TABLE 4

Concentrations (micromolar) and AUC values (micromolar/hour) of [³H]DM1-LNL897 in serum

Concentrations and pharmacokinetic parameters of intact ADCs, ADC complexes, and/or aggregates as well as free small molecule components in serum of tumor-bearing nude rats following a single intravenous administration of 10 mg/kg [³H]DM1-LNL897. Data were derived from SEC-LC with off-line radiodetection obtained after direct injection of serum.

Metabolite/Component	Sample Collection Time				Exposure
Metabolite/Component	1 Hour	24 Hours	96 Hours	168 Hours	AUC_0–168h	Percentage of AUC_0–168h	AUC_inf
	µM	µM	µM	µM	µM·h	%	µM·h
Aggregates/complexes^a	0.119	0.102	0.0558	0.0200	11.0	17.3	12.9
LNL897 monomer	1.31	0.483	0.147	0.0457	51.6	81.0	54.4
Total ADC^b	1.42	0.664	0.268	0.133	73.4	NC	85.4
Free small molecule components^c	0.0294	0.0106	0.00472	0.00199	1.27	1.99	1.44
Sum of additional metabolites	ND	ND	ND	ND
Total components detected	1.46	0.593	0.207	0.0679	63.7	100	68.2
Total components in original sample	1.46	0.593	0.207	0.0679	63.7	100	68.2

NC, not calculated; ND, not detected.
↵^a Total RA corresponding to ADC aggregates and/or complexes with endogenous proteins in the serum.
↵^b Values in italics denote conjugated antibody (LNL897 monomer + potential aggregates/complexes) concentrations measured by the ELISA method.
↵^c RA corresponding to small molecule–containing components of [³H]DM1-LNL897.