Reduction of stroke and SEE risk for patients with NVAF; treatment of DVT and PE following 5–10 days of parenteral anticoagulant; and reduction of recurrence risk for DVT and PE
Reduction of stroke and SEE risk for patients with NVAF; treatment of DVT and PE and reduction of recurrence risk for DVT and PE; prophylaxis of DVT in patients undergoing knee or hip replacement surgery
Reduction of stroke and SEE risk for patients with NVAF; treatment of DVT and PE and reduction of recurrence risk for DVT and PE; prophylaxis of DVT in patients undergoing knee or hip replacement surgery
Reduction of stroke and SEE risk for patients with NVAF and treatment of DVT and PE following 5–10 days of parenteral anticoagulant
Time to (h)
1-2
2–4
3-4
1-2
Half-life (h)
12–17
5–13
12
10–14
Renal elimination
80% of absorbed dose
66% of oral dose
27% of absorbed dose
50% of absorbed dose
Transporters
P-gp
P-gp/BCRP
P-gp/BCRP
P-gp
Cytochrome P450 metabolism
No
Yes
Yes
Minimal
Bioavailability (%)
3–7
≥80
50
62
Potential drug interactions
Potent P-gp inhibitors and P-gp/CYP3A4 dual inducer rifampin
Potent dual CYP3A4 and P-gp inhibitors or inducers
Potent dual CYP3A4 and P-gp inhibitors or inducers
Potent P-gp inhibitors and P-gp/CYP3A4 dual inducer rifampin
Edoxaban should not be used in NVAF patients with creatinine clearance >95 mL/min [16]. DOACs are substrates of these transporters. For 10 mg dose. For 20 mg dose in the fasted state, it is 66%. For doses up to 10 mg. BCRP, breast cancer resistance protein; , maximum observed plasma concentration; CYP3A4, cytochrome P450 3A4 enzyme; DOACs, direct-acting oral anticoagulants; DVT, deep-vein thrombosis; NVAF, nonvalvular atrial fibrillation; P-gp, P-glycoprotein; PE, pulmonary embolism; SEE, systemic embolic event; VTE, venous thromboembolism.
