Repositioning Candidate Details

Candidate ID: R0377
Source ID: DB01029
Source Type: approved; investigational
Compound Type: small molecule
Compound Name: Irbesartan
Synonyms: 2-butyl-3-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1,3-diazaspiro[4.4]non-1-en-4-one; Irbesartan
Molecular Formula: C25H28N6O
SMILES: CCCCC1=NC2(CCCC2)C(=O)N1CC1=CC=C(C=C1)C1=CC=CC=C1C1=NNN=N1
Structure:
DrugBank Description: Irbesartan is an angiotensin receptor blocker (ARB) indicated to treat hypertension or diabetic nephropathy. It can also be used as part of a combination product with for patients not well controlled or not expected to be well controlled on monotherapy. Unlike angiotensin converting enzyme inhibitors, ARBs are not associated with a dry cough. Irbesartan was granted FDA approval on 30 September 1997.
CAS Number: 138402-11-6
Molecular Weight: 428.5294
DrugBank Indication: Irbesartan is indicated to treat hypertension and diabetic nephropathy in hypertensive patients with type 2 diabetes, elevated serum creatinine, and proteinuria. A combination product with hydrochlorothiazide is indicated for hypertension in patients with uncontrolled hypertension with monotherapy or first line in patients not expected to be well controlled with monotherapy.
DrugBank Pharmacology: Irbesartan is an angiotensin receptor blocker used to treat hypertension and diabetic nephropathy. It has a long duration of action as it is usually taken once daily and a wide therapeutic index as doses may be as low as 150mg daily but doses of 900mg/day were well tolerated in healthy human subjects.
DrugBank MoA: Irbesartan prevents angiotensin II binding to the AT<sub>1</sub> receptor in tissues like vascular smooth muscle and the adrenal gland. Irbesartan and its active metabolite bind the AT<sub>1</sub> receptor with 8500 times more affinity than they bind to the AT<sub>2</sub> receptor. Irbesartan's prevention of angiotensin II binding causes vascular smooth muscle relaxation and prevents the secretion of aldosterone, lowering blood pressure. Angiotensin II would otherwise bind to the AT<sub>1</sub> receptor, inducing vasoconstriction and aldosterone secretion, raising blood pressure.
Targets: Type-1 angiotensin II receptor antagonist; Transcription factor AP-1 other/unknown
Inclusion Criteria: Target associated