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Table 2 Plasma pharmacokinetic variables of lucerastat

From: Lucerastat, an iminosugar with potential as substrate reduction therapy for glycolipid storage disorders: safety, tolerability, and pharmacokinetics in healthy subjects

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]
  1. 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