Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H28N6O |
Molecular Weight | 428.5294 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=C(C=CC=C4)C5=NN=NN5
InChI
InChIKey=YOSHYTLCDANDAN-UHFFFAOYSA-N
InChI=1S/C25H28N6O/c1-2-3-10-22-26-25(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/h4-5,8-9,11-14H,2-3,6-7,10,15-17H2,1H3,(H,27,28,29,30)
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 |
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.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
1.1 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | AVAPRO Approved UseAVAPRO 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 Date1997 |
|||
Primary | AVAPRO Approved UseAVAPRO 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 Date1997 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10% |
unknown, unknown |
IRBESARTAN serum | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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: Page: p.247, p.250 |
healthy, 20-45 n = 9 Health Status: healthy Age Group: 20-45 Sex: M+F Population Size: 9 Sources: 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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Hypertension|diabetic nephropathy Sources: Page: p.1 |
Disc. AE: Disorder fetal... AEs leading to discontinuation/dose reduction: Disorder fetal Sources: 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: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Diabetic nephropathy Sources: Page: p.6 |
Disc. AE: Hyperkalemia... AEs leading to discontinuation/dose reduction: Hyperkalemia (2.1%) Sources: Page: p.6 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Hypertension|diabetic nephropathy Sources: 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: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Diabetic nephropathy Sources: Page: p.6 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/10877007/ Page: - |
no [IC50 224 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10877007/ Page: - |
no [IC50 483 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10877007/ Page: - |
no [IC50 >1000 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10877007/ Page: - |
no [IC50 >1000 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10877007/ Page: - |
no [IC50 >1000 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/20222053/ Page: - |
no | |||
Page: 13.0 |
no | |||
Page: 13.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/20222053/ Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/20222053/ Page: - |
weak | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10877007/ Page: - |
yes [IC50 172 uM] | |||
Sources: https://jpet.aspetjournals.org/content/304/2/862 Page: - |
yes [IC50 7.2 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 12.0 |
yes | |||
Page: 12.0 |
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
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://jpet.aspetjournals.org/content/304/2/862 Page: - |
PubMed
Title | Date | PubMed |
---|---|---|
End-stage renal failure after irbesartan prescription in a diabetic patient with previously stable chronic renal insufficiency. | 2000 Nov |
|
The comparative pharmacology of angiotensin II receptor antagonists. | 2001 |
|
Irbesartan achieves consistent and effective use over 1 year. | 2001 Apr-May |
|
Irbesartan prevents the progression of kidney disease or death in patients with type 2 diabetes and high blood pressure. | 2001 Aug-Sep |
|
p38 Map kinase regulates vascular smooth muscle cell collagen synthesis by angiotensin II in SHR but not in WKY. | 2001 Feb |
|
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 |
|
Effect of the AT1-receptor antagonists losartan, irbesartan, and telmisartan on angiotensin II-induced facilitation of sympathetic neurotransmission in the rat mesenteric artery. | 2001 Jul |
|
Regression of left ventricular hypertrophy in human hypertension with irbesartan. | 2001 Jun |
|
Apoptosis and changes in contractile protein pattern in the skeletal muscle in heart failure. | 2001 Mar |
|
Headache, hypertension, and irbesartan therapy. | 2001 Mar 12 |
|
Beneficial effects on skeletal muscle of the angiotensin II type 1 receptor blocker irbesartan in experimental heart failure. | 2001 May 1 |
|
[Milestone studies provide evidence: sartans have a nephroprotective effect. Evidence is clear]. | 2001 May 31 |
|
Drug companies should not have the final say in the design of clinical trials. | 2001 Nov |
|
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 |
|
[Effect of irbesartan on the development of diabetic nephropathy in patients with type 2 diabetes]. | 2001 Oct 1 |
|
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 |
|
Comparative efficacy of olmesartan, losartan, valsartan, and irbesartan in the control of essential hypertension. | 2001 Sep-Oct |
|
Angiotensin peptides modulate bradykinin levels in the interstitium of the dog heart in vivo. | 2002 Jan |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/irbesartan.html
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12548077
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
Edited
Fri Dec 15 15:40:25 GMT 2023
by
admin
on
Fri Dec 15 15:40:25 GMT 2023
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Record UNII |
J0E2756Z7N
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Record Status |
Validated (UNII)
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Record Version |
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-
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Classification Tree | Code System | Code | ||
---|---|---|---|---|
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EMA ASSESSMENT REPORTS |
IFIRMACOMBI (AUTHORIZED: HYPERTENSION)
Created by
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WHO-ATC |
C09DA04
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EMA ASSESSMENT REPORTS |
SARBEVEL (AUTHORIZED: HYPERTENSION)
Created by
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EMA ASSESSMENT REPORTS |
IRBESARTAN HYDROCHLOROTHIAZIDE ZENTIVA (AUTHORIZED: HYPERTENSION)
Created by
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WHO-ATC |
C09DB05
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EMA ASSESSMENT REPORTS |
KARVEA (AUTHORIZED: HYPERTENSION)
Created by
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FDA ORPHAN DRUG |
496715
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EMA ASSESSMENT REPORTS |
IRBESARTAN TEVA (AUTHORIZED: HYPERTENSION)
Created by
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EMA ASSESSMENT REPORTS |
IRBESARTAN ZENTIVA (AUTHORIZED: HYPERTENSION)
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EMA ASSESSMENT REPORTS |
COAPROVEL (AUTHORIZED: HYPERTENSION)
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NCI_THESAURUS |
C66930
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NDF-RT |
N0000175561
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NDF-RT |
N0000000070
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EMA ASSESSMENT REPORTS |
IRBESARTAN BMS (WITHDRAWN: HYPERTENSION)
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EMA ASSESSMENT REPORTS |
IRBESARTAN HYDROCHLOROTHIAZIDE BMS (WITHDRAWN: HYPERTENSION)
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EMA ASSESSMENT REPORTS |
KARVEZIDE (AUTHORIZED: HYPERTENSION)
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WHO-VATC |
QC09DB05
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WHO-VATC |
QC09CA04
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WHO-ATC |
C09CA04
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WHO-VATC |
QC09DA04
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EMA ASSESSMENT REPORTS |
IRBESARTAN HYDROCHLOROTHIAZIDE TEVA (AUTHORIZED: HYPERTENSION)
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LIVERTOX |
NBK548450
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DB01029
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IRBESARTAN
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589
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m6397
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5959
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Irbesartan
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758696
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CHEMBL1513
Created by
admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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8215
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admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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1347700
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admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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C081309
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admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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7229
Created by
admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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J0E2756Z7N
Created by
admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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138402-11-6
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admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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SUB08293MIG
Created by
admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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100000085443
Created by
admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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1481
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C29130
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II-21
Created by
admin on Fri Dec 15 15:40:25 GMT 2023 , Edited by admin on Fri Dec 15 15:40:25 GMT 2023
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Related Record | Type | Details | ||
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TRANSPORTER -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT |
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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TARGET -> INHIBITOR |
IC50
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BINDER->LIGAND |
BINDING
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
USP
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
FECAL; PLASMA; URINE
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PARENT -> METABOLITE |
approximately 15% of the urinary radioactivity.
PLASMA; URINE
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METABOLITE -> PARENT |
about 5% of the plasma radioactivity
PLASMA; URINE
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METABOLITE -> PARENT |
approximately 25% of the urinary radioactivity
MAJOR
URINE
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METABOLITE -> PARENT |
M5+M6+M7 is 24.2(iv) and 25.3 (oral) in feces. Plasma content should be very low
URINE
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METABOLITE -> PARENT |
Feces low and plasma negligible
URINE
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METABOLITE -> PARENT |
Low in feces and negligible in plasma
URINE
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METABOLITE -> PARENT |
M5+M6+M7 is 24.2(iv) and 25.3 (oral) in feces. Plasma content should be very low
URINE
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PARENT -> METABOLITE |
about 9% of the plasma radioactivity at 6 hr; was found to be more than 1000-fold less potent than irbesartan as an inhibitor
MAJOR
PLASMA
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Related Record | Type | Details | ||
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IMPURITY GENOTOXIC->PARENT |
NDMA is an organic chemical that is in a family of potent carcinogens.
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
Priority toxic pollutant.
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IMPURITY -> PARENT |
Probable human carcinogen.
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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