Candesartan Cilexetil

Summary

Candesartan Cilexetil (CHEMBL1014) is an approved small molecule; indicated across 21 conditions including hypertensive disorder and congestive heart failure.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 21 conditions
• Clinical trials: 51
• Chemistry: 610.7 Da · C33H34N6O6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1014
Name	Candesartan Cilexetil
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	2540
Molecular formula	C33H34N6O6
Molecular weight	610.7
InChIKey	GHOSNRCGJFBJIB-UHFFFAOYSA-N

SMILES: CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)OC(C)OC(=O)OC6CCCCC6

IUPAC name: 1-cyclohexyloxycarbonyloxyethyl 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate

Also known as: Amias, Atacand, Candesartan cilexetil, NSC-758697, Ratacand, TCV-116, candesartancilexetil, SID26748952, Candensartan cilexetil, CANDESARTAN CILEXETIL, CANDESARTAN CILEXTIL, SID144212519

Patent coverage: 2,925 distinct patent families (11,194 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 10,900 (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

Broader ChEMBL bioactivity targets: 62 (assay-derived). Sample: Lysine-specific demethylase 4E, Ubiquitin carboxyl-terminal hydrolase 2, Nuclear receptor ROR-gamma, ATP-dependent DNA helicase Q1, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Cholecystokinin receptor type A.

Bioactivity

ChEMBL activities: 35 potent at pChembl ≥ 5 of 79 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CNR1	8.92	AC50	1.2	nM	CHEMBL_ACT_25116764
AGTR1	7.88	AC50	13.2	nM	CHEMBL_ACT_25177693
AGTR1	7.75	AC50	17.8	nM	CHEMBL_ACT_25176902
P34976	6.7	IC50	200	nM	CHEMBL_ACT_5202519
SLCO1B1	6.4	Ki	400	nM	CHEMBL_ACT_13800686
PPARG	6.17	AC50	680	nM	CHEMBL_ACT_25113928
NR1I2	6.16	AC50	700	nM	CHEMBL_ACT_25188112
SLCO1B1	6.14	IC50	724.4	nM	CHEMBL_ACT_13800622
USP2	6.1	Potency	794.3	nM	CHEMBL_ACT_4715724
PDE4D	5.86	AC50	1393	nM	CHEMBL_ACT_25185232
TBXA2R	5.77	AC50	1691	nM	CHEMBL_ACT_25155127
SLCO1B3	5.72	Ki	1900	nM	CHEMBL_ACT_13798687
ADORA3	5.72	AC50	1903	nM	CHEMBL_ACT_25134119
SLCO1B3	5.61	IC50	2455	nM	CHEMBL_ACT_13798623
PPARG	5.38	EC50	4200	nM	CHEMBL_ACT_22960963
HTR2A	5.34	AC50	4554	nM	CHEMBL_ACT_25173583
CHRM2	5.34	AC50	4583	nM	CHEMBL_ACT_25213650
OPRM1	5.33	AC50	4702	nM	CHEMBL_ACT_25157389
HTR2A	5.31	AC50	4899	nM	CHEMBL_ACT_25225086
ABCG2	5.3	IC50	5000	nM	CHEMBL_ACT_24777394
NR3C1	5.29	AC50	5100	nM	CHEMBL_ACT_25116000
HTR1A	5.29	AC50	5100	nM	CHEMBL_ACT_25215955
PGR	5.29	AC50	5148	nM	CHEMBL_ACT_25222077
ADRA1A	5.27	AC50	5409	nM	CHEMBL_ACT_25218002
POLK	5.25	IC50	5600	nM	CHEMBL_ACT_16667657
P15207	5.24	AC50	5700	nM	CHEMBL_ACT_25232291
POLI	5.21	IC50	6200	nM	CHEMBL_ACT_16667655
P25779	5.2	Potency	6310	nM	CHEMBL_ACT_4001880
HTR2B	5.11	AC50	7854	nM	CHEMBL_ACT_25227438
ESR1	5.07	AC50	8500	nM	CHEMBL_ACT_25116322

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

21 indications (7 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
congestive heart failure	4	MONDO:0005009	EFO:0000373
diabetes mellitus	4	MONDO:0005015	EFO:0000400
stroke disorder	4	MONDO:0005098	EFO:0000712
heart failure	4	MONDO:0005252	EFO:0003144
myocardial infarction	4	MONDO:0005068	EFO:0000612
proteinuria	3	MONDO:0003634	HP:0000093
atherosclerosis	3	MONDO:0005311	EFO:0003914
renal artery obstruction	3	MONDO:0006945	EFO:1001150
renovascular hypertension	3	MONDO:0006947	EFO:1001153
breast neoplasm	3	MONDO:0021100	MONDO:0007254
coronary artery disorder	3	MONDO:0005010	EFO:0001645
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
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
brain injury	2	MONDO:0043510	MONDO:0043510
cardiovascular disorder	1	MONDO:0004995	EFO:0000319

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

Clinical trials

Total trials: 51.

Phase distribution

Phase	Trials
PHASE3	16
PHASE1	12
PHASE4	10
PHASE2	7
Not specified	5
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07547878	PHASE4	NOT_YET_RECRUITING	Rapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD)
NCT00360763	PHASE4	UNKNOWN	Study of Optimal Treatment Plan in Hypertensives With Anti-AT1-Receptor Autoantibody
NCT00573430	PHASE4	COMPLETED	ARIA (Atacand Renoprotection In NephropAthy Pt.)
NCT00587470	PHASE4	COMPLETED	Angiotensin-II Blockade in Mitral Regurgitation
NCT00621153	PHASE4	COMPLETED	Candesartan Effect in Second Stage Arterial Hypertension
NCT01012479	PHASE4	COMPLETED	Efficacy and Safety of Candesartan Cilexetil Plus Hydrochlorothiazide in Subjects With Severe Hypertension
NCT01611077	PHASE4	COMPLETED	Efficacy and Safety of a Therapy Change From Candesartan 32 mg to Fixed Combination of Olmesartan 40 mg/Amlodipine 10 mg
NCT01682564	PHASE4	COMPLETED	To Evaluate the Efficacy and Safety on Blood Pressure In Patients With Hypertension Diagnosed Congestive Heart Failure
NCT01734096	PHASE4	COMPLETED	Renal Response to Lower Body Negative Pressure in Pre-hypertensive States
NCT03847506	PHASE4	COMPLETED	Evaluate Efficacy and Safety of Ezetimibe/Rosuvastatin and Candesartan Cilexetil/Amlodipine Besylate Combination Tablets
NCT00081731	PHASE3	COMPLETED	Benefits of Medical Therapy Plus Stenting for Renal Atherosclerotic Lesions
NCT00120003	PHASE3	COMPLETED	Scandinavian Candesartan Acute Stroke Trial (SCAST)
NCT00125463	PHASE3	UNKNOWN	Candesartan Antihypertensive Survival Evaluation in Japan (CASE-J) Trial of Cardiovascular Events in High-Risk Hypertensive Patients
NCT00227318	PHASE3	COMPLETED	TROPHY - Candesartan Cilexetil Long-term Hypertension Prevention Trial
NCT00242346	PHASE3	COMPLETED	High Doses of Candesartan Cilexetil on the Reduction of Proteinuria
NCT00252733	PHASE3	COMPLETED	Diabetic Retinopathy Candesartan Trials
NCT00383929	PHASE3	COMPLETED	Antihypertensive Efficacy and Safety of Candesartan/HCT 32/12.5 and 32/25 mg in Comparison With Candesartan 32 mg
NCT00434967	PHASE3	COMPLETED	Antihypertensive Efficacy and Safety of Candesartan/HCT 32/25 mg in Comparison With Individual Components and Placebo
NCT00679484	PHASE3	TERMINATED	Study to Demonstrate the Non-inferiority of Olmesartan Medoxomil Versus Candesartan Cilexetil in Reducing Blood B-type (or Brain) Natriuretic Peptide Levels at Week 24
NCT00690612	PHASE3	COMPLETED	Study to Characterize the Long-term Clinical Experience of Atacand in Hypertensive Children Ages 1 to<11 Years (Hypertension in Pediatrics)
NCT01052272	PHASE2/PHASE3	COMPLETED	Impact of Diabetes on Left Ventricular Remodeling
NCT01135212	PHASE3	COMPLETED	The Clinical Study to Evaluate the Efficacy and Safety of Fimasartan in Patients With Mild to Moderate Essential Hypertension
NCT01613209	PHASE3	COMPLETED	Sevicontrol-1: Efficacy and Safety of a Fixed Combination of Olmesartan/ Amlodipine
NCT01788358	PHASE3	COMPLETED	Open-Label Long-Term Safety and Efficacy Study of Fixed Dose Combination of Nifedipine Gastrointestinal Therapeutic System and Candesartan Cilexetil in Subjects With Moderate to Severe Essential Hypertension
NCT02047019	PHASE3	WITHDRAWN	Monotherapy-Controlled Study of Nifedipine Gastrointestinal Therapeutic System and Candesartan Cilexetil in Combination in Subjects With Essential Hypertension Inadequately Controlled on Candesartan Cilexetil
NCT02368652	PHASE3	COMPLETED	A Study to Evaluate the Efficacy and Safety of Amlodipine Besylate and Candesartan Cilexetil in Essential Hypertension Patient Who Are Not Adequately Controlled With Candesartan Cilexetil Monotherapy
NCT05920005	PHASE3	COMPLETED	Candesartan Cilexetil + Chlorthalidone + Amlodipine Versus Exforge HCT®️ for Systemic Arterial Hypertension
NCT05826912	PHASE2	ENROLLING_BY_INVITATION	Multi-Arm Multi-Stage Adaptive Platform Trial (APT) for the Acute Treatment of Traumatic Brain Injury
NCT00184587	PHASE2	COMPLETED	Prophylactic Treatment of Episodic Cluster Headache
NCT01289132	PHASE2	COMPLETED	Efficacy and Safety of Azilsartan in Participants With Mild to Moderate Uncomplicated Essential Hypertension
NCT02059616	PHASE2	UNKNOWN	A Phase 2 Dose Selection Trial of Candesartan Cilexetil and Amlodipine Besylate to Treat Essential Hypertension
NCT02332824	PHASE2	COMPLETED	A Phase 2 Dose-finding Study of TAK-272 in Participants With Type 2 Diabetes Mellitus and Microalbuminuria
NCT02944734	PHASE2	COMPLETED	Comparison of Efficacy and Safety of Combination Therapy and Monotherapy of Candesartan and Amlodipine for Dose-Finding in Patients With Essential Hypertension
NCT05122182	PHASE2	TERMINATED	Controlled Trial of Angiotensin Receptor Blocker (ARB) & Chemokine Receptor Type 2 (CCR2) Antagonist for the Treatment of COVID-19
NCT00844324	PHASE1	COMPLETED	Bioequivalence Study in Healthy Subjects
NCT00905333	PHASE1	COMPLETED	Evaluation of the Pharmacokinetic Interaction Between Candesartan and Felodipine After Ingestion of a Specific Meal
NCT01845272	PHASE1	UNKNOWN	Pharmacokinetic Interactions of Candesartan Cilexetil and Amlodipine Besylate
NCT01926652	PHASE1	COMPLETED	Safety and Pharmacokinetics Study of Amlodipine 10mg and Candesartan 32mg
NCT02006589	PHASE1	COMPLETED	Bioavailability Study of Candesartan Cilexetil 8mg Tablet Under Fasting Conditions
NCT02006602	PHASE1	COMPLETED	Bioavailability Study of Candesartan Cilexetil 16mg Tablet Under Fasting Conditions

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).