, Volume 18, Issue 3, pp 117-120
Date: 06 Mar 2009

Aliskiren: An Overview of the First Direct Renin Inhibitor

Rent the article at a discount

Rent now

* Final gross prices may vary according to local VAT.

Get Access
This is an excerpt from the content

Optimal blockade of the renin-angiotensin-aldosterone system (RAAS) is a key goal of pharmacotherapy in cardiovascular (CV) and renal disease. Aliskiren, the first commercially available direct renin inhibitor, constitutes a new target in RAAS blockade. Since renin-catalyzed conversion of angiotensinogen into angiotensin I is the rate-limiting step in the synthesis of angiotensin II (AII), it has been suggested that renin inhibition may have comparable or superior clinical efficacy to angiotensin converting enzyme inhibitors (ACEi) and angiotensin receptor blockers (ARB).

Aliskiren, which was approved by the FDA in 2007 for the treatment of hypertension, has a high specificity for renin and blocks the binding of angiotensinogen. It has a bioavailability of 2.6%, a serum peak at 2–4 h, and a half-life of 24–36 h. An analysis of seven randomized multicenter studies showed that overall incidence of adverse events with aliskiren monotherapy was similar to placebo, and an increased risk of d ...