New approaches to blockade of the renin-angiotensin-aldosterone system: Characteristics and usefulness of the direct renin inhibitor aliskiren

Atsuhiro Ichihara, Mariyo Sakoda, Asako Kurauchi-Mito, Tatsuya Narita, Kenichiro Kinouchi, Kanako Bokuda, Hiroshi Itoh

研究成果: Review article査読

19 被引用数 (Scopus)

抄録

Since renin inhibition interferes with the first and rate-limiting steps in the renin-angiotensin system, the renin step is a very attractive target for lowering blood pressure and minimizing target-organ damage. The newly developed direct renin inhibitor aliskiren has several attractive characteristics: it definitively reduces plasma renin activity among inhibitors of the renin-angiotensin system, is remarkably specific for human renin, exhibits a long half-life in plasma comparable to that of amlodipine, and has a high affinity for renal glomeruli and vasculature. Although these characteristics suggest the clinical usefulness and safety of aliskiren, several problems remain unsolved. Why does aliskiren have beneficial effects on the heart and kidneys of patients treated with angiotensin-converting enzyme (ACE) inhibitors and/or angiotensin II type 1-receptor blockers (ARBs)? Is the blood-pressure-lowering effect of aliskiren dependent on the plasma renin activity? Does aliskiren exert a possible adverse effect via (pro)renin receptor-dependent intracellular signals? Here, we review the characteristics and usefulness of aliskiren and discuss the current issues associated with this direct renin inhibitor.

本文言語English
ページ(範囲)296-300
ページ数5
ジャーナルJournal of Pharmacological Sciences
113
4
DOI
出版ステータスPublished - 2010

ASJC Scopus subject areas

  • 分子医療
  • 薬理学

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