There is activation of the renin-angiotensin-aldosterone system (RAAS) in the pathophysiological process of many kinds of cardiovascular and renal diseases. So, angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) become the first-line drugs for current antihypertensive therapies in medical practices. For a long period, rennin has been considered as the most classical and logical drug target. Aliskiren, however, as the first renin inhibitor, not until 2007, has been allowed for the treatment of hypertension. Nowadays, aliskiren attracts more and more attention because of its well-control in hypertension and greater protection from hypertensive complications. Since aliskiren has better effect on more complete RAAS inhibition, great achievements were made when it is used in combination therapy for its contribution to well-controlled baseline blood pressure and several cardioprotective and renoprotective effects. In this article, we reviewed extensively the progress of clinical application of aliskiren in recent years.