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Edoxaban tosylate monohydrate is a selective factor Xa inhibitor with Ki of 0.561 nM, >10000-fold selectivity over thrombin and FIXa, and is also an orally bioavailable anticoagulant compound.
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Source | Thromb Res (2015). Figure 2. Edoxaban |
| Method | Calibrated automated thrombogram assays | |
| Cell Lines | pooled citrated platelet-poor plasma | |
| Concentrations | 25 to 250 ng/mL | |
| Incubation Time | 15 min | |
| Results | A direct linear correlation was observed between plasma concentrations of edoxaban and the blood coagulation parameters PT ratio and INR across all thromboplastin reagents |
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Source | Thromb Res (2015). Figure 1. Edoxaban |
| Method | Thrombin generation test | |
| Cell Lines | pooled citrated platelet-poor plasma | |
| Concentrations | 0.02-3.65 μM | |
| Incubation Time | 15 min | |
| Results | Accordingly, the values of distributions of peak thrombin over time were significantly different between edoxaban and fondaparinux at the tested molar concentration (0.9 μM) |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Venous stasis thrombosis model in rats and rabbits |
| Formulation | 0.5% methylcellulose |
| Dosages | 0.3–3 mg/kg (Rabbit); 0.5–12.5 mg/kg (Rat) |
| Administration | p.o. |
| Molecular Weight | 738.27 |
| Formula | C24H30ClN7O4S.C7H8O3S.H2O |
| CAS Number | 1229194-11-9 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Bounameaux H, et al. Drugs. Edoxaban: an update on the new oral direct factor Xa inhibitor.
| Related Factor Xa Products |
|---|
| Apixaban
Apixaban is a highly selective, reversible and orally active direct factor Xa inhibitor with an IC50 of 0.22±0.02 µM. |
| Rivaroxaban
Rivaroxaban (Xarelto, BAY 59-7939) is oral direct factor Xa inhibitor with an IC50 value of 2.1nM. |
| Betrixaban
Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a). |
| BMS-740808
BMS-740808 is a highly potent, selective inhibitor of blood coagulation factor Xa (fXa) with Ki with 0.03 nM. |
| Ozagrel
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM. |
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