Table 2.
Pharmacokinetic parameters and statistical analyses after a single oral 90-mg dose of ticagrelor in the presence and absence of ketoconazole (200 mg twice daily).
| Parameter* | Ticagrelor (90 mg) alone n = 14 | Ticagrelor (90 mg) plus ketoconazole (200 mg bid) n = 14 | GLS mean ratio: point estimate (90% CI) |
|---|---|---|---|
| Ticagrelor | |||
| Cmax (ng/mL) | 654 (33) | 1537 (30) | 2.35 (2.13–2.60) |
| AUC (ng·h/mL) | 3640 (35) | 26,640 (36) | 7.32 (6.43–8.34) |
| t½ (h) | 7.1 (4.9–9.8) | 25.7 (16.6–31.9) | – |
| tmax (h) | 2.0 (1.0–3.0) | 2.0 (2.0–4.1) | – |
| AR-C124910XX | |||
| Cmax (ng/mL) | 207 (29) | 23 (33) | 0.11 (0.09–0.14) |
| AUC (ng·h/mL) | 1769 (28) | 782 (35) | 0.44 (0.38–0.51) |
| t½ (h) | 8.0 (6.3–16.7) | 20.0 (11.1–37.2) | – |
| tmax (h) | 2.0 (2.0–4.0) | 6.0 (4.0–12.0) | – |
| Metabolite:parent ratios | |||
| Cmax ratio | 0.32 (22) | 0.01 (36) | – |
| AUC ratio | 0.49 (24) | 0.03 (33) | – |
*Values are: geometric mean (% CV) for Cmax, AUC and metabolite:parent ratios; median (range) for t½, and tmax. bid, twice 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.