Fimasartan: A New Angiotensin Receptor Blocker
- 424 Downloads
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.
KeywordsLosartan Amlodipine Valsartan Blood Pressure Reduction Telmisartan
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.
Compliance with Ethical Standards
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.
- 15.Lee JY, Choi YJ, Oh SJ, Chi YH, Paik SH, Lee KH, et al. Characterization of fimasartan metabolites in human liver microsomes and human plasma. Xenobiotica. 2015;46(1):50–1.Google Scholar
- 21.Gu N, Kim BH, Lim KS, Kim SE, Nam WS, Yoon SH, et al. The effect of fimasartan, an angiotensin receptor type 1 blocker, on the pharmacokinetics and pharmacodynamics of warfarin in healthy Korean male volunteers: a one-sequence, two-period crossover clinical trial. Clin Ther. 2012;34(7):1592–600.CrossRefPubMedGoogle Scholar
- 24.Lee H, Yang HM, Lee HY, Kim JJ, Choi DJ, Seung KB, et al. Efficacy and tolerability of once-daily oral fimasartan 20 to 240 mg/d in Korean patients with hypertension: findings from two phase II, randomized, double-blind, placebo-controlled studies. Clin Ther. 2012;34(6):1273–89.CrossRefPubMedGoogle Scholar
- 25.Lee SE, Kim YJ, Lee HY, Yang HM, Park CG, Kim JJ, et al. Efficacy and tolerability of fimasartan, a new angiotensin receptor blocker, compared with losartan (50/100 mg): a 12-week, phase III, multicenter, prospective, randomized, double-blind, parallel-group, dose escalation clinical trial with an optional 12-week extension phase in adult Korean patients with mild-to-moderate hypertension. Clin Ther. 2012;34(3):552–68, 68 e1–9.Google Scholar
- 26.Lee H, Kim KS, Chae SC, Jeong MH, Kim DS, Oh BH. Ambulatory blood pressure response to once-daily fimasartan: an 8-week, multicenter, randomized, double-blind, active-comparator, parallel-group study in Korean patients with mild to moderate essential hypertension. Clin Ther. 2013;35(9):1337–49.CrossRefPubMedGoogle Scholar
- 36.Lee JY, Lee CW, Kim WJ, Ahn JM, Park DW, Kang SJ, et al. Antiatherosclerotic effects of the novel angiotensin receptor antagonist fimasartan on plaque progression and stability in a rabbit model: a double-blind placebo-controlled trial. J Cardiovasc Pharmacol. 2013;62(2):229–36.CrossRefPubMedGoogle Scholar
- 42.Lou M, Blume A, Zhao Y, Gohlke P, Deuschl G, Herdegen T, et al. Sustained blockade of brain AT1 receptors before and after focal cerebral ischemia alleviates neurologic deficits and reduces neuronal injury, apoptosis, and inflammatory responses in the rat. J Cereb Blood Flow Metab. 2004;24(5):536–47.CrossRefPubMedGoogle Scholar
- 45.Diener HC, Sacco RL, Yusuf S, Cotton D, Ounpuu S, Lawton WA, et al. Effects of aspirin plus extended-release dipyridamole versus clopidogrel and telmisartan on disability and cognitive function after recurrent stroke in patients with ischaemic stroke in the Prevention Regimen for Effectively Avoiding Second Strokes (PRoFESS) trial: a double-blind, active and placebo-controlled study. Lancet Neurol. 2008;7(10):875–84.CrossRefPubMedPubMedCentralGoogle Scholar
- 47.Kim C KM, Kang DR, Kim JY, Park JB, On behalf of the K-MetS study investigators. The efficacy of fimasartan for cardiovascular events and metabolic syndrome (K-MetS Study): rationale, design and participant characteristics. Pulse (Basel). 2013;1(1):177–85.Google Scholar