Table 3.
Dabigatran | Rivaroxaban | Apixaban | |
---|---|---|---|
Direct target | Factor IIa (thrombin) | Factor Xa | Factor Xa |
Pro-drug | Yes: dabigatran etexilate | No | No |
Bioavailability (%) | 6–10 | 66% without food 80–100% with food |
50 |
Time to peak plasma concentration (h) | 3 | 2–4 | 3 |
Half-life (h) | 12–17 | 5–13 | 9–14 |
Metabolism | P-gp | P-gp CYP3A4/3A5 CYP2J2 |
P-gp CYP3A4/3A5 |
Renal elimination (%) | 80 | 33 | 27 |
Note. From “2016 ESC Guidelines for the management of atrial fibrillation developed in collaboration with EACTS,” by P. Kirchhof, S. Benussi, D. Kotecha, A. Ahlsson, D. Atar, B. Casadei, et al., 2016, Eur Heart J, 37, p. 2893–62. Copyright 2016, The European Society of Cardiology. From “Updated European Heart Rhythm Association practical guide on the use of non-vitamin K antagonist anticoagulants in patients with non-valvular atrial fibrillation: executive summary,” by H. Heidbuchel, P. Verhamme, M. Alings, M. Antz, H.C. Diener, W. Hacke, et al, 2015, Europace, 17, p. 1467–507. Copyright 2016, The European Society of Cardiology. Adapted with permission.
NOACs = non-vitamin K antagonist oral anticoagulants; P-gp = P-glycoprotein.