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Furosemide

drug
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Also known as Aluzine 20Aluzine 40Aluzine 500AquamedDiuresalDryptalFroopFrumaxFrumilFrusemideFruseticFrusidFrusolFuroscixFurosemidaFurosemidumHydroledLasixLasix ret

Summary

Furosemide (CHEMBL35) is an approved small-molecule loop diuretic (ATC C03CA01) targeting GPR35, GABRA6, and SLC12A1; indicated across 43 conditions including congestive heart failure and heart failure.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C03CA01
  • Targets: 4 (GPR35, GABRA6, SLC12A1…)
  • Indications: 43 conditions
  • Clinical trials: 207
  • Chemistry: 330.74 Da · C12H11ClN2O5S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL35
NameFurosemide
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3440
ChEBICHEBI:47426
ATCC03CA01
Molecular formulaC12H11ClN2O5S
Molecular weight330.74
InChIKeyZZUFCTLCJUWOSV-UHFFFAOYSA-N

SMILES: C1=COC(=C1)CNC2=CC(=C(C=C2C(=O)O)S(=O)(=O)N)Cl

IUPAC name: 4-chloro-2-(furan-2-ylmethylamino)-5-sulfamoylbenzoic acid

ChEBI definition: A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.

Pharmacological roles (ChEBI): loop diuretic.

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

Also known as: Aluzine 20, Aluzine 40, Aluzine 500, Aquamed, Diuresal, Dryptal, Froop, Frumax, Frumil, Frusemide, Frusetic, Frusid

Parent form; salt/anhydrous children: CHEMBL1788133

Patent coverage: 126,181 distinct patent families (224,045 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 223,890 (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
GPR35GPR35Agonist5.630.2%Q9HC97
GABRA6GABAA receptor α6 subunitAntagonist0.1%Q16445
SLC12A1Kidney-specific Na-K-Cl symporterInhibition5.150.6%Q13621
SLC12A2Basolateral Na-K-Cl symporterInhibition5.130.1%P55011

Broader ChEMBL bioactivity targets: 24 (assay-derived). Sample: G-protein coupled receptor 35, Solute carrier family 22 member 6, CDGSH iron-sulfur domain-containing protein 1, Carbonic anhydrase 2, Solute carrier organic anion transporter family member 2A1, 5-hydroxytryptamine receptor 1A, Carbonic anhydrase 13, Carbonic anhydrase 7, Carbonic anhydrase 1, Carbonic anhydrase 6.

Bioactivity

ChEMBL activities: 34 potent at pChembl ≥ 5 of 44 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
CA147.28Ki52nMCHEMBL_ACT_2492029
CA147.28Ki52nMCHEMBL_ACT_29061803
CA17.21Ki62nMCHEMBL_ACT_2491952
CA17.21Ki62nMCHEMBL_ACT_29061767
CA27.19Ki65nMCHEMBL_ACT_2491959
CA27.19Ki65nMCHEMBL_ACT_29061770
CA17.1IC5080nMCHEMBL_ACT_27123884
CA66.84Ki143nMCHEMBL_ACT_29061788
CA66.64Ki230nMCHEMBL_ACT_29061785
CA66.61Ki245nMCHEMBL_ACT_2491994
CA126.58Ki261nMCHEMBL_ACT_2492015
CA126.58Ki261nMCHEMBL_ACT_29061797
CA5B6.49Ki322nMCHEMBL_ACT_2491987
CA5B6.49Ki322nMCHEMBL_ACT_29061782
CA96.38Ki420nMCHEMBL_ACT_2492008
CA96.38Ki420nMCHEMBL_ACT_29061794
CA5A6.3Ki499nMCHEMBL_ACT_2491980
CA5A6.3Ki499nMCHEMBL_ACT_29061779
CA76.29Ki513nMCHEMBL_ACT_2492001
CA76.29Ki513nMCHEMBL_ACT_29061791
Q9D6N16.26Ki550nMCHEMBL_ACT_2492022
Q9D6N16.26Ki550nMCHEMBL_ACT_29061800
CA46.25Ki564nMCHEMBL_ACT_2491973
CA46.25Ki564nMCHEMBL_ACT_29061776
CA26.2Kd630nMCHEMBL_ACT_26047528
CISD15.64Ki2285nMCHEMBL_ACT_16766167
ABCG25.5IC503200nMCHEMBL_ACT_24777398
CA25.5Kd3140nMCHEMBL_ACT_26047539
GPR355.49Ki3270nMCHEMBL_ACT_13445742
HSD11B15.42IC503760nMCHEMBL_ACT_2521192

Target pathways

Aggregated over 4 target gene(s): GPR35, GABRA6, SLC12A1, SLC12A2.

Top Reactome pathways

10 total, by targets touching each:

PathwayTargetsGenes
Transport of small molecules2SLC12A1, SLC12A2
R-HSA-4253932SLC12A1, SLC12A2
SLC-mediated transmembrane transport2SLC12A1, SLC12A2
Cation-coupled Chloride cotransporters2SLC12A1, SLC12A2
Disease1SLC12A1
Class A/1 (Rhodopsin-like receptors)1GPR35
SLC transporter disorders1SLC12A1
Defective SLC12A1 causes Bartter syndrome 1 (BS1)1SLC12A1
Disorders of transmembrane transporters1SLC12A1
GABA receptor activation1GABRA6

Dominant GO biological processes

GO termTargets
chloride transmembrane transport3
monoatomic ion transport3
signal transduction2
gamma-aminobutyric acid signaling pathway2
chloride transport2
monoatomic ion transmembrane transport2
cell volume homeostasis2
sodium ion transmembrane transport2
chloride ion homeostasis2
potassium ion homeostasis2
sodium ion homeostasis2
transepithelial ammonium transport2
potassium ion import across plasma membrane2
potassium ion transport2
sodium ion transport2

Indications & clinical

Indications

43 indications (8 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
congestive heart failure4MONDO:0005009EFO:0000373
heart failure4MONDO:0005252EFO:0003144
cardiovascular disorder4MONDO:0004995EFO:0000319
hypertensive disorder4MONDO:0005044EFO:0000537
nephrotic syndrome4MONDO:0005377EFO:0004255
cirrhosis of liver4MONDO:0005155EFO:0001422
pulmonary edema4MONDO:0006932EFO:1001134
syndromic disease4MONDO:0002254MONDO:0002254
lung disorder3MONDO:0005275EFO:0003818
pulmonary embolism3MONDO:0005279EFO:0003827
bronchiolitis3MONDO:0002465HP:0011950
kidney disorder3MONDO:0005240EFO:0003086
kidney failure3MONDO:0001106EFO:1002048
atherosclerosis3MONDO:0005311EFO:0003914
preeclampsia3MONDO:0005081EFO:0000668
coronary artery disorder3MONDO:0005010EFO:0001645
common wart3MONDO:0001209EFO:0009662
acute myocardial infarction3MONDO:0004781EFO:0008583
essential hypertension3MONDO:0001134MONDO:0001134
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
chronic obstructive pulmonary disease3MONDO:0005002EFO:0000341
nephrolithiasis3MONDO:0008171EFO:0004253
acute kidney injury2MONDO:0002492HP:0001919
acute lung injury2MONDO:0015796EFO:0004610
nasal cavity polyp2MONDO:0006314EFO:1000391
actinic keratosis2MONDO:0005173EFO:0002496
hypertension, pregnancy-induced2MONDO:0024664MONDO:0024664
chronic kidney disease2MONDO:0005300EFO:0003884
bronchopulmonary dysplasia2MONDO:0019091MONDO:0019091
neoplasm2MONDO:0005070MONDO:0004992
prostate adenocarcinoma2MONDO:0005082EFO:0000673
metabolic dysfunction-associated steatotic liver disease2MONDO:0013209EFO:0003095
acute myeloid leukemia1MONDO:0018874EFO:0000222
diabetes mellitus1MONDO:0005015EFO:0000400
leukemia1MONDO:0005059EFO:0000565
metastatic melanoma1MONDO:0005191EFO:0002617
sickle cell disease1MONDO:0011382MONDO:0011382

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

Clinical trials

Total trials: 207.

Phase distribution

PhaseTrials
Not specified51
PHASE450
PHASE334
PHASE133
PHASE220
EARLY_PHASE17
PHASE2/PHASE36
PHASE1/PHASE26

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04180397PHASE4RECRUITINGControlled Fluid Removal in Critical Ill Patients With Fluid Overload in the Intensive Care Unit.
NCT05276219PHASE4RECRUITINGOptimized Treatment of Pulmonary Edema or Congestion
NCT06094816PHASE4RECRUITINGForebrain Electroneutral Transporters in Salt-sensitive Hypertension: an MRI Study
NCT06218199PHASE4RECRUITINGDiuretics vs. Afterload Reduction for Treatment of HeartLogic Alerts
NCT06229990PHASE4RECRUITINGA Protocol Based-Furosemide Stress Test to Evaluate Renal Recovery During Continuous Renal Replacement Therapy
NCT06442280PHASE4NOT_YET_RECRUITINGSGLT-2 Inhibitor and High-Dose Furosemide Plus Small-Volume Hypertonic Saline Solution in Acute HF
NCT06979726PHASE4RECRUITINGGator SCALES-WHF: SubCutaneous Administration of Lasix to Eliminate Symptoms of Worsening Heart Failure
NCT07167862PHASE4NOT_YET_RECRUITINGOptimizing Preeclampsia Postpartum With Point-of-care Ultrasound
NCT07263035PHASE4RECRUITINGUrine Sodium-Driven Diuretic Adjustment Strategy in Acute Decompensated Heart Failure
NCT00115726PHASE4COMPLETEDTrial Assessing the Effect of Preoperative Furosemide on Intraoperative Blood Pressure
NCT00306696PHASE4COMPLETEDExamining the Effect of Different Diuretics on Fluid Retention in Diabetics Treated With Rosiglitazone.
NCT00355667PHASE4COMPLETEDComparison of Long- and Short-acting Diuretics in Congestive Heart Failure
NCT00409942PHASE4COMPLETEDEffect of a New Formulation of Torasemide (Prolonged Release)on Myocardial Fibrosis in Patients With Heart Failure.
NCT00421863PHASE4COMPLETEDItalian Study on the Cardiovascular Effects of Systolic Blood Pressure Control - CARDIOSIS Study
NCT00478543PHASE4COMPLETEDLoop Diuretics in Chronic Kidney Disease
NCT00535925PHASE4COMPLETEDNephropathy In Type 2 Diabetes and Cardio-renal Events
NCT00652652PHASE4COMPLETEDEvaluation of Combined Action Between Natrecor and Furosemide on Kidney and Neurohormone Responses in Chronic Heart Failure: A Phase-IV study704.351 / DSS
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)
NCT00937092PHASE4UNKNOWNDopamine in Acute Decompensated Heart Failure (DAD-HF) Trial
NCT01060293PHASE4TERMINATEDDopamine in Acute Decompensated Heart Failure II
NCT01073189PHASE4WITHDRAWNIntra-Renal Therapy of Diuretic Unresponsive Acute Kidney Injury
NCT01156220PHASE4WITHDRAWNInvestigation of Gender Specificity of the Effects of Furosemide in Healthy Female and Male Volunteers
NCT01419132PHASE4COMPLETEDTroponin I Release After High Diuretic Doses
NCT01441245PHASE4COMPLETEDLoop Diuretics Administration and Acute Heart Failure
NCT01815892PHASE4UNKNOWNThe Use of Furosemide in Patients on Dialysis
NCT01901809PHASE4COMPLETEDDiuretics and Dopamine in Heart Failure With Preserved Ejection Fraction
NCT01942109PHASE4UNKNOWNThe Impact of TORasemide oN hemodynAmic and Neurohormonal Stress, and carDiac remOdeling in Heart Failure
NCT01977430PHASE4UNKNOWNClinical Trial to Compare Effectiveness of Diuretics in Hemodialysis Patients With Residual Renal Function
NCT02163655PHASE4COMPLETEDDiuretics for Postpartum High Blood Pressure in Preeclampsia
NCT02183792PHASE4COMPLETEDAquaresis Utility for Hyponatremic Acute Heart Failure Study
NCT02351934PHASE4COMPLETEDEarly Diuresis Following Colorectal Surgery
NCT02427880PHASE4COMPLETEDRole of Acetazolamide and Hydrochlorothiazide Followed by Furosemide in Treating Nephrotic Edema
NCT02458157PHASE4TERMINATEDForced Fluid Removal in High Risk Acute Kidney Injury
NCT02531581PHASE4COMPLETEDDiuretic Vascular Filling in the Initial Management of Acute PE With Right Ventricular Dysfunction Normotensive
NCT02767024PHASE4WITHDRAWNIntravenous Vasodilator vs. Inotropic Therapy in Patients With Heart Failure
NCT02960412PHASE4COMPLETEDEffect of Furosemide on Confirmation of Ureteral Patency During Routine Cystoscopy
NCT03226457PHASE4COMPLETEDSGLT2 Inhibition in Combination With Diuretics in Heart Failure
NCT03731117PHASE4TERMINATEDFURosemide Stress Test to Predict Need of Renal Replacement THERapy in Ischemic Acute Tubular Necrosis in ICU

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 7 clinical and 17 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.

51 molecules share ≥1 primary target. Top 51 by shared-target count:

MoleculeSourceStatusShared targets
BumetanideChEMBL + PubChemPhase 4 (approved)GPR35, SLC12A1, SLC12A2
BAICALEINChEMBLPhase 2GABRA6, GPR35
APALUTAMIDEChEMBL + PubChemPhase 4 (approved)GABRA6
CLONAZEPAMChEMBL + PubChemPhase 4 (approved)GABRA6
CROMOLYNChEMBL + PubChemPhase 4 (approved)GPR35
DIAZEPAMChEMBL + PubChemPhase 4 (approved)GABRA6
ENZALUTAMIDEChEMBL + PubChemPhase 4 (approved)GABRA6
FLUMAZENILChEMBL + PubChemPhase 4 (approved)GABRA6
AMLEXANOXChEMBLPhase 4 (approved)GPR35
APREPITANTChEMBLPhase 4 (approved)GPR35
BREXANOLONEChEMBLPhase 4 (approved)GABRA6
CINACALCETChEMBLPhase 4 (approved)GPR35
DICUMAROLChEMBLPhase 4 (approved)GPR35
EMETINEChEMBLPhase 4 (approved)GPR35
ENTACAPONEChEMBLPhase 4 (approved)GPR35
FLUOXETINEChEMBLPhase 4 (approved)GPR35
GANAXOLONEChEMBLPhase 4 (approved)GABRA6
LINDANEChEMBLPhase 4 (approved)GABRA6
LIOTHYRONINEChEMBLPhase 4 (approved)GABRA6
LODOXAMIDEChEMBLPhase 4 (approved)GPR35
LOPERAMIDEChEMBLPhase 4 (approved)GPR35
NEFAZODONEChEMBLPhase 4 (approved)GPR35
PERPHENAZINEChEMBLPhase 4 (approved)GPR35
PIMAVANSERINChEMBLPhase 4 (approved)GPR35
PROPOFOLChEMBLPhase 4 (approved)GABRA6
TOLCAPONEChEMBLPhase 4 (approved)GPR35
VORAPAXARChEMBLPhase 4 (approved)GPR35
QUERCETINChEMBL + PubChemPhase 3 (approved)GPR35
2,4-DINITROPHENOLChEMBLPhase 2GPR35
ABECARNILChEMBLPhase 2GABRA6
BRETAZENILChEMBLPhase 2GABRA6
BUFROLINChEMBLPhase 2GPR35
BX 471 FREE BASEChEMBLPhase 2GPR35
DELORAZEPAMChEMBLPhase 2GABRA6
ELLAGIC ACIDChEMBLPhase 2GPR35
FLAVONEChEMBLPhase 2GABRA6
FORETINIBChEMBLPhase 2GPR35
LUTEOLINChEMBLPhase 2GPR35
NIFLUMIC ACIDChEMBLPhase 2GPR35
NIGULDIPINEChEMBLPhase 2GPR35
NITECAPONEChEMBLPhase 2GPR35
PANADIPLONChEMBLPhase 2GABRA6
PROGABIDEChEMBLPhase 2GABRA6
ZAPRINASTChEMBLPhase 2GPR35
.gamma.-aminobutyric acidPubChemApprovedGABRA6
alfaxalonePubChemApprovedGABRA6
CaffeinePubChemApprovedGABRA6
CiprofloxacinPubChemApprovedGABRA6
FipronilPubChemApprovedGABRA6
PhenytoinPubChemApprovedGABRA6
valproatePubChemApprovedGABRA6

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