Table 1.
Pharmacokinetic parameters and statistical analyses after a single oral 90-mg dose of ticagrelor in the presence and absence of diltiazem.
| Parameter* | Ticagrelor (90 mg) alone n = 17 | Ticagrelor (90 mg) plus diltiazem (240 mg qd) n = 17 | GLS mean ratio: point estimate (90% CI) |
|---|---|---|---|
| Ticagrelor | |||
| Cmax (ng/mL) | 519 (34) | 878 (30) | 1.69 (1.47–1.95) |
| AUC (ng·h/mL) | 3701 (37) | 10,099 (24) | 2.74 (2.40–3.13) |
| t½ (h) | 8.3 (2.3) | 16.3 (4.4) | – |
| tmax (h) | 2.0 (1.0–4.0) | 2.0 (2.0–4.0) | – |
| AR-C124910XX | |||
| Cmax (ng/mL) | 173 (38) | 109 (36) | 0.62 (0.57–0.68) |
| AUC (ng·h/mL) | 1630 (29) | 1424 (29) | 0.87 (0.83–0.92) |
| t½ (h) | 8.4 (1.3) | 12.5 (4.7) | – |
| tmax (h) | 3.0 (2.0–4.0) | 3.0 (2.0–4.0) | – |
| Metabolite:parent ratios | |||
| Cmax ratio | 0.3 (36) | 0.1 (24) | – |
| AUC ratio | 0.4 (39) | 0.1 (28) | – |
*Values are: geometric mean (% CV) for Cmax, AUC and metabolite:parent ratios; mean (standard deviation) for t½; median (range) for tmax. qd, once daily; GLS, geometric least-square; CI, confidence interval; Cmax, maximum plasma concentration; AUC, area under the plasma concentration–time curve from time 0 to infinity; t½, terminal elimination half-life; tmax, time to Cmax.