Renin Inhibitors

The first and rate-limiting step in RAS, the conversion of angiotensinogen to Ang I, is catalyzed by renin. Several renin inhibitors have been synthesized, but low efficacy, poor oral bioavailability, high cost of synthesis, and the availability of highly successful ARBs prevented their development. One of the first clinically tested renin inhibitors was enalkiren (ABT-64662) (Figure 4). More recently developed, aliskiren42 is currently in advanced clinical evaluation. At 75, 150, or 300 mg single doses, aliskiren effectively lowers ambulatory systolic pressure in hypertensive patients and is well tolerated. Its effects appear to be synergistic with valsartan. It still remains to be shown that aliskiren can affect vascular pathology and reduce morbidity and mortality in cardiovascular disease.

Figure 4 Chemical structures of aliskiren, enalkiren, and omapatrilat.

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Enalkiren

Figure 4 Chemical structures of aliskiren, enalkiren, and omapatrilat.

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