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Spironolactone

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Also known as AbbolactoneAldactoneCarospirDiatensecEspironolactonaGx spironolLaractoneNSC-150399QaialdoSC-9420SpireticSpiroctan 100Spiroctan 25Spiroctan 50Spironolactone cevaSpironolactone component of aldactazideSpironolactone component of cardalisSpironolactonumSpirospare 100

Summary

Spironolactone (CHEMBL1393) is an approved small-molecule diuretic (ATC C03DA01) targeting NR3C2; indicated across 44 conditions including heart failure and hypertensive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C03DA01
  • Targets: 1 (NR3C2)
  • Indications: 44 conditions
  • Clinical trials: 201
  • Chemistry: 416.6 Da · C24H32O4S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1393
NameSpironolactone
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID5833
ChEBICHEBI:9241
ATCC03DA01
Molecular formulaC24H32O4S
Molecular weight416.6
InChIKeyLXMSZDCAJNLERA-ZHYRCANASA-N

SMILES: CC(=O)S[C@@H]1CC2=CC(=O)CC[C@@]2([C@@H]3[C@@H]1[C@@H]4CC[C@]5([C@]4(CC3)C)CCC(=O)O5)C

IUPAC name: S-[(7R,8R,9S,10R,13S,14S,17R)-10,13-dimethyl-3,5’-dioxospiro[2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-17,2’-oxolane]-7-yl] ethanethioate

ChEBI definition: A steroid lactone that is 17α-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an α-acetylsulfanyl group at position 7.

Pharmacological roles (ChEBI): diuretic, antihypertensive agent.

Other ChEBI roles (chemical / environmental): environmental contaminant, xenobiotic.

Also known as: Abbolactone, Aldactone, Carospir, Diatensec, Espironolactona, Gx spironol, Laractone, NSC-150399, Qaialdo, SC-9420, Spiretic, Spiroctan 100

Patent coverage: 14,744 distinct patent families (49,171 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
NR3C2Mineralocorticoid receptorAntagonist8.630%P08235

Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Multidrug and toxin extrusion protein 1, 5-hydroxytryptamine receptor 2B, Androgen receptor, Mineralocorticoid receptor, Glucocorticoid receptor, Estrogen receptor, Progesterone receptor, Muscarinic acetylcholine receptor M2, Alpha-1A adrenergic receptor, Kappa-type opioid receptor.

Bioactivity

ChEMBL activities: 49 potent at pChembl ≥ 5 of 56 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
NR3C28.8IC501.6nMCHEMBL_ACT_3224290
NR3C28.63Ki2.32nMCHEMBL_ACT_2008173
NR3C28.3Ki5.01nMCHEMBL_ACT_19363717
NR3C28.06IC508.7nMCHEMBL_ACT_24808080
NR3C28.02IC509.62nMCHEMBL_ACT_24808037
NR3C27.96IC5011nMCHEMBL_ACT_13393481
NR3C27.96IC5011nMCHEMBL_ACT_14566205
NR3C27.96IC5011nMCHEMBL_ACT_22825220
NR3C27.89IC5013nMCHEMBL_ACT_3403606
NR3C17.49Ki32.6nMCHEMBL_ACT_2008189
AR7.41Ki39.4nMCHEMBL_ACT_2008193
AR7.32IC5048nMCHEMBL_ACT_24808042
NR3C27.31IC5049nMCHEMBL_ACT_15095258
NR3C27.31IC5049nMCHEMBL_ACT_7970151
NR3C27.3IC5050.12nMCHEMBL_ACT_19363718
PGR7.3AC5050nMCHEMBL_ACT_25192988
NR3C27.22IC5060nMCHEMBL_ACT_15099906
NR3C27.22IC5060nMCHEMBL_ACT_7970232
NR3C27.12IC5076nMCHEMBL_ACT_24697149
AR7.11IC5077nMCHEMBL_ACT_29092451
P152077.04Ki90.6nMCHEMBL_ACT_7796899
AR6.92IC50120nMCHEMBL_ACT_15095285
P152076.92AC50120nMCHEMBL_ACT_25187795
AR6.92IC50120nMCHEMBL_ACT_7970193
P152076.87IC50135.9nMCHEMBL_ACT_7796898
NR3C16.72AC50190nMCHEMBL_ACT_25176434
P152076.64AC50230nMCHEMBL_ACT_25233210
NR3C26.57IC50270nMCHEMBL_ACT_29241937
PGR6.4Ki399.7nMCHEMBL_ACT_2008197
NR3C26.31IC50490nMCHEMBL_ACT_29211760

Target pathways

Aggregated over 1 target gene(s): NR3C2.

Top Reactome pathways

9 total, by targets touching each:

PathwayTargetsGenes
Cellular responses to stress1NR3C2
SUMOylation1NR3C2
SUMO E3 ligases SUMOylate target proteins1NR3C2
HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand1NR3C2
Nuclear Receptor transcription pathway1NR3C2
Metabolism of proteins1NR3C2
SUMOylation of intracellular receptors1NR3C2
Post-translational protein modification1NR3C2
Cellular responses to stimuli1NR3C2

Dominant GO biological processes

GO termTargets
regulation of transcription by RNA polymerase II1
signal transduction1
nuclear receptor-mediated steroid hormone signaling pathway1
positive regulation of non-canonical NF-kappaB signal transduction1
regulation of DNA-templated transcription1
cellular response to hormone stimulus1
response to lipid1

Indications & clinical

Indications

44 indications (13 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
heart failure4MONDO:0005252EFO:0003144
hypertensive disorder4MONDO:0005044EFO:0000537
myocardial infarction4MONDO:0005068EFO:0000612
cardiovascular disorder4MONDO:0004995EFO:0000319
congestive heart failure4MONDO:0005009EFO:0000373
nephrotic syndrome4MONDO:0005377EFO:0004255
preeclampsia4MONDO:0005081EFO:0000668
cirrhosis of liver4MONDO:0005155EFO:0001422
essential hypertension4MONDO:0001134MONDO:0001134
hyperaldosteronism4MONDO:0003009HP:0011736
chronic kidney disease3MONDO:0005300EFO:0003884
atrial fibrillation3MONDO:0004981EFO:0000275
diastolic heart failure3MONDO:0006727EFO:1000899
acne3MONDO:0011438EFO:0003894
acute kidney injury3MONDO:0002492HP:0001919
ST-elevation myocardial infarction3MONDO:0041656EFO:0008585
autosomal dominant polycystic kidney disease3MONDO:0004691EFO:1001496
aortic valve stenosis3MONDO:0042981EFO:0000266
rheumatoid arthritis3MONDO:0008383EFO:0000685
Duchenne muscular dystrophy3MONDO:0010679MONDO:0010679
pulmonary arterial hypertension2MONDO:0015924EFO:0001361
polycystic ovary syndrome2MONDO:0008487EFO:0000660
fatty liver disease2MONDO:0004790HP:0001397
precocious puberty2MONDO:0000088MONDO:0000088
age-related macular degeneration2MONDO:0005150EFO:0001365
intracerebral hemorrhage2MONDO:0013792EFO:0005669
severe acute respiratory syndrome2MONDO:0005091MONDO:0100096
arrhythmogenic right ventricular cardiomyopathy2MONDO:0016587Orphanet:247
cardiomyopathy2MONDO:0004994EFO:0000318
neuroblastoma2MONDO:0005072EFO:0000621
neoplasm2MONDO:0005070MONDO:0004992
diabetic kidney disease1MONDO:0005016EFO:0000401
acute myeloid leukemia1MONDO:0018874EFO:0000222
leukemia1MONDO:0005059EFO:0000565
metabolic dysfunction-associated steatohepatitis1MONDO:0007027EFO:1001249
chorioretinitis1MONDO:0004674HP:0012424
diabetes mellitus1MONDO:0005015EFO:0000400
alcohol abuse1MONDO:0002046MONDO:0007079
dry eye syndrome0MONDO:0006733EFO:1000906

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

Clinical trials

Total trials: 201.

Phase distribution

PhaseTrials
PHASE464
PHASE239
Not specified38
PHASE326
PHASE114
PHASE2/PHASE38
PHASE1/PHASE27
EARLY_PHASE15

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03984591PHASE4ENROLLING_BY_INVITATIONA Registry-based Cluster Randomized Trial to Compare the Effect of Spironolactone vs. Eplerenone on Clinical Outcomes in Patients With Symptomatic Systolic Heart Failure
NCT04582383PHASE4ACTIVE_NOT_RECRUITINGComparative Effectiveness Study of Spironolactone Versus Doxycycline for Acne
NCT06457074PHASE4RECRUITINGFinerenone for Patients With Primary Aldosteronism (FAIRY)
NCT07281014PHASE4RECRUITINGUnmitigated Aldosterone Signaling During Standard Clinical MRA Dosing
NCT07523867PHASE4NOT_YET_RECRUITINGSpironolactone Alternate Dosing vs Finerenone in Elevated Potassium - K Safety Study
NCT00206232PHASE4COMPLETEDNovel Treatment for Diastolic Heart Failure in Women
NCT00226109PHASE4SUSPENDEDClinical Trial Studying the Effects of Spironolactone on Heart and Skeletal Muscle Function in Chronic Alcoholics
NCT00277693PHASE4UNKNOWNCardiovascular Protective Effect of Spironolactone in Hemodialysis
NCT00306696PHASE4COMPLETEDExamining the Effect of Different Diuretics on Fluid Retention in Diabetics Treated With Rosiglitazone.
NCT00317954PHASE4COMPLETEDSpironolactone in Diabetic Nephropathy
NCT00328809PHASE4WITHDRAWNSpironolactone Safety in Dialysis Patients
NCT00332904PHASE4UNKNOWNEffect of Betablocker or Aldosterone Antagonist Therapy on Patients With Liver Cirrhosis
NCT00335413PHASE4COMPLETEDAutoregulation of Glomerular Filtration Rate in Patients With Type 1 Diabetes During Spironolactone Therapy
NCT00391846PHASE4COMPLETEDEvaluation of Heart Failure Treatment Guided by N-terminal Pro B-type Natriuretic Peptide (NTproBNP) vs Clinical Symptoms and Signs Alone
NCT00524615PHASE4UNKNOWNAddition of Spironolactone in Patients With Resistant Arterial Hypertension
NCT00527059PHASE4UNKNOWNRenal Effects of Levosimendan in Patients Admitted With Acute Decompensated Heart Failure
NCT00548912PHASE4WITHDRAWNLeft Ventricular Hypertrophy and Spironolactone in End Stage Renal Disease
NCT00574119PHASE4COMPLETEDEffect of Aldosterone on Energy Starvation in Heart Failure
NCT00663195PHASE4COMPLETEDEffects of Spironolactone on Matrix Metalloproteinases (MMPs) in Heart Failure
NCT00664222PHASE4COMPLETEDSpironolactone and Insulin Resistance in Chronic Heart Failure (CHF)
NCT00741663PHASE4COMPLETEDSpironolactone Versus Spironolactone Plus Furosemide (SVSSF)
NCT00870402PHASE4UNKNOWNAldosterone in Diabetic Nephropathy
NCT00879060PHASE4COMPLETEDClinical and Therapeutic Implications of Fibrosis in Hypertrophic Cardiomyopathy
NCT01089309PHASE4COMPLETEDEffect of Aldosterone Blockade on Arterial Compliance
NCT01128101PHASE4UNKNOWNEffects of Spironolactone in Dialysis
NCT01388088PHASE4COMPLETEDThe Effect of Amiloride and Spironolactone in Patients With Hypertension
NCT01468571PHASE4UNKNOWNEffects of Spironolactone on Collagen Metabolism in Patients With Pulmonary Arterial Hypertension
NCT01510795PHASE4UNKNOWNMineralocorticoid Receptor Antagonist and Kidney Allograft Histology
NCT01602861PHASE4COMPLETEDThe Effects of Spironolactone on Calcineurin Inhibitor Induced Nephrotoxicity
NCT01643434PHASE4UNKNOWNResistant Hypertension Optimal Treatment
NCT01687699PHASE4COMPLETEDEffects of Spironolactone on Cardio- and Cerebrovascular Morbidity and Mortality in Hemodialysis Patients
NCT01843309PHASE4TERMINATEDUse of Spironolactone for the Prevention of Electrolyte Abnormalities in Patients Treated With Amphotericin B
NCT01855334PHASE4WITHDRAWNL-Arginine and Spironolactone Trial in Dialysis-Dependent ESRD
NCT01944384PHASE4COMPLETEDImpacts of Aldosterone Blockade on Myocardial Remodeling in Hypertensive Patients With Diastolic Failing Heart
NCT02046668PHASE4COMPLETEDThe Effect of Spironolactone on Pain in Older People With Osteoarthritis
NCT02053974PHASE4COMPLETEDSpironolactone Against Anthracycline-induced Cardiomyopathy
NCT02169089PHASE4COMPLETEDMineralocorticoid Receptor Antagonism Clinical Evaluation in Atherosclerosis Trial
NCT02369081PHASE4UNKNOWNOptimum Treatment for Drug-Resistant Hypertension
NCT02429388PHASE4WITHDRAWNHigh-Dose Aldactone for Treatment of Diuretic Resistant Heart Failure
NCT02483195PHASE4WITHDRAWNThe Use of 5mg Finasteride Versus 200mg Spironolactone and Topical 5% Minoxidil in Treating Postmenopausal Female Androgenetic Alopecia

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 8 clinical and 15 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

25 molecules share ≥1 primary target. Top 25 by shared-target count:

MoleculeSourceStatusShared targets
EPLERENONEChEMBL + PubChemPhase 4 (approved)NR3C2
BUDESONIDEChEMBLPhase 4 (approved)NR3C2
DEXAMETHASONEChEMBLPhase 4 (approved)NR3C2
FINERENONEChEMBLPhase 4 (approved)NR3C2
FLUTICASONE FUROATEChEMBLPhase 4 (approved)NR3C2
FLUTICASONE PROPIONATEChEMBLPhase 4 (approved)NR3C2
HYDROCORTISONEChEMBLPhase 4 (approved)NR3C2
HYDROCORTISONE BUTYRATEChEMBLPhase 4 (approved)NR3C2
MEDROXYPROGESTERONEChEMBLPhase 4 (approved)NR3C2
MIFEPRISTONEChEMBLPhase 4 (approved)NR3C2
PREDNISOLONEChEMBLPhase 4 (approved)NR3C2
PROGESTERONEChEMBLPhase 4 (approved)NR3C2
ASOPRISNILChEMBLPhase 3NR3C2
BALCINRENONEChEMBLPhase 3NR3C2
CORTICOSTERONEChEMBLPhase 3NR3C2
ALDOSTERONEChEMBLPhase 2NR3C2
LY2623091ChEMBLPhase 2NR3C2
METRIBOLONEChEMBLPhase 2NR3C2
MT-3995ChEMBLPhase 2NR3C2
ONAPRISTONEChEMBLPhase 2NR3C2
STANOLONEChEMBLPhase 2NR3C2
TUROFEXORATE ISOPROPYLChEMBLPhase 2NR3C2
EnzalutamidePubChemApprovedNR3C2
FludrocortisonePubChemApprovedNR3C2
ursodiolPubChemApprovedNR3C2

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