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fimasartan
Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure.〔Chi, Y., Lee, H., Paik, S., Lee, J.H., Yoo, B.W., Kim, S.L., Hyun, K.T., and Kim, S.L. Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Fimasartan Following Single and Repeated Oral Administration in the Fasted and Fed States in Healthy Subjects. (2011). American Journal Cardiovascular Drugs.11(5): 335-46.〕 Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys.〔DeMello, W.C., and Frohlich, E.D. "Systemic Versus Local Renin Angiotensin Systems. An Overview." Renin Angiotensin System and Cardiovascular Disease. New York, NY: Humana, 2009.〕 Concurrent administration of fimasartan with diuretic hydrochlorothiazide has shown to be safe in clinical trials.〔Jeon, H., Soo Lim, K., Shin, K., Kim, J.W., Hyun Yoon, S., Cho, J., Shin, S., Jang, I., and Yu, K. (2012) "Assessment of the Drug-Drug Interactions between Fimasartan and Hydrochlorothiazide in Healthy Volunteers." Journal of Cardiovascular Pharmacology. 59(1): 84-91.〕 Fimasartan was approved for use in South Korea in September 9th, 2010 and is available under the brand name Kanarb through Boryung Pharmaceuticals, who are presently seeking worldwide partnership.〔“Fimasartan.” (2011) American Journal Cardiovascular Drugs. 11(4): 249-252〕
== Mechanism of action ==
Fimasartan acts on the kidney’s rennin-angiotensin cascade, which begins when renin release from the kidney causes the breakdown of angiotensinogen into angiotensin I. Angiotensin-converting enzyme (ACE) then catalyzes the reaction that forms angiotensin II, which acts on AT1 receptors on the blood vessels, heart, and kidneys.〔Burnier, M. Angiotensin ll Type 1 Receptor Blockers. (2001). Circulation. 103: 904-912.〕 On blood vessels, the AT1 receptor is coupled to an intracellular pathway that causes smooth muscle contraction (vasoconstriction) of blood vessels.〔Soo Shin, B., Kim ,T.H., Paik, S., Chi, Y., Joo, H., Tan, H., Choi, Y., Kim, M., and Yoo, S. Simultaneous Determination of Fimasartan, a Novel Antihypertensive Agent, and Its Active Metabolite in Rat Plasma by Liquid Chromatography–tandem Mass Spectrometry."(2011) Biomedical Chromatography. 25:1208-214.〕 In blocking the AT1 receptor, fimasartan inhibits vasoconstriction, favouring vasodilation. At the kidney and adrenal gland, AT1 blockage and prevention of aldosterone formation increase excretion of water and salt by the kidneys, which decreases overall blood volume.〔Klabunde, Richard E. Angiotensin Receptor Blockers (ARBs).CV Pharmacology. N.p., 15 Mar. 2007. Web. 28 Feb. 2013. 〕 At the heart, AT1 blockage decreases contractility and the stimulatory effects of the sympathetic nervous system.〔 Collectively, fimasartain leads to a reduction in blood pressure and alleviation of hypertensive symptoms.
ARBs like fimasartan have also shown to be protective against stroke, myocardial infarction, and heart failure.〔Neal, B., MacMahon, S., Chapman, N. Effects of ACE inhibitors, calcium antagonists, and other blood-pressure- lowering drugs: results of prospectively designed overviews of randomised trials. (2000) Blood Pressure Lowering Treatment Trialists’ Collaboration. 356:1955–1964.〕 Fimasartan has been shown to reduce cardiac hypertrophy, fibrosis, remodelling, and unnecessary cell proliferation via blockage of AT1 activation 〔〔Harada, K., Sugaya, T., Murakami, K., Yazaki, Y., and Komuro, I. Remodeling and Improved Survival After Myocardial Infarction Angiotensin II Type 1A Receptor Knockout Mice Display Less Left Ventricular. (1991).Circulation. 100: 2093-2099.〕 conceivably through decreased Endothelin 1 production, a result of AT1 activation.[Phillips, PA. Interaction between endothelin and angiotensin II. (1999). Clinical and Experimental Pharmacology and Physiology. 26(7): 517-518.〕 Fimastartan can also block TGF-β1 production (also AT1 dependent), which contributes to fibrosis and ventricular damage post-infarct.〔Sun, Y., Zhang, J.Q., Zhang, J., Ramires, F.J. Angiotensin II, transforming growth factor-beta1 and repair in the infarcted heart. (1998). Journal of Molecular and Cellular Cardiology. 30: 1559-1569.〕 After ARB administration, mice showed improved prognosis after a myocardial infarcation,〔 though further studies still need to be done to assess fimasartan’s specific effects on decreasing cardiovascular damage.]
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