Summary statistics for PK parameters of unlabeled odanacatib after single doses of 13C-odanacatib 1 mg i.v. with oral or i.v. doses of unlabeled odanacatib
| PK parameter | Dose of unlabeled odanacatib | ||||
|---|---|---|---|---|---|
| 1 mg i.v. (N = 21–24) | 10 mg fasted (N = 23–24) | 50 mg fasted (N = 24) | 50 mg with low-fat meal (N = 12) | 50 mg with high-fat meal (N = 12) | |
| Geometric mean (%CV) | |||||
| AUC0-∞a (µM-h) | 2.7 (41.0) | 15.8 (40.3) | 33.6 (44.3) | 40.5 (55.9) | 52.5 (40.2) |
| AUC0-lasta (µM-h) | 2.1 (44.2) | 14.9 (37.1) | 33.1 (40.2) | 37.0 (50.8) | 49.7 (36.9) |
| Cmaxa (nM) | 56.2 (43.9) | 120.8 (19.9) | 240.3 (20.6) | 283.3 (20.4) | 450.4 (19.7) |
| Tmaxb (h) | 7.5 (1.7, 48.0) | 6.0 (1.7, 96.0) | 5.0 (2.8, 84.0) | 10.5 (2.8, 24.1) | |
| Vssa (liters) | 103.1 (20.4) | ||||
| Cla (l/h) | 0.7 (52.9) | ||||
| Terminal t1/2c (h) | 104.4 (32.7) | 85.8 (21.7) | 84.5 (19.7) | 87.9 (20.9) | 78.7 (13.2) |
| AUC%extrapa | 11.0 (38.6) | 6.6 (103.8) | 6.0 (76.7) | 6.4 (102.7) | 4.5 (67.7) |
N is less than 24 for certain PK parameters because for some subjects AUC0-∞ and t1/2 values could not be determined due to insufficient data in the terminal phase. AUC0-last, AUC from 0 to last time point; AUC%extrap, percentage of AUC extrapolated beyond last time point; Cl, clearance.
↵a Geometric means for indicated parameters are directly calculated, not model based.
↵b Values are reported as the median (minimum, maximum).
↵c Harmonic mean (pseudo-S.D.). Values are observed for terminal t1/2 for i.v. treatments and apparent terminal t1/2 for oral treatments.