Aliskiren ( SPP100 ) is the first in the new class of antihypertensive agents, called renin inhibitors.

Suppression of the renin angiotensin system ( RAS ) using angiotensin converting enzyme ( ACE ) inhibitors and angiotensin II receptor blockers ( ARB ) has widely shown to treat hypertension and reduce cardiovascular events.
Aliskiren's novel mechanism of action offers a new way to address the RAS by inhibiting renin and reducing plasma renin activity ( PRA ), thereby optimizing RAS suppression.
Other therapies which act on RAS provide incomplete suppression due to indirect pathways and compensatory feedback mechanisms which in turn result in increased PRA.

A 8-week study compared the antihypertensive efficacy and safety of Aliskiren with placebo and an active comparator, Irbesartan, an angiotensin II receptor blocker.

Six hundred and fifty-two patients with mild-to-moderate hypertension ( mean sitting diastolic blood pressure 95-110 mm Hg ) were randomized to oral once-daily Aliskiren at 150, 300, or 600 mg doses, Irbesartan 150 mg or placebo.

All doses of Aliskiren effectively lowered trough mean sitting diastolic blood pressure ( DBP ) and systolic blood pressure ( SBP ).

Diastolic blood pressure reductions for Aliskiren 150 mg, 300 mg, 600 mg were 9.3, 11.8, and 11.5 mmHg respectively while systolic blood pressure reductions were 11.4, 15.8, and 15.7 mmHg, respectively.

Aliskiren treatment was well tolerated at all doses in the study.
The most commonly reported events were headache, dizziness and diarrhea.
The incidence of adverse events and discontinuations due to adverse events was relatively low and was similar to that observed with the placebo or Irbesartan treatment.

Source : Circulation, 2005

XagenaMedicine2005