209187-02-0

YM-75466 is a factor Xa inhibitor potentially for the treatment of thrombosis. YM-75466 did not prolong coagulation time even at the dose which exerted significant antithrombotic effects, while it decreased TAT level in plasma in a dose-dependent manner. YM-75466 exerted anti-FXa activity but not anti-thrombin activity. YM-75466, unlike heparin, exerts its antithrombotic effect through specific inhibition of FXa without any effect on thrombin.

YM-60828 is an FXa inhibitor with antithrombotic properties. In the rat arteriovenous shunt model, YM-60828 does not prolong coagulation time but reduces the levels of thrombin-antithrombin III complex (TAT) in a dose-dependent manner. YM-60828 exhibits only anti-FXa activity and does not show anti-thrombin activity, indicating that its antithrombotic effect is independent of thrombin. Therefore, the antithrombotic effect of YM-60828 can be monitored by TAT[1].

[1] Sato K, et al. Relationship between the antithrombotic effect of YM-75466, a novel factor Xa inhibitor, and coagulation parameters in rats. Eur J Pharmacol. 1998 Apr 24;347(2-3):231-6. DOI:10.1016/s0014-2999(98)00101-0