Oral renin inhibitors

被引:213
作者
Staessen, Jan A. [1 ]
Li, Yan
Richart, Tom
机构
[1] Univ Leuven, Studies Coorfinating Ctr, Lab Hypertens,Dept Cardiovasc Dis, Div Hypertens & Cardiovasc Rehabil, Campus Gasthuisberg,Herestr 49,Box 702, B-3000 Louvain, Belgium
[2] Shanghai Jiao Tong Univ, Ctr Epidemiol Studies & Clin Trials, Ruijin Hosp, Shanghai Inst Hypertens, Shanghai 200030, Peoples R China
基金
中国国家自然科学基金;
关键词
D O I
10.1016/S0140-6736(06)69442-7
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
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.
引用
收藏
页码:1449 / 1456
页数:8
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