Table 2.
Apixaban pharmacokinetic parameters following a single- and multiple-dose (days 1 and 7) administration [21]
Reproduced with permission from Frost et al. Br J Clin Pharmacol. 2013;76:776–86
| Apixaban dose (mg) and regimen |
Cmax (ng/mL), GM (CV %) |
Cmina (ng/mL), GM (CV %) |
AUCtaub (ng·h/mL), GM (CV %) |
Tmax (h), median (min, max) |
AI, GM (CV %) |
t1/2 (h), mean (SD) |
|---|---|---|---|---|---|---|
| Day 1 | ||||||
| 2.5 BID (n = 6) | 51.0 (27) | 14.2 (53) | 353.3 (25) | 3.5 (2.0, 12.0) | – | – |
| 5 BID (n = 6) | 81.9 (18) | 25.3 (20) | 600.6 (20) | 3.5 (3.0, 6.0) | – | – |
| 10 BID (n = 6) | 226.2 (38) | 72.7 (27) | 1608.3 (30) | 4.0 (2.0, 4.0) | – | – |
| 25 BID (n = 6) | 425.3 (24) | 129.0 (33) | 3108.6 (25) | 3.5 (2.0, 4.0) | – | – |
| 10 QD (n = 6) | 178.4 (19) | 14.5 (27) | 1589.6 (20) | 4.0 (3.0, 4.0) | – | – |
| 25 QD (n = 6) | 310.0 (12) | 36.5 (31) | 2868.1 (7) | 4.0 (2.0, 6.0) | – | – |
| Day 7 | ||||||
| 2.5 BID (n = 5) | 62.3 (37) | 21.0 (17) | 462.8 (35) | 3.0 (3.0, 9.0) | 1.3 (18) | 8.1 (1.8) |
| 5 BID (n = 6) | 128.5 (10) | 49.6 (20) | 1051.9 (9) | 4.0 (2.0, 4.0) | 1.8 (22) | 11.7 (3.3) |
| 10 BID (n = 6) | 329.8 (45) | 103.8 (57) | 2424.9 (47) | 3.0 (2.0, 4.0) | 1.5 (33) | 10.9 (2.9) |
| 25 BID (n = 6) | 716.6 (21) | 281.1 (38) | 5850.3 (16) | 3.5 (1.0, 4.0) | 1.9 (17) | 15.2 (7.2) |
| 10 QD (n = 6) | 201.4 (15) | 26.8 (43) | 2015.7 (16) | 3.5 (3.0, 4.0) | 1.3 (23) | 14.9 (7.2) |
| 25 QD (n = 6) | 428.9 (20) | 55.3 (33) | 4248.3 (19) | 3.0 (2.0, 4.0) | 1.5 (17) | 15.3 (4.3) |
AI accumulation index, AUCtau area under the plasma concentration–time curve from time zero to the time of last measureable concentration, BID twice daily, Cmax maximum plasma concentration, Cmin minimum plasma concentration, CV % percentage coefficient of variance, GM geometric mean, h hours, QD once daily, SD standard deviation, t1/2 plasma terminal half-life, Tmax time to Cmax
aCmin defined as apixaban concentration 12 or 24 h after morning dosing for BID or QD regimens, respectively
btau = 12 h for BID panels and 24 h for QD panels