◎ Sugi Atlas

Atlas / Drug / Olmesartan

Olmesartan

drug
On this page

Also known as NSC-759810Olmesartan medoxomil impurityolmesartan-RNH-6270SID26719844SID174007156

Summary

Olmesartan (CHEMBL1516) is an approved small-molecule antihypertensive agent targeting AGTR1; indicated across 7 conditions including hypertensive disorder and atrial fibrillation.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • Targets: 1 (AGTR1)
  • Indications: 7 conditions
  • Clinical trials: 40
  • Chemistry: 446.5 Da · C24H26N6O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1516
NameOlmesartan
TypeSmall molecule
Max phase3
FDA approvedyes
PubChem CID158781
ChEBICHEBI:48416
Molecular formulaC24H26N6O3
Molecular weight446.5
InChIKeyVTRAEEWXHOVJFV-UHFFFAOYSA-N

SMILES: CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)O)C(C)(C)O

IUPAC name: 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid

Pharmacological roles (ChEBI): antihypertensive agent, angiotensin receptor antagonist.

Also known as: NSC-759810, Olmesartan, Olmesartan medoxomil impurity, olmesartan-, RNH-6270, SID26719844, olmesartan, OLMESARTAN, SID174007156

Patent coverage: 151 distinct patent families (359 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 receptorAntagonist8.10.4%P30556

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Beta-lactamase, Type-1 angiotensin II receptor, Type-1 angiotensin II receptor, Type-2 angiotensin II receptor.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 7 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
AGTR19.4AC500.4nMCHEMBL_ACT_25177075
AGTR19.1AC500.8nMCHEMBL_ACT_25177694
P251048.11IC507.7nMCHEMBL_ACT_5202090
P251048.09IC508.1nMCHEMBL_ACT_5202063
P251048.09IC508.1nMCHEMBL_ACT_565566

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

5 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
hypertensive disorder3MONDO:0005044EFO:0000537
atrial fibrillation3MONDO:0004981EFO:0000275
essential hypertension3MONDO:0001134MONDO:0001134
severe acute respiratory syndrome3MONDO:0005091EFO:0000694
stroke disorder2MONDO:0005098EFO:0000712

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

Clinical trials

Total trials: 40.

Phase distribution

PhaseTrials
PHASE314
PHASE49
PHASE27
Not specified7
PHASE13

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05917275PHASE4RECRUITINGMulti-Omics to Predict the Blood Pressure Response to Antihypertensives
NCT01089452PHASE4WITHDRAWNAngiotensin Receptor Blocker Combined With Calcium Antagonist Evaluation of Safety and Lowering of Systolic Blood Pressure Study
NCT01101009PHASE4COMPLETEDComparison of Sevikar® and the Combination of Perindopril/Amlodipine on Central Blood Pressure
NCT01271374PHASE4UNKNOWNChanges in Endothelial Function and Biomarkers in African Americans (AA) With Metabolic Syndrome
NCT01611077PHASE4COMPLETEDEfficacy and Safety of a Therapy Change From Candesartan 32 mg to Fixed Combination of Olmesartan 40 mg/Amlodipine 10 mg
NCT02373462PHASE4TERMINATEDEffect of olmesaRtan on Walking distancE and quaLIty of lifE in Peripheral Artery Disease Patients With Hypertension Treated For Intermittent Claudication (RELIEF)
NCT02996916PHASE4UNKNOWNEfficacy of Olmesartan on Cerebral Glucose Metabolism, Vascular Inflammation and Adipose Tissue
NCT04120753PHASE4COMPLETEDClinical Trial to Evaluate the Efficacy and Safety of OLOMAX Tab
NCT05189015PHASE4COMPLETEDEffect of Olmesartan on Angiotensin(1-7) Levels and Vascular Functions in Diabetes and Hypertension
NCT00098137PHASE3COMPLETEDTrial to Investigate the Efficacy of Olmesartan in Paroxysmal Atrial Fibrillation
NCT00696241PHASE3COMPLETEDEfficacy and Safety of Azilsartan Medoxomil in Participants With Essential Hypertension
NCT00696436PHASE3COMPLETEDAn Efficacy and Safety Study of Azilsartan Medoxomil Compared to Valsartan and Olmesartan in Participants With Essential Hypertension.
NCT00846365PHASE3COMPLETEDEfficacy and Safety of Azilsartan Medoxomil Plus Chlorthalidone in Participants With Moderate to Severe Hypertension
NCT00902538PHASE3COMPLETEDHydrochlorothiazide as add-on to Olmesartan/Amlodipine in Hypertension
NCT01599104PHASE3COMPLETEDEfficacy and Safety of LCZ696 in Comparison to Olmesartan in Japanese Patients With Essential Hypertension
NCT01613209PHASE3COMPLETEDSevicontrol-1: Efficacy and Safety of a Fixed Combination of Olmesartan/ Amlodipine
NCT01615198PHASE3COMPLETEDEfficacy and Safety of LCZ696 in Comparison to Olmesartan in Elderly Patients With Essential Hypertension
NCT01764295PHASE3COMPLETEDClinical Study for Patients With Hypertension Associated With Dyslipidemia
NCT01785472PHASE3COMPLETEDEfficacy and Safety of LCZ696 in Comparison to Olmesartan in Asian Patients With Essential Hypertension
NCT01876368PHASE3COMPLETEDEfficacy and Safety of LCZ696 Compared to Olmesartan in Essential Hypertensive Patients Not Responsive to Olmesartan
NCT03009487PHASE3COMPLETEDA Clinical Trial to Evaluate the Efficacy and Safety of Olmesartan/Amlodipine/Rosuvastatin Combination Treatment in Patients With Concomitant Hypertension and Hyperlipidemia
NCT04161001PHASE3UNKNOWNClinical Trail to Evaluate the Efficacy and Safety of DWJ1451
NCT04606563PHASE3TERMINATEDHost Response Mediators in Coronavirus (COVID-19) Infection - Is There a Protective Effect of Losartan and Other ARBs on Outcomes of Coronavirus Infection?
NCT00362115PHASE2COMPLETEDSafety and Efficacy of Azilsartan Medoxomil in Participants With Mild to Moderate Hypertension
NCT00759551PHASE2COMPLETEDEfficacy and Safety of Azilsartan in Subjects With Essential Hypertension
NCT01692301PHASE2COMPLETEDStudy of the Safety and Efficacy of LCZ696 on Arterial Stiffness in Elderly Patients With Hypertension
NCT01870739PHASE2COMPLETEDA Study to Evaluate the Effect of LCZ696 on Aortic Stiffness in Subjects With Hypertension
NCT02516826PHASE2UNKNOWNThe Effect of Rosuvastatin and Olmesartan on the Progression of Coronary Atherosclerotic Disease
NCT03655964PHASE2COMPLETEDEffect of Olmesartan and Nebivolol on Ambulatory Blood Pressure and Arterial Stiffness in Acute Stage of Ischemic Stroke
NCT05103332PHASE2COMPLETEDZilebesiran as Add-on Therapy in Patients With Hypertension Not Adequately Controlled by a Standard of Care Antihypertensive Medication (KARDIA-2)
NCT01831479PHASE1COMPLETEDInvestigation of Pharmacokinetic Interaction Between Rosuvastatin and Olmesartan in Healthy Male Volunteers
NCT03753477PHASE1COMPLETEDClinical Trial to Investigate the Efficacy and Safety of DWJ1351
NCT04856969PHASE1COMPLETEDClinical Trial to Evaluate Pharmacokinetic Interaction of ATB-1011 and ATB-1012 in Healthy Adult Volunteers
NCT00122447Not specifiedCOMPLETEDCardiovascular Disease (CVD) Risk and Prevention in Early Glucose Intolerance
NCT00834600Not specifiedCOMPLETEDRenin Profiling in Selection of Initial Antihypertensive Drug
NCT00854763Not specifiedUNKNOWNOlmesartan on Ambulatory Blood Pressure Change
NCT01028534Not specifiedCOMPLETEDEffects of Antihypertensive Drugs in Patients With Hypertension and Obstructive Sleep Apnea (OSA)
NCT01053026Not specifiedCOMPLETEDEvaluation of Effects of Exercise Training and ARB in DM Patients
NCT02449811Not specifiedCOMPLETEDRAS Peptide Profiles in Patients With Arterial Hypertension
NCT03560804Not specifiedCOMPLETEDUse of Impedance Cardiography and Applanation Tonometry for Prediction of the Antihypertensive Effect of Two Drugs

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 100 by shared-target count:

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)AGTR1
LOSARTANChEMBL + 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
TRICLOSANChEMBLPhase 4 (approved)AGTR1
TROGLITAZONEChEMBLPhase 4 (approved)AGTR1
VALSARTANChEMBLPhase 4 (approved)AGTR1
ZAFIRLUKASTChEMBLPhase 4 (approved)AGTR1
AZELNIDIPINEChEMBLPhase 3AGTR1
CAFFEIC ACIDChEMBLPhase 3AGTR1
CANDESARTANChEMBLPhase 3AGTR1
FIMASARTANChEMBLPhase 3AGTR1
NILVADIPINEChEMBLPhase 3AGTR1
OTILONIUM BROMIDEChEMBLPhase 3AGTR1
TEPRENONEChEMBLPhase 3AGTR1
TIRATRICOLChEMBLPhase 3AGTR1
BENZETHONIUMChEMBLPhase 2AGTR1
DOMIPHENChEMBLPhase 2AGTR1
FORASARTANChEMBLPhase 2AGTR1
LASELIPAGChEMBLPhase 2AGTR1
LIDOFLAZINEChEMBLPhase 2AGTR1
OLODANRIGANChEMBLPhase 2AGTR1
OXATOMIDEChEMBLPhase 2AGTR1
PRATOSARTANChEMBLPhase 2AGTR1
RIPISARTANChEMBLPhase 2AGTR1
SOFALCONEChEMBLPhase 2AGTR1
TASOSARTANChEMBLPhase 2AGTR1
TRV-120027ChEMBLPhase 2AGTR1
ZOLASARTANChEMBLPhase 2AGTR1
AbirateronePubChemApprovedAGTR1
acetylcysteinePubChemApprovedAGTR1
Aclidinium BromidePubChemApprovedAGTR1
AcyclovirPubChemApprovedAGTR1
AfatinibPubChemApprovedAGTR1
AllopurinolPubChemApprovedAGTR1
AlmotriptanPubChemApprovedAGTR1
AlogliptinPubChemApprovedAGTR1
aminolevulinic acidPubChemApprovedAGTR1
AnagrelidePubChemApprovedAGTR1
ApixabanPubChemApprovedAGTR1
ApremilastPubChemApprovedAGTR1
AprepitantPubChemApprovedAGTR1
AtazanavirPubChemApprovedAGTR1

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
v1.1.4
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