TABLE 2.
PK parameters following single intravenous dose of difelikefalin or pentazocine
| Parameter mean (SD) | Difelikefalin 5 mcg/kg (n = 41) | Difelikefalin 15 mcg/kg (n = 40) | Pentazocine 0.5 mg/kg (n = 40) |
|---|---|---|---|
| Cmax (ng/ml) | 61.9 (23.9) | 168.8 (52.6) | 296.0 (197.7) |
| Tmax (h) a | 0.1 [0.1, 0.3] | 0.1 [0.1, 0.3] | 0.1 [0.1, 0.8] |
| AUC0–t (h*ng/ml) | 94.0 (23.8) | 246.0 (40.1) | 487.4 (133.5) |
| t 1/2 (h) | 2.0 (0.2) | 2.0 (0.2) | 3.7 (1.2) |
| V d (ml/kg) | 155 (39.3) | 171 (28.0) | 4280 (1079.8) |
PK population = all randomized subjects who received ≥1 dose of study drug in the treatment phase and had adequate plasma concentration‐time data to allow for meaningful PK analysis.
Each treatment was separated by a 48‐hour washout period, which largely exceeded each treatment half‐life (t1/2) of 2 to 4 hours.
Abbreviations: AUC0–t, area under the plasma concentration‐time curve from time zero to the last quantifiable concentration; Cmax, maximum observed plasma concentration; PK, pharmacokinetic; SD, standard deviation; Tmax, time to maximum observed plasma concentration; t1/2, apparent plasma terminal elimination half‐life; Vd, apparent volume of distribution.
Median [range].