Table 12.
Drug transport/metabolism/elimination characteristics of the direct oral anticoagulants [11, 12, 15, 16, 48, 49, 128, 129]
P-gp substrate | CYP3A4 substrate (% of drug metabolized via CYP3A4) | % renal elimination | |
---|---|---|---|
Dabigatran | Yes | No | ≈80 |
Rivaroxaban | Yes | Yes (≈33)a | ≈33 |
Apixaban | Yes | Yes (≈25)b | ≈25 |
Edoxaban | Yes | No | ≈50 |
CYP3A4 Cytochrome 3A4, p-gp permeability-glycoprotein
aTotal of ≈66 % hepatic metabolism equally distributed between CYP3A4 and CYP2J2
bTotal of ≈25 % hepatic metabolism, mostly by CYP3A4, with minor contributions by CYP1A2, 2J2, 2C8, 2C9, and 2C19