Table 1.
Pharmacokinetic parameters for ticagrelor and AR‐C124910XX on day 1 and day 7 in Chinese patients with stable coronary artery disease treated with low dose aspirin plus ticagrelor 45 mg twice daily, 60 mg twice daily or 90 mg twice daily
| Parameter * | Ticagrelor 45 mg twice daily (n = 12) | Ticagrelor 60 mg twice daily (n = 12) | Ticagrelor 90 mg twice daily (n = 12) | |||
|---|---|---|---|---|---|---|
| Day 1 | Day 7 | Day 1 | Day 7 | Day 1 | Day 7 | |
| Ticagrelor | ||||||
| C max (ng ml –1 ) | 464 (38) | 616 (37) | 414 (34) | 689 (34) | 822 (37) | 1273 (43) |
| t max (h) † | 2.00 (1.00–2.00) | 2.00 (1.00–3.03) | 3.00 (1.00–6.00) | 2.00 (1.00–3.00) | 2.00 (1.00–3.03) | 2.00 (1.00–3.00) |
| t ½ (h) | 10.72 (16.18) | – | 9.42 (13.53) | – | 10.14 (17.54) | – |
| AUC (ng ml –1 h) | 3220 (51) | – | 3633 (32) | – | 6234 (54) | – |
| AUC0−12h (ng ml–1 h) | 2114 (42) | 3882 (42) | 2313 (30) | 4351 (37) | 3983 (42) | 8206 (51) |
| R ac | – | 1.84 (23.6) | – | 1.88 (20.7) | – | 2.06 (22.8) |
| AR‐C124910XX | ||||||
| C max (ng ml –1 ) | 88.3 (24.6) | 144 (26) | 77.1 (54) | 180 (50) | 139 (38) | 301 (32) |
| t max (h) † | 2.00 (2.00–3.00) | 2.00 (1.00–6.00) | 3.00 (2.00–6.00) | 2.00 (2.00–3.00) | 3.00 (2.00–3.03) | 2.54 (2.00–3.10) |
| t ½ (h) | 12.65 (22.94)‡ | – | 11.38 (24.27)‡ | – | 11.62 (24.64) | – |
| AUC (ng ml−1 h) | 922 (29)‡ | – | 1108 (35)‡ | – | 1644 (31) | – |
| AUC0−12h (ng ml–1 h) | 464 (19) | 1069 (25) | 504 (55) | 1314 (41) | 836 (30) | 2254 (37) |
| R ac | – | 2.30 (24.7) | – | 2.61 (28.3) | – | 2.70 (27.4) |
*
Values are geometric mean (percentage coefficient of variation) unless otherwise indicated;
†
Median (range);
‡
n = 11.
AUC area under the plasma concentration–time curve; AUC0−12h area under the plasma concentration–time curve from zero to 12 h; C max maximum plasma concentration; Rac accumulation ratio; t ½ half‐life; t max time to maximum plasma concentration.