Endocrinol. Invest.

Konturek et al., 2003, Pioglitazone, a specific ligand of peroxisome proliferator-activated receptor-gamma, accelerates gastric ulcer healing in rat., Eur. J. Pharmacol.

Kajosaari et al., 2006, Pioglitazone, an in vitro inhibitor of CYP2C8 and CYP3A4, does not increase the plasma concentrations of the CYP2C8 and CYP3A4 substrate repaglinide., Eur. J. Clin. Pharmacol.

DTC: PIOGLITAZONE

Version: 02-September-2020

Alternate Names:

CHEMBL595 ChEMBL Drug ID

Drug Info:

Publications:

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

Usui S et al., 2005, Design, synthesis, and biological activity of novel PPARgamma ligands based on rosiglitazone and 15d-PGJ2., Bioorg Med Chem Lett

Choi J et al., 2010, 1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists., Bioorg Med Chem

PharmGKB: pioglitazone

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Yin SJ et al., 2017, Effects of functional CYP2C8,CYP2C9,CYP3A5,and ABCB1 genetic variants on the pharmacokinetics of insulin sensitizer pioglitazone in Chinese Han individuals., Pharmacogenet Genomics

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

Blüher M et al., 2003, Analysis of the relationship between the Pro12Ala variant in the PPAR-gamma2 gene and the response rate to therapy with pioglitazone in patients with type 2 diabetes., Diabetes Care

GuideToPharmacology: 135650829
- Version: 29-September-2020
Alternate Names:

PIOGLITAZONE GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Pioglitazone
- Version: 2020.06.01
Alternate Names:

D03OFF TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL595
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False
Direct Interaction?	True

Specific Action of the Ligand	None
Details of Interaction	independent of PPAR-γ
Endogenous Drug?	False

PIOGLITAZONE Drug Record

PIOGLITAZONE chembl:CHEMBL595 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17063547

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17251278

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16682836

Sources: NCI

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False Direct Interaction? True

PMIDs: 12610044 21030263 24890090 15745794 16680159 20018750 9568680 8576907 11752352 15356026 7768881

Sources: DTC TdgClinicalTrial TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Specific Action of the Ligand None Details of Interaction independent of PPAR-&gamma; Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15649489

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12871756

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17407709

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28099407

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16447051

Sources: NCI

TEND: PIOGLITAZONE

Alternate Names: PIOGLITAZONE Primary Drug Name

Drug Info: Drug Class hypoglycemic agents Year of Approval 1999

Publications:

TdgClinicalTrial: PIOGLITAZONE

Alternate Names:

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

Publications:

NCI: PIOGLITAZONE

Alternate Names: C29367 NCI drug code

Drug Info:

Interaction Types & Directionality:

n/a

PMIDs:
17063547

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
17251278

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16682836

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12610044 21030263 24890090 15745794 16680159 20018750 9568680 8576907 11752352 15356026 7768881

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Details of Interaction independent of PPAR-γ

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
15649489

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12871756

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
17407709

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
18695978

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
28099407

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16447051

Sources:
NCI

Alternate Names:

PIOGLITAZONE Primary Drug Name

Drug Info:

Drug Class hypoglycemic agents

Year of Approval 1999

Drug Info:

Drug Indications antidiabetic

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C29367 NCI drug code

Alternate Names:

CHEMBL595 ChEMBL Drug ID

Alternate Names:

PIOGLITAZONE GuideToPharmacology Ligand Name

Alternate Names:

D03OFF TTD Drug ID