NDLI: RETRACTED ARTICLE: Direct renin inhibition: clinical pharmacology

Content Provider	Springer Nature Link
Author	Azizi, Michel
Copyright Year	2008
Abstract	Initial attempts to inhibit renin in humans have faced numerous difficulties. Molecular modeling and X-ray crystallography of the active site of renin have led to the development of new orally active renin inhibitors such as aliskiren. Aliskiren has a low bioavailality (2.6% to 5%) compensated by its high potency to inhibit renin and a long plasma half-life (24 to 40 h), which makes it suitable for once-daily dosing. The once-daily administration of aliskiren to hypertensive patients lowers blood pressure as strongly as standard doses of established AT1 receptor blockers (losartan, valsartan, and irbesartan), angiotensin-converting enzyme inhibitors (ramipril and lisnopril), hydrochlorothiazide, or long-acting calcium channel blockers (amlodipine). In combination therapy, aliskiren further decreases blood pressure when combined with either hydrochlorothiazide, amlodipine, valsartan, irbesartan, or ramipril. However, the biochemical consequences of renin inhibition differ from those of angiotensin I-converting enzyme inhibition and angiotensin II antagonism, particularly in terms of angiotensin profiles and interactions with the bradykinin-NO-cGMP pathway. Blockade of the renin–angiotensin system with angiotensin I-converting enzyme inhibitors, AT1 receptor blockers, or a combination of these drugs has become one of the most successful therapeutic approaches in medicine. However, it remains unclear how to optimize renin–angiotensin system blockade to maximize cardiovascular and renal benefits. In this context, renin inhibition to render the renin–angiotensin system fully quiescent is a new possibility requiring further study. Preliminary results show that short-term administration of aliskiren has beneficial antialbuminuric effects in diabetic patients with chronic nephropathy and favorable neurohormonal effects in patients with chronic heart failure.
Starting Page	647
Ending Page	654
Page Count	8
File Format	PDF
ISSN	09462716
Journal	Journal of Molecular Medicine
Volume Number	86
Issue Number	6
e-ISSN	14321440
Language	English
Publisher	Springer-Verlag
Publisher Date	2008-03-27
Publisher Place	Berlin/Heidelberg
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Renin Inhibitor Pharmacology Hypertension Human Genetics Internal Medicine Molecular Medicine
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Molecular Medicine Genetics (clinical)

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RETRACTED ARTICLE: Direct renin inhibition: clinical pharmacology