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Atlas / Drug / Losartan

Losartan

drug
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Also known as AllisartanAngizaarDup-89E-3174Exp-3174EXP3174HGP-1405HGP1405Losartan carboxylic acidLosarticLozapNSC-758699SID26748956SID144204988SID170465135[14C]-losartanLOSARTAN POTASSIUM

Summary

Losartan (CHEMBL191) is an approved small-molecule antihypertensive agent (ATC C09CA01) targeting AGTR1; indicated across 45 conditions including cardiovascular disorder and diabetic kidney disease.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C09CA01
  • Targets: 1 (AGTR1)
  • Indications: 45 conditions
  • Clinical trials: 304
  • Chemistry: C22H23ClN6O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL191
NameLosartan
TypeSmall molecule
Max phase4
ChEBICHEBI:6541
ATCC09CA01
Molecular formulaC22H23ClN6O
InChIKeyPSIFNNKUMBGKDQ-UHFFFAOYSA-N

SMILES: CCCCc1nc(Cl)c(CO)n1Cc1ccc(-c2ccccc2-c2nnnn2)cc1

ChEBI definition: A biphenylyltetrazole where a 1,1’-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4’-position

Pharmacological roles (ChEBI): antihypertensive agent, angiotensin receptor antagonist, endothelin receptor antagonist, anti-arrhythmia drug.

Also known as: Allisartan, Angizaar, Dup-89, E-3174, Exp-3174, EXP3174, HGP-1405, HGP1405, Losartan, Losartan carboxylic acid, Losartic, Lozap

Parent form; salt/anhydrous children: CHEMBL995, CHEMBL367465

Patent coverage: 23,253 distinct patent families (88,932 SureChEMBL compound mentions), from 3 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
AGTR1AT1 receptorAntagonist8.210.4%P30556

Broader ChEMBL bioactivity targets: 29 (assay-derived). Sample: Type-1 angiotensin II receptor, Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, Angiotensin-converting enzyme, Adrenergic receptor alpha-1, Thromboxane A2 receptor, Progesterone receptor, Phosphodiesterase 4, Angiotensin II receptor, Phosphodiesterase 3.

Bioactivity

ChEMBL activities: 141 potent at pChembl ≥ 5 of 157 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
AGTR19.48IC500.33nMCHEMBL_ACT_10956584
CNR18.92AC501.2nMCHEMBL_ACT_25116762
AGTR18.8Kd1.58nMCHEMBL_ACT_318902
P349768.8Kd1.58nMCHEMBL_ACT_656832
AGTR18.8Kd1.58nMCHEMBL_ACT_718164
P250958.74IC501.8nMCHEMBL_ACT_258259
P250958.72Ki1.9nMCHEMBL_ACT_1488493
P349768.52IC503nMCHEMBL_ACT_263892
AGTR18.49IC503.24nMCHEMBL_ACT_16650273
AGTR18.48Kd3.31nMCHEMBL_ACT_1035099
AGTR18.48Kd3.31nMCHEMBL_ACT_5202034
P290898.44Ki3.6nMCHEMBL_ACT_393695
AGTR18.43Kd3.71nMCHEMBL_ACT_1190866
P349768.43Kd3.71nMCHEMBL_ACT_793953
P250958.34IC504.6nMCHEMBL_ACT_671055
AGTR18.3Ki5.01nMCHEMBL_ACT_18880679
P250958.3IC505nMCHEMBL_ACT_271865
P250958.3IC505nMCHEMBL_ACT_271869
P290898.3IC505nMCHEMBL_ACT_575411
AGTR18.28AC505.2nMCHEMBL_ACT_25176897
P349768.27Kd5.37nMCHEMBL_ACT_309548
AGTR28.26Ki5.5nMCHEMBL_ACT_27155606
AGTR28.26Ki5.5nMCHEMBL_ACT_27725312
AGTR18.25IC505.62nMCHEMBL_ACT_10973608
AGTR18.25IC505.62nMCHEMBL_ACT_12710846
P250958.24Ki5.7nMCHEMBL_ACT_569086
AGTR18.22IC506nMCHEMBL_ACT_10973632
P250958.17IC506.7nMCHEMBL_ACT_1776079
P250958.17IC506.7nMCHEMBL_ACT_2153787
P290898.17IC506.7nMCHEMBL_ACT_637000

Target pathways

Aggregated over 1 target gene(s): AGTR1.

Top Reactome pathways

11 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction1AGTR1
Membrane Trafficking1AGTR1
Signaling by GPCR1AGTR1
Class A/1 (Rhodopsin-like receptors)1AGTR1
Peptide ligand-binding receptors1AGTR1
GPCR downstream signalling1AGTR1
G alpha (q) signalling events1AGTR1
GPCR ligand binding1AGTR1
Vesicle-mediated transport1AGTR1
Cargo recognition for clathrin-mediated endocytosis1AGTR1
Clathrin-mediated endocytosis1AGTR1

Dominant GO biological processes

GO termTargets
regulation of cell growth1
kidney development1
renin-angiotensin regulation of aldosterone production1
maintenance of blood vessel diameter homeostasis by renin-angiotensin1
regulation of systemic arterial blood pressure by renin-angiotensin1
inflammatory response1
G protein-coupled receptor signaling pathway1
phospholipase C-activating G protein-coupled receptor signaling pathway1
positive regulation of cytosolic calcium ion concentration1
Rho protein signal transduction1
positive regulation of macrophage derived foam cell differentiation1
regulation of vasoconstriction1
calcium-mediated signaling1
low-density lipoprotein particle remodeling1
regulation of renal sodium excretion1

Indications & clinical

Indications

45 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
cardiovascular disorder4MONDO:0004995EFO:0000319
diabetic kidney disease3MONDO:0005016EFO:0000401
glioblastoma3MONDO:0018177EFO:0000519
hypertensive disorder3MONDO:0005044EFO:0000537
kidney disorder3MONDO:0005240EFO:0003086
heart failure3MONDO:0005252EFO:0003144
chronic kidney disease3MONDO:0005300EFO:0003884
IgA glomerulonephritis3MONDO:0005342EFO:0004194
metabolic dysfunction-associated steatohepatitis3MONDO:0007027EFO:1001249
proteinuria3MONDO:0003634HP:0000093
severe acute respiratory syndrome3MONDO:0005091EFO:0000694
pulmonary hypertension3MONDO:0005149MONDO:0005149
essential hypertension3MONDO:0001134MONDO:0001134
primary hyperoxaluria3MONDO:0002474MONDO:0002474
Marfan syndrome3MONDO:0007947MONDO:0007947
metabolic dysfunction-associated steatotic liver disease3MONDO:0013209EFO:0003095
hypertrophic cardiomyopathy2MONDO:0005045EFO:0000538
HIV infectious disease2MONDO:0005109EFO:0000764
idiopathic pulmonary fibrosis2MONDO:0800504EFO:0000768
post-traumatic stress disorder2MONDO:0005146EFO:0001358
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
focal segmental glomerulosclerosis2MONDO:0100313EFO:0004236
acute respiratory distress syndrome2MONDO:0006502EFO:1000637
aortic valve insufficiency2MONDO:0005648EFO:0007148
type 1 diabetes mellitus2MONDO:0005147MONDO:0005147
breast neoplasm2MONDO:0021100MONDO:0007254
cystic fibrosis2MONDO:0009061MONDO:0009061
sickle cell disease2MONDO:0011382MONDO:0011382
schwannoma2MONDO:0002546EFO:0000693
acoustic neuroma2MONDO:0001569HP:0009588
peripheral neuropathy2MONDO:0005244EFO:0003100
injury1MONDO:0021178EFO:0000546
osteosarcoma1MONDO:0009807EFO:0000637
metastatic melanoma1MONDO:0005191EFO:0002617
osteoarthritis, knee1MONDO:0005416EFO:0004616
type 2 diabetes mellitus1MONDO:0005148MONDO:0005148
keloid1MONDO:0005348EFO:0004212
head and neck squamous cell carcinoma1MONDO:0010150EFO:0000181
peripheral arterial disease0MONDO:0005386EFO:0004265

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

Clinical trials

Total trials: 304.

Phase distribution

PhaseTrials
PHASE472
PHASE361
Not specified57
PHASE248
PHASE138
EARLY_PHASE116
PHASE1/PHASE27
PHASE2/PHASE35

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03264352PHASE4RECRUITINGIntervention for High-normal Blood Pressure in Adults With Type 2 Diabetes
NCT04111419PHASE4ACTIVE_NOT_RECRUITINGIntensive Management of Blood Pressure and Cholesterol in Elderly Chinese With Hypertension and Atrial Fibrillation
NCT04715568PHASE4RECRUITINGSecondhand Tobacco Smoke and Cardiovascular Disease
NCT06431477PHASE4RECRUITINGEfficacy and Safety of Telmisartan Compared With Losartan
NCT07099859PHASE4RECRUITINGEffect of Losartan on the Neurohumoral Axis and Ventricular Remodeling of Patients With Severe Aortic Regurgitation Undergoing Valve Surgery.
NCT07135687PHASE4NOT_YET_RECRUITINGStudy to Use Oral Losartan to Decrease the Risk of Postoperative Scarring Following (ACL) Reconstruction
NCT07160361PHASE4NOT_YET_RECRUITINGExploration of Postoperative Adjuvant Therapy for HCC Patients With Positive TB
NCT07241338PHASE4NOT_YET_RECRUITINGSacubitril/Allisartan for Hypertensive Patients With Overweight or Obesity
NCT00067990PHASE4COMPLETEDAngiotensin II Blockade for Chronic Allograft Nephropathy
NCT00140907PHASE4COMPLETEDALLOGRAFT, A Study to Evaluate the Renal Protective Effects of Losartan (0954-222)(COMPLETED)
NCT00168857PHASE4COMPLETEDA Prospective, Randomised, Double-blind, Double-dummy, Forced-titration, Multicentre, Parallel Group, One Year Treatment Trial to Compare Telmisartan (MICARDIS) 80 mg Versus Losartan (COZAAR) 100 mg, in Hypertensive Type 2 Diabetic Patients With Overt Nephropathy (AMADEO Study)
NCT00185094PHASE4COMPLETEDA Comparison of the Effect of Olmesartan Medoxomil, Losartan Potassium, and Atenolol on the Ability of Overweight Patients With High Blood Pressure to Respond to Insulin
NCT00198562PHASE4UNKNOWNHypertension Control Based on Home Blood Pressure
NCT00239096PHASE4UNKNOWNPrevention of Decompensation in Liver Cirrhosis
NCT00274638PHASE4COMPLETEDPROBE Parallel 6-week Treatment Comparing Telmisartan/Hydrochlorothiazide (HCT) (40/12.5 or 80/12.5) With Losartan/HCT (50/12.5) Using Ambulatory Blood Pressure Monitoring (ABPM)
NCT00298714PHASE4COMPLETEDEffects of Losartan on Hepatic Fibrogenesis in Chronic Hepatitis C
NCT00369538PHASE4SUSPENDEDSpecific Blockage of Angiotensine 2 and Podocyturia in Glomerular Nephropathies With Hypertension and Proteinuria
NCT00407862PHASE4COMPLETEDTelmisartan and Losartan in Hypertensive IGT
NCT00419835PHASE4COMPLETEDEffect of Enalapril and Losartan Association Therapy on Proteinuria and Inflammatory Biomarkers in Diabetic Nephropathy: a Clinical Trial on Type 2 Diabetes Mellitus
NCT00456963PHASE4TERMINATEDPrevention of Diabetes and Hypertension
NCT00492128PHASE4COMPLETEDKanagawa Combination Anti-hypertensive Therapy (K-CAT)
NCT00496834PHASE4COMPLETEDLAAS (Losartan Anti-Atherosclerosis Study)(0954-330)(COMPLETED)
NCT00663377PHASE4COMPLETEDEffects of Losartan on Insulin Resistance in Patients With Heart Failure
NCT00669435PHASE4UNKNOWNLosartan and Simvastatin in Hypertensive Obeses With Liver Steatosis
NCT00675987PHASE4COMPLETEDA Randomized Clinical Trial To Study Losartan On Endothelial Dysfunction and Insulin Resistance In Obese Patients
NCT00701428PHASE4COMPLETEDLosartan in Hypertensive Men and Women With Sleep Apnea Before and on Continuous Positive Airway Pressure (CPAP) Treatment
NCT00716950PHASE4UNKNOWNValsartan and Amlodipine Compared to Losartan and Amlodipine in Hypertensive Patients
NCT00720226PHASE4COMPLETEDEfficacy of Losartan in Preventing Progression of COPD
NCT00754429PHASE4COMPLETEDThe Effect of Losartan Versus Amlodipine-based Therapy in Ischemic Stroke (0954-338)(COMPLETED)
NCT00805311PHASE4TERMINATEDAggressive Medical Treatment Evaluation for Asymptomatic Carotid Artery Stenosis
NCT00813722PHASE4UNKNOWNEffect of Active Telephone Calls in the Compliance of Hypertensive Patients With Treatment
NCT00931710PHASE4COMPLETEDValsartan/Amlodipine As Compared to Losartan Treatment in Stage 2 Systolic Hypertension
NCT00949884PHASE4COMPLETEDOlmesartan Comparison to Losartan in Hypertensive Subjects
NCT00994617PHASE4UNKNOWNMonotherapy Versus Dual Therapy for Initial Treatment for Hypertension
NCT01150201PHASE4COMPLETEDAliskiren Combined With Losartan in Proteinuric, Non-diabetic Chronic Kidney Disease
NCT01176032PHASE4COMPLETEDALiskiren or Losartan Effects on bioMARKers of Myocardial Remodeling
NCT01180413PHASE4COMPLETEDIntensive Vasodilator Therapy in Patients With Essential Hypertension
NCT01271374PHASE4UNKNOWNChanges in Endothelial Function and Biomarkers in African Americans (AA) With Metabolic Syndrome
NCT01603940PHASE4COMPLETEDComparison Between Losartan and Benazepril in Diabetic Hypertensive Patients Not Controlled by Amlodipine
NCT01766050PHASE4COMPLETEDStudy to Evaluate Effect of Belatacept on Pharmacokinetics of Inje Cocktail in Healthy Volunteers

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.

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

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)AGTR1
OLMESARTAN MEDOXOMILChEMBL + PubChemPhase 4 (approved)AGTR1
RIFAMPINChEMBL + PubChemPhase 4 (approved)AGTR1
SPARSENTANChEMBL + PubChemPhase 4 (approved)AGTR1
TEGASERODChEMBL + PubChemPhase 4 (approved)AGTR1
ALFACALCIDOLChEMBLPhase 4 (approved)AGTR1
AMITRIPTYLINEChEMBLPhase 4 (approved)AGTR1
ANGIOTENSIN IIChEMBLPhase 4 (approved)AGTR1
ARIPIPRAZOLEChEMBLPhase 4 (approved)AGTR1
BALSALAZIDEChEMBLPhase 4 (approved)AGTR1
BENZBROMARONEChEMBLPhase 4 (approved)AGTR1
BUTOCONAZOLEChEMBLPhase 4 (approved)AGTR1
CALCITRIOLChEMBLPhase 4 (approved)AGTR1
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)AGTR1
CARVEDILOLChEMBLPhase 4 (approved)AGTR1
CLOTRIMAZOLEChEMBLPhase 4 (approved)AGTR1
DABIGATRAN ETEXILATEChEMBLPhase 4 (approved)AGTR1
DESOGESTRELChEMBLPhase 4 (approved)AGTR1
DISULFIRAMChEMBLPhase 4 (approved)AGTR1
DOFETILIDEChEMBLPhase 4 (approved)AGTR1
DONEPEZILChEMBLPhase 4 (approved)AGTR1
EFAVIRENZChEMBLPhase 4 (approved)AGTR1
EPALRESTATChEMBLPhase 4 (approved)AGTR1
EPROSARTANChEMBLPhase 4 (approved)AGTR1
FELODIPINEChEMBLPhase 4 (approved)AGTR1
FENTICONAZOLEChEMBLPhase 4 (approved)AGTR1
GUAIFENESINChEMBLPhase 4 (approved)AGTR1
HALOPERIDOLChEMBLPhase 4 (approved)AGTR1
IBANDRONIC ACIDChEMBLPhase 4 (approved)AGTR1
INDOCYANINE GREEN ACID FORMChEMBLPhase 4 (approved)AGTR1
IRBESARTANChEMBLPhase 4 (approved)AGTR1
IVACAFTORChEMBLPhase 4 (approved)AGTR1
LEFLUNOMIDEChEMBLPhase 4 (approved)AGTR1
LOVASTATINChEMBLPhase 4 (approved)AGTR1
MILTEFOSINEChEMBLPhase 4 (approved)AGTR1
NIFEDIPINEChEMBLPhase 4 (approved)AGTR1
NIMESULIDEChEMBLPhase 4 (approved)AGTR1
NITAZOXANIDEChEMBLPhase 4 (approved)AGTR1
NORGESTIMATEChEMBLPhase 4 (approved)AGTR1
NOSCAPINEChEMBLPhase 4 (approved)AGTR1
OXYMETHOLONEChEMBLPhase 4 (approved)AGTR1
PIMOZIDEChEMBLPhase 4 (approved)AGTR1
PONATINIBChEMBLPhase 4 (approved)AGTR1
PRAZOSINChEMBLPhase 4 (approved)AGTR1
PROPRANOLOLChEMBLPhase 4 (approved)AGTR1
PYRVINIUMChEMBLPhase 4 (approved)AGTR1
RIMONABANTChEMBLPhase 4 (approved)AGTR1
RITONAVIRChEMBLPhase 4 (approved)AGTR1
ROCURONIUMChEMBLPhase 4 (approved)AGTR1
ROSIGLITAZONEChEMBLPhase 4 (approved)AGTR1
SARALASINChEMBLPhase 4 (approved)AGTR1
SELEXIPAGChEMBLPhase 4 (approved)AGTR1
SIMVASTATINChEMBLPhase 4 (approved)AGTR1
SORAFENIBChEMBLPhase 4 (approved)AGTR1
SULCONAZOLEChEMBLPhase 4 (approved)AGTR1
SUNITINIBChEMBLPhase 4 (approved)AGTR1
TELMISARTANChEMBLPhase 4 (approved)AGTR1
TELOTRISTATChEMBLPhase 4 (approved)AGTR1
TELOTRISTAT ETHYLChEMBLPhase 4 (approved)AGTR1
TIPRANAVIRChEMBLPhase 4 (approved)AGTR1

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