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Differential pharmacology and benefit/risk of azilsartan compared to other sartans

Authors Kurtz T, Kajiya T

Received 11 January 2012

Accepted for publication 9 February 2012

Published 28 February 2012 Volume 2012:8 Pages 133—143


Review by Single anonymous peer review

Peer reviewer comments 3

Theodore W Kurtz1, Takashi Kajiya2
1Department of Laboratory Medicine, University of California, San Francisco, CA, USA ; 2Department of Cardiovascular, Respiratory, and Metabolic Medicine, Graduate School of Medicine, Kagoshima University, Kagoshima, Japan

Abstract: Azilsartan, an angiotensin II type 1 (AT1) receptor blocker (ARB), was recently approved by regulatory authorities for treatment of hypertension and is the 8th ARB to join the clinical market. This article discusses the medical reasons for introducing a new AT1 receptor blocker and reviews the experimental and clinical studies that have compared the functional properties of azilsartan to those of other ARBs. The main question addressed is: Does azilsartan have distinguishing features that should motivate choosing it over any of the other sartans for use in clinical practice? Based on studies conducted to date in hypertensive patients without serious comorbidities, azilsartan appears to be characterized by a superior ability to control 24-hour systolic blood pressure (BP) relative to other widely used ARBs including valsartan, olmesartan, and candesartan, and presumably others as well (eg, losartan). Compared to these other ARBs, azilsartan may increase the BP target control and response rate by an absolute value of 8%–10%. Greater antihypertensive effects of azilsartan might be due in part to its unusually potent and persistent ability to inhibit binding of angiotensin II to AT1 receptors. Preclinical studies have indicated that azilsartan may also have potentially beneficial effects on cellular mechanisms of cardiometabolic disease and insulin sensitizing activity that could involve more than just blockade of AT1 receptors and/or reduction in BP. However, the clinical relevance of these additional actions is unknown. Given that the general ability of antihypertensive drugs to protect against target organ damage is largely mediated by their ability to decrease BP, the enhanced antihypertensive effects of azilsartan should serve to justify clinical interest in this ARB relative to other molecules in the class that have a lower capacity to reduce BP.

Keywords: azilsartan, azilsartan medoxomil, angiotensin II type 1 receptor blockers, angiotensins, hypertension, TAK-491, TAK-536, candesartan, olmesartan, valsartan, losartan, telmisartan, irbesartan, eprosartan

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