Table 3.
Study | Patients | Weight (kg) | Daily dose | Sampling day | C max (µg/mL) | C trough (µg/mL) | t max (h) | k a (h−1) | V d/F (L) | CL/F (L/h) | AUC (mg·h/mL) | t ½ (h) |
---|---|---|---|---|---|---|---|---|---|---|---|---|
Compartmental | ||||||||||||
Kanyok et al. [36] | Healthy volunteers | |||||||||||
12 mg/kg | 68.2±14.0 | 12 mg/kg (9 mg/kg base), single dose | Single dose | 21.6 ± 2.3 | <LLOQ | 1.19 ± 0.46 | 6.27 ± 4.41 | 0.35±0.04b,c | 7.1 ± 0.78d | AUC∞: 86.3 ± 15.0 | 2.21 ± 0.17 | |
15 mg/kg | 70.7±13.0 | 15 mg/kg (11 mg/kg base), single dose | Single dose | 23.4 ± 3.9 | <LLOQ | 1.51 ± 0.40 | 2.65 ± 1.29 | 0.41 ± 0.06b,c | 7.6 ± 1.94d | AUC∞: 104.5 ± 26.3 | 2.64 ± 0.82 | |
Kshirsagar et al. [38] | Visceral leishmaniasis patients | 35.5±11.8a | 15 mg/kg (11 mg/kg base), 21 days | Day 1 | 20.5 ± 7.01 | 4.53 ± 6.71 | NA | 2.11 (7.68%)e | 15.3 (2.27%)e | 4.06 (3.05%)e
IIV: 30.7% |
NA | 2.62 |
Day 21 | 18.3 ± 8.86 | 1.31 ± 4.16 |
Data given as mean ± standard deviation, unless indicated otherwise
AUC area under the concentration–time curve, AUC 24 AUC from time zero to 24 h, AUC ∞ AUC from time zero to infinity, CL clearance, C max peak plasma concentration, C trough trough plasma concentration 24 h after dose, F bioavailability, IIV inter-individual variability, k a absorption rate constant, <LLOQ below lower limit of quantitation, NA not available, t ½ plasma elimination half-life, t max time to C max, V d volume of distribution
aNot provided on poster [38], but provided for 501 patients included in clinical results of trial [33]: used as proxy for 448 of these 501 patients included in population pharmacokinetic model
b V β, apparent volume of distribution during the β-elimination phase
cPer kg
dPer 1.73 m2, reported as 117.7 and 126.0 mL/min, converted to L/h
eMean (% standard error)