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Fimasartan: A New Angiotensin Receptor Blocker

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Abstract

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.

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Acknowledgments

Drs. B.H. Oh and H.Y. Lee each contributed to writing the manuscript and figure creation. Drs. B.H. Oh and H.Y. Lee contributed equally to the data collection, data interpretation, and literature search, and were involved in all stages of manuscript development.

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Authors and Affiliations

  1. Seoul National University Hospital, Seoul, Republic of Korea

    Hae-Young Lee & Byung-Hee Oh

  2. Department of Internal Medicine, Seoul National University College of Medicine, 101 Daehak-Ro, Chongno-gu, Seoul, 03080, Korea

    Byung-Hee Oh

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  1. Hae-Young Lee
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Correspondence to Byung-Hee Oh.

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No external funding was used in the preparation of this manuscript.

Conflict of interest

Dr. B.H. Oh has been involved in the study design of fimasartan phase II and III studies and received consulting fees from Boryung Pharmaceuticals for this. Dr. H.Y. Lee has received a basic research grant from Boryung Pharmaceuticals. Drs. B.H. Oh and H.Y. Lee have given several lectures including discussion of fimasartan in scientific sessions. Drs. B.H. Oh and H.Y. Lee declare that they have no other conflicts of interest that might be relevant to the contents of this manuscript.

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Lee, HY., Oh, BH. Fimasartan: A New Angiotensin Receptor Blocker. Drugs 76, 1015–1022 (2016). https://doi.org/10.1007/s40265-016-0592-1

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