Aliskiren is the first member of a novel class of antihypertensive agents, the renin inhibitors, that has been approved by the US Food and Drug Administration for the treatment of hypertension. This review discusses its potential differences compared with existing renin-angiotensin-aldosterone system blockers, focusing also on the inactive precursor of renin, prorenin, and the recently discovered (pro)renin receptor. The review summarizes the findings from all clinical trials with aliskiren published so far, and provides overview of the safety and tolerability of the new drug. Copyright