Novel non-peptide renin inhibitors, particularly aliskiren, show efficacy in animal models and early human studies, representing a potential new class of orally-effective antihypertensive agents.
AbstractThe renin–angiotensin system (RAS) plays an important role in the development of cardiovascular diseases such as hypertension and heart failure. Inhibitors of renin (EC 3.4.99.19) block the RAS at its first and rate-limiting step and may therefore offer major potential benefits in blood pressure control. Despite intensive research, however, previous attempts to develop clinically useful renin inhibitors have failed. This review discusses recent patent applications for the development of two novel classes of non-peptide renin inhibitors: 3-alkoxy-4-aryl-piperidines, such as Ro 66-1132 (Hoffmann-La Roche), and alkanecarboxamides, such as aliskiren (SPP-100; Novartis). Both classes are effective in animal models, while results from studies in humans suggest that aliskiren may represent the first in a new class of orally-effective renin inhibitors. Patents claiming the use of renin inhibitors in combination therapy are also discussed.Keywords4-aryl-piperidinealiskirenangiotensinantihypertensiveaspartyl proteasehypertensionleft ventricular dysfunctionrenal blood flowreninangiotensin systemrenin inhibitorsynthetic inhibitortransition-state peptidomimetic
Maibaum et al. (Thu,) conducted a review in Cardiovascular disease (hypertension and heart failure). Renin inhibitors (3-alkoxy-4-aryl-piperidines and alkanecarboxamides) was evaluated. Novel non-peptide renin inhibitors, particularly aliskiren, show efficacy in animal models and early human studies, representing a potential new class of orally-effective antihypertensive agents.
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