Table 3.
Pharmacokinetic Parameters (Mean ± SD) of Fosnetupitant, Netupitant, and Its Metabolites M1, M2, and M3 After IV Infusion of 235‐mg Dose of Fosnetupitant—PK‐R Analysis Set
| Pharmacokinetic Parameter | Fosnetupitant (N = 30) | Netupitant (N = 30) | M1 (N = 30) | M2 (N = 30) | M3 (N = 30) |
|---|---|---|---|---|---|
| Cmax, μg/L | 6431 ± 911.3 | 840.8 ± 172.6 | 26.1 ± 4.6 | 172.0 ± 78.7 | 54.1 ± 12.1 |
| AUC0‐last, μg • h/L | 2934 ± 362.3 | 12014 ± 2340 | 2326 ± 352.9 | 2583 ± 1254 | 3454 ± 739.9 |
| AUC0‐inf, μg • h/L | 2938 ± 362.1 | 13854 ± 2957 | 4070 ± 1667 | 2935 ± 1456 | 4313 ± 1183 |
|
tmax, h Median [min–max] |
0.5 [0.3–0.5] |
0.5 [0.5–4] |
12 [2–48] |
3 [0.5–4] |
24 [4–48] |
| t1/2, h | 0.956 ± 0.553 | 36.05 ± 6.812 | 89.34 ± 47.41 | 36.09 ± 24.77 | 47.32 ± 22.73 |
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; IV, intravenous; 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.