. Author manuscript; available in PMC: 2020 Oct 1.

Published in final edited form as: Invest New Drugs. 2019 Feb 6;37(5):1052–1060. doi: 10.1007/s10637-019-00731-5

Table 3.

Pharmacokinetic Properties (n = 46): [No. pts, value +/−SD]

	0.3 mg/kg (N=3)	0.6 mg/kg (N=3)	1.2 mg/kg (N=3)	1.8 mg/kg (N=3)	2.4 mg/kg (N=17)	2.7 mg/kg (N=15)	3.0 mg/kg (N=2)
ADC
Study Week 1
AUC(d0–21): day*mg/mL	3, 26.9 +/− 2.06	3, 55.3 +/− 12.54	3, 122.3 +/− 4.93	3, 131.7 +/− 10.02	3, 239.0 +/− 28.00	4, 213.3 +/− 34.80	-
Cmax: mg/mL	3, 7.1 +/− 0.44	3, 13.1 +/− 3.38	3, 28.1 +/− 1.78	3, 30.9 +/− 2.75	16, 52.3 +/− 9.63	15, 48.9 +/− 21.60	2, 52.1 +/− 2.26
T1/2: days	3, 6.59 +/− 2.015	3, 11.21 +/− 4.643	3, 5.51 +/− 1.373	3, 6.75 +/− 0.718	14, 7.03 +/− 2.142	11, 37.00 +/− 98.515	2, 6.54 +/− 1.810
Tmax: days	3, 0.04 +/− 0.036	3, 0.02 +/− 0.000	3, 0.09 +/− 0.073	3, 0.09 +/− 0.073	16, 0.05 +/− 0.075	15, 0.35 +/− 0.678	2, 0.02 +/− 0.000
Vz: mL/kg	3, 33.6 +/− 8.84	3, 51.9 +/− 24.25	3, 40.5 +/− 40.45	3, 60.2 +/− 38.15	4, 40.8 +/− 14.15	5, 140.1 +/− 122.61	2, 82.1 +/− 16.12
Study Week 4
Cmax: mg/mL	3, 7.5 +/− 1.43	3, 13.8 +/− 3.66	2, 26.6 +/− 3.32	2, 29.1 +/− 6.29	7, 79.8 +/− 48.42	6, 63.0 +/− 47.68	-
T1/2: days	3, 5.8 +/− 3.26	3, 8.1 +/− 1.85	2, 10.0 +/− 0.70	2, 8.3 +/− 3.68	5, 6.7 +/− 1.62	5, 7.4 +/− 1.74	-
TAb
Study Week 1
AUC(d0–21): day*mg/mL	3, 41.6 +/− 5.06	3, 83.4 +/− 14.35	3, 158.3 +/− 6.43	3, 209.7 +/− 39.55	3, 333.7 +/− 32.47	4, 270.3 +/− 27.18	-
Cmax: mg/mL	3, 7.7 +/− 0.56	3, 15.1 +/− 3.76	3, 29.1 +/− 1.50	3, 32.9 +/− 2.72	16, 60.2 +/− 9.80	15, 51.2 +/− 19.02	2, 64.3 +/− 7.78
T1/2: days	3, 10.16 +/− 3.781	3, 9.96 +/− 1.283	3, 6.84 +/− 1.820	3, 9.23 +/− 2.185	14, 8.77 +/− 1.892	11, 9.14 +/− 2.064	2, 9.97 +/− 3.295
Tmax: days	3, 0.1 +/− 0.07	3, 0.0 +/− 0.00	3, 0.1 +/− 0.07	3, 0.1 +/− 0.07	16, 0.1 +/− 0.11	15, 0.4 +/− 0.87	2, 0.1 +/− 0.00
Vz: mL/kg	3, 22.2 +/− 10.86	3, 21.8 +/− 11.26	3, 31.3 +/− 34.86	3, 42.6 +/− 33.16	4, 27.8 +/− 8.54	5, 55.3 +/− 26.74	2, 65.7 +/− 8.98
Study Week 4
Cmax: mg/mL	3, 9.4 +/− 2.22	3, 16.8 +/− 3.80	2, 32.6 +/− 0.64	2, 36.9 +/− 6.93	7, 55.5 +/− 16.47	6, 49.0 +/− 10.34	-
T1/2: days	3, 8.06 +/− 4.178	3, 11.54 +/− 1.577	2, 8.44 +/− 1.266	2, 8.71 +/− 1.259	5, 8.53 +/− 1.753	4, 10.60 +/− 2.717	-
MMAE
Study Week 1
AUC(d0–21): day*mg/mL	2, 9835.0 +/−5465.94	3, 10390.0 +/−2493.81	3, 24733.3 +/−8894.01	2, 35350.0 +/−12798.63	4, 34575.0 +/−1497.50	4, 51675.0 +/−24000.47	1, 122000 +/− -
Cmax: mg/mL	3, 0.7 +/− 0.35	3, 1.1 +/− 0.36	3, 2.2 +/− 0.93	3, 2.7 +/− 1.50	16, 5.3 +/− 3.46	15, 4.8 +/− 2.02	2, 6.1 +/− 4.77
T1/2: days	3, 4.20 +/− 0.441	3, 4.79 +/− 0.534	3, 4.53 +/− 0.099	3, 5.85 +/− 1.584	4, 4.06 +/− 0.281	4, 4.39 +/− 0.976	-
Tmax: days	3, 3.3 +/− 0.58	3, 2.7 +/− 0.58	3, 1.4 +/− 2.26	3, 3.0 +/− 1.00	5, 3.6 +/− 0.55	6, 4.3 +/− 1.86	2, 6.0 +/− 2.83
Study Week 4
Cmax: mg/mL	3, 0.9 +/− 0.72	3, 1.0 +/− 0.09	2, 2.1 +/− 1.11	2, 2.4 +/− 1.47	7, 4.3 +/− 1.34	5, 3.7 +/− 1.12	-