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Literature summary for 3.4.23.15 extracted from

  • Hong, Y.; Dingemanse, J.; Mager, D.E.
    Pharmacokinetic/pharmacodynamic modeling of renin biomarkers in subjects treated with the renin inhibitor aliskiren (2008), Clin. Pharmacol. Ther., 84, 136-143.
    View publication on PubMed

Application

Application Comment Organism
pharmacology detailed pharmacodynamic analysis of aliskiren in humans. Development of an integrated pharmacokinetik/pharmacodynamic model for aliskiren, including an empirical submodel to account for additional complexities arising from multiple dosing Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
aliskiren aliskiren produces a parallel, dose-related, sustained decrease in plasma renin activity, angiotensin I, and angiotensin II levels and a slightly delayed increase in active renin. The effect is described by an indirect stimulatory response model in conjunction with an empirical submodel of functional adaptation. Estimated concentration of aliskiren necessary for producing 50% inhibition of plasma renin activity is 0.66 ng/ml Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
aliskiren estimated Km1 value is 0.516 ng/ml, Km2 value is 135 ng/ml Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
aliskiren + H2O
-
Homo sapiens ?
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
estimated concentration of aliskiren necessary for producing 50% inhibition of plasma renin activity is 0.66 ng/ml Homo sapiens aliskiren