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Chemical Compound Review

Tekturna     (2S,4S,5S,7R)-5-amino-N-(2- aminocarbonyl-2...

Synonyms: Aliskiren, Rasilez, CHEMBL1639, Rasilez (TN), SureCN455490, ...
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Disease relevance of SPP100


High impact information on SPP100

  • Hormonal and BP effects were compared for 48 h after administration of single oral doses of 300 mg (high dose) of the renin inhibitor aliskiren (A300) and 160 mg (standard antihypertensive dose) of the AT1 receptor antagonist valsartan (V160) and their combination each at half dose (A150+V80) in 12 mildly sodium-depleted normotensive individuals [5].
  • This study compared the pharmacokinetics and pharmacodynamics of the orally active direct renin inhibitor, aliskiren, in healthy volunteers and patients with type 2 diabetes [2].
  • RESULTS: Aliskiren exhibited similar pharmacokinetics in patients with type 2 diabetes and healthy volunteers [2].
  • CONCLUSIONS: Aliskiren is an orally effective, long-lasting renin inhibitor that shows antihypertensive efficacy in animals superior to previous renin inhibitors and at least equivalent to angiotensin-converting enzyme inhibitors and AT1-receptor blockers [1].
  • OBJECTIVES: Aliskiren is a new renin inhibitor of a novel structural class that has recently been shown to be efficacious in hypertensive patients after once-daily oral dosing [1].

Chemical compound and disease context of SPP100


Biological context of SPP100


Associations of SPP100 with other chemical compounds


Gene context of SPP100

  • While, to date, aliskiren has only been shown to reduce BP, it appears likely that orally-active renin inhibitors could prove useful in the management of a wide range of cardiovascular pathologies [14].

Analytical, diagnostic and therapeutic context of SPP100


  1. Aliskiren, a novel, orally effective renin inhibitor, lowers blood pressure in marmosets and spontaneously hypertensive rats. Wood, J.M., Schnell, C.R., Cumin, F., Menard, J., Webb, R.L. J. Hypertens. (2005) [Pubmed]
  2. Aliskiren exhibits similar pharmacokinetics in healthy volunteers and patients with type 2 diabetes mellitus. Zhao, C., Vaidyanathan, S., Yeh, C.M., Maboudian, M., Armin Dieterich, H. Clinical pharmacokinetics. (2006) [Pubmed]
  3. Pharmacokinetics, safety, and tolerability of the oral Renin inhibitor aliskiren in patients with hepatic impairment. Vaidyanathan, S., Warren, V., Yeh, C., Bizot, M.N., Dieterich, H.A., Dole, W.P. Journal of clinical pharmacology (2007) [Pubmed]
  4. Complement activation in angiotensin II-induced organ damage. Shagdarsuren, E., Wellner, M., Braesen, J.H., Park, J.K., Fiebeler, A., Henke, N., Dechend, R., Gratze, P., Luft, F.C., Muller, D.N. Circ. Res. (2005) [Pubmed]
  5. Pharmacologic demonstration of the synergistic effects of a combination of the renin inhibitor aliskiren and the AT1 receptor antagonist valsartan on the angiotensin II-renin feedback interruption. Azizi, M., Ménard, J., Bissery, A., Guyenne, T.T., Bura-Rivière, A., Vaidyanathan, S., Camisasca, R.P. J. Am. Soc. Nephrol. (2004) [Pubmed]
  6. Lack of pharmacokinetic interactions of aliskiren, a novel direct renin inhibitor for the treatment of hypertension, with the antihypertensives amlodipine, valsartan, hydrochlorothiazide (HCTZ) and ramipril in healthy volunteers. Vaidyanathan, S., Valencia, J., Kemp, C., Zhao, C., Yeh, C.M., Bizot, M.N., Denouel, J., Dieterich, H.A., Dole, W.P. International journal of clinical practice. (2006) [Pubmed]
  7. Aliskiren reduces blood pressure and suppresses plasma renin activity in combination with a thiazide diuretic, an angiotensin-converting enzyme inhibitor, or an angiotensin receptor blocker. O'Brien, E., Barton, J., Nussberger, J., Mulcahy, D., Jensen, C., Dicker, P., Stanton, A. Hypertension (2007) [Pubmed]
  8. Effect of the oral renin inhibitor aliskiren on the pharmacokinetics and pharmacodynamics of a single dose of warfarin in healthy subjects. Dieterle, W., Corynen, S., Mann, J. British journal of clinical pharmacology. (2004) [Pubmed]
  9. Renin inhibition. Azizi, M. Curr. Opin. Nephrol. Hypertens. (2006) [Pubmed]
  10. The future of angiotensin II inhibition in cardiovascular medicine. Meier, P., Maillard, M., Burnier, M. Current drug targets. Cardiovascular & haematological disorders (2005) [Pubmed]
  11. Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine. Dieterle, W., Corynen, S., Vaidyanathan, S., Mann, J. International journal of clinical pharmacology and therapeutics. (2005) [Pubmed]
  12. Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Gradman, A.H., Schmieder, R.E., Lins, R.L., Nussberger, J., Chiang, Y., Bedigian, M.P. Circulation (2005) [Pubmed]
  13. Angiotensin II suppression in humans by the orally active renin inhibitor Aliskiren (SPP100): comparison with enalapril. Nussberger, J., Wuerzner, G., Jensen, C., Brunner, H.R. Hypertension (2002) [Pubmed]
  14. Potential of renin inhibition in cardiovascular disease. Stanton, A. Journal of the renin-angiotensin-aldosterone system : JRAAS. (2003) [Pubmed]
  15. Conformational changes in prorenin during renin inhibition in vitro and in vivo. Ménard, J., Guyene, T.T., Peyrard, S., Azizi, M. J. Hypertens. (2006) [Pubmed]
  16. Pharmacokinetics, safety, and tolerability of the novel oral direct Renin inhibitor aliskiren in elderly healthy subjects. Vaidyanathan, S., Reynolds, C., Yeh, C.M., Bizot, M.N., Dieterich, H.A., Howard, D., Dole, W.P. Journal of clinical pharmacology (2007) [Pubmed]
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