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- W306827441 abstract "Direct renin inhibition is a promising new type of treatment for high blood pressure (BP). The renin-angiotensin-aldosterone system (RAAS) is a key physiological regulator of BP and fluid homeostasis. The first and rate-limiting step of this cascade is catalyzed by the highly specific aspartic protease renin. The direct blockade of this step has long been recognized as most attractive for therapeutic intervention. Recently, an unprecedented topological structure-based drug design strategy enabled the discovery of novel, highly potent, and selective non-peptide transition-state mimetic (TSM) rennin inhibitors. These efforts culminated in the discovery of TEKTURNA®/RASILEZ® (aliskiren) that has been recently approved as a new therapy for the treatment of hypertension. As a first-in-class direct renin inhibitor, aliskiren has demonstrated orally active anti-hypertensive efficacy and end-organ protection. It is safe and well-tolerated in pre-clinical and clinical trials. In addition, the extent to which this new mechanism of action provides improved organ protection is determined by ongoing clinical trials with this direct renin inhibitor." @default.
- W306827441 created "2016-06-24" @default.
- W306827441 creator A5005195767 @default.
- W306827441 creator A5030814313 @default.
- W306827441 date "2009-01-01" @default.
- W306827441 modified "2023-10-17" @default.
- W306827441 title "Chapter 5 Case History on Tekturna®/Rasilez® (Aliskiren), a Highly Efficacious Direct Oral Renin Inhibitor as a New Therapy for Hypertension" @default.
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- W306827441 doi "https://doi.org/10.1016/s0065-7743(09)04405-4" @default.
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