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

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. It provides a selective type 1 angiotensin II receptor antagonist effect with noncompetitive, in surmountable 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. 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 oram lodipine, 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, it remains to test the benefit of using fimasartan on clinical outcomes.