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

Bioorganic & Medicinal Chemistry
Katrin Groebke ZbindenUlrike Obst-Sander

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.

References

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Citations

Mar 23, 2012·Chemical Reviews·Alexander DömlingKan Wang
Jan 5, 2010·Chemical & Pharmaceutical Bulletin·Takuya ShiraishiToshiro Kozono
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Jun 30, 2007·Arteriosclerosis, Thrombosis, and Vascular Biology·Rebecca A Shirk, George P Vlasuk
Jan 21, 2017·ACS Medicinal Chemistry Letters·Jeremy M RichterE Scott Priestley
Aug 5, 2008·Bioorganic & Medicinal Chemistry Letters·Takuya ShiraishiToshiro Kozono

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