PK/PD evaluation of fimasartan for the treatment of hypertension Current evidences and future perspectives.

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PK/PD evaluation of fimasartan for the treatment of hypertension Current evidences and future perspectives.

Expert Opin Drug Metab Toxicol. 2018 Apr 20;:

Authors: Angeli F, Verdecchia P, Trapasso M, Pane M, Signorotti S, Reboldi G

Abstract
INTRODUCTION: Fimasartan is the ninth and latest Angiotensin Receptor Blockers for the treatment of hypertension. Fimasartan is a derivative of losartan in which the imidazole ring has been replaced, a change that provided higher potency and longer duration than losartan. It provides a selective type 1 angiotensin II receptor antagonist effect with noncompetitive, insurmountable binding. Fimasartan is rapidly absorbed following oral administration with an oral bioavailability of 18.6 ± 7.2 %. Fimasartan is relatively stable in terms of metabolism and more than 90 % of circulating fimasartan moieties in the plasma are in the parent form; fecal elimination and biliary excretion are the predominant elimination pathways of fimasartan. Areas covered. We reviewed data from clinical trials that investigated safety and efficacy of fimasartan in hypertension. The literature search was conducted using PubMed and Scopus together with the Google Scholar database. Expert opinion. Fimasartan proved good efficacy in blood pressure reduction. In large clinical studies, fimasartan showed an excellent safety profile and when combined with hydrochlorothiazide or amlodipine, it showed a better effect on controlling blood pressure than monotherapy. Fimasartan 60-120 mg once daily has also shown an antihypertensive effect over 24-h. Moreover, preclinical studies demonstrated organ-protecting effects of fimasartan. These results make fimasartan an attractive candidate for the treatment of hypertension. However, given the evidence of potentially important pharmacological differences from other agents of the same class, it remains to test the benefit of using fimasartan on clinical outcomes.

PMID: 29676941 [PubMed - as supplied by publisher]

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