Angiotensin-converting enzyme inhibitors and angiotensin II type 1 receptor antagonists (angiotensin receptor blockers) have been shown to be effective drugs in the management of hypertension and to have beneficial effects along the cardiovascular continuum. However, due to compensatory mechanisms, both of these types of agent increase plasma renin activity, which has been reported to have deleterious effects on patient outcomes. Aliskiren is the first nonpeptide orally administered direct renin inhibitor available on the market. Reported data have shown that aliskiren effectively reduces BP alone or in combination with other antihypertensive agents, and has a good tolerability profile. Moreover, this agent reduces plasma renin activity, which in theory could have additional clinical benefits. However, clinical trials analyzing the effects of aliskiren on mortality are still ongoing.