Journal Article10.1016/S0140-6736(06)69442-7
Oral renin inhibitors
TL;DR: Aliskiren is the first non-peptide orally active renin inhibitors to progress to phase-III clinical trials and might become the first renin inhibitor with indications for the treatment of hypertension and cardiovascular and renal disorders.
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About: This article is published in The Lancet. The article was published on 21 Oct 2006. The article focuses on the topics: Renin inhibitor & Aliskiren.
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Citations
Renin-angiotensin-aldosterone system blockade in high-risk hypertensive patients: current approaches and future trends.
TL;DR: Aliskiren is the first US Food and Drug Administration-approved direct renin inhibitor with good oral bioavailability and ASPIRE HIGHER is an ongoing series of clinical trials designed to investigate the effect of aliskiren on cardiovascular/renal surrogate endpoints and morbidity/mortality in patients with hypertension and high risk for cardiovascular or renal disease.
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Renin Inhibition by Aliskiren Protects Rats Against Isoproterenol Induced Myocardial Infarction.
TL;DR: Evidence is provided for the protective effects of aliskiren in isoproterenol-induced myocardial infarction as well as the changes in antioxidant enzymes, which was confirmed by histopathological analysis.
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It is time to reconsider the cardiovascular protection afforded by RAAS blockade -- overview of RAAS systems.
TL;DR: The latest findings in this field are still providing new and unexpected insights into the pathophysiology of cardiovascular diseases, and developments include dual blockade therapy with angiotensin I converting enzyme inhibitors (ACEIs) and angiotENSin II receptor blockers (ARBs), and a new class of RAAS blockers, renin inhibitors.
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Enzyme and Bioactive Peptides—A Strategy for Discovery and Identification of Antihypertensive Peptides
Naufal Arshad,Hwee-Leng Siow,Ying-Yuan Ngoh,Nurul Afifah Hidayatul Saufi Sofian,Chee-Yuen Gan +4 more
- 01 Jan 2019
TL;DR: This chapter will discuss the potential of enzymes in extracting and identifying the bioactive peptides, and a strategy of antihypertensive bio active peptide discovery using this enzymatic approach is outlined.
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Formulary Drug Reviews - Aliskiren
TL;DR: The August 2007 monograph topics are temsirolimus, formoterol fumarate inhalation solution, levocetirizine, ambrisentan, and raltegravir, and the DUE is on temsIROlimus.
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References
Design of specific inhibitors of angiotensin-converting enzyme: new class of orally active antihypertensive agents
TL;DR: A hypothetical model of the active site of angiotensin-converting enzyme, based on known chemical and kinetic properties of the enzyme, has enabled a new class of potent and specific inhibitors, carboxyalkanoyl and mercaptoalkanoysl derivatives of proline, to be designed.
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•Journal Article
Molecular and Cellular Mechanisms of Angiotensin II-Mediated Cardiovascular and Renal Diseases
Shokei Kim,Hiroshi Iwao +1 more
TL;DR: In vivo recent evidence suggest that the activation of mitogen-activated protein kinases and activator protein-1 by Ang II may play the key role in cardiovascular and renal diseases, however, there are still unresolved questions and controversies on the mechanism of Ang II-mediated cardiovascular and kidneys diseases.
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Effect of inhibitors of the renin-angiotensin system and other antihypertensive drugs on renal outcomes: systematic review and meta-analysis.
Juan P. Casas,Weiliang Chua,Stavros P. Loukogeorgakis,Patrick Vallance,Liam Smeeth,Aroon D. Hingorani,Raymond J. MacAllister +6 more
TL;DR: The benefits of ACE inhibitors or ARBs on renal outcomes in placebo-controlled trials probably result from a blood-pressure-lowering effect, and in patients with diabetes, additional renoprotective actions of these substances beyond lowering blood pressure remain unproven.
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Plasma bradykinin in angio-oedema
Juerg Nussberger,Massimo Cugno,Catherine Amstutz,Marco Cicardi,Andrea Pellacani,Angelo Agostoni +5 more
TL;DR: Although the differences between patients in remission and healthy controls did not reach statistical significance, there were substantial rises in bradykinin during acute attacks of hereditary, acquired, or captopril-induced angio-oedema.
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Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients.
Alan H. Gradman,Roland E. Schmieder,R. Lins,Juerg Nussberger,Yanntong Chiang,Martin P. Bedigian +5 more
TL;DR: Once-daily oral treatment with aliskiren lowers blood pressure effectively, with a safety and tolerability profile comparable to that of irbesartan and placebo, in patients with mild-to-moderate hypertension.
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