Olmesartan Medoxomil
drugOn this page
Also known as BenicarCS-866NSC-758924Olmesartan medoxomil component of azorOlmesartan medoxomiloOlmetecSID26748978SID144204998olmesartan medoxomil esterOlmesartanC0164744
Summary
Olmesartan Medoxomil (CHEMBL1200692) is an approved small molecule (ATC C09CA08) targeting AGTR1; indicated across 12 conditions including hypertensive disorder and heart failure.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: C09CA08
- Targets: 1 (AGTR1)
- Indications: 12 conditions
- Clinical trials: 106
- Chemistry: 558.6 Da · C29H30N6O6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1200692 |
| Name | Olmesartan Medoxomil |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 130881 |
| ATC | C09CA08 |
| Molecular formula | C29H30N6O6 |
| Molecular weight | 558.6 |
| InChIKey | UQGKUQLKSCSZGY-UHFFFAOYSA-N |
SMILES: CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)OCC5=C(OC(=O)O5)C)C(C)(C)O
IUPAC name: (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
Also known as: Benicar, CS-866, NSC-758924, Olmesartan medoxomil, Olmesartan medoxomil component of azor, Olmesartan medoxomilo, Olmetec, SID26748978, OLMESARTAN MEDOXOMIL, olmesartan medoxomil, SID144204998, olmesartan medoxomil ester
Patent coverage: 4,727 distinct patent families (17,268 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 17,105 (99%) 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).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| AGTR1 | AT1 receptor | Antagonist | 8.1 | 0.4% | P30556 |
Broader ChEMBL bioactivity targets: 12 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, ATP-binding cassette sub-family C member 4, Type-1 angiotensin II receptor, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, 3’,5’-cyclic-AMP phosphodiesterase 4D, Cytochrome P450 3A4, Cruzipain, Type-2 angiotensin II receptor.
Bioactivity
ChEMBL activities: 11 potent at pChembl ≥ 5 of 16 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| AGTR1 | 9.05 | AC50 | 0.9 | nM | CHEMBL_ACT_25177110 |
| AGTR1 | 8.77 | AC50 | 1.7 | nM | CHEMBL_ACT_25177695 |
| TDP1 | 7.65 | Potency | 22.4 | nM | CHEMBL_ACT_3942045 |
| SLCO1B1 | 6.27 | Ki | 540 | nM | CHEMBL_ACT_13800687 |
| SLCO1B3 | 6.12 | Ki | 750 | nM | CHEMBL_ACT_13798688 |
| SLCO1B3 | 6.01 | IC50 | 977.2 | nM | CHEMBL_ACT_13798624 |
| SLCO1B1 | 6.01 | IC50 | 977.2 | nM | CHEMBL_ACT_13800623 |
| ABCC3 | 5.7 | IC50 | 2000 | nM | CHEMBL_ACT_18130215 |
| PDE4D | 5.41 | AC50 | 3900 | nM | CHEMBL_ACT_25185453 |
| ABCB11 | 5.33 | IC50 | 4730 | nM | CHEMBL_ACT_18129045 |
| P25779 | 5.1 | Potency | 7943 | nM | CHEMBL_ACT_3980593 |
Target pathways
Aggregated over 1 target gene(s): AGTR1.
Top Reactome pathways
11 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | AGTR1 |
| Membrane Trafficking | 1 | AGTR1 |
| Signaling by GPCR | 1 | AGTR1 |
| Class A/1 (Rhodopsin-like receptors) | 1 | AGTR1 |
| Peptide ligand-binding receptors | 1 | AGTR1 |
| GPCR downstream signalling | 1 | AGTR1 |
| G alpha (q) signalling events | 1 | AGTR1 |
| GPCR ligand binding | 1 | AGTR1 |
| Vesicle-mediated transport | 1 | AGTR1 |
| Cargo recognition for clathrin-mediated endocytosis | 1 | AGTR1 |
| Clathrin-mediated endocytosis | 1 | AGTR1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| regulation of cell growth | 1 |
| kidney development | 1 |
| renin-angiotensin regulation of aldosterone production | 1 |
| maintenance of blood vessel diameter homeostasis by renin-angiotensin | 1 |
| regulation of systemic arterial blood pressure by renin-angiotensin | 1 |
| inflammatory response | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 1 |
| positive regulation of cytosolic calcium ion concentration | 1 |
| Rho protein signal transduction | 1 |
| positive regulation of macrophage derived foam cell differentiation | 1 |
| regulation of vasoconstriction | 1 |
| calcium-mediated signaling | 1 |
| low-density lipoprotein particle remodeling | 1 |
| regulation of renal sodium excretion | 1 |
Indications & clinical
Indications
12 indications (6 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).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| hypertensive disorder | 4 | MONDO:0005044 | EFO:0000537 |
| heart failure | 4 | MONDO:0005252 | EFO:0003144 |
| cardiovascular disorder | 4 | MONDO:0004995 | EFO:0000319 |
| diabetes mellitus | 4 | MONDO:0005015 | EFO:0000400 |
| myocardial infarction | 4 | MONDO:0005068 | EFO:0000612 |
| stroke disorder | 4 | MONDO:0005098 | EFO:0000712 |
| diabetic kidney disease | 3 | MONDO:0005016 | EFO:0000401 |
| atherosclerosis | 3 | MONDO:0005311 | EFO:0003914 |
| proteinuria | 3 | MONDO:0003634 | HP:0000093 |
| kidney disorder | 3 | MONDO:0005240 | EFO:0003086 |
| essential hypertension | 3 | MONDO:0001134 | MONDO:0001134 |
| glomerulonephritis | 2 | MONDO:0002462 | MONDO:0002462 |
Clinical trials
Total trials: 106.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 41 |
| PHASE4 | 33 |
| Not specified | 13 |
| PHASE2 | 9 |
| PHASE1 | 9 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05917275 | PHASE4 | RECRUITING | Multi-Omics to Predict the Blood Pressure Response to Antihypertensives |
| NCT07547878 | PHASE4 | NOT_YET_RECRUITING | Rapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD) |
| NCT00134160 | PHASE4 | COMPLETED | OlmeSartan and Calcium Antagonists Randomized (OSCAR) Study |
| NCT00185055 | PHASE4 | COMPLETED | The Relative Effects of Olmesartan Medoxomil, Irbesartan and Valsartan on the Activity of the Blood Pressure Control System in Healthy Subjects |
| NCT00185068 | PHASE4 | COMPLETED | An Examination of the Safety and Blood Pressure Lowering Effect of Increasing Doses of Benicar® and Benicar® HCT in Patients With Hypertension |
| NCT00185094 | PHASE4 | COMPLETED | A 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 |
| NCT00185120 | PHASE4 | COMPLETED | Treatment of High Blood Pressure Using Olmesartan With Hydrochlorothiazide Compared to an ACE Inhibitor With a Calcium Channel Blocker |
| NCT00311155 | PHASE4 | COMPLETED | Olmesartan and an add-on Treatment in Patients With Mild to Moderate Hypertension |
| NCT00403481 | PHASE4 | COMPLETED | An Examination of the Blood Pressure Lowering Ability and Safety of Olmesartan Medoxomil in Patients With Type II Diabetes |
| NCT00412932 | PHASE4 | COMPLETED | An Examination of the Blood Pressure Lowering Ability and Safety of Olmesartan Medoxomil in Elderly Patients With Hypertension |
| NCT00430638 | PHASE4 | COMPLETED | A Study of the Blood Pressure Lowering Ability and Safety of Olmesartan Medoxomil in Stage I and Stage II Hypertension |
| NCT00454662 | PHASE4 | COMPLETED | Combination of OLMesartan and CCB or Low Dose Diuretics in High Risk Elderly Hypertensive Patients Study (COLM-Study) |
| NCT00607035 | PHASE4 | COMPLETED | The Japan-Combined Treatment With Olmesartan and a Calcium Channel Blocker Versus Olmesartan and Diuretics Randomized Efficacy Study (J-CORE) |
| NCT00772499 | PHASE4 | COMPLETED | Vascular Improvement With Olmesartan Medoxomil Study |
| NCT00791258 | PHASE4 | COMPLETED | A Dose Escalation Study of a Combination Antihypertensive Drug in the Treatment of Various Groups of Patients Who do Not Respond to Single Drug Treatment of Their High Blood Pressure |
| NCT00858702 | PHASE4 | COMPLETED | Calcium Channel Blockers (CCBs) or Diuretics as an Add-on to Olmesartan Medoxomil in Hypertension |
| NCT00890591 | PHASE4 | COMPLETED | Efficacy and Safety of Olmesartan Medoxomil in Stage 1 and 2 Essential Hypertension |
| NCT00949884 | PHASE4 | COMPLETED | Olmesartan Comparison to Losartan in Hypertensive Subjects |
| NCT01089452 | PHASE4 | WITHDRAWN | Angiotensin Receptor Blocker Combined With Calcium Antagonist Evaluation of Safety and Lowering of Systolic Blood Pressure Study |
| NCT01101009 | PHASE4 | COMPLETED | Comparison of Sevikar® and the Combination of Perindopril/Amlodipine on Central Blood Pressure |
| NCT01132768 | PHASE4 | TERMINATED | The Confirmatory Olmesartan Plaque Regression Study |
| NCT01180205 | PHASE4 | UNKNOWN | Telmisartan, Amlodipine and Flow Mediated Dilation |
| NCT01271374 | PHASE4 | UNKNOWN | Changes in Endothelial Function and Biomarkers in African Americans (AA) With Metabolic Syndrome |
| NCT01611077 | PHASE4 | COMPLETED | Efficacy and Safety of a Therapy Change From Candesartan 32 mg to Fixed Combination of Olmesartan 40 mg/Amlodipine 10 mg |
| NCT01684748 | PHASE4 | COMPLETED | Angiotensin II Blockade and Inflammation in Obesity |
| NCT01907373 | PHASE4 | COMPLETED | Drug Interaction Study of Olmesartan in Healthy Chinese Volunteers |
| NCT02360956 | PHASE4 | UNKNOWN | Efficacy Study of Olmesartan Medoxomil on Coronary Atherosclerosis and Epicardial Adipose Tissue(EAT) |
| NCT02373462 | PHASE4 | TERMINATED | Effect of olmesaRtan on Walking distancE and quaLIty of lifE in Peripheral Artery Disease Patients With Hypertension Treated For Intermittent Claudication (RELIEF) |
| NCT02377661 | PHASE4 | COMPLETED | Lowering Blood Pressure in Primary Care in Vienna |
| NCT02495324 | PHASE4 | COMPLETED | Fimasartan Achieving SBP Target (FAST) Study |
| NCT02996916 | PHASE4 | UNKNOWN | Efficacy of Olmesartan on Cerebral Glucose Metabolism, Vascular Inflammation and Adipose Tissue |
| NCT04120753 | PHASE4 | COMPLETED | Clinical Trial to Evaluate the Efficacy and Safety of OLOMAX Tab |
| NCT05189015 | PHASE4 | COMPLETED | Effect of Olmesartan on Angiotensin(1-7) Levels and Vascular Functions in Diabetes and Hypertension |
| NCT00098137 | PHASE3 | COMPLETED | Trial to Investigate the Efficacy of Olmesartan in Paroxysmal Atrial Fibrillation |
| NCT00141453 | PHASE3 | COMPLETED | ORIENT: Olmesartan Reducing Incidence of End Stage Renal Disease in Diabetic Nephropathy Trial |
| NCT00151775 | PHASE2/PHASE3 | COMPLETED | Assessment of Efficacy and Safety of Olmesartan Medoxomil in Children and Adolescent Patients With High Blood Pressure |
| NCT00151827 | PHASE3 | COMPLETED | Olmesartan Medoxomil in Hypertension and Renal Impairment |
| NCT00185133 | PHASE3 | COMPLETED | Study of Co-administration of Olmesartan Medoxomil Plus Amlodipine in Patients With Mild to Severe Hypertension |
| NCT00185159 | PHASE3 | COMPLETED | Olmesartan Medoxomil in Diabetes Mellitus |
| NCT00185172 | PHASE3 | COMPLETED | Olmesartan in Essential Hypertension |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
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:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | AGTR1 |
| LOSARTAN | ChEMBL + PubChem | Phase 4 (approved) | AGTR1 |
| RIFAMPIN | ChEMBL + PubChem | Phase 4 (approved) | AGTR1 |
| SPARSENTAN | ChEMBL + PubChem | Phase 4 (approved) | AGTR1 |
| TEGASEROD | ChEMBL + PubChem | Phase 4 (approved) | AGTR1 |
| ALFACALCIDOL | ChEMBL | Phase 4 (approved) | AGTR1 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | AGTR1 |
| ANGIOTENSIN II | ChEMBL | Phase 4 (approved) | AGTR1 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | AGTR1 |
| BALSALAZIDE | ChEMBL | Phase 4 (approved) | AGTR1 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | AGTR1 |
| BUTOCONAZOLE | ChEMBL | Phase 4 (approved) | AGTR1 |
| CALCITRIOL | ChEMBL | Phase 4 (approved) | AGTR1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | AGTR1 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | AGTR1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | AGTR1 |
| DABIGATRAN ETEXILATE | ChEMBL | Phase 4 (approved) | AGTR1 |
| DESOGESTREL | ChEMBL | Phase 4 (approved) | AGTR1 |
| DISULFIRAM | ChEMBL | Phase 4 (approved) | AGTR1 |
| DOFETILIDE | ChEMBL | Phase 4 (approved) | AGTR1 |
| DONEPEZIL | ChEMBL | Phase 4 (approved) | AGTR1 |
| EFAVIRENZ | ChEMBL | Phase 4 (approved) | AGTR1 |
| EPALRESTAT | ChEMBL | Phase 4 (approved) | AGTR1 |
| EPROSARTAN | ChEMBL | Phase 4 (approved) | AGTR1 |
| FELODIPINE | ChEMBL | Phase 4 (approved) | AGTR1 |
| FENTICONAZOLE | ChEMBL | Phase 4 (approved) | AGTR1 |
| GUAIFENESIN | ChEMBL | Phase 4 (approved) | AGTR1 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | AGTR1 |
| IBANDRONIC ACID | ChEMBL | Phase 4 (approved) | AGTR1 |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | AGTR1 |
| IRBESARTAN | ChEMBL | Phase 4 (approved) | AGTR1 |
| IVACAFTOR | ChEMBL | Phase 4 (approved) | AGTR1 |
| LEFLUNOMIDE | ChEMBL | Phase 4 (approved) | AGTR1 |
| LOVASTATIN | ChEMBL | Phase 4 (approved) | AGTR1 |
| MILTEFOSINE | ChEMBL | Phase 4 (approved) | AGTR1 |
| NIFEDIPINE | ChEMBL | Phase 4 (approved) | AGTR1 |
| NIMESULIDE | ChEMBL | Phase 4 (approved) | AGTR1 |
| NITAZOXANIDE | ChEMBL | Phase 4 (approved) | AGTR1 |
| NORGESTIMATE | ChEMBL | Phase 4 (approved) | AGTR1 |
| NOSCAPINE | ChEMBL | Phase 4 (approved) | AGTR1 |
| OXYMETHOLONE | ChEMBL | Phase 4 (approved) | AGTR1 |
| PIMOZIDE | ChEMBL | Phase 4 (approved) | AGTR1 |
| PONATINIB | ChEMBL | Phase 4 (approved) | AGTR1 |
| PRAZOSIN | ChEMBL | Phase 4 (approved) | AGTR1 |
| PROPRANOLOL | ChEMBL | Phase 4 (approved) | AGTR1 |
| PYRVINIUM | ChEMBL | Phase 4 (approved) | AGTR1 |
| RIMONABANT | ChEMBL | Phase 4 (approved) | AGTR1 |
| RITONAVIR | ChEMBL | Phase 4 (approved) | AGTR1 |
| ROCURONIUM | ChEMBL | Phase 4 (approved) | AGTR1 |
| ROSIGLITAZONE | ChEMBL | Phase 4 (approved) | AGTR1 |
| SARALASIN | ChEMBL | Phase 4 (approved) | AGTR1 |
| SELEXIPAG | ChEMBL | Phase 4 (approved) | AGTR1 |
| SIMVASTATIN | ChEMBL | Phase 4 (approved) | AGTR1 |
| SORAFENIB | ChEMBL | Phase 4 (approved) | AGTR1 |
| SULCONAZOLE | ChEMBL | Phase 4 (approved) | AGTR1 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | AGTR1 |
| TELMISARTAN | ChEMBL | Phase 4 (approved) | AGTR1 |
| TELOTRISTAT | ChEMBL | Phase 4 (approved) | AGTR1 |
| TELOTRISTAT ETHYL | ChEMBL | Phase 4 (approved) | AGTR1 |
| TIPRANAVIR | ChEMBL | Phase 4 (approved) | AGTR1 |
Related Atlas pages
- Genes: AGTR1
- Diseases: hypertensive disorder, heart failure, cardiovascular disorder, diabetes mellitus, myocardial infarction, stroke disorder, diabetic kidney disease, atherosclerosis, proteinuria, kidney disorder, essential hypertension
- Drugs: Crizotinib, Losartan, Rifampin, Sparsentan, Tegaserod, Alfacalcidol, Amitriptyline, Angiotensin Ii, Aripiprazole, Balsalazide, Benzbromarone, Butoconazole, Calcitriol, Candesartan Cilexetil, Carvedilol, Clotrimazole, Dabigatran Etexilate, Desogestrel, Disulfiram, Dofetilide, Donepezil, Efavirenz, Epalrestat, Eprosartan, Felodipine, Fenticonazole, Guaifenesin, Haloperidol, Ibandronic Acid, Indocyanine Green Acid Form, Irbesartan, Ivacaftor, Leflunomide, Lovastatin, Miltefosine, Nifedipine, Nimesulide, Nitazoxanide, Norgestimate, Noscapine, Oxymetholone, Pimozide, Ponatinib, Prazosin, Propranolol, Pyrvinium, Rimonabant, Ritonavir, Rocuronium, Rosiglitazone, Saralasin, Selexipag, Simvastatin, Sorafenib, Sulconazole, Sunitinib, Telmisartan, Telotristat, Telotristat Ethyl, Tipranavir