Oral Renin Inhibitors.
From: Studies Coordinating Centre, Division of Hypertension and Cardiovascular Rehabilitation, Department of Cardiovascular Diseases, University of Leuven, Leuven, Belgium. jan.staessen@med.kuleuven.be
Lancet
- Publish Date: Oct 2006
- ISSN: 1474-547X
- Volume: 368
- Issue: 9545
- Pages: 1449-56
- Medium: Internet
- Language: English
- Citation (JAMA): Staessen Jan A, Li Yan, Richart Tom, et al. Oral Renin Inhibitors.. Lancet Oct 2006;368:1449-56
Abstract
Use of drugs that inhibit the renin-angiotensin system is an effective way to intervene in the pathogenesis of cardiovascular and renal disorders. The idea of blocking the renin system at its origin by inhibition of renin has existed for more than 30 years. Renin inhibition suppresses the generation of the active peptide angiotensin II. The first generation of orally active renin inhibitors were never used clinically because of low bioavailability and weak blood-pressure-lowering activity. At present, aliskiren is the first non-peptide orally active renin inhibitor to progress to phase-III clinical trials. It might become the first renin inhibitor with indications for the treatment of hypertension and cardiovascular and renal disorders. Novel compounds with improved oral bioavailability, specificity, and efficacy are now in preclinical development. This Review summarises the development of oral renin inhibitors and their pharmacokinetic and pharmacodynamic properties, with a focus on aliskiren.
Mesh Headings (Keywords): Administration, Oral, Adult, Aged, Amides, Animals, Biological Availability, Blood Pressure, Female, Fumarates, Half-Life, Humans, Hypertension, Kidney, Male, Middle Aged, Randomized Controlled Trials as Topic, Renin, Renin-Angiotensin System, Structure-Activity Relationship
Check for Full Text / PubMed Unique Identifier (PMID): 17055947
This abstract is part of PubMed, a service of the U.S. National Library of Medicine. PubMed includes more than 17 million citations from MEDLINE and other life science journals for biomedical articles. See Copyright and Disclaimers.
Linked medical terms appearing on this page are added by Healia to help readers find more information and are not part of the original PubMed document.
The data herein was last updated on July 8th, 2008 and may not reflect the most current and accurate data available from NLM.