Table I. .
Steady state pharmacokinetic parameters of ticagrelor and AR-C124910XX following the administration of ticagrelor ± once-daily aspirin.
| Study A |
Study B | ||||||
|---|---|---|---|---|---|---|---|
| Ticagrelor 50 mg bida
|
Ticagrelor 200 mg bidb
|
Ticagrelor 200 mg bidc | |||||
| Parameter | Ticagrelor alone (n = 13) | Ticagrelor + aspirin 300 mg qd (n = 13) | LS means ratio % (90% CI) | Ticagrelor alone (n = 13) | Ticagrelor + aspirin 300 mg qd (n = 13) | LS means ratio % (90% CI) | Ticagrelor + aspirin 75 mg qd (n = 16) |
| Ticagrelor | |||||||
| C max (ng/ml) | 353 (41) | 334 (32) | 96 (80–115) | 1777 (48) | 1697 (47) | 96 (80–116) | 1478 (37) |
| AUC0– τ (ng·h/ml) | 2218 (36) | 2193 (38) | 99 (86–114) | 12 026 (60) | 11 576 (54) | 97 (84–111) | 10 391 (33) |
| t max (h) | 3.0 (2.0–4.0) | 3.0 (1.0–6.0) | NA | 3.0 (1.0–4.0) | 3.0 (2.0–6.0) | NA | 3.1 (1.1–4.2) |
| AR-C124910XX | |||||||
| C max (ng/ml) | 92 (40) | 97 (25) | 106 (92–122) | 490 (20) | 495 (29) | 102 (88–117) | 501 (27) |
| AUC0– τ (ng·h/ml) | 682 (29) | 678 (23) | 100 (90–111) | 4038 (20) | 3951 (26) | 98 (89–109) | 4134 (23) |
| t max (h) | 3.0 (2.0–6.0) | 3.0 (2.0–6.0) | NA | 3.0 (2.0–4.0) | 4.0 (2.0–6.0) | NA | 3.1 (2.0–4.2) |
Data are geometric mean (coefficient of variation) for C max, and AUC0– τ, and median (range) for t max. AUC0– τ = area under the plasma concentration-time curve for the dosing interval; bid = twice daily; C max = maximum plasma concentration; LS mean ratio = least squares mean for ticagrelor as a percentage of the least squares mean for ticagrelor/aspirin; NA = not applicable; qd = once daily; t max = time to reach peak or maximum concentration.
a
50 mg bid for 5 days.
b
200 mg bid for 4 days, then a single 200 mg dose for one day.
c
200 mg bid for 5 days, then a single 200 mg dose for one day.