Andexanet PK parameters in the absence of apixaban (phase 1 study)
| Pharmacokinetic parameters (mean ± SD) . | 30 mg (n = 6) . | 90 mg (n = 6) . | 300 mg (n = 6) . | 600 mg (n = 6) . |
|---|---|---|---|---|
| Cmax, ng/mL | 3080 ± 389 | 10 800 ± 4 110 | 52 800 ± 13 200 | 93 300 ± 14 200 |
| tmax,* h | 0.21 (0.17, 0.29) | 0.23 (0.18, 0.29) | 0.26 (0.17, 0.34) | 0.51 (0.42, 0.52) |
| AUC0-last, ng*h/mL | 4510 ± 472 | 12 500 ± 3 470 | 61 000 ± 15 400 | 117 000 ± 17 400 |
| AUC0-∞, ng*h/mL | 4710 ± 508 | 12 600 ± 3 450 | 61 400 ± 15 400 | 118 000 ± 17 300 |
| t1/2, h | 7.25 ± 2.14 | 7.38 ± 2.21 | 7.46 ± 1.58 | 6.40 ± 1.88 |
| lz, 1/h | 0.10 ± 0.03 | 0.11 ± 0.06 | 0.10 ± 0.02 | 0.11 ± 0.02 |
| CL, L/h | 6.30 ± 0.68 | 6.24 ± 0.92 | 5.13 ± 1.16 | 5.18 ± 0.64 |
| Vd, L | 65.27 ± 17.61 | 67.29 ± 23.05 | 55.39 ± 19.89 | 48.49 ± 18.46 |
| Vss, L | 24.95 ± 5.58 | 14.80 ± 4.16 | 8.27 ± 2.40 | 7.82 ± 1.81 |
| Pharmacokinetic parameters (mean ± SD) . | 30 mg (n = 6) . | 90 mg (n = 6) . | 300 mg (n = 6) . | 600 mg (n = 6) . |
|---|---|---|---|---|
| Cmax, ng/mL | 3080 ± 389 | 10 800 ± 4 110 | 52 800 ± 13 200 | 93 300 ± 14 200 |
| tmax,* h | 0.21 (0.17, 0.29) | 0.23 (0.18, 0.29) | 0.26 (0.17, 0.34) | 0.51 (0.42, 0.52) |
| AUC0-last, ng*h/mL | 4510 ± 472 | 12 500 ± 3 470 | 61 000 ± 15 400 | 117 000 ± 17 400 |
| AUC0-∞, ng*h/mL | 4710 ± 508 | 12 600 ± 3 450 | 61 400 ± 15 400 | 118 000 ± 17 300 |
| t1/2, h | 7.25 ± 2.14 | 7.38 ± 2.21 | 7.46 ± 1.58 | 6.40 ± 1.88 |
| lz, 1/h | 0.10 ± 0.03 | 0.11 ± 0.06 | 0.10 ± 0.02 | 0.11 ± 0.02 |
| CL, L/h | 6.30 ± 0.68 | 6.24 ± 0.92 | 5.13 ± 1.16 | 5.18 ± 0.64 |
| Vd, L | 65.27 ± 17.61 | 67.29 ± 23.05 | 55.39 ± 19.89 | 48.49 ± 18.46 |
| Vss, L | 24.95 ± 5.58 | 14.80 ± 4.16 | 8.27 ± 2.40 | 7.82 ± 1.81 |
tmax is presented as median (minimum, maximum).