Table 2.
Relative Neutralization of the Direct Anti-Xa Agents by Andexanet Alfa.
| Test | Apixaban | Betrixaban | Edoxaban | Rivaroxaban | ||||
|---|---|---|---|---|---|---|---|---|
| Saline | Andexxa | Saline | Andexxa | Saline | Andexxa | Saline | Andexxa | |
| Thrombin generation assay—IC50 | 0.28 µg/mL (0.61 µM) | Not definite | 0.26 µg/mL (0.57 µM) | Not definite | 0.12 µg/mL (0.26 µM) | Not definite | 0.18 µg/mL (0.39 µM) | Not definite |
| ACT (2.5 µg/mL) | 164.5 | 165.5 | 259 | 164 | 302.5 | 210.5 | 149.5 | 163 |
| PICT test (1 µg/mL) | 198.8 | 67.5 | 180.1 | 69.0 | 300 | 94.7 | 221.8 | 82.9 |
| aPTT (1 µg/mL) | 40.7 | 38.2 | 62.5 | 38.7 | 63.7 | 41 | 59.2 | 40 |
| PT test (1 µg/mL) | 26.2 | 12.5 | 27.1 | 12.4 | 29 | 12.5 | 33.5 | 12.8 |
| Anti-Xa activity—IC50 ng/mL (µM) | 0.34 µg/mL (0.74 µM) | 0.52 µg/mL (1.13 µM) | 1.3 µg/mLa (>2.88 µM) | 5.5 µg/mLa (>12.17 µM) | 0.37 µg/mL (0.68 µM) | 0.75 µg/mL (1.37 µM) | 0.635 µg/mL (1.46 µM) | 1.42 µg/mLa (>3.26 µM) |
Abbreviations: ACT, activated clotting time; aPTT, activated partial thromboplastin time; PiCT, prothrombinase-induced clotting time; PT, prothrombin time.
aThe values represent the apparent IC50 based on the extrapolated values.