Overview of Selected Oral Anticoagulant Agents in the U.S.
| Drug | Rivaroxaban | Apixaban | Edoxaban |
|---|---|---|---|
| Mech. of action | Factor Xa inhibitor | Factor Xa inhibitor | Factor Xa inhibitor |
| Prodrug | No | No | No |
| Bioavailability | 66 – 100% (dose dependent) | 50% | 62% |
| Protein Binding | 92 – 95% | 87% | 40 – 50% |
| Coagulation Monitoring Required | No | No | No |
| Half-life (hours) | 5 - 9 | 12 | 5.8 – 10.7 |
| Elimination | Renal and Hepatic | Renal and Hepatic | Renal and Hepatic |
| Renal Dose Adjustment | Yes | Yes | Yes (based on clinical trials) |
| Drug Interactions | Substrate of CYP450 3A4/5, 2J2 and P-gp | Substrate of CYP450 3A4/5, and P-gp | Substrate of P-gp |
| Reversal Agent Approved | No | No | No |
| Dialyzable | Not expected | Not expected | Data not available |
| Indications | Reduce stroke and systemic embolism in nonvalvular AF; treatment of DVT or PE or prevention of their recurrence; prophylaxis of DVT in those undergoing hip or knee surgery | Reduce stroke and systemic embolism in nonvalvular AF; treatment of DVT or PE or prevention of their recurrence; prophylaxis of DVT in those undergoing hip or knee surgery | Reduce stroke and systemic embolism in nonvalvular AF; treatment of DVT or PE or prevention of their recurrent, symptomatic VTE |
A comparison and summary of selected characteristics of the direct oral anticoagulants Rivaroxaban, Apixaban and Edoxaban
AF = atrial fibrillation, DVT = deep vein thrombosis, PE = pulmonary embolism; P-gp = P=glycoprotein; VTE = venous thromboembolism Adapted from (2) with permission of authors.