Irbesartan

Summary

Irbesartan (CHEMBL1513) is an approved small-molecule antihypertensive agent (ATC C09CA04) targeting AGTR1 and SLC10A1; indicated across 21 conditions including hypertensive disorder and cardiovascular disorder; with CIViC clinical evidence for 2 variant-indication associations (e.g. FOS Overexpression in colon adenocarcinoma).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C09CA04
• Targets: 2 (AGTR1, SLC10A1)
• Indications: 21 conditions
• Clinical trials: 94
• Precision-oncology evidence (CIViC): 2 variant–indication associations
• Chemistry: 428.5 Da · C25H28N6O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1513
Name	Irbesartan
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3749
ChEBI	CHEBI:5959
ATC	C09CA04
Molecular formula	C25H28N6O
Molecular weight	428.5
InChIKey	YOSHYTLCDANDAN-UHFFFAOYSA-N

SMILES: CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5

IUPAC name: 2-butyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one

ChEBI definition: A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.

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

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

Also known as: Aprovel, Avapro, BMS-186295, Ifirmasta, Irbesartan, Irbesartan bms, Irbesartan component of avalide, Irbesartan component of coaprovel, Irbesartan component of ifirmacombi, Irbesartan teva, Irbesartan zentiva, Karvea

Parent form; salt/anhydrous children: CHEMBL6068339

Patent coverage: 7,990 distinct patent families (31,667 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 31,142 (98%) 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	8.8	0.4%	P30556
SLC10A1	Sodium/bile acid and sulphated solute cotransporter 1	Inhibition	4.92	0.1%	Q14973

Broader ChEMBL bioactivity targets: 20 (assay-derived). Sample: Prelamin-A/C, ATP-binding cassette sub-family C member 4, 5-hydroxytryptamine receptor 2B, Angiotensin II receptor, Angiotensin II receptor (AT-1) type-1, Angiotensin II receptor, Type-1 angiotensin II receptor, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Endothelin-1 receptor, Lysosomal alpha-glucosidase.

Bioactivity

ChEMBL activities: 28 potent at pChembl ≥ 5 of 39 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
AGTR1	9.1	Ki	0.8	nM	CHEMBL_ACT_12149695
AGTR1	9.1	Ki	0.8	nM	CHEMBL_ACT_1618826
AGTR1	9.1	AC50	0.8	nM	CHEMBL_ACT_25177669
P29089	9.1	Ki	0.8	nM	CHEMBL_ACT_83699
AGTR1	9.05	AC50	0.9	nM	CHEMBL_ACT_25176501
P25095	9.05	IC50	0.9	nM	CHEMBL_ACT_418686
AGTR1	8.96	Ki	1.1	nM	CHEMBL_ACT_83700
P25095	8.89	IC50	1.3	nM	CHEMBL_ACT_1065927
P25095	8.89	IC50	1.3	nM	CHEMBL_ACT_1229748
P29089	8.89	IC50	1.3	nM	CHEMBL_ACT_322852
P25095	8.89	IC50	1.3	nM	CHEMBL_ACT_451487
P29089	8.89	IC50	1.3	nM	CHEMBL_ACT_861803
AGTR1	8.77	AC50	1.7	nM	CHEMBL_ACT_25177689
AGTR1	8.7	Ki	2	nM	CHEMBL_ACT_659924
AGTR1	8.7	Ki	2	nM	CHEMBL_ACT_835312
AGTR1	8.52	IC50	3	nM	CHEMBL_ACT_25751489
AGTR1	8.52	IC50	3	nM	CHEMBL_ACT_835313
AGTR1	8.22	IC50	6	nM	CHEMBL_ACT_23289907
AGTR1	7.68	IC50	20.8	nM	CHEMBL_ACT_5202082
LMNA	6.4	Potency	398.1	nM	CHEMBL_ACT_3661053
LTB4R2	6.39	EC50	410	nM	CHEMBL_ACT_23289874
GAA	6.35	Potency	446.7	nM	CHEMBL_ACT_4957025
GAA	6.35	Potency	446.7	nM	CHEMBL_ACT_5062518
PDE3A	5.39	AC50	4099	nM	CHEMBL_ACT_25190177
ABCB11	5.14	IC50	7310	nM	CHEMBL_ACT_18052024
ABCB11	5.14	IC50	7310	nM	CHEMBL_ACT_18129062
ABCB11	5.14	IC50	7300	nM	CHEMBL_ACT_22396459
EDNRA	5	Ki	10000	nM	CHEMBL_ACT_12149694

Target pathways

Aggregated over 2 target gene(s): AGTR1, SLC10A1.

Top Reactome pathways

12 total, by targets touching each:

Pathway	Targets	Genes
Recycling of bile acids and salts	1	SLC10A1
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
symbiont entry into host cell	2
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

Indications & clinical

Indications

21 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
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
diabetic kidney disease	4	MONDO:0005016	EFO:0000401
chronic kidney disease	4	MONDO:0005300	EFO:0003884
type 2 diabetes mellitus	4	MONDO:0005148	MONDO:0005148
atrial fibrillation	3	MONDO:0004981	EFO:0000275
chronic hepatitis C virus infection	3	MONDO:0005354	EFO:0004220
congestive heart failure	3	MONDO:0005009	EFO:0000373
focal segmental glomerulosclerosis	3	MONDO:0100313	EFO:0004236
IgA glomerulonephritis	3	MONDO:0005342	EFO:0004194
myocardial ischemia	3	MONDO:0024644	EFO:1001375
acute kidney injury	3	MONDO:0002492	HP:0001919
essential hypertension	3	MONDO:0001134	MONDO:0001134
Ehlers-Danlos syndrome	3	MONDO:0020066	MONDO:0017314
severe acute respiratory syndrome	3	MONDO:0005091	EFO:0000694
Marfan syndrome	2	MONDO:0007947	MONDO:0007947
Ebola hemorrhagic fever	1	MONDO:0005737	EFO:0007243

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

Clinical trials

Total trials: 94.

Phase distribution

Phase	Trials
PHASE4	33
PHASE3	30
Not specified	13
PHASE2	8
PHASE1	6
PHASE2/PHASE3	2
PHASE1/PHASE2	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06660940	PHASE4	NOT_YET_RECRUITING	Clinical Trial of Keluoxin Capsules in the Treatment of Diabetic Kidney Disease with Diabetic Retinopathy
NCT07547878	PHASE4	NOT_YET_RECRUITING	Rapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD)
NCT00095290	PHASE4	COMPLETED	Irbesartan Versus Placebo in Combination With Ramipril for Treatment of Albuminuria
NCT00110422	PHASE4	COMPLETED	Irbesartan in the Treatment of Hypertensive Patients With Metabolic Syndrome
NCT00125645	PHASE4	COMPLETED	Left Ventricular Function After Acute Myocardial Infarction (AMI). Treatment With Angiotensin 2-Receptor Blockade (GLOBAL-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
NCT00264212	PHASE4	COMPLETED	AMISH : Aprovel for Management of Isolated Systolic Hypertension
NCT00265967	PHASE4	COMPLETED	Irbesartan in Hypertension
NCT00283036	PHASE4	COMPLETED	APROVE : Irbesartan in Hypertension
NCT00320879	PHASE4	COMPLETED	Optimal Dose of Irbesartan for Renoprotection in Type 2 Diabetic Patients With Persistent Microalbuminuria
NCT00334581	PHASE4	COMPLETED	Irbesartan in Chinese Hypertensive Diabetics With Microalbuminuria
NCT00335673	PHASE4	COMPLETED	I SAVE - Irbesartan in Mild to Moderate Hypertensive Patients
NCT00347087	PHASE4	COMPLETED	Effect of Irbesartan on Insulin Sensitivity in Chronic Heart Failure
NCT00350038	PHASE4	COMPLETED	Irbesartan, Ciprofibrate and Their Combination Onto the Endothelial Functions
NCT00362037	PHASE4	COMPLETED	I SELECT - Irbesartan In Hypertensive Patients With Left Ventricular Hypertrophy
NCT00362258	PHASE4	COMPLETED	I PREVENT - Irbesartan In Hypertensive Diabetic Patients
NCT00443612	PHASE4	COMPLETED	Irbesartan/Hydrochlorothiazide National Taiwan University Hospital Listing
NCT00500604	PHASE4	COMPLETED	Efficacy of Irbesartan/Hydrochlorothiazide Versus Valsartan/Hydrochlorothiazide in Mild to Moderate Hypertension
NCT00517322	PHASE4	UNKNOWN	Left Atrial Remodelling in Hypertension: Effects of Ramipril or Irbesartan
NCT00529750	PHASE4	COMPLETED	Effect of the Angiotensin II Receptor Antagonist Irbesartan on Biochemical and Functional Markers of Endothelial Dysfunction in Patients With Hypertension
NCT00535925	PHASE4	COMPLETED	Nephropathy In Type 2 Diabetes and Cardio-renal Events
NCT00549133	PHASE4	COMPLETED	Irbesartan Effects on Endothelial Dysfunction in Hypertensive Type II Diabetic Patients Comparing Atenolol
NCT00562809	PHASE4	COMPLETED	The Efficacy and Safety of Irbesartan 150/12.5 mg and 300/25 mg in Patients With Mild Hypertension
NCT00564187	PHASE4	COMPLETED	Evaluation of Efficacy and Safety of the Dosage Adjustment of Aprovel® (Irbesartan) in Hypertensive Outpatients in Current Clinical Practice
NCT00613496	PHASE4	UNKNOWN	Irbesartan and Adhesion Molecules in AF
NCT00660309	PHASE4	COMPLETED	A Clinical Study to Evaluate Renal Hemodynamic Responses to Aliskiren in Patients With Type 2 Diabetes Mellitus
NCT00670566	PHASE4	COMPLETED	Irbesartan/Hydrochlorothiazide to Control Elevated Blood Pressure to Target in Moderate to Severe Hypertensive Patients
NCT00847834	PHASE4	COMPLETED	Irbesartan-Hydrochlorothiazide Phase IV Study: Treatment of Hypertension in Chinese Population
NCT00987662	PHASE4	WITHDRAWN	Irbesartan Versus Amlodipine: The OBI Study
NCT01360710	PHASE4	UNKNOWN	The Effect of Moxonidine on Blood Pressure and Regression of Early Target Organ Damage in Young Subjects With Abdominal Obesity and Hypertension
NCT02842359	PHASE4	COMPLETED	Evaluation of the Fixed-dose Combination of Irbesartan/Atorvastatin in Type 2 Diabetic Patients Diagnosed With Hyperlipidemia and Hypertension
NCT03147677	PHASE4	COMPLETED	Clinical Study of Treating Type 2 Diabetic Nephropathy With Alfacalcidol and Irbesartan
NCT05243199	PHASE4	COMPLETED	Sacubitril/Valsartan for CKD5 Stage Dialysis Patients
NCT03762850	PHASE3	ACTIVE_NOT_RECRUITING	A Study of the Effect and Safety of Sparsentan in the Treatment of Patients With IgA Nephropathy
NCT05272878	PHASE3	ACTIVE_NOT_RECRUITING	Impact of a Treatment With Angiotensin Receptor Blocker on Outcome After Acute Kidney Injury in Patients Discharged From the ICU.
NCT00005010	PHASE3	COMPLETED	Prevention of Kidney Transplant Rejection
NCT00095238	PHASE3	COMPLETED	Irbesartan in Heart Failure With Preserved Systolic Function (I-Preserve)
NCT00095394	PHASE3	COMPLETED	Irbesartan/Hydrochlorothiazide (HCTZ) Combination Therapy as First Line Treatment for Severe Hypertension
NCT00095550	PHASE3	COMPLETED	Irbesartan/Hydrochlorothiazide (HCTZ) Combination Therapy for Patients With Moderate Hypertension
NCT00106561	PHASE2/PHASE3	COMPLETED	Using the Drug Spironolactone to Test If It Reduces Protein Leakage From the Kidney

Clinical evidence (CIViC)

Variant × indication × effect (2 predictive associations from 2 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
FOS Overexpression	Colon Adenocarcinoma	Sensitivity/Response	Irbesartan	CIViC C	EID1634
JUN Overexpression	Colorectal Adenocarcinoma	Sensitivity/Response	Irbesartan	CIViC C	EID1633

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 10 clinical and 32 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.

155 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
PROPRANOLOL	ChEMBL + PubChem	Phase 4 (approved)	AGTR1, SLC10A1
RITONAVIR	ChEMBL + PubChem	Phase 4 (approved)	AGTR1, SLC10A1
ROSIGLITAZONE	ChEMBL + PubChem	Phase 4 (approved)	AGTR1, SLC10A1
ZAFIRLUKAST	ChEMBL + PubChem	Phase 4 (approved)	AGTR1, SLC10A1
OLMESARTAN	ChEMBL + PubChem	Phase 3 (approved)	AGTR1, SLC10A1
TIRATRICOL	ChEMBL	Phase 3	AGTR1, SLC10A1
Bosentan	PubChem	Approved	AGTR1, SLC10A1
chenodiol	PubChem	Approved	AGTR1, SLC10A1
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
CYCLOSPORINE	ChEMBL + PubChem	Phase 4 (approved)	SLC10A1
EZETIMIBE	ChEMBL + PubChem	Phase 4 (approved)	SLC10A1
FUROSEMIDE	ChEMBL + PubChem	Phase 4 (approved)	SLC10A1
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
URSODIOL	ChEMBL + PubChem	Phase 4 (approved)	SLC10A1
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
FLUVASTATIN	ChEMBL	Phase 4 (approved)	SLC10A1
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
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
PYRVINIUM	ChEMBL	Phase 4 (approved)	AGTR1
RIMONABANT	ChEMBL	Phase 4 (approved)	AGTR1
ROCURONIUM	ChEMBL	Phase 4 (approved)	AGTR1