Key result
Aliskiren emerges as an effective first-in-class oral non-peptide renin inhibitor for hypertension.
Why the study?
Inhibiting renin blocks the renin-angiotensin aldosterone system at its rate-limiting step to control blood pressure, yet potential renin inhibitors developed over the past two decades have not been clinically useful.
Animal studies of renin inhibitors suggest potential RAAS benefits; leaves open translation to human hypertension or heart failure.
The renin-angiotensin aldosterone system (RAAS) plays a key role in the regulation of blood pressure, acting via the effects of the hormone angiotensin (Ang) II. Ang II increases blood pressure and can exert growth-promoting effects leading to end-organ damage. Excess RAAS activity has been shown to be a major underlying cause of hypertension, heart failure, and related cardiovascular disorders. Inhibitors of renin block the RAAS at its first and rate-limiting step and thus appear to offer an excellent opportunity for blood pressure control. In the past two decades various potential renin inhibitors have been developed but have not been clinically useful. This review discusses a recent patent in the development of a novel class of non-peptide renin inhibitors: an alkanecarboxamide, aliskiren (SPP-100; Novartis). Aliskiren is effective in animal models, while recent results from studies in humans indicate that aliskiren is the first in a new class of orally effective renin inhibitors for the treatment of hypertension.
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Saez et al. (2006) conducted a review in Hypertension, heart failure, and related cardiovascular disorders. Aliskiren (SPP-100) was evaluated. Aliskiren (SPP-100) is the first in a new class of orally effective non-peptide renin inhibitors for treating hypertension in animal models and human studies.
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