Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity

…, M Stahl, TB Tschopp, U Obst-Sander

Index: Zbinden, Katrin Groebke; Banner, David W.; Hilpert, Kurt; Himber, Jacques; Lave, Thierry; Riederer, Markus A.; Stahl, Martin; Tschopp, Thomas B.; Obst-Sander, Ulrike Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 15 p. 5357 - 5369

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Citation Number: 24

Abstract

The discovery of a highly potent and selective tissue factor/factor VIIa inhibitor is described. Upon oral administration of its double prodrug in the guinea pig, a dose-dependent antithrombotic effect is observed in an established model of arterial thrombosis without prolonging bleeding time. The pharmacodynamic properties of this selective inhibitor are compared to the behaviour of a mixed factor VIIa/factor Xa inhibitor.