A3690
Description:
IC50: 0.4 nM
Otamixaban is a factor Xa inhibitor.
Factor Xa (fXa) is a key serine protease involved in the confluence of the blood coagulation cascade pathways. FXa can catalyse the conversion of prothrombin to thrombin through the prothrombinase complex.
In vitro: Otamixaban was found to be a synthetically derived parenteral fXa inhibitor. Otamixaban is a potent, selective, reversible and competitive fXa inhibitor that effectively inhibited both free and prothrombinase-bound fXa [1].
In vivo: Otamixaban was evaluated in a rat model of ferrous chlorideinduced arterial thrombosis. A dose-dependent increase in time to occlusion was found with a maximal effective dose at ~50 μg/kg bolus and 5 μg/kg/min i.v. maintenance infusion. Compared with control group, this dose corresponded to a 40% reduction in thrombus mass [1]. …show more content…
The results showed that the lower doses of otamixaban caused fewer bleeds than UFH, the higher otamixaban doses resulted in more bleeds relative to UFH, however all bleeds were determined to be clinically insignificant. In addition, it was found that otamixaban bolus of 0.14 mg/kg followed by 0.2 mg/kg/h maintenance infusion provided a significant reduction in fXa mediated thrombin generation
Description:
IC50: 0.4 nM
Otamixaban is a factor Xa inhibitor.
Factor Xa (fXa) is a key serine protease involved in the confluence of the blood coagulation cascade pathways. FXa can catalyse the conversion of prothrombin to thrombin through the prothrombinase complex.
In vitro: Otamixaban was found to be a synthetically derived parenteral fXa inhibitor. Otamixaban is a potent, selective, reversible and competitive fXa inhibitor that effectively inhibited both free and prothrombinase-bound fXa [1].
In vivo: Otamixaban was evaluated in a rat model of ferrous chlorideinduced arterial thrombosis. A dose-dependent increase in time to occlusion was found with a maximal effective dose at ~50 μg/kg bolus and 5 μg/kg/min i.v. maintenance infusion. Compared with control group, this dose corresponded to a 40% reduction in thrombus mass [1]. …show more content…
The results showed that the lower doses of otamixaban caused fewer bleeds than UFH, the higher otamixaban doses resulted in more bleeds relative to UFH, however all bleeds were determined to be clinically insignificant. In addition, it was found that otamixaban bolus of 0.14 mg/kg followed by 0.2 mg/kg/h maintenance infusion provided a significant reduction in fXa mediated thrombin generation