Aliskiren is an orally-available, nonpeptide piperidine-based inhibitor renin (IC50 0.6 nM) for the treatment of hypertension. [1] Despite it's 2.5% bioavailability in humans, the absorbed aliskiren is slowly cleared such that the drug can accumulate to therapeutic levels within several doses.

Aliskiren is highly selective for the Renin-Angiotensin System (RAS) and therefore does not interfere with bradykinin metabolism; therefore side effects often associated with ACE inhibitors are not likely to occur with aliskiren. [2] Aliskiren is effective in reducing blood pressure and is well tolerated, and has shown promising target organ protection in animal models and clinical trials. [3]