Pharmacokinetics of Fimasartan, a novel angiotensin II receptor type 1 antagonist in Russian population

Objective. Fimasartan, a novel potent angiotensin II receptor blocker, was evaluated in various preclinical and clinical studies in Korea. Considering that Korean population were studied in pivotal clinical trials, determination of Fimasartan pharmacokinetics in Russian patients was performed.

Design and methods. Open-label study on fimasartan pharmacokinetics after single use of fimasartan 60 mg included 15 patients with established arterial hypertension (HTN) 1–2 grade. Drug concentration was evaluated by protein precipitation for sample extraction followed by liquid chromatograph mass spectrometry.

Results. Fimasartan 60 mg was quickly absorbed after oral uptake, and maximal product concentrations in plasma were observed after 1,0 hour (tmax median), individual range of tmax values was from 0,50 to 4,00 hours after product uptake. After Сmax was achieved fimasartan concentration biphasic reduction started, and elimination phase began 2,5–8 hours after medication uptake in all patients. Fimasartan plasma concentration was identifiable until last timepoint of sampling 24 hours after drug uptake in the range of 1,33 to 11,2 ng/ml. Apparent terminal half-life period (t1/2) was 5.8 hours, individual data was in the range of 4,40 to 7,93 hours.

Conclusions. Pharmacokinetics of fimasartan in HTN patients in Russian population correlates well to the data obtained in Korean patients with HTN as well as in healthy volunteers.

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