TABLE 1

Measured concentrations and derived pharmacokinetic data of [³H]DM1-LNL897

Concentrations of total radiolabeled components measured by LSC, total and conjugated antibody measured by ELISA, conjugated antibody measured by SEC-RA (expressed in micromolars), and corresponding pharmacokinetic parameters in serum of female tumor-bearing nude rats after a single intravenous administration of [³H]DM1-LNL897 (nominal dose: 10 mg/kg).

Parameter	Total RA (LSC)			ELISA						Conjugated Antibody (SEC)^{^a}
	Total RA (LSC)			Total Antibody			Conjugated Antibody
	Mean	S.D.	CV	Mean	S.D.	CV	Mean	S.D.	CV
			%			%			%
1 hour	1.39	0.0764	5.48	1.25	0.0557	4.46	1.42	0.0279	1.97	1.31
24 hours	0.585	0.0286	4.89	0.577	0.0128	2.22	0.664	0.00873	1.31	0.483
96 hours	0.197	0.0159	8.05	0.214	0.0034	1.61	0.268	0.012	4.47	0.147
168 hours	0.0835	0.00683	8.18	0.107	0.00979	9.17	0.133	0.0133	9.98	0.0457
Actual dose (mg/kg)	10	0.0808	0.807	10	0.0808	0.807	10	0.0808	0.807	10
T_max (hour)	1.0^{^b} (1.0–1.0)]^{^c}			1.0^{^b} (1.0–1.0)^{^c}			1.0^{^b} (1.0–1.0)^{^c}
C_max (µM)	1.39	0.0764	5.48	1.25	0.0557	4.46	1.42	0.0279	1.97
C_max/dose (µM)/(mg/kg)	0.139	0.00717	5.16	0.125	0.0055	4.43	0.142	0.0021	1.49
T_last (hour)	168^{^b} (168–168)^{^c}			168^{^b} (168–168)^{^c}			168^{^b} (168–168)^{^c}
AUC_last (h·µM)	62.4	2.08	3.34	62.3	0.749	1.2	73.4	1.33	1.81
AUC_inf (h·µM)	68.6	1.72	2.5	71.5	0.721	1.01	85.4	2.77	3.25
T_1/2 (hour)	51.3	2.45	4.77	59.2	4.02	6.79	62.2	4.09	6.58
T_1/2 range (hour)	(24–168)			(24–168)			(24–168)
V_ss (l/kg)	NC			NC			0.617	0.00295	4.77

NC, not calculated.
↵^a Aggregate peak and ADC peak values were summed to calculate concentrations.
↵^b Median.
↵^c Range.