Table 2.
Plasma pharmacokinetic variables of lucerastat
Study | Dose regimen | Cmax [μg/mL] | tmax [h] | AUC0–12 [μg · h/mL] | AUC0–∞ [μg · h/mL] | t1/2 [h] | |
---|---|---|---|---|---|---|---|
SAD | 100 mg | 1.07 [0.83, 1.39] | 1.25 [1.00, 3.00] | 4.85 [4.13, 5.69] | 5.67 [4.77, 6.71] | 4.43 [3.59, 5.46] | |
300 mg | 2.95 [2.17, 4.01] | 2.00 [1.50, 4.00] | 19.12 [16.27, 22.46] | 19.75 [16.81, 23.20] | 4.98 [4.65, 5.33] | ||
500 mg | 4.27 [3.75, 4.85] | 2.75 [1.50, 3.50] | 26.11 [22.94, 29.72] | 27.27 [24.13, 30.83] | 5.70 [5.11, 6.36] | ||
1000 mg | 10.31 [6.62, 16.05] | 2.25 [1.00, 3.50] | 57.81 [45.07, 74.14] | 60.09 [47.26, 76.41] | 5.40 [4.70, 6.22] | ||
2x1000 mg | 10.52 [7.50, 14.74] | 2.00 [1.50, 2.50] | 116.374 [94.74, 142.96]1 | 118.01 [95.96, 145.12] | 6.47 [5.42, 7.72] | ||
MAD | 200 mg | Day 1 | 1.99 [1.61, 2.47] | 2.00 [1.00, 3.00] | 9.18 [7.35, 11.48] | 22.77 [19.26, 26.92] | 6.10 [4.78, 7.78] |
Day 7 | 2.33 [1.68, 3.24] | 2.00 [1.50, 3.50] | 11.59 [9.72, 13.83] | 28.07 [24.69, 31.91] | 5.88 [4.68, 7.39] | ||
500 mg | Day 1 | 4.82 [4.41, 5.26] | 2.50 [1.50, 3.50] | 23.20 [20.84, 25.83] | 56.87 [50.94, 63.50] | 5.84 [4.88, 6.99] | |
Day 7 | 5.18 [4.54, 5.90] | 2.50 [0.50, 3.50] | 29.37 [25.36, 34.00] | 65.83 [56.70, 76.42] | 6.33 [5.55, 7.21] | ||
1000 mg | Day 1 | 11.39 [9.06, 14.34] | 2. 50 [1.50, 3.00] | 51.67 [47.47, 56.24] | 121.62 [112.03, 132.03] | 5.41 [4.05, 7.23] | |
Day 7 | 11.10 [8.69, 14.19] | 2.50 [1.50, 4.00] | 59.84 [50.97, 70.24] | 132.02 [113.28, 153.87] | 6.83 [5.76, 8.10] |
Data are geometric means (95% CI), except for tmax, for which medians (range) are given. C max maximum plasma concentration, t max time to reach maximum plasma concentration, AUC 0–12 area under plasma concentration–time curve over a dosing interval (12 h), 1area under plasma concentration–time curve from zero to 24 h; AUC 0–∞ area under plasma concentration–time curve from zero to infinity, t 1/2 terminal half–life, CI confidence interval, SAD single ascending dose, MAD multiple ascending dose