Fimasartan (BR-A-657) is an orally active, highly potent angiotensin II receptor AT1 (AGTR1) antagonist (blocker) that selectively blocks AngII-, but not KCl- or noradrenaline-, induced contraction of rabbit thoracic aortic rings (IC50 = 0.42 nM) with 615-fold higher AT1 affinity than losartan (IC50 = 0.13 nM vs. 80 nM against 0.05 nM AngII for binding rat adrenal cortex). Fimasartan significantly decreases mean arterial blood pressure with rapid onset (in 0.5 h) in spontaneously hypertensive rats (Emax of 75% reduction, 5-24 hr post 10 mg/kg p.o.) and is ~19-fold more effective than losartan against AngII (100 ng/kg i.v.)-induced pressor response in rats in vivo (ED50 = 18 ng/kg vs. 336 ng/kg i.v.).
Orally active, highly potent angiotensin II receptor AT1 (AGTR1) antagonist with superior in vivo antihypertensive efficacy than Losartan.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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International journal of cardiology, 168(3), 2851-2859 (2013-05-07)
The aim of this study was to investigate the cardioprotective effect of fimasartan, a newly developed angiotensin II receptor type I blocker (ARB), against myocardial ischemia/reperfusion (I/R) injury and to identify the mechanism by which it reduces mitochondrial damage. Fimasartan
Xenobiotica; the fate of foreign compounds in biological systems, 44(10), 913-925 (2014-05-03)
1. The objectives of this study were to evaluate the pharmacokinetics and metabolism of fimasartan in rats. 2. Unlabeled fimasartan or radiolabeled [(14)C]fimasartan was dosed by intravenous injection or oral administration to rats. Concentrations of unlabeled fimasartan in the biological
The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology, 17(1), 99-109 (2013-02-27)
The aim of this study was to determine whether fimasartan, a newly developed AT(1) receptor blocker, can affect the CA release in the isolated perfused model of the adrenal medulla of spontaneously hypertensive rats (SHRs). Fimasartan (5~50 µM) perfused into
The discovery, in vitro and in vivo studies of the highly potent AT(1) antagonist 12a (BR-A-657, Fimasartan) antagonists are presented. A series of pyrimidin-4(3H)-one derivatives as losartan analogue were synthesized and evaluated for a novel class of AT(1) receptor antagonists.
Expert opinion on drug metabolism & toxicology, 14(5), 533-541 (2018-04-21)
Fimasartan is the ninth and latest Angiotensin Receptor Blockers for the treatment of hypertension. Fimasartan is a derivative of losartan in which the imidazole ring has been replaced. It provides a selective type 1 angiotensin II receptor antagonist effect with
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