Efficacy and tolerability of tasosartan, a novel angiotensin II receptor blocker: Results from a 10-week, double-blind, placebo-controlled, dose-titration study

Background Angiotensin II receptor antagonists are selective blockers of th e renin-angiotensin system and represent an alternative to angiotensin-conv erting enzyme inhibitors in the treatment of hypertension. Tasosartan is a newly developed nonpeptide ATI receptor blocker. Methods and Results In this double-blind, randomized, dose-titration, multi center trial, tasosartan and placebo were compared in patients with stage I and stage II hypertension. A prequalification washout period (antihyperten sive medications withdrawn) and a 2-week qualification period (patients rec eived single-blind placebo) preceded a 10-week, double-blind treatment peri od. The patients received either 50 mg tasosartan (n = 132) or placebo (n = 130) once per day and were evaluated once per week. The dose of tasosartan was increased at 3-week intervals to 100 mg and then to 200 mg if the mean sitting diastolic blood pressure (SiDBP) exceeded 90 mm Hg. Compared with placebo, tasosartan produced significantly (P < .05) greater reductions in both SiDBP (-9.4 +/- 0.7 vs -2.0 +/- 0.7 mm Hg) and sitting systolic blood pressure (SBP) (-12.2 +/- 1.2 vs +0.4 +/- 1.2 mm Hg). The rate of response (SiDBP less than or equal to 90 mm Hg or a decrease from baseline of greate r than or equal to 10 mm Hg) was significantly (P < .05) greater in the tas osartan group than in the placebo group (55% vs 19%). The mean 24-hour bloo d pressure reduction with tasosartan was -12.6 + 0.9/-8.1 +/- 0.6, signific antly greater (P < .05) than the reduction with placebo (+0.6 +/- 0.9/+0.5 +/- 0.6 mm Hg). The trough-to-peak ratio (determined from the ambulatory da ta) was 0.66 for DBP and 0.72 for SEP for the tasosartan treatment group, d emonstrating 24-hour efficacy with once-a-day administration. The safety pr ofile of tasosartan was similar to placebo. Conclusions These results demonstrate that tasosartan at 50 to 200 mg given once a day over a titration period of 10 weeks was effective and safe in t he treatment of essential hypertension.