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
C_max, 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
T_max, 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)
AUC_last, μg·day/mL	0.86 ± 0.61	23.2 ± 6.03	124 ± 12.4	423 ± 29.7	943 ± 72.5	2570 ± 457	2340 ± 558
AUC_tau, μg·day/mL	1.62 ± 1.03	24.4 ± 4.99	125 ± 12.1	423 ± 29.6	944 ± 73.1	2570 ± 460	2270 ± 534
AUC_inf, μg·day/mL	NC^a ± NC^b	33.1 ± 7.27	227 ± 15.8	671 ± 188	1530 ± 439	4520 ± 1910	4500 ± 1700
T_1/2, day	NC^a ± NC^b	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
C_max, μg/mL	1.60 ± NC^b	9.54 ± 2.78	32.2 ± 2.12	86.8 ± 10.7	–	618 ± 151	489 ± 105
C_trough, μg/mL	0.00 ± NC^b	0.54 ± 0.76	10.5 ± 0.23	28.4 ± 0.50	–	188 ± 67.7	148 ± 54.6
T_max, 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)
AUC_tau, μg·day/mL	9.14 ± NC^b	37.1 ± 5.93	259 ± 27.1	715 ± 13.8	–	4630 ± 1140	3500 ± 1140
T_1/2, day	4.78 ± NC^b	4.08 ± 0.91	13.3 ± 1.73	10.8 ± 0.13	–	12.4 ± 6.76	13.6 ± 8.14

Data are presented as mean ± standard deviation, or median (min, max), pharmacokinetic analysis set
Abbreviations: C concentration, T time, AUC area under the curve, T_1/2 terminal elimination half-life, NC not calculated
^aDate and time data of DS-8895a were not available so values were NC
^bTwo or fewer values were available so standard deviation could not be calculated

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