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Fimasartan Sale

(Synonyms: 非马沙坦; BR-A-657) 目录号 : GC36046

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.

Fimasartan Chemical Structure

Cas No.:247257-48-3

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产品描述

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.

Fimasartan is a selective AT1 receptor antagonist. The concentration that inhibits the binding of [125I]Ang II to the AT1 receptor from rat adrenal cortex by 50% (IC50) is 0.13 nM. Fimasartan shows superior inhibitory activity in the contraction of isolated rabbit thoracic aorta compared to other ARBs such as losartan and candesartan[1]. Fimasartan potently attenuates myocardial apoptotic death in reperfused rat heart and H9c2 cells. Fimasartan could attenuate mitochondrial damage which is associated with minimizing the reduction in Bcl-2 and connected with the reduction in p53 and activation of Akt and GSK-3β, and inhibiting mitochondrial Ca2+ overload by suppressing the ICa,L and MCU[2].

In various animal models including renal hypertensive rats, spontaneously hypertensive rats and Beagle dogs, fimasartan effectively reduces blood pressure in a dose-dependent manner following single or repeated oral and intravenous administration. Fimasartan does not affect general behavior, respiratory rate or tidal volume in experimental animals, and shows no adverse findings in the human ether-a-go-go-related gene (hERG) test or monkey telemetry study. A number of general toxicity, carcinogenic toxicity, genetic toxicity, and developmental toxicity studies given either orally or intravenously in various species including mice, rats, monkeys and dogs are conducted and these preclinical results demonstrate the safety and tolerability of fimasartan for long-term clinical use and offer sufficient safety margins to support the expected human therapeutic dose. Fimasartan is rapidly absorbed following oral administration with the time to peak plasma concentration (Tmax) ranging 0.5-3 h and the terminal half-life (t1/2) being 5-16 h at doses of 20 to 480 mg in healthy subjects. Similar results are obtained in patients with hypertension, i.e., Tmax ranges 0.5-1.3 h and t1/2 is 7-10 h following fimasartan administration at doses 20-180 mg in the subsequent phase II study. The urinary excretion of fimasartan is low, with the overall urinary excretion of unchanged drug over the first 24 h after dosing being less than 3% of the administered dose. Fimasartan undergoes nonrenal elimination with minimal metabolism[1]. Fimasartan treatment before myocardial ischemia significantly attenuates reperfusion injury and apoptotic changes, possibly by suppressing mitochondrial damage during reperfusion[2]. In various preclinical studies, including aortic balloon injury, myocardial infarct ischemia/reperfusion, doxorubicin cardiotoxicity, and ischemic stroke models, fimasartan shows anti-inflammatory and organ-protecting effects[3].

[1] Kim JH, et al. Arch Pharm Res. 2012, 35(7):1123-6. [2] Han J, et al. Int J Cardiol. 2013, 168(3):2851-9. [3] Lee HY, et al. Drugs. 2016, 76(10):1015-22.

Chemical Properties

Cas No. 247257-48-3 SDF
别名 非马沙坦; BR-A-657
Canonical SMILES O=C1N(C(CCCC)=NC(C)=C1CC(N(C)C)=S)CC2=CC=C(C3=C(C4=NN=NN4)C=CC=C3)C=C2
分子式 C27H31N7OS 分子量 501.65
溶解度 DMSO: ≥ 49 mg/mL (97.68 mM) 储存条件 Store at -20°C
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1 mM 1.9934 mL 9.9671 mL 19.9342 mL
5 mM 0.3987 mL 1.9934 mL 3.9868 mL
10 mM 0.1993 mL 0.9967 mL 1.9934 mL
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Research Update

Fimasartan

Am J Cardiovasc Drugs 2011 Aug 1;11(4):249-52.PMID:21740078DOI:10.2165/11533640-000000000-00000.

Fimasartan (BR-A-657; BR-A-657-K; Kanarb®), an angiotensin II receptor antagonist with selectivity for the AT(1) receptor subtype, is being developed by Boryung Pharmaceutical as an oral treatment for hypertension. Fimasartan has been approved for use in patients with hypertension in South Korea and has been evaluated in three phase III clinical trials (i.e. NCT00922480, NCT01135212, and NCT01258673). This review discusses the development history and scientific profile of this new compound. This summary has been extracted from Wolters Kluwer's Adis R&D Insight drug pipeline database. Adis R&D Insight tracks and evaluates drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch.

Fimasartan: A New Angiotensin Receptor Blocker

Drugs 2016 Jul;76(10):1015-22.PMID:27272555DOI:10.1007/s40265-016-0592-1.

Fimasartan is the ninth, and most recent, angiotensin II receptor antagonist approved as an antihypertensive agent. Fimasartan, a pyrimidin-4(3H)-one derivative of losartan with the imidazole ring replaced, which enables higher potency and longer duration than losartan. Fecal elimination and biliary excretion are the predominant elimination pathways of Fimasartan and the urinary excretion was found to be less than 3 % 24 h after administration. Fimasartan is primarily catabolized by cytochrome P450 isoform 3A and no significant drug interaction was observed when used in combination with hydrochlorothiazide, amlodipine, warfarin, or digoxin. Fimasartan at a dosage range of 60-120 mg once daily showed an antihypertensive effect over 24 h. In a large, population-based observational study, Fimasartan showed an excellent safety profile. Anti-inflammatory and organ-protecting effects of Fimasartan have been shown in various preclinical studies, including aortic balloon injury, myocardial infarct ischemia/reperfusion, doxorubicin cardiotoxicity, and ischemic stroke models.

Fimasartan: A new armament to fight hypertension

J Family Med Prim Care 2019 Jul;8(7):2184-2188.PMID:31463228DOI:10.4103/jfmpc.jfmpc_300_19.

Hypertension is a major public health problem of modern era. Fimasartan is a new Angiotensin Receptor Blocker approved for treatment of hypertension. It is more potent and longer acting angiotensin receptor blocker with effects lasting over 24 hours. Many clinical studies have affirmed its role in pharmacotherapy of hypertension. Further, it is renoprotective and has proven beneficial in diabetes also. This article briefly discusses the pharmacology and clinical evidence with Fimasartan with a short summary of previous angiotensin receptor blockers.

PK/PD evaluation of Fimasartan for the treatment of hypertension Current evidences and future perspectives

Expert Opin Drug Metab Toxicol 2018 May;14(5):533-541.PMID:29676941DOI:10.1080/17425255.2018.1468435.

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 noncompetitive, in surmountable binding. Fimasartan is rapidly absorbed following oral administration with an oral bioavailability of 18.6 ± 7.2%. Fimasartan is relatively stable in terms of metabolism and more than 90% of circulating Fimasartan moieties in the plasma are in the parent form; fecal elimination and biliary excretion are the predominant elimination pathways of Fimasartan. Areas covered: We reviewed data from clinical trials that investigated safety and efficacy of Fimasartan in hypertension. Expert opinion: Fimasartan proved good efficacy in blood pressure reduction. In large clinical studies,Fimasartan showed an excellent safety profile and when combined with hydrochlorothiazide oram lodipine, it showed a better effect on controlling blood pressure than monotherapy. Fimasartan 60-120 mg once daily has also shown an antihypertensive effect over 24-h. Moreover, preclinical studies demonstrated organ-protecting effects of Fimasartan. These results make Fimasartan an attractive candidate for the treatment of hypertension. However, it remains to test the benefit of using Fimasartan on clinical outcomes.

Fimasartan, a novel angiotensin II receptor antagonist

Arch Pharm Res 2012 Jul;35(7):1123-6.PMID:22864732DOI:10.1007/s12272-012-0700-z.

Fimasartan (Kanarb®), an angiotensin II receptor antagonist with selectivity for the AT1 receptor subtype, is a pyrimidinone-related heterocyclic compound that was developed by Boryung Pharm. Co., Ltd. Among numerous synthetic derivatives, Fimasartan was chosen as a new drug candidate through in vitro and in vivo screening studies. Pharmadynamic-pharmacokinetic properties and safety profiles were determined in a series of nonclinical and clinical studies. Fimasartan is a new angiotensin receptor blocker, and the first new molecular entity acting on cardiovascular system approved by Korean Food and Drug Administration for the treatment of essential hypertension in September 2010. Further development process for combination therapy and overseas registration is currently ongoing.