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A Systematic Comparison of the Properties of Clinically Used Angiotensin II Type 1 Receptor Antagonists

Martin C. Michel, Carolyn Foster, Hans R. Brunner and Lisheng Liu
Dianne M. Perez, ASSOCIATE EDITOR
Pharmacological Reviews April 2013, 65 (2) 809-848; DOI: https://doi.org/10.1124/pr.112.007278
Martin C. Michel
Department of Clinical Development & Medical Affairs, Boehringer Ingelheim, Ingelheim, Germany (M.C.M.); Department of Pharmacology, Johannes Gutenberg University, Mainz, Germany (M.C.M.); Department of Research Networking, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, Connecticut (C.F.); Emeritus of Lausanne University, Riehen, Switzerland (H.R.B.); and Beijing Hypertension League Institute, Fu Wai Hospital, Beijing, China (L.L.)
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Carolyn Foster
Department of Clinical Development & Medical Affairs, Boehringer Ingelheim, Ingelheim, Germany (M.C.M.); Department of Pharmacology, Johannes Gutenberg University, Mainz, Germany (M.C.M.); Department of Research Networking, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, Connecticut (C.F.); Emeritus of Lausanne University, Riehen, Switzerland (H.R.B.); and Beijing Hypertension League Institute, Fu Wai Hospital, Beijing, China (L.L.)
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Hans R. Brunner
Department of Clinical Development & Medical Affairs, Boehringer Ingelheim, Ingelheim, Germany (M.C.M.); Department of Pharmacology, Johannes Gutenberg University, Mainz, Germany (M.C.M.); Department of Research Networking, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, Connecticut (C.F.); Emeritus of Lausanne University, Riehen, Switzerland (H.R.B.); and Beijing Hypertension League Institute, Fu Wai Hospital, Beijing, China (L.L.)
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Lisheng Liu
Department of Clinical Development & Medical Affairs, Boehringer Ingelheim, Ingelheim, Germany (M.C.M.); Department of Pharmacology, Johannes Gutenberg University, Mainz, Germany (M.C.M.); Department of Research Networking, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, Connecticut (C.F.); Emeritus of Lausanne University, Riehen, Switzerland (H.R.B.); and Beijing Hypertension League Institute, Fu Wai Hospital, Beijing, China (L.L.)
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Dianne M. Perez
Department of Clinical Development & Medical Affairs, Boehringer Ingelheim, Ingelheim, Germany (M.C.M.); Department of Pharmacology, Johannes Gutenberg University, Mainz, Germany (M.C.M.); Department of Research Networking, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, Connecticut (C.F.); Emeritus of Lausanne University, Riehen, Switzerland (H.R.B.); and Beijing Hypertension League Institute, Fu Wai Hospital, Beijing, China (L.L.)
Roles: ASSOCIATE EDITOR
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Abstract

Angiotensin II type 1 receptor antagonists (ARBs) have become an important drug class in the treatment of hypertension and heart failure and the protection from diabetic nephropathy. Eight ARBs are clinically available [azilsartan, candesartan, eprosartan, irbesartan, losartan, olmesartan, telmisartan, valsartan]. Azilsartan (in some countries), candesartan, and olmesartan are orally administered as prodrugs, whereas the blocking action of some is mediated through active metabolites. On the basis of their chemical structures, ARBs use different binding pockets in the receptor, which are associated with differences in dissociation times and, in most cases, apparently insurmountable antagonism. The physicochemical differences between ARBs also manifest in different tissue penetration, including passage through the blood-brain barrier. Differences in binding mode and tissue penetration are also associated with differences in pharmacokinetic profile, particularly duration of action. Although generally highly specific for angiotensin II type 1 receptors, some ARBs, particularly telmisartan, are partial agonists at peroxisome proliferator-activated receptor-γ. All of these properties are comprehensively reviewed in this article. Although there is general consensus that a continuous receptor blockade over a 24-hour period is desirable, the clinical relevance of other pharmacological differences between individual ARBs remains to be assessed.

Footnotes

  • M.C.M. and C.F. are present and past employees of Boehringer Ingelheim, respectively. H.R.B. has been a consultant to practically all ARB manufacturers in the past but reports no present conflict of interest. L.L. reports no conflict of interest.

  • dx.doi.org/10.1124/pr.112.007278.

  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 65 (2)
Pharmacological Reviews
Vol. 65, Issue 2
1 Apr 2013
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Review ArticleReview Articles

AT1 Receptor Blocker Pharmacology

Martin C. Michel, Carolyn Foster, Hans R. Brunner and Lisheng Liu
Pharmacological Reviews April 1, 2013, 65 (2) 809-848; DOI: https://doi.org/10.1124/pr.112.007278

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Review ArticleReview Articles

AT1 Receptor Blocker Pharmacology

Martin C. Michel, Carolyn Foster, Hans R. Brunner and Lisheng Liu
Pharmacological Reviews April 1, 2013, 65 (2) 809-848; DOI: https://doi.org/10.1124/pr.112.007278
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  • Article
    • Abstract
    • I. Introduction
    • II. Physicochemical Properties
    • III. Tissue Distribution
    • IV. Direct AT1R Effects
    • V. Receptor Selectivity and Ancillary Effects
    • VI. Pharmacokinetic Properties
    • VII. Conclusions
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