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Details

Stereochemistry ACHIRAL
Molecular Formula 2C25H28N6O.2ClH.3H2O
Molecular Weight 984.027
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IRBESARTAN HYDROCHLORIDE SESQUIHYDRATE

SMILES

O.O.O.Cl.Cl.CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=C(C=CC=C4)C5=NN=NN5.CCCCC6=NC7(CCCC7)C(=O)N6CC8=CC=C(C=C8)C9=C(C=CC=C9)C%10=NN=NN%10

InChI

InChIKey=WCTHVUNSKZGLLG-UHFFFAOYSA-N
InChI=1S/2C25H28N6O.2ClH.3H2O/c2*1-2-3-10-22-26-25(15-6-7-16-25)24(32)31(22)17-18-11-13-19(14-12-18)20-8-4-5-9-21(20)23-27-29-30-28-23;;;;;/h2*4-5,8-9,11-14H,2-3,6-7,10,15-17H2,1H3,(H,27,28,29,30);2*1H;3*1H2

HIDE SMILES / InChI
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C25H28N6O
Molecular Weight 428.5294
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Irbesartan is an angiotensin receptor blocker (ARB) used mainly for the treatment of hypertension. It was developed by Sanofi Research (now part of Sanofi-Aventis). It is marketed under the trade names Aprovel, Karvea, and Avapro. AVAPRO is an angiotensin II receptor blocker (ARB) indicated for: • Treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. • Treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes, an elevated serum creatinine, and proteinuria. Irbesartan is a specific competitive antagonist of AT1 receptors with a much greater affinity (more than 8500-fold) for the AT1 receptor than for the AT2 receptor and no agonist activity.

CNS Activity

CNS Penetrant
2554
Curator's Comment: Studies in animals indicate that radiolabeled irbesartan weakly crosses the blood-brain barrier and placenta.

Originator

Approval Year

1997
172
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 1.1 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
AVAPRO

Approved Use

AVAPRO is an angiotensin II receptor blocker (ARB) indicated for: • Treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. (1.1) • Treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes, an elevated serum creatinine, and proteinuria

Launch Date

1997
Primary
Approved
8429
AVAPRO

Approved Use

AVAPRO is an angiotensin II receptor blocker (ARB) indicated for: • Treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. (1.1) • Treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes, an elevated serum creatinine, and proteinuria

Launch Date

1997
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
3.3 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.9 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
4.4 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
4.9 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5.6 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
900 mg 1 times / day multiple, oral
dose: 900 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5.3 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.04 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
150 mg 1 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1.9 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
19.8 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
20 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
31.9 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
32.6 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
34.2 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
900 mg 1 times / day multiple, oral
dose: 900 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
44.8 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
9.3 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
150 mg 1 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
9.7 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
11 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
14 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
15 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
14 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
14 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
900 mg 1 times / day multiple, oral
dose: 900 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
17 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
11 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
150 mg 1 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
16 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/9549663
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IRBESARTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
10%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020758s079lbl.pdf
unknown, unknown
 IRBESARTAN serum
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
900 mg 1 times / day multiple, oral
Highest studied dose
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9549663
Page: p.247, p.250
healthy, 20-45
n = 9
Health Status: healthy
Age Group: 20-45
Sex: M+F
Population Size: 9
Sources:
https://pubmed.ncbi.nlm.nih.gov/9549663
Page: p.247, p.250
Sources:
https://pubmed.ncbi.nlm.nih.gov/9549663
Page: p.247, p.250
300 mg 1 times / day multiple, oral (max)
Recommended
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Hypertension|diabetic nephropathy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.1
Disc. AE: Disorder fetal...
AEs leading to
discontinuation/dose reduction:
Disorder fetal
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.1
300 mg 1 times / day multiple, oral
Recommended
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.6
unhealthy
Health Status: unhealthy
Condition: Diabetic nephropathy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.6
Disc. AE: Hyperkalemia...
AEs leading to
discontinuation/dose reduction:
Hyperkalemia (2.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.6
AEs

AEs

AESignificanceDosePopulation
Disorder fetal Disc. AE
300 mg 1 times / day multiple, oral (max)
Recommended
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Hypertension|diabetic nephropathy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.1
Hyperkalemia 2.1%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.6
unhealthy
Health Status: unhealthy
Condition: Diabetic nephropathy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf
Page: p.6
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inhibitor
1587
substrate
1037

inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A1
110

CYP1A2
1524

CYP2A6
707

CYP2B6
810

CYP2E1
882

Kv4.3
16

P-gp
1461

BCRP
699

MRP2
383
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1925
 no [IC50 224 uM]
CYP1A2
1692
 no [IC50 483 uM]
CYP2A6
739
 no [IC50 >1000 uM]
CYP2D6
1891
 no [IC50 >1000 uM]
CYP2E1
970
 no [IC50 >1000 uM]
BCRP
773
 no
CYP1A1
218
 no
CYP2B6
1001
 no
MRP2
475
 no
P-gp
1650
 weak
CYP2C9
1819
 yes [IC50 172 uM]
Kv4.3
16
 yes [IC50 7.2 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1737
 yes
CYP2C9
1037
 yes
yes (co-administration study)
Comment: in clinical studies the consequences of concomitant irbesartan on the pharmacodynamics of warfarin were negligible
Page: 12.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:5959
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:5959
ChemicalBook
CB4454663
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB4454663
MolPort
MolPort-003-666-550
https://www.molport.com/shop/molecule-link/MolPort-003-666-550
MolPort
MolPort-006-167-687
https://www.molport.com/shop/molecule-link/MolPort-006-167-687
Selleck Chemicals
Irbesartan(Avapro)
http://www.selleckchem.com/products/Irbesartan(Avapro).html
ZINC
ZINC000003872931
http://zinc15.docking.org/substances/ZINC000003872931
eMolecules
32278040
https://www.emolecules.com/cgi-bin/more?vid=32278040
eMolecules
901986
https://www.emolecules.com/cgi-bin/more?vid=901986
PubMed

PubMed

TitleDatePubMed
Pharmacology of AT1-receptor blockers.
2001
The relationship between dose and antihypertensive effect for different AT1-receptor blockers.
2001
Clinical comparative trials of angiotensin II type 1 (AT1)-receptor blockers.
2001
[Current treatment of diabetic nephropathy in patients with type II diabetes mellitus. Most recent progress].
2001
Drug interactions with irbesartan.
2001
[Choosing the dose of aprovel (irbesartan) in patients with chronic heart insufficiency].
2001
Hypertension and diabetes: the scope of the problem.
2001
Clinical differences among angiotensin II receptor antagonists.
2001
Perindopril/indapamide 2/0.625 mg/day: a review of its place in the management of hypertension.
2001
Different types of antagonism by losartan and irbesartan on the effects of angiotensin II and its degradation products in rabbit arteries.
2001 Apr
Acute oliguric renal failure associated with angiotensin II receptor antagonists.
2001 Aug
Hemodynamic effects of the angiotensin II receptor antagonist irbesartan in patients with cirrhosis and portal hypertension.
2001 Aug
[Treatment of hypertension in patients with type 2 diabetes. Sartan also protects the kidneys].
2001 Aug 9
Irbesartan slows the development of diabetic nephropathy by up to 70% in hypertensive diabetic patients.
2001 Aug-Sep
Irbesartan prevents the progression of kidney disease or death in patients with type 2 diabetes and high blood pressure.
2001 Aug-Sep
The protective effect of blocking angiotensin in both type I and type II diabetics with nephropathy.
2001 Dec
AT(2) receptor-mediated vasodilation in the heart: effect of myocardial infarction.
2001 Dec
Irbesartan normalises the deficiency in glomerular nephrin expression in a model of diabetes and hypertension.
2001 Jul
Angiotensin receptor blockers -- finally the evidence is coming in: IDNT and RENAAL.
2001 Jul
Insurmountable AT(1) receptor antagonism: the need for different antagonist binding states of the receptor.
2001 Jul
New stuff about the diabetic kidney.
2001 Jul-Aug
[Effects of inhibitors of angiotensin-converting enzyme combined with antagonists of angiotensin II receptors on endothelial function in patients with chronic cardiac insufficiency].
2001 Mar-Apr
Drug companies should not have the final say in the design of clinical trials.
2001 Nov
Influence of irbesartan and enalapril on changes of renal function associated with the established phase of l-NAME hypertension.
2001 Nov
Irbesartan, an angiotensin type 1 receptor inhibitor, regulates the vascular oxidative state in patients with coronary artery disease.
2001 Nov 15
[Clinical study of the month. Nephroprotective role of angiotensin II receptor antagonists in type 2 diabetes: results of the IDNT and RENAAL trials].
2001 Oct
Selective angiotensin II receptor antagonism reduces insulin resistance in obese Zucker rats.
2001 Oct
Relation between clinical and therapeutic variables and quality of life in hypertension.
2001 Oct
Comparative effects of losartan and irbesartan on serum uric acid in hypertensive patients with hyperuricaemia and gout.
2001 Oct
Treatment with irbesartan or atenolol improves endothelial function in essential hypertension.
2001 Oct
Angiotensin converting enzyme gene polymorphism predicts blood pressure response to angiotensin II receptor type 1 antagonist treatment in hypertensive patients.
2001 Oct
A clinical trial in type 2 diabetic nephropathy.
2001 Oct
Angiotensin II receptor blockers and nephropathy trials.
2001 Oct
pK(a) determination of angiotensin II receptor antagonists (ARA II) by spectrofluorimetry.
2001 Oct
[Effect of irbesartan on the development of diabetic nephropathy in patients with type 2 diabetes].
2001 Oct 1
Renal protection by angiotensin II receptor antagonists in patients with type 2 diabetes.
2001 Oct 15
[Irbesartan in hypertension. A plus for therapy compliance].
2001 Oct 4
Vasoconstrictor effect of the angiotensin-converting enzyme-resistant, chymase-specific substrate [Pro(11)(D)-Ala(12)] angiotensin I in human dorsal hand veins: in vivo demonstration of non-ace production of angiotensin II in humans.
2001 Oct 9
Adenovirus-mediated overexpression and stimulation of the human angiotensin II type 2 receptor in porcine cardiac fibroblasts does not modulate proliferation, collagen I mRNA expression and ERK1/ERK2 activity, but inhibits protein tyrosine phosphatases.
2001 Sep
Effect of angiotensin II type 1 receptor blockade on experimental hepatic fibrogenesis.
2001 Sep
Differentiation in the angiotensin II receptor 1 blocker class on autonomic function.
2001 Sep
Angiotensin II-induced apoptosis in rat cardiomyocyte culture: a possible role of AT1 and AT2 receptors.
2001 Sep
The pharmacokinetics and pharmacodynamics of irbesartan in heart failure.
2001 Sep
Irbesartan effects on renal function in patients with renal impairment and hypertension: a drug-withdrawal study.
2001 Sep
Impact of the renin-angiotensin system on cerebral perfusion following subarachnoid haemorrhage in the rat.
2001 Sep 1
The effect of irbesartan on the development of diabetic nephropathy in patients with type 2 diabetes.
2001 Sep 20
Renoprotective effect of the angiotensin-receptor antagonist irbesartan in patients with nephropathy due to type 2 diabetes.
2001 Sep 20
Comparative efficacy of olmesartan, losartan, valsartan, and irbesartan in the control of essential hypertension.
2001 Sep-Oct
Vasoconstriction is determined by interstitial rather than circulating angiotensin II.
2002 Jan
Angiotensin peptides modulate bradykinin levels in the interstitium of the dog heart in vivo.
2002 Jan
Patents

Patents

JP2001089393A
6
JP2005041875A
12
JP2006513266A
25
JP2006515566A
3
JP2010053048A
3
JP2011510003A
48

Sample Use Guides

In Vivo Use Guide
Usual Adult Dose for Hypertension Initial dose: 150 mg orally once a day Maximum dose: 300 mg orally once a day Usual Adult Dose for Diabetic Nephropathy Target maintenance dose: 300 mg orally once a day Use: Treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria (greater than 300 mg/day) in patients with type 2 diabetes and hypertension.
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment: Contraction responses to increasing concentrations of Ang I (1 nM-1 uM) were evaluated in organ baths in the presence of captopril (10 uM-1 mM) with or without a chymase inhibitor (1 uM soybean trypsin inhibitor), or irbesartan (0.1 nM-uM), in internal mammary arteries from 25 patients undergoing coronary bypass surgery.
0.1 uM irbesartan completely blocked the maximum response to Ang I (from 45.8 +/- 6.7% to 1.9 +/- 1.9%, p < 0.001)
Substance Class Chemical
Created
by admin
on Sat Dec 16 18:29:03 GMT 2023
Edited
by admin
on Sat Dec 16 18:29:03 GMT 2023
Record UNII
B4WCH9U6Q3
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
IRBESARTAN HYDROCHLORIDE SESQUIHYDRATE
Common Name English
1,3-DIAZASPIRO(4.4)NON-1-EN-4-ONE, 2-BUTYL-3-((2'-(1H-TETRAZOL-5-YL)(1,1'-BIPHENYL)-4-YL)METHYL)-, MONOHYDROCHLORIDE, HYDRATE (2:3)
Systematic Name English
1,3-DIAZASPIRO(4.4)NON-1-EN-4-ONE, 2-BUTYL-3-((2'-(2H-TETRAZOL-5-YL)(1,1'-BIPHENYL)-4-YL)METHYL)-, HYDROCHLORIDE, HYDRATE (2:2:3)
Systematic Name English
Code System Code Type Description
CAS
874657-02-0
Created by admin on Sat Dec 16 18:29:03 GMT 2023 , Edited by admin on Sat Dec 16 18:29:03 GMT 2023
PRIMARY
FDA UNII
B4WCH9U6Q3
Created by admin on Sat Dec 16 18:29:03 GMT 2023 , Edited by admin on Sat Dec 16 18:29:03 GMT 2023
PRIMARY
PUBCHEM
162625107
Created by admin on Sat Dec 16 18:29:03 GMT 2023 , Edited by admin on Sat Dec 16 18:29:03 GMT 2023
PRIMARY
SMS_ID
300000000781
Created by admin on Sat Dec 16 18:29:03 GMT 2023 , Edited by admin on Sat Dec 16 18:29:03 GMT 2023
PRIMARY
Related Record Type Details
Structure of IRBESARTAN
PARENT -> SALT/SOLVATE
Structure of IRBESARTAN HYDROCHLORIDE
ANHYDROUS->SOLVATE
NIH
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