Table 3.
AZD5718 Pharmacokinetic Parameters
| AZD5718 200 mg | ||||
|---|---|---|---|---|
| Fasted | Fed | |||
| Parameter | Tablet Plus Rosuvastatin 10 mg (n = 12) | Tablet (n = 12) | Suspension (n = 12) | Tablet (n = 12) |
| AUC0‐∞, nmol·h/L | ||||
| Arithmetic mean (SD) | 3674 (824.0) | 3623 (710.4)a | 5000 (1102)a | 3397 (748.4) |
| Geometric mean (%CV) | 3591 (22.6) | 3559 (20.1)a | 4892 (22.2)a | 3330 (20.5) |
| AUC0‐last, nmol·h/L | ||||
| Arithmetic mean (SD) | 3548 (832.9) | 3491 (667.5) | 4751 (1046) | 3268 (699.5) |
| Geometric mean (%CV) | 3459 (24.0) | 3432 (19.7) | 4649 (21.8) | 3207 (19.9) |
| Cmax, nmol/L | ||||
| Artihmetic mean (SD) | 567.1 (165.3) | 565.3 (191.2) | 1246 (485.1) | 426.8 (147.7) |
| Geometric mean (%CV) | 544.9 (30.4) | 530.2 (41.1) | 1170 (37.3) | 409.2 (29.0) |
| t½λz, h | ||||
| Arithmetic mean (SD) | 15.0 (7.24) | 14.0 (5.35)a | 13.6 (3.36)a | 13.7 (2.46) |
| Geometric mean (%CV) | 13.9 (38.4) | 13.2 (34.4)a | 13.2 (25.2)a | 13.5 (18.4) |
| tmax, h | ||||
| Median (range) | 2.01 (2.00‐5.05) | 3.00 (2.00‐5.00) | 1.00 (0.98‐2.02) | 4.00 (3.00‐5.98) |
| CL/F, L/h | ||||
| Arithmetic mean (SD) | 127.6 (28.12) | 128.1 (25.63)a | 93.55 (20.40)a | 136.9 (25.53) |
| Geometric mean (%CV) | 124.6 (22.6) | 126.0 (20.1)a | 91.5 (22.2)a | 134.4 (20.4) |
AUC0‐∞, area under the plasma concentration‐time curve from time 0 to infinity; AUC0‐last, area under the plasma concentration‐time curve from time 0 to time of last quantifiable concentration; Cmax, maximum observed plasma concentration; CL/F, total body clearance of drug from plasma; CV, coefficient of variation; SD, standard deviation; tmax, time to reach maximum observed plasma concentration; t½λz, plasma half‐life associated with terminal slope of a semilogarithmic concentration‐time curve.
Molecular weight of AZD5718 is 446.5 g/mol.
a
n = 10.