Table 5.
Predicted apixaban steady‐state exposure and anti‐FXa activity in VTE treatment population
|
Steady‐state parameter (units) |
2.5 mg b.i.d. | 5 mg b.i.d. | 10 mg b.i.d. | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Median (90% CI) | 5th Percentile (90% CI) | 95th Percentile (90% CI) | Median (90% CI) | 5th Percentile (90% CI) | 95th Percentile (90% CI) | Median (90% CI) | 5th Percentile (90% CI) | 95th Percentile (90% CI) | |
| Daily (0‐24 hours) AUCss (ng*hr/mL) |
1,240 (1,185, 1,301) |
655 (606, 707) |
2,437 (2,240, 2,649) |
2,446 (2,346, 2,554) |
1,293 (1,197, 1,398) |
4,807 (4,433, 5,174) |
4,649 (4,439, 4,875) |
2,456 (2,271, 2,664) |
9,136 (8,445, 9,836) |
|
Cmax
(ng/mL) |
67.0 (63.7, 70.7) |
29.7 (26.9, 33.1) |
153.2 (138.9, 168.4) |
132.3 (125.2, 139.3) |
58.6 (52.9, 64.7) |
302.2 (273.3, 331.9) |
251.2 (237.5, 265.2) |
111.4 (100.2, 123.2) |
572.4 (516.0, 630.1) |
|
Cmin
(ng/mL) |
32.0 (29.9, 34.2) |
11.0 (9.4, 12.6) |
89.5 (79.6, 100.0) |
63.2 (59.0, 67.9) |
21.7 (18.8, 25.3) |
176.5 (156.5, 196.2) |
120.2 (112.1, 129.2) |
41.1 (35.0, 47.6) |
334.5 (295.8, 378.8) |
| Anti‐FXa activity at Cmax (IU/mL) |
1.07 (1.01, 1.12) |
0.47 (0.43, 0.53) |
2.44 (2.21, 2.68) |
2.10 (1.99, 2.21) |
0.93 (0.84, 1.03) |
4.80 (4.35, 5.28) |
3.99 (3.78, 4.22) |
1.77 (1.59, 1.96) |
9.10 (8.20, 10.02) |
| Anti‐FXa activity at Cmin (IU/mL) |
0.51 (0.48, 0.54) |
0.17 (0.15, 0.20) |
1.42 (1.27, 1.59) |
1.00 (0.94, 1.08) |
0.35 (0.30, 0.40) |
2.81 (2.49, 3.12) |
1.91 (1.78, 2.05) |
0.65 (0.56, 0.76) |
5.32 (4.70, 6.02) |
AUCss, area under the concentration–time curve; b.i.d., twice daily; CI, confidence interval; Cmax, peak plasma concentration; Cmin, trough plasma concentration; VTE, venous thromboembolism.