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Fimasartan, an angiotensin II receptor blocker (ARB), is approved for treatment of hypertension. This drug has higher potency and longer duration than losartan. The use of 60 to 120 mg of fimasartan once daily is able to control blood pressure for 24 h. The efficacy of fimasartan in reducing blood pressure is not inferior to that of candesartan but fimasartan provides greater effect than losartan and valsartan. The combination of fimasartan with hydrochlorothiazide or amlodipine increases blood pressure reduction. The most common adverse effects of fimasartan are headache and dizziness. Fimasartan is mainly excreted in bile. The hepatic uptake of fimasartan is dependent on organic anion-transporting polypeptide (OATP)1B1 transporters, thus causing drug-drug interaction when used in combination with OATP1B1 substrates such as rifampicin and atorvastatin. In addition to anti-hypertensive effect, preclinical studies in cell culture and animal models demonstrated the anti-inflammatory effect of fimasartan, which is related to cardioprotective and neuroprotective effects on ischemic injury as well as renoprotective and anti-atherosclerotic effect. The clinical studies in Korean patients found that fimasartan was beneficial for vascular function in patients with stroke and increased glucose-dependent insulin secretion in type 2 diabetic patients.
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