Candesartan

Summary

Candesartan (CHEMBL1016) is an approved small-molecule antihypertensive agent (ATC C09CA06) targeting AGTR1; indicated across 27 conditions including cardiovascular disorder and hypertensive disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C09CA06
• Targets: 1 (AGTR1)
• Indications: 27 conditions
• Clinical trials: 82
• Chemistry: 440.5 Da · C24H20N6O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1016
Name	Candesartan
Type	Small molecule
Max phase	3
FDA approved	yes
PubChem CID	2541
ChEBI	CHEBI:3347
ATC	C09CA06
Molecular formula	C24H20N6O3
Molecular weight	440.5
InChIKey	HTQMVQVXFRQIKW-UHFFFAOYSA-N

SMILES: CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O

IUPAC name: 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid

ChEBI definition: A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2’-(1H-tetrazol-5-yl)[1,1’-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.

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

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

Also known as: Blopress, Candemore, Candesartan, Candesartan cilexetil related compound g, CV-11974, NSC-759858, candesartan, SID50112728, CANDESARTAN, SID144206031, SID170466386, Candersartan

Patent coverage: 9,602 distinct patent families (37,149 SureChEMBL compound mentions), from 5 matched compound structure(s). One matched structure accounts for 26,342 (71%) 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	9.72	0.4%	P30556

Broader ChEMBL bioactivity targets: 20 (assay-derived). Sample: Receptor tyrosine-protein kinase erbB-2, 5-hydroxytryptamine receptor 2B, Thromboxane-A synthase, Alpha-2B adrenergic receptor, Epidermal growth factor receptor, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2C, Type-1 angiotensin II receptor, Peroxisome proliferator-activated receptor gamma, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A.

Bioactivity

ChEMBL activities: 27 potent at pChembl ≥ 5 of 34 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
AGTR1	9.4	AC50	0.4	nM	CHEMBL_ACT_25177692
AGTR1	9.3	AC50	0.5	nM	CHEMBL_ACT_25176898
P34976	9.19	Ki	0.64	nM	CHEMBL_ACT_1033744
AGTR1	9.16	IC50	0.69	nM	CHEMBL_ACT_16528775
P25095	8.5	Kd	3.16	nM	CHEMBL_ACT_2262120
AGTR1	8.46	Ki	3.5	nM	CHEMBL_ACT_16528719
P25095	8	Kd	10	nM	CHEMBL_ACT_2234188
AGTR1	7.98	Ki	10.4	nM	CHEMBL_ACT_18386076
AGTR1	7.97	IC50	10.72	nM	CHEMBL_ACT_16528725
P34976	7.55	IC50	28	nM	CHEMBL_ACT_1033745
P25104	6.96	IC50	110	nM	CHEMBL_ACT_1032470
P25104	6.96	IC50	110	nM	CHEMBL_ACT_1149848
P25104	6.96	IC50	110	nM	CHEMBL_ACT_182822
AGTR1	6.96	IC50	110	nM	CHEMBL_ACT_5202515
ADORA3	6.16	Ki	689.5	nM	CHEMBL_ACT_7610013
ADORA3	5.91	IC50	1220	nM	CHEMBL_ACT_7610012
ADRA2B	5.76	Ki	1754	nM	CHEMBL_ACT_7610025
SLC6A2	5.52	Ki	3040	nM	CHEMBL_ACT_7610035
CYP2C9	5.52	IC50	3000	nM	CHEMBL_ACT_7610082
SLC6A2	5.51	IC50	3065	nM	CHEMBL_ACT_7610034
TBXAS1	5.51	IC50	3059	nM	CHEMBL_ACT_7612655
ADRB3	5.5	Ki	3200	nM	CHEMBL_ACT_7610033
EGFR	5.49	IC50	3277	nM	CHEMBL_ACT_7611407
ADRA2B	5.42	IC50	3843	nM	CHEMBL_ACT_7610024
ADRB3	5.37	IC50	4300	nM	CHEMBL_ACT_7610032
ERBB2	5.23	IC50	5947	nM	CHEMBL_ACT_7611411
CYP3A4	5.05	IC50	9000	nM	CHEMBL_ACT_7610088

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

27 indications (0 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
cardiovascular disorder	3	MONDO:0004995	EFO:0000319
hypertensive disorder	3	MONDO:0005044	EFO:0000537
heart failure	3	MONDO:0005252	EFO:0003144
congestive heart failure	3	MONDO:0005009	EFO:0000373
aortic valve stenosis	3	MONDO:0042981	EFO:0000266
atrial fibrillation	3	MONDO:0004981	EFO:0000275
heart disorder	3	MONDO:0005267	EFO:0003777
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
dilated cardiomyopathy	3	MONDO:0005021	EFO:0000407
essential hypertension	3	MONDO:0001134	MONDO:0001134
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148
cocaine dependence	2	MONDO:0005186	EFO:0002610
hepatitis C virus infection	2	MONDO:0005231	EFO:0003047
hypertrophic cardiomyopathy	2	MONDO:0005045	EFO:0000538
peripheral neuropathy	2	MONDO:0005244	EFO:0003100
migraine disorder	2	MONDO:0005277	MONDO:0005277
migraine with aura	2	MONDO:0005475	MONDO:0005475
migraine without aura	2	MONDO:0100431	MONDO:0100431
methamphetamine dependence	1	MONDO:0005419	EFO:0004701
alcoholic liver disease	1	MONDO:0043693	EFO:0008573
substance-related disorder	1	MONDO:0002494	MONDO:0002491
Barrett esophagus	0	MONDO:0013662	EFO:0000280
bipolar disorder	0	MONDO:0004985	MONDO:0004985

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

Clinical trials

Total trials: 82.

Phase distribution

Phase	Trials
PHASE4	23
PHASE3	21
PHASE2	11
Not specified	11
PHASE1	10
EARLY_PHASE1	3
PHASE2/PHASE3	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00108706	PHASE4	UNKNOWN	Acute Candesartan Cilexetil Outcomes Stroke Trial (ACCOST)
NCT00139386	PHASE4	COMPLETED	Candesartan for Prevention of Cardiovascular Events After Cypher or Taxus Coronary Stenting (4C) Trial
NCT00192803	PHASE4	UNKNOWN	Non-Insulin Dependent Diabetes Mellitus (NIDDM) and Angiotensin Converting Enzyme 2 (ACE2): Diabetic Patients Treated With Antihypertensive Drugs
NCT00232882	PHASE4	COMPLETED	Pharmacodynamic Influences of Candesartan, Atenolol, Hydrochlorothiazide and Drug Combinations in Hypertensive Patients.
NCT00235287	PHASE4	UNKNOWN	Pulse Wave Velocity, Pulse Wave Morphology and Blocking of the Reninangiotensin System in Patients With Chronic Kidney Disease
NCT00319202	PHASE4	TERMINATED	Clinical Trial to Assess the Effects of Candesartan on the Carbohydrate Metabolism of Obese Subjects
NCT00328302	PHASE4	UNKNOWN	Diabetes Type 1, Treatment Study Atacand/Placebo After Kidney Biopsy
NCT00348686	PHASE4	COMPLETED	Candesartan Effectiveness Study in Pro-B Type Natriuretic Peptides (BNP)
NCT00356395	PHASE4	COMPLETED	Safety and Effects of Ramipril Combined With Candesartan
NCT00391846	PHASE4	COMPLETED	Evaluation of Heart Failure Treatment Guided by N-terminal Pro B-type Natriuretic Peptide (NTproBNP) vs Clinical Symptoms and Signs Alone
NCT00468923	PHASE4	COMPLETED	Heart Outcomes Prevention Evaluation-3
NCT00538486	PHASE4	COMPLETED	A Randomized, Double-Blind, Active Control Trial Comparing Effects of Telmisartan, Candesartan and Amlodipine, Alone or Plus Metformin, on Non-Diabetic, Obese Hypertensive Patients
NCT00541853	PHASE4	UNKNOWN	CCB Safety Study in Treatment of Hypertension of ADPKD
NCT00564057	PHASE4	UNKNOWN	Effects of Antihypertensive Treatment in HIV Infected Patients: Candesartan Versus Lercanidipine
NCT00587470	PHASE4	COMPLETED	Angiotensin-II Blockade in Mitral Regurgitation
NCT00607672	PHASE4	COMPLETED	The RAS, Fibrinolysis and Cardiopulmonary Bypass
NCT00775814	PHASE4	COMPLETED	Efficacy of Candesartan on Reducing Blood Pressure in Insulin-Resistant, Obese Patients With Hypertension.
NCT01629225	PHASE4	UNKNOWN	GRK4 Polymorphisms Blood Pressure Response to Candesartan
NCT01682564	PHASE4	COMPLETED	To Evaluate the Efficacy and Safety on Blood Pressure In Patients With Hypertension Diagnosed Congestive Heart Failure
NCT01766505	PHASE4	TERMINATED	The Study to Evaluate Efficacy and Safety of Candesartan vs Losartan in Hypertension With Heart Failure (HONOR)
NCT01794455	PHASE4	TERMINATED	Effects of Cerebral Hypoperfusion and Its Reversal on Late-Life Depression
NCT01827202	PHASE4	COMPLETED	RAS Quantification in Patients With Aliskiren or Candesartan
NCT02261116	PHASE4	COMPLETED	Study to Assess Potential Different Properties of Telmisartan Compared to Candesartan in Healthy Volunteers
NCT03770936	PHASE3	RECRUITING	Effect of Some Drugs on Liver Fibrosis
NCT05321875	PHASE3	RECRUITING	Early Treatment With Candesartan vs Placebo in Genetic Carriers of Dilated Cardiomyopathy (EARLY-GENE Trial)
NCT06646354	PHASE3	ENROLLING_BY_INVITATION	To Evaluate the Efficacy and Safety of Co-administrated HODO-2224-1 and HODO-2224-2 in Patients With Essential Hypertension and Primary Hypercholesterolemia
NCT00130975	PHASE3	COMPLETED	Candesartan in the Prevention of Relapsing Atrial Fibrillation
NCT00150631	PHASE3	UNKNOWN	Danish Hypertension Prevention Project - DHYPP
NCT00252694	PHASE3	COMPLETED	DIabetic Retinopathy Candesartan Trials
NCT00252720	PHASE3	COMPLETED	DIabetic Retinopathy Candesartan Trials.
NCT00294775	PHASE3	UNKNOWN	Effect of Angiotensin II Receptor Blockers (ARB) on Left Ventricular Reverse Remodelling After Aortic Valve Replacement in Severe Valvular Aortic Stenosis
NCT00434967	PHASE3	COMPLETED	Antihypertensive Efficacy and Safety of Candesartan/HCT 32/25 mg in Comparison With Individual Components and Placebo
NCT00634309	PHASE3	COMPLETED	Candesartan Cilexetil in Heart Failure Assessment of Reduction in Mortality and Morbidity (CHARM Added)
NCT00634400	PHASE3	COMPLETED	Candesartan in Heart Failure Assessment of Reduction in Mortality and Morbidity (CHARM Alternative)
NCT00634712	PHASE3	COMPLETED	Candesartan Cilexetil in Heart Failure Assessment of Reduction in Mortality and Morbidity (CHARM Preserved)
NCT00644475	PHASE3	UNKNOWN	Imidapril and Candesartan on Fibrinolysis and Insulin-Sensitivity in Patients With Mild to Moderate Hypertension
NCT00699452	PHASE3	UNKNOWN	The Potential of Candesartan to Retard the Progression of Aortic Stenosis
NCT00775840	PHASE3	COMPLETED	Efficacy of Candesartan on Symptomatic Heart Failure in Treating Diabetic and Hypertensive Patients.
NCT00843154	PHASE3	TERMINATED	Efficacy of Candesartan on Brain Natriuretic Peptide Levels in Subjects With Chronic Heart Failure
NCT00867490	PHASE3	COMPLETED	Safety and Efficacy of Aliskiren + Hydrochlorothiazide (± Amlodipine 5 mg) in Patients With Moderate Hypertension

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 11 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