Table 2.
Summary of metabolite activity, protein binding and abundance in relation to parent drug (data on file)
| Moiety | Anti-FXa IC50 (nM) | Protein binding (%) | Exposure (%) relative to edoxaban in adults, presented by renal function | |||
|---|---|---|---|---|---|---|
| Normal: CLCR >80 mL/min | Mild impairment: CLCR >50–80 mL/min | Moderate impairment: CLCR >30–50 mL/min | Severe impairment: CLCR >15–30 mL/min | |||
| M-4 | 1.8 | ~80 | 5.70 | 9.02 | 11.2 | 12.4 |
| M-6 | 6.9 | NA | 2.75 | 3.69 | 5.09 | 4.63 |
| M-8 | 2.7 | NA | Not quantifiable at most time points | |||
Edoxaban is ~55 % protein bound and has an anti-FXa IC50 value of 3.0 nM
CL CR creatinine clearance, FXa factor Xa, IC 50 half-maximal inhibitory concentration, NA not assessed