Andexanet PK parameters in the presence of apixaban (phase 2 study)
| Pharmacokinetic parameters (mean ± SD) . | Andexanet dose (n = 6/cohort) . | |||||
|---|---|---|---|---|---|---|
| 90 mg bolus (cohort 1) . | 210 mg bolus (cohort 2) . | 420 mg bolus (cohort 3) . | 420/4 × 45 min (cohort 4) . | 420/180 (cohort 5) . | 420/4 × 2 h (cohort 6) . | |
| Cmax, ng/mL | 21 200 ± 2 400 | 42 800 ± 5 620 | 81 400 ± 10 900 | 93 300 ± 18 400 | 88 000 ± 9 010 | 90 800 ± 29 600 |
| tmax,* h | 0.07 (0.07, 0.08) | 0.15 (0.14, 0.30) | 0.27 (0.26, 0.29) | 0.43 (0.25, 0.52) | 0.27 (0.26, 0.31) | 0.28 (0.272, 0.29) |
| AUC0-last, ng*h/mL | 23 200 ± 3 490 | 49 100 ± 3 980 | 93 400 ± 15 500 | 131 000 ± 20 500 | 155 000 ± 16 200 | 213 000 ± 33 900 |
| AUC0-∞, ng*h/mL | 23 400 ± 3 460 | 49 200 ± 3 960 | 93 500 ± 15 500 | 131 000 ± 20 500 | 155 000 ± 16 200 | 213 000 ± 33 900 |
| t1/2, h | 5.51 ± 0.84 | 5.12 ± 1.66 | 5.02 ± 2.02 | 4.35 ± 1.40 | 5.79 ± 2.00 | 6.45 ± 0.41 |
| lz, 1/h | 0.13 ± 0.02 | 0.14 ± 0.03 | 0.16 ± 0.05 | 0.17 ± 0.04 | 0.14 ± 0.06 | 0.11 ± 0.01 |
| CL, L/h | 3.93 ± 0.63 | 4.29 ± 0.33 | 4.60 ± 0.81 | 4.70 ± 0.89 | ND | 4.30 ± 0.61 |
| Vss, L | 6.97 ± 1.42 | 6.18 ± 1.31 | 6.26 ± 0.74 | 5.11 ± 1.64 | ND | 4.01 ± 0.95 |
| Pharmacokinetic parameters (mean ± SD) . | Andexanet dose (n = 6/cohort) . | |||||
|---|---|---|---|---|---|---|
| 90 mg bolus (cohort 1) . | 210 mg bolus (cohort 2) . | 420 mg bolus (cohort 3) . | 420/4 × 45 min (cohort 4) . | 420/180 (cohort 5) . | 420/4 × 2 h (cohort 6) . | |
| Cmax, ng/mL | 21 200 ± 2 400 | 42 800 ± 5 620 | 81 400 ± 10 900 | 93 300 ± 18 400 | 88 000 ± 9 010 | 90 800 ± 29 600 |
| tmax,* h | 0.07 (0.07, 0.08) | 0.15 (0.14, 0.30) | 0.27 (0.26, 0.29) | 0.43 (0.25, 0.52) | 0.27 (0.26, 0.31) | 0.28 (0.272, 0.29) |
| AUC0-last, ng*h/mL | 23 200 ± 3 490 | 49 100 ± 3 980 | 93 400 ± 15 500 | 131 000 ± 20 500 | 155 000 ± 16 200 | 213 000 ± 33 900 |
| AUC0-∞, ng*h/mL | 23 400 ± 3 460 | 49 200 ± 3 960 | 93 500 ± 15 500 | 131 000 ± 20 500 | 155 000 ± 16 200 | 213 000 ± 33 900 |
| t1/2, h | 5.51 ± 0.84 | 5.12 ± 1.66 | 5.02 ± 2.02 | 4.35 ± 1.40 | 5.79 ± 2.00 | 6.45 ± 0.41 |
| lz, 1/h | 0.13 ± 0.02 | 0.14 ± 0.03 | 0.16 ± 0.05 | 0.17 ± 0.04 | 0.14 ± 0.06 | 0.11 ± 0.01 |
| CL, L/h | 3.93 ± 0.63 | 4.29 ± 0.33 | 4.60 ± 0.81 | 4.70 ± 0.89 | ND | 4.30 ± 0.61 |
| Vss, L | 6.97 ± 1.42 | 6.18 ± 1.31 | 6.26 ± 0.74 | 5.11 ± 1.64 | ND | 4.01 ± 0.95 |
ND, not determined.
tmax is presented as median (minimum, maximum); time relative to the start of the first andexanet bolus dose.