Fimasartan: A New Angiotensin Receptor Blocker

Lee, Hae Young; Oh, Byung Hee

doi:10.1007/s40265-016-0592-1

Cited by 27 publications

(22 citation statements)

References 44 publications

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“…Another challenge we faced is whether the findings in the present study were ARB class effects or fimasartan‐specific effects. Since its launch in 2011, use of 60 to 120 mg/day of fimasartan has shown excellent efficacy in BP reduction and an excellent safety profile in a large, population‐based observational study, and cardiovascular‐protective effects in various preclinical studies . A large‐scale prospective cohort study (K‐MetS study) is currently ongoing to evaluate whether the reduction in BP and/or correction of metabolic derangements with fimasartan will affect major adverse cardiovascular events and the development of diabetes after long‐term use in people with hypertension .…”

Section: Discussionmentioning

confidence: 99%

“…In the present study, we investigated the effects of fimasartan on insulin secretion in patients with type 2 diabetes and hypertension. Fimasartan, a newly developed ARB approved as an antihypertensive agent, is a pyrimidin‐4(3H)‐one derivative of losartan with the imidazole ring replaced, which enables higher potency and longer duration of action of the angiotensin II type 1 receptor, compared with losartan …”

Section: Introductionmentioning

confidence: 99%

“…Fimasartan, a newly developed ARB approved as an antihypertensive agent, is a pyrimidin-4(3H)-one derivative of losartan with the imidazole ring replaced, which enables higher potency and longer duration of action of the angiotensin II type 1 receptor, compared with losartan. 23 2 | MATERIALS AND METHODS…”

Section: Introductionmentioning

confidence: 99%

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Fimasartan increases glucose‐stimulated insulin secretion in patients with type 2 diabetes and hypertension compared with amlodipine

Yang

Lim

Lee

et al. 2018

Diabetes Obesity Metabolism

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Fimasartan increases glucose‐stimulated insulin secretion in patients with type 2 diabetes and hypertension compared with amlodipine

Yang

Lim

Lee

et al. 2018

Diabetes Obesity Metabolism

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“…Fimasartan is the ninth and the most recent ARB to be approved by the Korean Food and Drug Association as an antihypertensive agent [7][8][9]. In previous studies, fimasartan was shown to exert protective effects in animal models of myocardial ischemia: the suppression of apoptosis [10] and the prevention of intimal thickening and plaque rupture [11].…”

Section: Introductionmentioning

confidence: 99%

Fimasartan, an angiotensin II receptor antagonist, ameliorates an in vivo zebrafish model of heart failure

Quan

Seok

et al. 2020

Korean J Intern Med

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Background/Aims: Angiotensin II in the failing heart initially helps to maintain cardiac output and blood pressure, but ultimately accelerates its deterioration. In this study, we established a model of arrhythmia-induced heart failure (HF) in zebrafish and investigated the role of renin-angiotensin-aldosterone system (RAAS) modulation by using an angiotensin II type 1 receptor blocker, fimasartan, through the assessment of cellular and physiologic responses, morbidity, and mortality. Methods: HF was induced in zebrafish larvae by exposure to 20 μM terfenadine.Morphologic, physiologic, and functional parameters were assessed in the presence or absence of fimasartan treatment. Results: Zebrafish exposed to terfenadine showed marked dilatation of the ventricle and reduced systolic function. Treatment with terfenadine was associated with 10-fold higher expression of atrial natriuretic peptide (p < 0.001 vs. vehicle), increased p53 mRNA expression, and chromatin fragmentation in the TUNEL assay, all of which were significantly reduced by fimasartan treatment. Moreover, fimasartan improved fractional shortening (terfenadine + fimasartan 16.9% ± 3.1% vs. terfenadine + vehicle 11.4% ± 5.6%, p < 0.05) and blood flow (terfenadine + fimasartan 479.1 ± 124.1 nL/sec vs. terfenadine + vehicle 273.0 ± 109.0 nL/sec, p < 0.05). Finally, treatment with fimasartan remarkably reduced mortality (terfenadine + fimasartan 36.0% vs. terfenadine + vehicle 96.0%, p < 0.001). Conclusions: Fimasartan effectively protected against the progression of HF in zebrafish by improving hemodynamic indices, which improved survival. A reduction in apoptotic cell death and an improvement in hemodynamics may be the mechanisms behind these effects. Further human studies are warranted to evaluate the possible role of fimasartan in the treatment of HF.

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“…6 It is the ninth and most recent ARB approved for use in HTN by the Korea Food and Drug Administration, and is also available for worldwide use. 7 Fimasartan has been shown to have non-inferior, or even superior blood pressurelowering capabilities compared with losartan, 8,9 and has also proven its safety in previous trials. 10,11 Unlike other ARBs, fimasartan is predominantly excreted through the hepatobiliary system, with less than 3% of the administered dose detected in the urine.…”

Section: Introductionmentioning

confidence: 99%

<p>Long-Term Safety of a Novel Angiotensin Receptor Blocker, Fimasartan, According to the Absence or Presence of Underlying Liver Disease in Korean Hypertensive Patients: A Prospective, 12-Month, Observational Study</p>

Joo

Kim

et al. 2020

DDDT

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Purpose: Fimasartan, the ninth and most recent angiotensin receptor blocker (ARB) approved by the Korea Food and Drug Administration, has shown similar efficacy and safety profiles compared to other ARBs. However, due to being predominantly excreted by the hepatobiliary system, concerns on safety have been raised regarding its use in patients with underlying liver disease. Patients and Methods: This prospective, 12-month, observational study evaluated patients with essential hypertension (HTN) receiving ≥1 dose of fimasartan. Self-reported and physician-reported events were recorded and classified according to organ class and severity. Outcomes were compared according to the absence and presence of underlying liver disease. Results: A total of 601 patients were screened, and 566 patients who met predefined inclusion criteria were grouped according to the presence of underlying liver disease. Adverse events (AE) were reported in 28.7% (128/446) of patients without prior liver disease, while 42.5% (51/120) experienced events in the group with chronic liver disease. There was no difference in discontinuations due to liver function between patients with and without baseline liver disease (1.1% [5] vs 2.5% [3], p=0.376), and only a non-significant increase was observed in events associated to the hepatobiliary system in patients with chronic liver disease (9.7% [7] vs 2.7% [9], p=0.061). There were no deaths or serious adverse drug reactions (SADR) during the study period. In multivariate regression analysis, the presence of chronic liver disease (OR 2.01), female sex (OR 1.49) and old age (OR 1.12 for every 5-year increase) were independent predictors for the development of AE. Finally, no significant difference was observed in the reduction of systolic blood pressure after 12 months of treatment (least square mean change −6.57 ± 0.80 mmHg for normal liver function group; −7.65 ± 1.59 mmHg for chronic liver disease group; p=0.546). Conclusion: Long-term use of fimasartan for treatment of HTN was associated with a low rate of adverse events overall, especially in the absence of underlying liver disease. Even for patients with chronic liver disease, fimasartan treatment was well tolerated. Fimasartan could be a safe option for long-term treatment of essential HTN. ClinicalTrials.gov identifier: NCT02385721.

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Fimasartan: A New Angiotensin Receptor Blocker

Cited by 27 publications

References 44 publications

Fimasartan increases glucose‐stimulated insulin secretion in patients with type 2 diabetes and hypertension compared with amlodipine

Fimasartan increases glucose‐stimulated insulin secretion in patients with type 2 diabetes and hypertension compared with amlodipine

Fimasartan, an angiotensin II receptor antagonist, ameliorates an in vivo zebrafish model of heart failure

<p>Long-Term Safety of a Novel Angiotensin Receptor Blocker, Fimasartan, According to the Absence or Presence of Underlying Liver Disease in Korean Hypertensive Patients: A Prospective, 12-Month, Observational Study</p>

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