Table 4.
Pharmacokinetic Parameters (Mean ± SD) of Netupitant and Its Metabolites M1, M2, and M3 After Oral Dose of NEPA (300‐mg Netupitant/0.50‐mg Palonosetron)—PK‐R Analysis Set
| Pharmacokinetic Parameter | Netupitant (N = 129) | M1 (N = 129) | M2 (N = 129) | M3 (N = 129) |
|---|---|---|---|---|
| Cmax, μg/L | 477.3 ± 231.6 | 39.3 ± 14.0 | 213.9 ± 108.1 | 66.0 ± 22.2 |
| AUC0‐last, μg • h/L | 11317 ± 4278 | 3057 ± 879.5 | 2640 ± 1541 | 3783 ± 1303 |
| AUC0‐inf, μg • h/L | 13899 ± 5549 | 4819 ± 1847 | 2993 ± 1766 | 4620 ± 1845 |
|
tmax, h Median [min–max] |
4 [2–12] |
8 [5–72] |
4 [2–6] |
12 [4–48] |
| t1/2, h | 51.6 ± 30.9 | 76.9 ± 27.6 | 43.2 ± 50.0 | 46.4 ± 16.3 |
AUC0‐inf, 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 the time of last measurable concentration; Cmax, maximum plasma concentration; M1, M2, and M3, main netupitant metabolites; Max, maximum; Min, minimum; P, pilot crossover part; PK‐R, restricted pharmacokinetic; S, single‐ascending‐dose/single‐ascending‐dose crossover part; SD, standard deviation; t1/2, elimination half‐life; tmax, time to reach maximum concentration of drug in plasma.