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
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inducers
Drug Categories	cytochrome p-450 cyp3a4 inducers (strength unknown)
Drug Categories	cytochrome p-450 enzyme inducers
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	hypoglycemia-associated agents
Drug Categories	oatp1b1/slco1b1 inhibitors
Drug Categories	oatp1b3 inhibitors
Drug Categories	peroxisome proliferator receptor gamma agonist
Drug Categories	peroxisome proliferator-activated receptor activity
Drug Categories	thiazolidinediones

(5 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
Lehmann et al., 1995, An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma)., J. Biol. 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
Miyazaki et al., 2004, Effect of pioglitazone on circulating adipocytokine levels and insulin sensitivity in type 2 diabetic patients., J. Clin. Endocrinol. Metab.
Willson et al., 1996, The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones., J. Med. Chem.
Spiegelman, 1998, PPAR-gamma: adipogenic regulator and thiazolidinedione receptor., Diabetes
Usui S et al., 2005, Design, synthesis, and biological activity of novel PPARgamma ligands based on rosiglitazone and 15d-PGJ2., Bioorg Med Chem Lett
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Choi J et al., 2010, 1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists., Bioorg Med Chem
Sugii et al., 2009, PPARgamma activation in adipocytes is sufficient for systemic insulin sensitization., Proc. Natl. Acad. Sci. U.S.A.
MacDonald ML et al., 2006, Identifying off-target effects and hidden phenotypes of drugs in human cells., Nat Chem Biol
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.
Binda C et al., 2011, Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs., ACS Med Chem Lett

PIOGLITAZONE THBS1

Interaction Score: 0.84

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17063547

Sources:
NCI
PIOGLITAZONE ADIPOQ

Interaction Score: 0.67

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PIOGLITAZONE PTPRD

Interaction Score: 0.67

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PIOGLITAZONE GHRL

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16682836

Sources:
NCI
PIOGLITAZONE SLC2A1

Interaction Score: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17251278

Sources:
NCI
PIOGLITAZONE PPARG

Interaction Score: 0.34

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

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

Sources:
TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology
PIOGLITAZONE TRPM3

Interaction Score: 0.3

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: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15649489

Sources:
NCI
PIOGLITAZONE HSPA4

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12871756

Sources:
NCI
PIOGLITAZONE TGFB1

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17407709

Sources:
NCI
PIOGLITAZONE MAOB

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
22282722

Sources:
DrugBank
PIOGLITAZONE CYP3A5

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
PIOGLITAZONE G6PD

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PIOGLITAZONE NR1I2

Interaction Score: 0.02

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

DrugBank: DB01132

Version: 5.1.7

Alternate Names:

Act Pioglitazone Drug Brand

Actoplus Met Drug Brand

Actoplus Met XR Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Binda C et al., 2011, Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs., ACS Med Chem Lett

Miyazaki et al., 2004, Effect of pioglitazone on circulating adipocytokine levels and insulin sensitivity in type 2 diabetic patients., J. Clin. Endocrinol. Metab.

Willson et al., 1996, The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones., J. Med. Chem.

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

Act Pioglitazone	Drug Brand
Actoplus Met	Drug Brand
Actoplus Met XR	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

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: 16682836

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17251278

Sources: NCI

Interaction Types & Directionality: agonist (activating)

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

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

Sources: TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

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: inhibitor (inhibitory)

Interaction Info:

PMIDs: 22282722

Sources: DrugBank

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

DrugBank: DB01132

Alternate Names: Act Pioglitazone Drug Brand Actoplus Met Drug Brand Actoplus Met XR Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

TEND: PIOGLITAZONE

Alternate Names: PIOGLITAZONE Primary Drug Name

Drug Info: Drug Class hypoglycemic agents Year of Approval 1999

Publications:

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:
16682836

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
17251278

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

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

Sources:
TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

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:

inhibitor (inhibitory)

PMIDs:
22282722

Sources:
DrugBank

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:

Act Pioglitazone Drug Brand

Actoplus Met Drug Brand

Actoplus Met XR Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

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