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
Direct renin inhibitors in arterial hypertension treatment
TL;DR: Aliskiren, an octanamide, is the first of a new class of completely non-peptide, low-molecular-weight, orally active transition-state renin inhibitors and only approved for the treatment of hypertension.
Biocatálisis aplicada a la síntesis de fármacos (i) enzimas hidrolíticas
María José Hernáiz
- 01 Jan 2012
TL;DR: In this article, el capitulo presenta una introduccion sobre la versatilidad de las enzimas hidroliticas en biotransformaciones and sus principales aplicaciones in la sintesis de farmacos.
2
Effects of antihypertensive therapy on glucose, insulin metabolism, left ventricular diastolic dysfunction and renin system in overweight and obese hypertensives
Maria Leonarda De Rosa,Francesca Musella,Federica Ilardi,Carmen D'Amore,Rossella Luciano,Fabio Maresca +5 more
TL;DR: In high-risk, overweight/obese patients with hypertension, traditional therapy provides significantly greater BP- versus aliskiren-lowering throughout the 24-hour dosing interval; overall aliskirens-based treatment offers sustained control of PRA.
2
•Dissertation
Characterisation of the pharmacological actions in humans of multiple vasoactive enzyme inhibitors with therapeutic potential in heart failure
Alison Seed
- 01 Jan 2007
TL;DR: For the first time in heart failure patients, the benefits of a more specific approach to neurohumoral manipulation using a recently developed renin inhibitor, aliskiren, are reported.
2
Direct renin inhibition: update on clinical investigations with aliskiren
Natale Daniele Brunetti,Luisa De Gennaro,Pier Luigi Pellegrino,Andrea Cuculo,Luigi Ziccardi,Antonio Gaglione,Matteo Di Biase +6 more
TL;DR: Aliskiren is the first of these new non-peptide direct renin inhibitors to be approved for the treatment of hypertension and is reviewed in relation to those studies that compared clinical efficacy of aliskiren in comparison and in addition to other antihypertensive drug strategies.
2
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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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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