Valsartan
drugOn this page
Also known as CGP 48933CGP-48933DiovanNSC-758927PrexxartanValsartan component of agsav301Valsartan component of byvalsonValsartan component of copaliaValsartan component of copalia-hctValsartan component of dafiroValsartan component of dafiro-hctValsartan component of diovan hctValsartan component of entrestoValsartan component of exforgeValsartan component of exforge hctValsartan component of impridaValsartan component of imprida-hctValsartan component of valturnaSID26719825
Summary
Valsartan (CHEMBL1069) is an approved small-molecule antihypertensive agent (ATC C09CA03) targeting AGTR1; indicated across 31 conditions including congestive heart failure and heart failure.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: C09CA03
- Targets: 1 (AGTR1)
- Indications: 31 conditions
- Clinical trials: 304
- Chemistry: 435.5 Da · C24H29N5O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1069 |
| Name | Valsartan |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 60846 |
| ChEBI | CHEBI:9927 |
| ATC | C09CA03 |
| Molecular formula | C24H29N5O3 |
| Molecular weight | 435.5 |
| InChIKey | ACWBQPMHZXGDFX-QFIPXVFZSA-N |
SMILES: CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)[C@@H](C(C)C)C(=O)O
IUPAC name: (2S)-3-methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid
ChEBI definition: A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2’-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.
Pharmacological roles (ChEBI): antihypertensive agent, angiotensin receptor antagonist.
Also known as: CGP 48933, CGP-48933, Diovan, NSC-758927, Prexxartan, Valsartan, Valsartan component of agsav301, Valsartan component of byvalson, Valsartan component of copalia, Valsartan component of copalia-hct, Valsartan component of dafiro, Valsartan component of dafiro-hct
Patent coverage: 10,475 distinct patent families (38,585 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 37,573 (97%) 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 | 8.61 | 0.4% | P30556 |
Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Angiotensin II receptor (AT-1) type-1, Type-1 angiotensin II receptor, Type-1 angiotensin II receptor B, Leukotriene B4 receptor 2, Type-1 angiotensin II receptor A, Platelet glycoprotein VI, Bile salt export pump.
Bioactivity
ChEMBL activities: 7 potent at pChembl ≥ 5 of 10 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P29089 | 8.72 | IC50 | 1.9 | nM | CHEMBL_ACT_640689 |
| P25095 | 8.57 | IC50 | 2.7 | nM | CHEMBL_ACT_1058431 |
| AGTR1 | 8.57 | IC50 | 2.7 | nM | CHEMBL_ACT_790154 |
| AGTR1 | 8.52 | Ki | 3 | nM | CHEMBL_ACT_18386077 |
| P25095 | 8.47 | IC50 | 3.4 | nM | CHEMBL_ACT_2153786 |
| AGTR1 | 8.13 | IC50 | 7.4 | nM | CHEMBL_ACT_24352567 |
| AGTR1 | 5.33 | Ki | 4700 | nM | CHEMBL_ACT_166061 |
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
31 indications (9 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 |
|---|---|---|---|
| congestive heart failure | 4 | MONDO:0005009 | EFO:0000373 |
| heart failure | 4 | MONDO:0005252 | EFO:0003144 |
| hypertensive disorder | 4 | MONDO:0005044 | EFO:0000537 |
| diabetes mellitus | 4 | MONDO:0005015 | EFO:0000400 |
| myocardial infarction | 4 | MONDO:0005068 | EFO:0000612 |
| cardiovascular disorder | 4 | MONDO:0004995 | EFO:0000319 |
| stroke disorder | 4 | MONDO:0005098 | EFO:0000712 |
| acute myocardial infarction | 4 | MONDO:0004781 | EFO:0008583 |
| atrial fibrillation | 3 | MONDO:0004981 | EFO:0000275 |
| kidney disorder | 3 | MONDO:0005240 | EFO:0003086 |
| atherosclerosis | 3 | MONDO:0005311 | EFO:0003914 |
| metabolic syndrome X | 3 | MONDO:0011565 | EFO:0000195 |
| coronary artery disorder | 3 | MONDO:0005010 | EFO:0001645 |
| ST-elevation myocardial infarction | 3 | MONDO:0041656 | EFO:0008585 |
| Chagas cardiomyopathy | 3 | MONDO:0005491 | EFO:0005529 |
| pulmonary hypertension | 3 | MONDO:0005149 | MONDO:0005149 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| essential hypertension | 3 | MONDO:0001134 | MONDO:0001134 |
| type 2 diabetes mellitus | 3 | MONDO:0005148 | MONDO:0005148 |
| hypertrophic cardiomyopathy | 2 | MONDO:0005045 | EFO:0000538 |
| chronic kidney disease | 2 | MONDO:0005300 | EFO:0003884 |
| acute coronary syndrome | 2 | MONDO:0005542 | EFO:0005672 |
| peripheral arterial disease | 2 | MONDO:0005386 | EFO:0004265 |
| aortic valve insufficiency | 2 | MONDO:0005648 | EFO:0007148 |
| hereditary nephritis | 2 | MONDO:0005334 | MONDO:0018965 |
| diabetic kidney disease | 2 | MONDO:0005016 | EFO:0000401 |
5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 304.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 127 |
| PHASE3 | 78 |
| Not specified | 38 |
| PHASE1 | 27 |
| PHASE2 | 26 |
| PHASE2/PHASE3 | 5 |
| PHASE1/PHASE2 | 2 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03938389 | PHASE4 | ACTIVE_NOT_RECRUITING | The Renin-Angiotensin-Aldosterone System in Adiposity, Blood Pressure and Glucose in African Americans |
| NCT04263922 | PHASE4 | RECRUITING | Huaiqihuang Granule in the Treatment of Primary Glomerulonephritis of Stage CKD3 |
| NCT06218199 | PHASE4 | RECRUITING | Diuretics vs. Afterload Reduction for Treatment of HeartLogic Alerts |
| NCT06501651 | PHASE4 | NOT_YET_RECRUITING | Sacubitril/Valsartan Treats Patients With Essential Hypertension and Type 2 Diabetic Nephropathy |
| NCT06536309 | PHASE4 | NOT_YET_RECRUITING | Neprilysin Inhibition to Reduce Myocardial Fibrosis in Heart Failure With Preserved Ejection Fraction |
| NCT06917664 | PHASE4 | RECRUITING | Treatment of Moderate Ischemic Mitral Regurgitation in Patients With Coronary Artery Disease |
| NCT07547878 | PHASE4 | NOT_YET_RECRUITING | Rapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD) |
| NCT07572032 | PHASE4 | NOT_YET_RECRUITING | Delayed Initiation of ARNI and SGLT2i in Heart Failure With Corrected Aetiology (DELAY-HF), Pilot Study |
| NCT00034840 | PHASE4 | COMPLETED | Telmisartan vs. Valsartan in Patients With Mild to Moderate Hypertension Following a Missed Dose |
| NCT00129233 | PHASE4 | COMPLETED | Comparison of Valsartan With Amlodipine in Hypertensive Patients With Glucose Intolerance |
| NCT00133328 | PHASE4 | UNKNOWN | A Morbidity-Mortality and Remodeling Study With Valsartan |
| NCT00140790 | PHASE4 | TERMINATED | Valsartan in Cardiovascular Disease With Renal Dysfunction (The V-CARD) Study |
| NCT00149227 | PHASE4 | COMPLETED | Add-on Effects of Valsartan on Morbi- Mortality (KYOTO HEART Study) |
| NCT00153023 | PHASE4 | COMPLETED | 1 Year Trial Telmisartan 80 mg Versus Valsartan 160 mg in Hypertensive Type 2 Diabetic Patients With Overt Nephropathy |
| NCT00154271 | PHASE4 | COMPLETED | Effects of Blood Pressure Reduction on High Sensitivity C-Reactive Protein (hsCRP) |
| NCT00162955 | PHASE4 | COMPLETED | Prevention of CHOP-induced Chronic Cardiotoxicity |
| NCT00170924 | PHASE4 | COMPLETED | To Find Out Whether Valsartan With or Without Other Blood Pressure Medications Would Improve the Ability of the Heart to Fill and Empty, and the Ability of the Heart Muscle to Relax Adequately in People With High Blood Pressure. |
| NCT00171054 | PHASE4 | COMPLETED | Efficacy and Safety of Valsartan Versus Amlodipine in Postmenopausal Women With Hypertension |
| NCT00171106 | PHASE4 | COMPLETED | Efficacy and Safety of Valsartan Versus Placebo on Exercise Tolerance in Patients With Heart Failure |
| NCT00171119 | PHASE4 | TERMINATED | A Study in Patients With Diabetes Mellitus Type II of the Effect on Albuminuria of 24 Week Treatment With Valsartan, Benazepril, and Valsartan+Benazepril |
| NCT00171132 | PHASE4 | COMPLETED | VALENCE: Valsartan Versus Atenolol on Exercise Capacity in Hypertensive Overweight Postmenopausal Women |
| NCT00171327 | PHASE4 | COMPLETED | Efficacy and Safety of Fluvastatin or Valsartan and Their Combination in Dyslipidemic Patients With Hypertension and Endothelial Dysfunction |
| NCT00171353 | PHASE4 | COMPLETED | A Study to Describe Vascular and Renal Effects and Safety of Valsartan in Patients With High Blood Pressure |
| NCT00171561 | PHASE4 | COMPLETED | Valsartan/Hydrochlorothiazide Combination vs Amlodipine in Patients With Hypertension, Diabetes, and Albuminuria. |
| NCT00171574 | PHASE4 | COMPLETED | Antiproteinuric Effect of Valsartan and Lisinopril |
| NCT00171600 | PHASE4 | TERMINATED | Antialbuminuric Effects of Valsartan and Lisinopril |
| NCT00171756 | PHASE4 | COMPLETED | Study to Compare the Effect of Valsartan vs Atenolol on Pro-thrombotic State in Hypertensive Patients. |
| NCT00171782 | PHASE4 | COMPLETED | Hypertension and Cardiovascular Risk Factors |
| NCT00185055 | PHASE4 | COMPLETED | The Relative Effects of Olmesartan Medoxomil, Irbesartan and Valsartan on the Activity of the Blood Pressure Control System in Healthy Subjects |
| NCT00190580 | PHASE4 | COMPLETED | Kanagawa Valsartan Trial (KVT): Effects of Valsartan on Renal and Cardiovascular Disease |
| NCT00202618 | PHASE4 | UNKNOWN | Rationale and Design for Shiga Microalbuminuria Reduction Trial |
| NCT00240448 | PHASE4 | COMPLETED | A Randomized, Double-blind, Placebo Controlled Comparison of Telmisartan Hydrochlorothiazide (HCT) and Valsartan HCT in Hypertension (HTN) Stage I/II Patients |
| NCT00241072 | PHASE4 | COMPLETED | Clinical Trial To Evaluate The Effect Of Valsartan On Insulin Sensitivity In Subjects With Impaired Glucose Tolerance |
| NCT00241085 | PHASE4 | COMPLETED | Effect of Valsartan on Proteinuria in Patients With Hypertension and Diabetes Mellitus |
| NCT00241098 | PHASE4 | COMPLETED | The VALIDATE Study of Valsartan for Patients With Early Stage Heart Failure |
| NCT00241124 | PHASE4 | COMPLETED | Comparison Of Morning And Evening Dosing Of Valsartan And Lisinopril In Patients With Diabetes |
| NCT00241150 | PHASE4 | COMPLETED | Diva - The Effects Of 12 Weeks Of Treatment With High Dose Valsartan (320 Mg) To Amlodipine On Endothelial Function In Hypertensive Subjects With The Metabolic Syndrome |
| NCT00277472 | PHASE4 | COMPLETED | Efficacy and Safety of Valsartan/Hydrochlorothiazide Combination Therapy in Patients With Hypertension |
| NCT00280540 | PHASE4 | COMPLETED | Efficacy and Safety of Valsartan/Hydrochlorothiazide Combination Therapy in Patients With Hypertension |
| NCT00302705 | PHASE4 | COMPLETED | Comparison of the Antihypertensive Efficacy of Valsartan and Enalapril After Missing One Dose |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 1 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 |
| OLMESARTAN MEDOXOMIL | 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 |
Related Atlas pages
- Genes: AGTR1
- Diseases: congestive heart failure, heart failure, hypertensive disorder, diabetes mellitus, myocardial infarction, cardiovascular disorder, stroke disorder, acute myocardial infarction, atrial fibrillation, kidney disorder, atherosclerosis, metabolic syndrome X, coronary artery disorder, ST-elevation myocardial infarction, Chagas cardiomyopathy, pulmonary hypertension, severe acute respiratory syndrome, essential hypertension, type 2 diabetes mellitus
- Drugs: Crizotinib, Losartan, Olmesartan Medoxomil, 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