腎素-血管昇壓素系统（renin-angiotensin system，RAS )對於調節血壓、平衡電解質濃度、血管生長等扮演著很重要的角色。藉由血管昇壓素轉換酵素抑制劑（angiotensin converting enzyme inhibitor, ACEI)、血管昇壓素 ATI 接受器阻斷劑（angiotensin ATI-receptor blocker, ARB)來抑制RAS，對於治療高血壓、心衰竭等疾病已經被證實爲一種有效的方法。腎素是催化RAS的第一步驟，長久以來就被視爲抑制RAS的較好標靶。經過三十年來的研究，終於有腎素抑制劑一aliskiren的上市。Aliskiren可以有效降低血清腎素活性(plasmareninactivity, PRA)，進而抑制血管昇壓素I、II的生成。在治療高血壓的臨床試驗顯示，aliskiren的降壓效果與ACEI、ARB是可相比的。至於其對心血管疾病的發病率、死亡率等是否有長期效益，或是其安全性問題，則尚需長期的試驗來求證。

The renin-angiotensin system (RAS) is important in regulation of blood pressure, electrolyte balance and vascular growth. Suppression of the RAS, through angiotensin converting enzyme inhibitor (ACEI) or angiotensin AT1-receptor blocker (ARB), is a proven effective therapeutic approach to the treatment of hypertension, heart failure and renal disorders. Renin, is the first step of the RAS, has long been recognized as the preferred target for RAS blockade. Intensive efforts have been devoted to the development of potent renin inhibitors over past twenty years. Aliskiren is the first in a new class of agents known as oral renin inhibitors and is approved for the treatment of high blood pressure as monotherapy or in combination with other antihypertensive medications. The effectiveness of aliskiren in lowering blood pressure was demonstrated in clinical trials, which included patients with mild to moderate hypertension. Given the success of ACE inhibitors and angiotensin receptor blockers in reducing morbidity and mortality amongst patients with hypertension, diabetes mellitus, cardiac failure, nephropathy and atherosclerosis, renin inhibitors may have the potential to be beneficial in the same disease states. In the long term, obviously, large studies comparing renin inhibition with the other blockers of the RAS will be needed.