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Rosiglitazone

drug
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Also known as AvandiaAvandametAvandarylBRL-49653GaudilNSC-758698NyractaRezultRosiglitazonaRosiglizoleRosvelTDZ-01VenviaSID26748954(R,S)-rosiglitazoneSID144204987SID170465417SID174007204ROSIGLITAZONE MALEATE

Summary

Rosiglitazone (CHEMBL121) is an approved small-molecule insulin-sensitizing drug (ATC A10BG02) targeting FFAR1, TRPC5, and TRPM3; indicated across 37 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: A10BG02
  • Targets: 4 (FFAR1, TRPC5, TRPM3…)
  • Indications: 37 conditions
  • Clinical trials: 167
  • Chemistry: C18H19N3O3S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL121
NameRosiglitazone
TypeSmall molecule
Max phase4
ChEBICHEBI:50122
ATCA10BG02
Molecular formulaC18H19N3O3S
InChIKeyYASAKCUCGLMORW-UHFFFAOYSA-N

SMILES: CN(CCOc1ccc(CC2SC(=O)NC2=O)cc1)c1ccccn1

Pharmacological roles (ChEBI): insulin-sensitizing drug, ferroptosis inhibitor, EC 6.2.1.3 (long-chain-fatty-acid—CoA ligase) inhibitor.

Also known as: Avandia, Avandamet, Avandaryl, BRL-49653, Gaudil, NSC-758698, Nyracta, Rezult, Rosiglitazona, Rosiglitazone, Rosiglizole, Rosvel

Parent form; salt/anhydrous children: CHEMBL843, CHEMBL1704605

Patent coverage: 15,358 distinct patent families (58,849 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 58,822 (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
FFAR1FFA1 receptorFull agonist5.60.4%O14842
TRPC5TRPC5Activation4.510%Q9UL62
TRPM3TRPM30.1%Q9HCF6
PPARGPeroxisome proliferator-activated receptor-γAgonist6.922.6%P37231

Broader ChEMBL bioactivity targets: 39 (assay-derived). Sample: Lysine-specific demethylase 4E, Prelamin-A/C, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], ATP-binding cassette sub-family C member 4, CDGSH iron-sulfur domain-containing protein 1, 5-hydroxytryptamine receptor 2B, Thromboxane-A synthase, Alpha-2A adrenergic receptor, Amine oxidase [flavin-containing] A, Amine oxidase [flavin-containing] B.

Bioactivity

ChEMBL activities: 285 potent at pChembl ≥ 5 of 312 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P250959.64Ki0.23nMCHEMBL_ACT_12462149
PPARG9EC501nMCHEMBL_ACT_17771349
PPARG8.92Kd1.2nMCHEMBL_ACT_18034057
LMNA8.66Potency2.2nMCHEMBL_ACT_3640358
PPARG8.62EC502.4nMCHEMBL_ACT_10964645
PPARG8.57EC502.7nMCHEMBL_ACT_2182591
PPARG8.42EC503.8nMCHEMBL_ACT_2182570
PPARG8.4EC504nMCHEMBL_ACT_12703891
PPARG8.4EC504nMCHEMBL_ACT_1615148
PPARG8.4EC504nMCHEMBL_ACT_18346876
PPARG8.4EC504nMCHEMBL_ACT_18987707
PPARA8.4EC504nMCHEMBL_ACT_2080399
PPARG8.24Ki5.8nMCHEMBL_ACT_13342008
PPARG8.15Kd7nMCHEMBL_ACT_12703900
PPARG8.11IC507.7nMCHEMBL_ACT_22773174
PPARG8.1Ki8nMCHEMBL_ACT_1615150
PPARG8.1EC508nMCHEMBL_ACT_18758366
PPARG8.1Ki8nMCHEMBL_ACT_2080368
PPARG8.05EC509nMCHEMBL_ACT_25100673
PPARG8EC5010nMCHEMBL_ACT_1178659
PPARG8Ki10nMCHEMBL_ACT_12712909
PPARG8EC5010nMCHEMBL_ACT_13295537
PPARG8EC5010nMCHEMBL_ACT_15068925
PPARG8IC5010nMCHEMBL_ACT_16501803
PPARG8IC5010nMCHEMBL_ACT_16838444
PPARG8EC5010nMCHEMBL_ACT_6232173
PPARG7.96EC5011nMCHEMBL_ACT_10918803
PPARG7.96IC5011nMCHEMBL_ACT_13342080
PPARG7.96EC5011nMCHEMBL_ACT_3256965
PPARG7.96EC5011nMCHEMBL_ACT_8024377

Target pathways

Aggregated over 4 target gene(s): FFAR1, TRPC5, TRPM3, PPARG.

Top Reactome pathways

15 total, by targets touching each:

PathwayTargetsGenes
TRP channels2TRPC5, TRPM3
PPARA activates gene expression1PPARG
Transcriptional regulation of white adipocyte differentiation1PPARG
Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1)1FFAR1
Nuclear Receptor transcription pathway1PPARG
Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP)1FFAR1
SUMOylation of intracellular receptors1PPARG
G alpha (q) signalling events1FFAR1
Role of second messengers in netrin-1 signaling1TRPC5
Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion1FFAR1
Free fatty acid receptors1FFAR1
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
G protein-coupled receptor signaling pathway2
positive regulation of cytosolic calcium ion concentration2
glucose homeostasis2
calcium ion transport2
calcium ion transmembrane transport2
monoatomic ion transport2
monoatomic ion transmembrane transport2
transmembrane transport2
phospholipase C-activating G protein-coupled receptor signaling pathway1
insulin secretion1
positive regulation of insulin secretion1
negative regulation of interleukin-1 beta production1
positive regulation of calcium ion transport1
response to fatty acid1
ligand-gated ion channel signaling pathway1

Indications & clinical

Indications

37 indications (2 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
type 2 diabetes mellitus4MONDO:0005148MONDO:0005148
prostate adenocarcinoma3MONDO:0005082EFO:0000673
diabetic neuropathy3MONDO:0006626EFO:1000783
metabolic syndrome X3MONDO:0011565EFO:0000195
multiple organ dysfunction syndrome3MONDO:0043726EFO:1001373
hypertensive disorder3MONDO:0005044EFO:0000537
metabolic disease3MONDO:0005066EFO:0000589
glucose intolerance3MONDO:0001076EFO:0002546
atherosclerosis3MONDO:0005311EFO:0003914
coronary artery disorder3MONDO:0005010EFO:0001645
Alzheimer disease3MONDO:0004975MONDO:0004975
cardiovascular disorder3MONDO:0004995EFO:0000319
metabolic dysfunction-associated steatotic liver disease2MONDO:0013209EFO:0003095
ulcerative colitis2MONDO:0005101EFO:0000729
HIV infectious disease2MONDO:0005109EFO:0000764
rheumatoid arthritis2MONDO:0008383EFO:0000685
endometriosis2MONDO:0005133EFO:0001065
Sezary syndrome2MONDO:0017844EFO:1000785
mycosis fungoides2MONDO:0009691EFO:1001051
prediabetes syndrome2MONDO:0006920EFO:1001121
asthma2MONDO:0004979MONDO:0004979
inflammatory bowel disease2MONDO:0005265EFO:0003767
erectile dysfunction1MONDO:0005362EFO:0004234
focal segmental glomerulosclerosis1MONDO:0100313EFO:0004236
Plasmodium falciparum malaria1MONDO:0005920EFO:0007444
neoplasm1MONDO:0005070EFO:0000616
malaria1MONDO:0005136EFO:0001068
anemia1MONDO:0002280EFO:0004272
breast neoplasm1MONDO:0021100MONDO:0007254

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

Clinical trials

Total trials: 167.

Phase distribution

PhaseTrials
PHASE345
PHASE437
Not specified31
PHASE227
PHASE119
PHASE2/PHASE35
PHASE1/PHASE23

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00044460PHASE4COMPLETEDEfficacy and Safety In Poorly Controlled Type 2 Diabetics
NCT00121966PHASE4COMPLETEDSouth Danish Diabetes Study: Evaluation of the Antidiabetic Treatment of Type 2 Diabetes Mellitus
NCT00123643PHASE4COMPLETEDVascular Effects of Rosiglitazone Versus Glyburide in Type 2 Diabetic Patients
NCT00207402PHASE4COMPLETEDInfergen, Ribavirin & Avandia in Previous Relapsers or Nonresponders to Pegylated Interferon and Ribavirin
NCT00225342PHASE4WITHDRAWNStudy Protocol for Rosiglitazone Versus Gliclazide in Diabetics With Angina
NCT00225355PHASE4TERMINATEDRosiglitazone Versus Placebo in Chronic Stable Angina
NCT00241605PHASE4COMPLETEDAVANDAMET Versus Metformin For Type 2 Diabetes Mellitus
NCT00304993PHASE4COMPLETEDStudy of Niacin and Rosiglitazone in Dysmetabolic Dyslipidemia
NCT00306176PHASE4COMPLETEDRosiglitazone and Exercise in Patients With Type 2 Diabetes Mellitus
NCT00306644PHASE4COMPLETEDEffect Of Rosiglitazone On Carotid Intima Media Thickness In Patients With Insulin Resistance Syndrome And/Or Type 2 Diabetes
NCT00306696PHASE4COMPLETEDExamining the Effect of Different Diuretics on Fluid Retention in Diabetics Treated With Rosiglitazone.
NCT00314561PHASE4COMPLETEDThe Effect of Pioglitazone and Rosiglitazone on Atherosclerotic and Inflammatory Markers in Patients With Metabolic Syndrome
NCT00329225PHASE4COMPLETEDRosiglitazone In Subjects With Type 2 Diabetes Mellitus Who Are Inadequately Controlled On Insulin
NCT00333723PHASE4COMPLETEDAVANDIA With Glyburide In African American And Hispanic Patients With Type 2 Diabetes Not Controlled by Glyburide Alone
NCT00337350PHASE4COMPLETEDRosiglitazone for Clozapine Induced Glucose Metabolism Impairment
NCT00343395PHASE4TERMINATEDRosiglitazone and Metformin: Outcomes Trial in Nondiabetic Patients With Stable Coronary Syndromes (Romance) Pilot Study
NCT00358124PHASE4COMPLETEDInsulin Glargine v Rosiglitazone as add-on Therapy in Patients Failing Sulfonylurea and Metformin Combination Therapy
NCT00364221PHASE4COMPLETEDEffect of Rosiglitazone in Nondiabetic Patients With the Metabolic Syndrome
NCT00372086PHASE4COMPLETEDRosiglitazone and Insulin in T1DM Adolescents
NCT00373178PHASE4COMPLETEDMetabolic Effects of Treatment in Patients With Recently Diagnosed Type 2 Diabetes
NCT00424762PHASE4COMPLETEDEffect of Rosiglitazone Versus Placebo on Cardiovascular Performance and Myocardial Triglyceride
NCT00440375PHASE4COMPLETEDEffects of Rosiglitazone on Bone in Postmenopausal Diabetic Women
NCT00501020PHASE4COMPLETEDComparison of the Efficacy and Tolerability of the Addition of AVANDIA to Submaximal Doses of Metformin
NCT00522470PHASE4COMPLETEDEffects of Rosiglitazone on Serum Ghrelin and Peptide YY Levels
NCT00567593PHASE4COMPLETEDGene Regulation by Thiazolidinediones
NCT00571506PHASE4COMPLETEDEffect of Thiazolidinedione Treatment Vascular Risk Markers
NCT00640224PHASE4COMPLETEDInsulin Resistance, Polycystic Ovary Syndrome, and Bone Research Study
NCT00675740PHASE4COMPLETEDPhysical Exercise Versus Rosiglitazone in CAD and Prediabetes
NCT00679939PHASE4COMPLETEDStudy In Postmenopausal Women With Type 2 Diabetes Looking At Approved Diabetes Drugs And How They Affect Bone Health
NCT00733174PHASE4UNKNOWNRosiglitazone Therapy In The Prevention Of Coronary Artery Disease In Patients With Impaired Glucose Tolerance
NCT00738023PHASE4COMPLETEDFree Fatty Acid-Induced Hypertension in Obese Subjects With Type 2 Diabetes
NCT00746174PHASE4COMPLETEDInsulin Resistance and Intramyocellular Lipid Content in Glucose Intolerant Subjects Receiving Rosiglitazone
NCT00819910PHASE4TERMINATEDRosiglitazone And Fenofibrate Additive Effects on Lipids (RAFAEL)
NCT00879970PHASE4TERMINATEDThiazolidinedione Intervention With Vitamin D Evaluation
NCT00953498PHASE4COMPLETEDInfluence of Glitazones on the Vasodilatory Effect of High-density Lipoprotein (HDL) Lipoproteins
NCT01406704PHASE4TERMINATEDEffects of Rosiglitazone and Alpha-lipoic Acid on the Patients With Pathologically Proved NASH
NCT02526615PHASE4COMPLETEDEffects of Rosiglitazone and Metformin on Metabolism in Type 2 Diabetes
NCT00032487PHASE3COMPLETEDGlycemic Control and Complications in Diabetes Mellitus Type 2 (VADT)
NCT00067951PHASE3COMPLETEDA Study To Evaluate The Safety And Efficacy Of An Investigational Diabetes Drug In Poorly Controlled Type II Diabetics
NCT00069836PHASE3COMPLETEDStudy Of AVANDAMET® With Or Without Insulin In Type II Diabetes Mellitus Patients. AVANDAMET® is a Registered Trademark of the GSK Group of Companies.

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.

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

MoleculeSourceStatusShared targets
PioglitazoneChEMBL + PubChemPhase 4 (approved)PPARG, TRPM3
QUERCETINChEMBL + PubChemPhase 3 (approved)PPARG, TRPC5
DOCONEXENTChEMBLPhase 3FFAR1, PPARG
GAMOLENIC ACIDChEMBLPhase 3FFAR1, PPARG
LINOLEIC ACIDChEMBLPhase 2FFAR1, PPARG
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
FASIGLIFAMChEMBLPhase 3FFAR1
ICOSAPENTChEMBLPhase 3PPARG
IMIGLITAZARChEMBLPhase 3PPARG
LANIFIBRANORChEMBLPhase 3PPARG
LERIGLITAZONEChEMBLPhase 3PPARG
LOBEGLITAZONEChEMBLPhase 3PPARG
MURAGLITAZARChEMBLPhase 3PPARG
NAMODENOSONChEMBLPhase 3PPARG
RESVERATROLChEMBLPhase 3PPARG
RIVOGLITAZONEChEMBLPhase 3PPARG
TESAGLITAZARChEMBLPhase 3PPARG
TIRATRICOLChEMBLPhase 3PPARG
ARHALOFENATEChEMBLPhase 2PPARG
ATX08-001ChEMBLPhase 2PPARG
CANNABIGEROLChEMBLPhase 2PPARG
CIGLITAZONEChEMBLPhase 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