Table 3.

Selected mean (SD) pharmacokinetic parameters for total antibody and unconjugated MMAE after DLYE5953A treatment at cycle 1.

Total antibody	Number of patients^a	C_max (μg/mL)	AUC_0-inf (day*μg/mL)	t_1/2 (day)	V_ss (mL/kg)	CL (mL/day/kg)
Cohorts:
0.2 mg/kg	3	3.45	13.6	7.05	126	16.6
		(1.14)	(6.2)	(1.61)	(39)	(6.1)
0.4 mg/kg	3	7.74	29.8	8.38	109	13.6
		(0.62)	(3.6)	(1.89)	(13.9)	(1.8)
0.8 mg/kg	3	16.1	89.7	13.3	129	10.1
		(4.6)	(37.1)	(1.2)	(41)	(4.0)
1.6 mg/kg	4	36.9	141	4.97	71.6	12.0
		(8.9)	(37)	(1.94)	(27.3)	(2.5)
2.4 mg/kg	7	44.1	219	7.60	90.5	11.9
		(11.5)	(69)	(2.709)	(20.4)	(3.3)
2.4 mg/kg	22	47.0	258	7.02	88.0	10.0
MBC		(9.7)	(77)	(2.31)	(24.4)	(2.7)
2.4 mg/kg	24	46.4	253	7.27	87.4	10.9
NSCLC		(7.6)	(101)	(2.38)	(20.9)	(4.4)

Unconjugated MMAE	Number of patients^a	C_max (ng/mL)	AUC_0-inf (day*ng/mL)	t_max (day)
Cohorts:
0.2 mg/kg	3	0.461	3.18	1.64
		(0.057)	(0.61)	(0.57)
0.4 mg/kg	3	0.728	7.13	1.65
		(0.161)	(NA)	(0.57)
0.8 mg/kg	3	1.69	13.4	2.01
		(1.05)	(11.7)	(0.05)
1.6 mg/kg	4	6.17	66.6	5.43
		(3.85)	(35.6)	(6.95)
2.4 mg/kg	7	6.07	53.1	3.01
		(2.26)	(27)	(2.62)
2.4 mg/kg	14	4.08	34.9	3.10
MBC		(2.08)	(18.2)	(3.46)
2.4 mg/kg	10	4.85	36.5	2.71
NSCLC		(2.44)	(16.8)	(2.23)

Abbreviations: AUC_0-inf, area under the concentration−time curve from time zero extrapolated to infinite time; CL, clearance; C_max, maximum observed plasma concentration; V_ss, volume of distribution at steady state; t_1/2, terminal half-life; t_max, time to reach maximum concentration.
↵^aNumber of patients with at least one pharmacokinetic parameter estimated.