Fimasartan

Synonym(s):2-Butyl-1,6-dihydro-N,N,4-trimethyl-6-oxo-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-5-pyrimidineethanethioamide;2-n-Butyl-5-dimethylaminothiocarbonylmethyl-6-methyl-3-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3H)-one;BR-A657;BR-A-657

CAS NO.：247257-48-3
Empirical Formula: C27H31N7OS
Molecular Weight: 501.65
MDL number: MFCD13194795
EINECS: 207-981-6
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-19 20:33:22

What is Fimasartan?

Description

Fimasartan is an angiotensin II receptor antagonist (ARB) drug employed in the treatment of both hypertension and heart failure. It has been found to be safe when administered with hydrochlorothiazide (a diuretic) in clinical trials. Fimasartan was initially approved September 9th, 2010 in South Korea and is marketed under the brand name Kanarb by Boryung Pharmaceuticals.

The Uses of Fimasartan

Fimasartan is a new angiotensin II receptor blocker antagonist and also functions as an antihypertensive agent.

Definition

ChEBI: Fimasartan is a member of biphenyls.

Biological Activity

Fimasartan (Kanarb) is a non-peptide angiotensin II receptor antagonist (ARB) with noncompetitive, insurmountable binding with the AT1 receptor. It is used for the treatment of hypertension and heart failure.

Mechanism of action

Angiotensin II activates AR1 leading to vasoconstriction and increased noradrenaline release which further increases vasoconstriction via action at α1-adrenergic receptors. It also stimulates secretion of aldosterone which acts to increase sodium and water reabsorption in the renal tubules. Fimasartan bind to and antagonizes AR1 preventing vasoconstriction and reducing aldosterone secretion to increase natriuresis leading to a reduction in blood volume. Together these effects produce an anti-hypertensive effect.

Properties of Fimasartan

Melting point:	>155°C (dec.)
Boiling point:	693.0±65.0 °C(Predicted)
Density	1.25
storage temp.	2-8°C
solubility	DMSO (Slightly), Methanol (Slightly)
form	Solid
pka	4.16±0.10(Predicted)
color	White to Off-White

Safety information for Fimasartan

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral
Precautionary Statement Codes	P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.