Azilsartan: from bench to bedside

Abstract

Renin-angiotensin-aldosterone system inhibitors are commonly used to control blood pressure (BP) because of their excellent efficacy and tolerability profiles. Oral azilsartan, an angiotensin receptor blocker (ARB), is indicated for the treatment of adults with essential hypertension. This article reviews the unique structure, pharmacology, therapeutic efficacy, and tolerability of azilsartan in this patient population. Azilsartan has shown higher affinity, a more potent inhibitory effect, and slower dissociation from angiotensin receptor II type I than other ARBs in in vitro studies. In several phase III randomized, double-blind, controlled clinical trials, oral azilsartan 40 or 80 mg once daily, as monotherapy or in combination therapy with chlorthalidone, hydrochlorothiazide, or amlodipine, provided superior BP control to control therapy. In head-to-head clinical studies, azilsartan at its highest therapeutic dose of 80 mg/day provided a BP reduction that was superior to that with olmesartan at its highest therapeutic dose of 40 mg/day. The safety and tolerability of azilsartan was similar to that of placebo and other ARBs. Apart from reducing BP, azilsartan also exhibited pleiotropic effects in in vitro studies. Future studies are needed to prove the role of azilsartan in cardiometabolic diseases.