Table 2.
Effect of administration with food compared with fasting on pharmacokinetics of ticagrelor and AR-C124910XX and % IPA (Final Extent, 20 µm ADP) after administration of ticagrelor 200 mg once daily or bid
| Pharmacokinetics | Mean % IPA (range) | ||||||
|---|---|---|---|---|---|---|---|
| AUC(0,τ) (ng ml−1 h) | Cmax(ng ml−1) | tmax(h) | 4 h | 8 h | 12 h | 24 h | |
| Once daily ticagrelor | |||||||
| 200 mg, fasting, day 5 (n = 7) | 10 603 (41) | 1304 (44) | 3.00 (1.50–4.00) | 99 (97–100) | 98 (93–100) | 98 (91–100) | 89 (67–100) |
| 200 mg, fed, Day 1 (n = 7) | 12 768 (42) | 1525 (39) | 3.00 (1.33–4.00) | 100 (100–100) | 95 (86–100) | 97 (89–100) | 80 (34–100) |
| Twice daily ticagrelor | |||||||
| 200 mg, fasting, day 5 (n = 6) | 10 160 (26) | 1583 (26) | 2.00 (2.00–4.00) | 97 (85–100) | 98 (89–100) | 96 (79–100) | 96 (76–100) |
| 200 mg, fed, day 1 (n = 6) | 13 335 (14) | 1763 (24) | 4.00 (3.00–12.00) | 96 (79–100) | 95 (73–100) | 95 (69–100) | 94 (66–100) |
| AR-C124910XX (after once daily dosing) | |||||||
| 200 mg, fasting, day 5 (n = 7) | 4 164 (35) | 385 (35) | 4.00 (2.00–4.12) | – | – | – | – |
| 200 mg, fed, day 1 (n = 7) | 4 079 (39) | 358 (23) | 4.00 (1.83–6.00) | – | – | – | – |
| AR-C124910XX (after twice daily dosing) | |||||||
| 200 mg, fasting, day 5 (n = 6) | 4 423 (71) | 555 (65) | 3.50 (2.00–4.00) | – | – | – | – |
| 200 mg, fed, day 1 (n = 6) | 4 887 (56) | 568 (52) | 5.00 (3.00–12.00) | – | – | – | – |
Data for tmax are median (range); all other pharmacokinetic data are geometric mean (coefficient of variation, %).