物质信息
ID:1132
名称和标识
IUPAC标准名
(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2,2-dimethylethyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-8-methyl-2-(propan-2-yl)nonanamide
别名
SPP 100aliskirenRasilezAliskiren
IUPAC传统名
tekturna
商标名
RasilezTekturna
化合物性质
理化性质
溶解度
Highly soluble in water (as hemifumarate salt)
疏水性(logP)
3.3
描述信息
Drug Groups
approved; investigational
Description
Aliskiren is a renin inhibitor. It was approved by the U.S. Food and Drug Administration in 2007 for the treatment of hypertension.
Indication
For the treatment of mild to moderate hypertension. It may be used alone or in combination with other antihypertensive agents.
Pharmacology
Aliskiren is a nonpeptide renin inhibitor marketed under the trade name Tekturna by Novartis.
Toxicity
The most likely manifestation of overdosage would be hypotension.
Affected Organisms
Humans and other mammals
Biotransformation
Approximately 80% of the drug in plasma following oral administration is unchanged. Cytochrome P450 (CYP) 3A4 oxidation produces two major metabolites that account for approximately 5% of the drug in plasma. Aliskiren is eliminated primarily through the biliary/fecal route as unchanged drug and, to a lesser extent, via oxidative metabolism via CYP3A4. Only 0.6% of the oral dose is recovered in urine.
Absorption
Rapidly absorbed following oral administration. Absolute bioavailability = 2.6%
Half Life
24-41 hours
Protein Binding
47-51%
Elimination
About one fourth of the absorbed dose appears in the urine as parent drug.
References
•
Gradman AH, Schmieder RE, Lins RL, Nussberger J, Chiang Y, Bedigian MP: Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation. 2005 Mar 1;111(8):1012-8. Epub 2005 Feb 21.
[Pubmed]
•
Staessen JA, Li Y, Richart T: Oral renin inhibitors. Lancet. 2006 Oct 21;368(9545):1449-56.
[Pubmed]
•
Vaidyanathan S, Jarugula V, Dieterich HA, Howard D, Dole WP: Clinical pharmacokinetics and pharmacodynamics of aliskiren. Clin Pharmacokinet. 2008;47(8):515-31.
[Pubmed]
External Links
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参考文献
• Vaidyanathan S, Jarugula V, Dieterich HA, Howard D, Dole WP: Clinical pharmacokinetics and pharmacodynamics of aliskiren. Clin Pharmacokinet. 2008;47(8):515-31. Pubmed
• Gradman AH, Schmieder RE, Lins RL, Nussberger J, Chiang Y, Bedigian MP: Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation. 2005 Mar 1;111(8):1012-8. Epub 2005 Feb 21. Pubmed
• Staessen JA, Li Y, Richart T: Oral renin inhibitors. Lancet. 2006 Oct 21;368(9545):1449-56. Pubmed