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Aliskiren

Abstract

Aliskiren (Tekturna; Speedel/Novartis) is the first in a new class of drugs that inhibit the protease renin, which has a key role in the regulation of blood pressure. It was approved by the US FDA for the treatment of hypertension in March 2007, and approved in Europe in August 2007 (where it will be marketed as Rasilez).

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Figure 1: Drugs targeting the renin–angiotensin–aldosterone system.

References

  1. Kearney, P. M. et al. Global burden of hypertension: analysis of worldwide data. Lancet 365, 217–223 (2005).

    Article  Google Scholar 

  2. Chobanian, A. V. et al. Seventh report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure. Hypertension 42, 1206–1252 (2003).

    Article  CAS  Google Scholar 

  3. Amin Zaman, M. et al. Drugs targeting the renin–angiotensin–aldosterone system. Nature Rev. Drug Discov. 1, 621–636 (2002).

    Article  Google Scholar 

  4. Rahuel, J. et al. Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin. Chem. Biol. 7, 493–504 (2000).

    Article  CAS  Google Scholar 

  5. Wood, J. M. et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem. Biophys. Res. Commun. 308, 698–705 (2003).

    Article  CAS  Google Scholar 

  6. Göschke, R. et al. Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin. J. Med. Chem. 8 Sep 2007 (doi:10.1021/jm070314y).

    Article  Google Scholar 

  7. Maibaum, J. et al. Structural modification of the P2′ position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets. J. Med. Chem. 8 Sep 2007 (doi: 10.1021/jm070316i).

    Article  CAS  Google Scholar 

  8. Food and Drug Administration. FDA labelling information [online], (2007).

  9. Gradman, A. H. Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation 111, 1012–1018 (2005).

    Article  CAS  Google Scholar 

  10. Oh, B. H. et al. Aliskiren, an oral renin inhibitor, provides dose-dependent efficacy and sustained 24-hour blood pressure control in patients with hypertension. J. Am. Coll. Cardiol. 49, 1157–1163 (2007).

    Article  CAS  Google Scholar 

  11. Villamil, A. et al. Renin inhibition with aliskiren provides additive antihypertensive efficacy when used in combination with hydrochlorothiazide. J. Hypertens. 25, 217–226 (2007).

    Article  CAS  Google Scholar 

  12. Oparil, S. et al. Efficacy and safety of combined use of aliskiren and valsartan in patients with hypertension: a randomised, double-blind trial. Lancet 370, 221–229 (2007).

    Article  CAS  Google Scholar 

  13. IMS Health, IMS MIDAS Quantum (2007).

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Siragy, H., Kar, S. & Kirkpatrick, P. Aliskiren. Nat Rev Drug Discov 6, 779–780 (2007). https://doi.org/10.1038/nrd2421

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