Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMKJ485)

Drug Name
Pioglitazone Drug Info
Synonyms
111025-46-8; Actos; Pioglitazona; Pioglitazonum; Glustin; Zactos; 105355-27-9; Pioglitazonum [INN-Latin]; Pioglitazona [INN-Spanish]; Duetact; Pioglitazone [INN:BAN]; Pioglitazone [BAN:INN]; 5-(4-(2-(5-ethylpyridin-2-yl)ethoxy)benzyl)thiazolidine-2,4-dione; AD-4833; U 72107; CHEBI:8228; Pioglitazone (Actos); HSDB 7322; Actos (TN); 5-{4-[2-(5-ethylpyridin-2-yl)ethoxy]benzyl}-1,3-thiazolidine-2,4-dione; C19H20N2O3S; AD 4833; 5-[4-[2-(5-ETHYL-2-PYRIDYL)ETHOXY]BENZYL]-2,4-THIAZOLIDINEDIONE; U 72107A; Actos; Actost; Glustin (TN); HS-0047; Pioglitazone (INN); U-72107; U72,107A; Zactos (TN); (+-)-5-((4-(2-(5-ethyl-2-pyridinyl)ethoxy)phenyl)methyl)-2,4-thiazolidinedione; (+/-)-5-[[4-[2-(5-Ethyl-2-pyridinyl)-ethoxy]phenyl]methyl]-2,4-thiazolidinedione; (+/-)-5-[p-[2-(ethyl-2-pyridyl)ethoxy]benzyl]-2,4-thiazolidinedione; 2,4-Thiazolidinedione, 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-(9CI); 5-((4-(2-(5-Ethyl-2-pyridinyl)ethoxy)phenyl)methyl)-2,4-thiazolidinedione; 5-(4-(2-(5-ethyl-2-pyridyl)ethoxy)benzyl)-2,4-thiazolidinedione; 5-[4-[2-(5-Ethyl-2-pyridyl)ethoxy]benzyl]thiazolidine-2,4-dione; 5-[[4-[2-(5-Ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione; 5-[[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione; 5-[[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]methyl]thiazolidine-2,4-dione; 5-[[4-[2-[(5-ethyl-2-pyridyl)]ethoxy]phenyl]methyl]thiazolidine-2,4-dione; Linagliptin + pioglitazone; PCG1
Indication
Disease Entry ICD 11 Status REF
Amyotrophic lateral sclerosis 8B60.0 Approved [1]
Diabetic complication 5A2Y Approved [2]
Non-insulin dependent diabetes 5A11 Approved [1]
Type-2 diabetes 5A11 Phase 3 [3]
Endometriosis GA10 Investigative [1]
Obesity 5B81 Investigative [4]
Therapeutic Class
Hypoglycemic Agents
Cross-matching ID
PubChem CID
4829
ChEBI ID
CHEBI:8228
CAS Number
CAS 111025-46-8
TTD Drug ID
DMKJ485
VARIDT Drug ID
DR00518
INTEDE Drug ID
DR1295
ACDINA Drug ID
D00534

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Peroxisome proliferator-activated receptor gamma (PPAR-gamma) TTZMAO3 PPARG_HUMAN Agonist [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [6]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [7]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [8]
Prostaglandin G/H synthase 1 (COX-1) DE073H6 PGH1_HUMAN Approved [9]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Peroxisome proliferator-activated receptor gamma (PPAR-gamma) DTT PPARG 5.576 6.977 5.736 5.758
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Prostaglandin G/H synthase 1 (COX-1) DME PTGS1 6.09 7.747 6.04 7.023
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

ICD Disease Classification 16 Disease of the genitourinary system
Disease Class ICD-11: GA10 Endometriosis
The Studied Tissue Endometrium tissue
The Studied Disease Endometriosis [ICD-11:GA10]
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Peroxisome proliferator-activated receptor gamma (PPAR-gamma) DTT PPARG 2.42E-02 0.17 0.19
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 7.97E-02 -4.55E-02 -3.54E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 9.10E-03 4.31E-01 9.29E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 9.50E-01 8.27E-02 3.14E-01
Prostaglandin G/H synthase 1 (COX-1) DME PTGS1 2.17E-01 6.85E-01 4.32E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Pioglitazone FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2694).
3 ClinicalTrials.gov (NCT01183013) 30 Week Parallel Group Comparison Study of Linagliptin + Pioglitazone (5+15, 5+30 and 5+45 mg) qd Versus Respective Monotherapies, Followed by a Comparison of 5mg+30mg and 5mg+45mg Versus Respective Monotherapies in Type 2 Diabetes for up to 54 Weeks. U.S. National Institutes of Health.
4 Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.
5 Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7.
6 Pioglitazone is metabolised by CYP2C8 and CYP3A4 in vitro: potential for interactions with CYP2C8 inhibitors. Basic Clin Pharmacol Toxicol. 2006 Jul;99(1):44-51.
7 Current clinical evidence on pioglitazone pharmacogenomics. Front Pharmacol. 2013 Nov 26;4:147.
8 The role of human CYP2C8 and CYP2C9 variants in pioglitazone metabolism in vitro. Basic Clin Pharmacol Toxicol. 2009 Dec;105(6):374-9.
9 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.