Aliskiren, the future of renin–angiotensin system blockade?

Abstract

The suppression of the renin–angiotensin system by angiotensin-converting enzyme inhibitors and angiotensin receptor blockers has been proven in many studies to treat hypertension and reduce cardiovascular events; however, reducing angiotensin I receptor stimulation results in the loss of the negative-feedback signal, leading to increased plasma renin activity. Numerous direct renin inhibitors were synthesized, but abandoned owing to low potency, poor bioavailability and short half-life. Aliskiren, a direct renin inhibitor of a novel structural class, inhibits the activity of the renin produced and, thus, its capacity to form angiotensin I, as measured by plasma renin activity. Aliskiren has been recently shown to be efficacious in hypertensive patients at once-daily oral dosing with favorable pharmacokinetics and the potential to improve end-organ protection.

Keywords::

• aliskiren
• angiotensin-converting enzyme inhibitors
• angiotensin receptor blockers
• hypertension
• oral renin inhibitors
• renin–angiotensin–aldosterone system

Acknowledgments

The authors would like to thank Novartis for the data provided and Serhan Sevgi for his efforts.

Financial disclosure

The authors have no relevant financial interests related to this manuscript, including employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.