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Atlas / Drug / Pioglitazone

Pioglitazone

drug
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Also known as AD-4833DuetactPioglitazonaU-72107ZactosSID26756476(R,S)-pioglitazoneSID137275816SID174007207PIOGLITAZONE HYDROCHLORIDEPiglitazone[3H]-PioglitazonePioglitazine

Summary

Pioglitazone (CHEMBL595) is an approved small-molecule insulin-sensitizing drug (ATC A10BG03) targeting TRPM3 and PPARG; indicated across 74 conditions including diabetes mellitus and metabolic syndrome x.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: A10BG03
  • Targets: 2 (TRPM3, PPARG)
  • Indications: 74 conditions
  • Clinical trials: 414
  • Chemistry: C19H20N2O3S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL595
NamePioglitazone
TypeSmall molecule
Max phase4
ChEBICHEBI:8228
ATCA10BG03
Molecular formulaC19H20N2O3S
InChIKeyHYAFETHFCAUJAY-UHFFFAOYSA-N

SMILES: CCc1ccc(CCOc2ccc(CC3SC(=O)NC3=O)cc2)nc1

ChEBI definition: A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.

Pharmacological roles (ChEBI): insulin-sensitizing drug, EC 2.7.1.33 (pantothenate kinase) inhibitor, EC 6.2.1.3 (long-chain-fatty-acid—CoA ligase) inhibitor, ferroptosis inhibitor, cardioprotective agent, PPARγ agonist, antidepressant, geroprotector, hypoglycemic agent.

Other ChEBI roles (chemical / environmental): xenobiotic.

Also known as: AD-4833, Duetact, Pioglitazona, Pioglitazone, U-72107, Zactos, pioglitazone, SID26756476, (R,S)-pioglitazone, SID137275816, PIOGLITAZONE, SID174007207

Parent form; salt/anhydrous children: CHEMBL1715

Patent coverage: 14,605 distinct patent families (57,130 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 56,855 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
TRPM3TRPM30.1%Q9HCF6
PPARGPeroxisome proliferator-activated receptor-γFull agonist6.22.6%P37231

Broader ChEMBL bioactivity targets: 22 (assay-derived). Sample: ATP-binding cassette sub-family C member 4, CDGSH iron-sulfur domain-containing protein 1, Alpha-2A adrenergic receptor, Amine oxidase [flavin-containing] A, Amine oxidase [flavin-containing] B, Carbonic anhydrase 2, Thromboxane A2 receptor, Bile salt export pump, Peroxisome proliferator-activated receptor alpha, Peroxisome proliferator-activated receptor gamma.

Bioactivity

ChEMBL activities: 100 potent at pChembl ≥ 5 of 109 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PPARG7.21Ki62nMCHEMBL_ACT_18960166
PPARG7.06EC5088nMCHEMBL_ACT_3256964
PPARG7.02Ki96nMCHEMBL_ACT_22778916
PPARG7.01EC5098nMCHEMBL_ACT_18758365
PPARG7EC50100nMCHEMBL_ACT_18779882
ABCB117AC50100nMCHEMBL_ACT_25126972
CA26.94IC50114nMCHEMBL_ACT_7730301
PPARG6.85EC50140nMCHEMBL_ACT_3408719
PPARG6.82Ki150nMCHEMBL_ACT_25697237
PPARG6.7EC50200nMCHEMBL_ACT_12163170
MAOB6.7Ki199.4nMCHEMBL_ACT_15163790
PPARG6.7EC50200nMCHEMBL_ACT_16469374
PPARG6.7EC50200nMCHEMBL_ACT_24989786
PPARG6.68EC50210nMCHEMBL_ACT_15073983
PPARG6.62EC50240nMCHEMBL_ACT_18666618
PPARG6.6EC50250nMCHEMBL_ACT_19302641
ABCB116.58IC50262.1nMCHEMBL_ACT_18081092
PPARG6.58EC50260nMCHEMBL_ACT_19302631
ABCB116.58IC50260nMCHEMBL_ACT_22396449
MAOB6.57Ki270.8nMCHEMBL_ACT_15163797
MAOB6.53IC50298nMCHEMBL_ACT_24965008
MAOB6.53IC50298nMCHEMBL_ACT_3422687
ABCB116.52IC50300nMCHEMBL_ACT_15460422
PPARG6.52Ki300nMCHEMBL_ACT_24989828
PPARG6.52Ki300nMCHEMBL_ACT_25084871
PPARG6.52EC50300nMCHEMBL_ACT_3246517
PPARG6.52EC50300nMCHEMBL_ACT_6337282
PPARG6.5EC50320nMCHEMBL_ACT_16811191
PPARG6.47Ki340nMCHEMBL_ACT_22393624
PPARG6.46EC50350nMCHEMBL_ACT_19302643

Target pathways

Aggregated over 2 target gene(s): TRPM3, PPARG.

Top Reactome pathways

9 total, by targets touching each:

PathwayTargetsGenes
PPARA activates gene expression1PPARG
TRP channels1TRPM3
Transcriptional regulation of white adipocyte differentiation1PPARG
Nuclear Receptor transcription pathway1PPARG
SUMOylation of intracellular receptors1PPARG
Regulation of PTEN gene transcription1PPARG
MECP2 regulates transcription factors1PPARG
MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis1PPARG
Transcriptional regulation of brown and beige adipocyte differentiation by EBF21PPARG

Dominant GO biological processes

GO termTargets
monoatomic cation transport1
calcium ion transport1
protein homotetramerization1
calcium ion transmembrane transport1
zinc ion transmembrane transport1
monoatomic cation transmembrane transport1
monoatomic ion transport1
monoatomic ion transmembrane transport1
protein tetramerization1
transmembrane transport1
negative regulation of transcription by RNA polymerase II1
placenta development1
regulation of transcription by RNA polymerase II1
fatty acid metabolic process1
response to nutrient1

Indications & clinical

Indications

74 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
diabetes mellitus4MONDO:0005015EFO:0000400
metabolic syndrome X3MONDO:0011565EFO:0000195
rheumatoid arthritis3MONDO:0008383EFO:0000685
liver disorder3MONDO:0005154EFO:0001421
metabolic dysfunction-associated steatotic liver disease3MONDO:0013209EFO:0003095
metabolic dysfunction-associated steatohepatitis3MONDO:0007027EFO:1001249
fatty liver disease3MONDO:0004790HP:0001397
hypertensive disorder3MONDO:0005044EFO:0000537
atherosclerosis3MONDO:0005311EFO:0003914
coronary artery disorder3MONDO:0005010EFO:0001645
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
Friedreich ataxia3MONDO:0100339MONDO:0100339
HIV infectious disease3MONDO:0005109EFO:0000764
acute myeloid leukemia2MONDO:0018874EFO:0000222
cardiovascular disorder2MONDO:0004995EFO:0000319
chronic myeloid leukemia2MONDO:0011996EFO:0000339
polycystic ovary syndrome2MONDO:0008487EFO:0000660
psoriasis2MONDO:0005083EFO:0000676
squamous cell carcinoma2MONDO:0005096EFO:0000707
squamous cell lung carcinoma2MONDO:0005097EFO:0000708
stroke disorder2MONDO:0005098EFO:0000712
obesity disorder2MONDO:0011122EFO:0001073
pulmonary arterial hypertension2MONDO:0015924EFO:0001361
glucose intolerance2MONDO:0001076EFO:0002546
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
hepatitis C virus infection2MONDO:0005231EFO:0003047
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
autism spectrum disorder2MONDO:0005258EFO:0003756
chronic kidney disease2MONDO:0005300EFO:0003884
chronic hepatitis C virus infection2MONDO:0005354EFO:0004220
opiate dependence2MONDO:0005530EFO:0005611
intracerebral hemorrhage2MONDO:0013792EFO:0005669
hepatitis2MONDO:0002251HP:0012115
polycystic kidney disease2MONDO:0020642EFO:0008620
major depressive disorder2MONDO:0002009MONDO:0002009
lung neoplasm2MONDO:0021117MONDO:0008903
myxoid liposarcoma2MONDO:0013280EFO:0000613
dedifferentiated liposarcoma2MONDO:0020563EFO:0003085
Alzheimer disease2MONDO:0004975MONDO:0004975
amyotrophic lateral sclerosis2MONDO:0004976MONDO:0004976
asthma2MONDO:0004979MONDO:0004979
Parkinson disease2MONDO:0005180MONDO:0005180
alcohol abuse2MONDO:0002046MONDO:0007079
adrenoleukodystrophy2MONDO:0018544MONDO:0015339
oral mucosa leukoplakia2MONDO:0004844MONDO:0004844
Crohn disease1MONDO:0005011EFO:0000384
glioblastoma1MONDO:0018177EFO:0000519
neoplasm1MONDO:0005070EFO:0000616
prostate adenocarcinoma1MONDO:0005082EFO:0000673
melanoma1MONDO:0005105EFO:0000756
plasma cell myeloma1MONDO:0009693EFO:0001378
anaplastic astrocytoma1MONDO:0016684EFO:0002499
relapsing-remitting multiple sclerosis1MONDO:0005314EFO:0003929
anemia1MONDO:0002280EFO:0004272
brain cancer1MONDO:0001657MONDO:0001657
type 1 diabetes mellitus1MONDO:0005147MONDO:0005147
multiple sclerosis1MONDO:0005301MONDO:0005301
cystic fibrosis1MONDO:0009061MONDO:0009061
chronic granulomatous disease1MONDO:0018305MONDO:0018305
systemic lupus erythematosus1MONDO:0007915MONDO:0007915
brain neoplasm1MONDO:0021211EFO:0003833
pulmonary alveolar proteinosis1MONDO:0001437MONDO:0012579
meningioma1MONDO:0016642MONDO:0020635
peripheral arterial disease0MONDO:0005386EFO:0004265
gastroparesis0MONDO:0006769EFO:1000948

9 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 414.

Phase distribution

PhaseTrials
PHASE4110
PHASE288
PHASE381
Not specified62
PHASE141
PHASE1/PHASE213
EARLY_PHASE111
PHASE2/PHASE38

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03471117PHASE4RECRUITINGPioglitazone to Reduce Sympathetic Overactivity in CKD Patients
NCT03878459PHASE4RECRUITINGDapagliflozin Plus Pioglitazone in T1DM
NCT05305287PHASE4RECRUITINGQuantifying Hepatic Mitochondrial Fluxes in Humans
NCT05838287PHASE4RECRUITINGPioglitazone on Heart Failure in Type-2 Diabetes Mellitus Participants
NCT06399835PHASE4RECRUITINGEnavogliflozin vs. Pioglitazone on Glucose and Atherosclerosis
NCT06657209PHASE4RECRUITINGNormal-weight Diabetes: Adipocyte-directed Therapy With Pioglitazone or Tirzepatide
NCT06851962PHASE4ACTIVE_NOT_RECRUITINGImpact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes.
NCT06922656PHASE4NOT_YET_RECRUITINGCan the Addition of Pioglitazone to SGLT2 Inhibitor in Type 1 Diabetic Patients Amplify the Decrease in HbA1c and Prevent the Increase in Plasma Ketone Concentration?
NCT06972732PHASE4RECRUITINGA Phase IV Clinical Trial to Compare the Efficacy and Safety of Metformin+Sodium-Glucose Cotransporter 2 Inhibitor(SGLT2-i)+Thiazolidinedione (TZD) in Patients With Type 2 Diabetes
NCT06989723PHASE4RECRUITINGPioglitazone and Empagliflozin for Fatty Liver Disease in Type 2 Diabetes
NCT07180745PHASE4NOT_YET_RECRUITINGEmpagliflozin Versus Statins in Non-Alcoholic Fatty Liver Disease
NCT00108615PHASE4COMPLETEDEffects of Insulin Sensitizers in Subjects With Impaired Glucose Tolerance
NCT00145340PHASE4COMPLETEDPioglitazone Treatment in Polycystic Ovary Syndrome
NCT00155350PHASE4UNKNOWNTreatment of Coronary Atherosclerosis by Insulin Sensitizers in Insulin-Resistant Patients
NCT00179400PHASE4COMPLETEDThe Role of Acute Combined PPAR Alpha and Gamma Stimulation on Insulin Action in Humans
NCT00189163PHASE4COMPLETEDPioglitazone in Hepatitis C
NCT00203996PHASE4TERMINATEDPolycystic Ovary Syndrome (PCOS) and Sleep Apnea
NCT00212004PHASE4TERMINATEDPioglitazone Protects Diabetes Mellitus (DM) Patients Against Re-Infarction (PPAR Study)
NCT00212290PHASE4COMPLETEDInsulin Resistance and Central Nervous System (CNS) Function in Type 2 Diabetes
NCT00227110PHASE4COMPLETEDRole of Pioglitazone in the Treatment of Non-alcoholic Steatohepatitis (NASH)
NCT00231894PHASE4COMPLETEDPioglitazone as a Treatment for Lipid and Glucose Abnormalities In Patients With Schizophrenia
NCT00306826PHASE4WITHDRAWNPioglitazone in Impaired Glucose Tolerance
NCT00314561PHASE4COMPLETEDThe Effect of Pioglitazone and Rosiglitazone on Atherosclerotic and Inflammatory Markers in Patients With Metabolic Syndrome
NCT00315146PHASE4COMPLETEDOptimizing Body Composition for Function in Older Adults
NCT00402012PHASE4COMPLETEDTAKE TIME Pioglitazone Reverses Defects in Mitochondrial Biogenesis in Patients With T2DM
NCT00437970PHASE4WITHDRAWNMedication in Early Diabetes (MED) Study
NCT00479986PHASE4COMPLETEDEffects of Pioglitazone in Type 2 Diabetes Mellitus and Coronary Heart Disease
NCT00485056PHASE4COMPLETEDPioglitazone on Cardiac Function and Large Arteries (PICCOLA Study)
NCT00494312PHASE4COMPLETEDSafety Study of Pioglitazone Compared To Glyburide on Liver Function
NCT00494559PHASE4COMPLETEDThe Effect of Pioglitazone on Neointima Volume and Inflammatory Markers
NCT00545233PHASE4COMPLETEDA Study of PEGASYS (Peginterferon Alfa-2a (40KD)) Plus COPEGUS (Ribavirin) With or Without Pioglitazone in Treatment-Naive Patients With Chronic Hepatitis C and Insulin Resistance.
NCT00570622PHASE4COMPLETEDEffect of Pioglitazone on Portal and Systemic Hemodynamics in Patients With Advanced Cirrhosis
NCT00571506PHASE4COMPLETEDEffect of Thiazolidinedione Treatment Vascular Risk Markers
NCT00576784PHASE4COMPLETEDMetabolic Effects of Pioglitazone in Type II Diabetic Patients Previously Treated With Insulin
NCT00579813PHASE4COMPLETEDMechanisms Underlying Metabolic Syndrome in Obesity
NCT00609856PHASE4COMPLETEDPioglitazone vs. Insulin Glargine in the Treatment of Secondary Drug Failure in Type 2 Diabetes
NCT00656864PHASE4COMPLETEDPioglitazone Incretin Study
NCT00672919PHASE4COMPLETEDPioglitazone Study of Triglyceride Changes in Subjects With Type 2 Diabetes After Conversion From Rosiglitazone.
NCT00700856PHASE4UNKNOWNThiazolidinediones Or Sulphonylureas and Cardiovascular Accidents.Intervention Trial
NCT00708175PHASE4COMPLETEDEfficacy of Pioglitazone on Bone Metabolism in Postmenopausal Women With Impaired Fasting Glucose.

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

84 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
RosiglitazoneChEMBL + PubChemPhase 4 (approved)PPARG, TRPM3
FULVESTRANTChEMBL + PubChemPhase 4 (approved)PPARG
BENZBROMARONEChEMBLPhase 4 (approved)PPARG
BEXAROTENEChEMBLPhase 4 (approved)PPARG
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)PPARG
CANNABIDIOLChEMBLPhase 4 (approved)PPARG
CARVEDILOLChEMBLPhase 4 (approved)PPARG
CEFAMANDOLEChEMBLPhase 4 (approved)PPARG
CEFOTAXIMEChEMBLPhase 4 (approved)PPARG
CEFOXITINChEMBLPhase 4 (approved)PPARG
CEFTAZIDIMEChEMBLPhase 4 (approved)PPARG
CEFTRIAXONEChEMBLPhase 4 (approved)PPARG
CLOBETASOL PROPIONATEChEMBLPhase 4 (approved)PPARG
EFAVIRENZChEMBLPhase 4 (approved)PPARG
ELAFIBRANORChEMBLPhase 4 (approved)PPARG
FENOFIBRATEChEMBLPhase 4 (approved)PPARG
FENOFIBRIC ACIDChEMBLPhase 4 (approved)PPARG
GEMFIBROZILChEMBLPhase 4 (approved)PPARG
GLYBURIDEChEMBLPhase 4 (approved)PPARG
INDOMETHACINChEMBLPhase 4 (approved)PPARG
LASOFOXIFENEChEMBLPhase 4 (approved)PPARG
LEVOTHYROXINEChEMBLPhase 4 (approved)PPARG
LIOTHYRONINEChEMBLPhase 4 (approved)PPARG
LUMIRACOXIBChEMBLPhase 4 (approved)PPARG
MASOPROCOLChEMBLPhase 4 (approved)PPARG
METHYLENE BLUEChEMBLPhase 4 (approved)PPARG
MONTELUKASTChEMBLPhase 4 (approved)PPARG
NINTEDANIBChEMBLPhase 4 (approved)PPARG
PEMAFIBRATEChEMBLPhase 4 (approved)PPARG
RIMONABANTChEMBLPhase 4 (approved)PPARG
SULINDACChEMBLPhase 4 (approved)PPARG
TELMISARTANChEMBLPhase 4 (approved)PPARG
TERIFLUNOMIDEChEMBLPhase 4 (approved)PPARG
TIPRANAVIRChEMBLPhase 4 (approved)PPARG
TROGLITAZONEChEMBLPhase 4 (approved)PPARG
ZAFIRLUKASTChEMBLPhase 4 (approved)PPARG
ALEGLITAZARChEMBLPhase 3PPARG
BALAGLITAZONEChEMBLPhase 3PPARG
BEZAFIBRATEChEMBLPhase 3PPARG
CANDESARTANChEMBLPhase 3PPARG
DOCONEXENTChEMBLPhase 3PPARG
GAMOLENIC ACIDChEMBLPhase 3PPARG
ICOSAPENTChEMBLPhase 3PPARG
IMIGLITAZARChEMBLPhase 3PPARG
LANIFIBRANORChEMBLPhase 3PPARG
LERIGLITAZONEChEMBLPhase 3PPARG
LOBEGLITAZONEChEMBLPhase 3PPARG
MURAGLITAZARChEMBLPhase 3PPARG
NAMODENOSONChEMBLPhase 3PPARG
QUERCETINChEMBLPhase 3PPARG
RESVERATROLChEMBLPhase 3PPARG
RIVOGLITAZONEChEMBLPhase 3PPARG
TESAGLITAZARChEMBLPhase 3PPARG
TIRATRICOLChEMBLPhase 3PPARG
ARHALOFENATEChEMBLPhase 2PPARG
ATX08-001ChEMBLPhase 2PPARG
CANNABIGEROLChEMBLPhase 2PPARG
CIGLITAZONEChEMBLPhase 2PPARG
CXA-10ChEMBLPhase 2PPARG
DIHOMO-GAMMA-LINOLENIC ACIDChEMBLPhase 2PPARG

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot