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Table 3 Pharmacokinetic parameters

From: Safety, tolerability, pharmacokinetics, and pharmacodynamics of the afucosylated, humanized anti-EPHA2 antibody DS-8895a: a first-in-human phase I dose escalation and dose expansion study in patients with advanced solid tumors

  Step 1 Step 2
0.1 mg/kg (N = 3) 0.3 mg/kg (N = 3) 1.0 mg/kg (N = 3) 3.0 mg/kg (N = 3) 10 mg/kg (N = 3) 20 mg/kg (N = 7) 20 mg/kg
(N = 15)
Cycle 1, n 2 3 3 3 3 6 14
 Cmax, μg/mL 1.70 ± 0.02 5.90 ± 1.18 21.3 ± 8.30 64.4 ± 15.2 169 ± 31.9 545 ± 170 369 ± 73.2
 Tmax, h 3.88 (3.77, 4.00) 3.97 (1.05, 4.07) 3.96 (1.12, 7.00) 4.00 (3.97, 6.90) 6.73 (4.33, 6.97) 3.91 (2.25, 6.88) 3.43 (2.22, 7.00)
 AUClast, μg·day/mL 0.86 ± 0.61 23.2 ± 6.03 124 ± 12.4 423 ± 29.7 943 ± 72.5 2570 ± 457 2340 ± 558
 AUCtau, μg·day/mL 1.62 ± 1.03 24.4 ± 4.99 125 ± 12.1 423 ± 29.6 944 ± 73.1 2570 ± 460 2270 ± 534
 AUCinf, μg·day/mL NCa ± NCb 33.1 ± 7.27 227 ± 15.8 671 ± 188 1530 ± 439 4520 ± 1910 4500 ± 1700
 T1/2, day NCa ± NCb 4.94 ± 1.32 12.6 ± 4.43 9.69 ± 4.39 9.95 ± 3.62 11.6 ± 7.52 13.9 ± 6.60
Cycle 2, n 1 2 3 2 0 4 11
 Cmax, μg/mL 1.60 ± NCb 9.54 ± 2.78 32.2 ± 2.12 86.8 ± 10.7 618 ± 151 489 ± 105
 Ctrough, μg/mL 0.00 ± NCb 0.54 ± 0.76 10.5 ± 0.23 28.4 ± 0.50 188 ± 67.7 148 ± 54.6
 Tmax, h 1.18 (1.18, 1.18) 5.48 (3.97, 7.00) 3.68 (1.13, 24.13) 5.44 (4.00, 6.88) 3.11 (2.13, 6.70) 4.00 (2.05, 6.88)
 AUCtau, μg·day/mL 9.14 ± NCb 37.1 ± 5.93 259 ± 27.1 715 ± 13.8 4630 ± 1140 3500 ± 1140
 T1/2, day 4.78 ± NCb 4.08 ± 0.91 13.3 ± 1.73 10.8 ± 0.13 12.4 ± 6.76 13.6 ± 8.14
  1. Data are presented as mean ± standard deviation, or median (min, max), pharmacokinetic analysis set
  2. Abbreviations: C concentration, T time, AUC area under the curve, T1/2 terminal elimination half-life, NC not calculated
  3. aDate and time data of DS-8895a were not available so values were NC
  4. bTwo or fewer values were available so standard deviation could not be calculated