. Author manuscript; available in PMC: 2014 Aug 28.

Published in final edited form as: J Am Chem Soc. 2013 Aug 15;135(34):12707–12721. doi: 10.1021/ja4049493

Table 1.

Chemical and in vitro biological characterization data for ¹¹¹In- and ¹⁷⁷Lu-octapa-trastuzumab and ¹¹¹In- and ¹⁷⁷Lu-DOTA-trastuzumab radioimmunoconjugates.

Immunoconjugate	Isotope	Radiolabeling conditions and yield	Chelates/mAb^a	Specific activity (mCi/mg)	Immunoreactive fraction (%)^b	Serum stability 120 h (%)^c
H₄octapa-trastuzumab	¹¹¹In	15 min, 25 °C, 94%	3.0 ± 0.1	4.0 ± 0.3	99.9 ± 0.02	94.9 ± 0.6
H₄octapa-trastuzumab	¹⁷⁷Lu	15 min, 25 °C, 95%	3.0 ± 0.1	3.5 ± 0.4	99.2 ± 0.8	92.4 ± 0.6
DOTA-trastuzumab	¹¹¹In	60 min, 37 °C, 50-85%	3.4 ± 0.1	2.0 ± 0.2	93.2 ± 0.5	91.1 ± 0.6
DOTA-trastuzumab	¹⁷⁷Lu	60 min, 37 °C, 50-88%	3.4 ± 0.1	3.4 ± 0.3	95.2 ± 0.2	98.6± 0.6

Isotopic dilution assays, n = 3.

Determined immediately prior to in vivo experimentation, n = 6.

Calculated for incubation in human serum at 37 °C for 120 h, n = 3.