. 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 2.

Biodistribution data of ¹¹¹In/¹⁷⁷Lu-H₄octapa-trastuzumab and ¹¹¹In/¹⁷⁷Lu-DOTA-trastuzumab. Performed over a 5 day period in mice bearing SKOV-3 ovarian cancer xenografts, tumor volume ~ 100–150 mm³ (n = 4 for each time point).

¹¹¹In-octapa-trastuzumab						¹¹¹In-DOTA-trastuzumab
Organ	24 h	48 h	72 h	96 h	120 h	Organ	24 h	48 h	72 h	96 h	120 h
Blood	6.9 ± 5.1	7.6 ± 6.5	10.5 ± 7.1	6.9 ± 6.6	11.4 ± 6	Blood	18 ± 1.7	17.3 ± 2.6	16.8 ± 2.2	15 ± 3.6	14.3 ± 1.6
Tumor	57.4 ± 22	58.3 ± 17.2	57.8 ± 14.6	68.7 ± 20.5	72.4 ± 21.3	Tumor	22.3 ± 6.4	28.4 ± 5.2	30.6 ± 9.1	32.8 ± 7.3	31.5 ± 3.8
Heart	2.6 ± 0.5	2.5 ± 1.5	2.7 ± 1.4	1.9 ± 1.4	3.6 ± 1.6	Heart	6.1 ± 0.9	6.6 ± 2	5.6 ± 1.3	5.2 ± 1.8	5.2 ± 0.9
Lungs	4.4 ± 2.1	3.9 ± 2.3	5 ± 2.8	3.8 ± 3.3	6.3 ± 3	Lungs	7.2 ± 1.6	6.8 ± 3.3	5.2 ± 1.4	6.3 ± 1.2	5.7 ± 2.2
Liver	12 ± 2.4	10.6 ± 1.2	9.1 ± 0.8	8.5 ± 2	6.6 ± 0.6	Liver	6.2 ± 0.4	5.5 ± 1.4	4.8 ± 1.3	4.4 ± 1.7	5.2 ± 1.2
Spleen	8.9 ± 2.4	7.6 ± 1	8.1 ± 0.8	7.4 ± 1.1	6.5 ± 1.6	Spleen	3.6 ± 0.8	3.7 ± 1.6	3 ± 0.7	2.7 ± 0.7	3.4 ± 1.4
Stomach	1.4 ± 0.2	0.8 ± 0.2	1.2 ± 0.1	0.7 ± 0.3	0.7 ± 0.2	Stomach	0.7 ± 0.1	0.7 ± 0.4	0.8 ± 0.2	0.3 ± 0.2	0.6 ± 0.3
Lg Intestine	3.7 ± 0.4	2.5 ± 0.7	2 ± 0.9	1.7 ± 0.4	1.2 ± 0.1	Lg Intestine	0.5 ± 0.1	0.6 ± 0.1	0.7 ± 0.1	0.5 ± 0.1	0.5 ± 0.1
Sm Intestine	3.8 ± 0.7	2.1 ± 0.4	2.5 ± 0.6	2.1 ± 0.4	1.5 ± 0.1	Sm Intestine	1.9 ± 0.1	1.6 ± 0.5	1.7 ± 0.1	1.1 ± 0.2	1.3 ± 0.1
Kidney	3.6 ± 1.2	4.2 ± 2.1	4.3 ± 2.1	3.5 ± 2	4.3 ± 1.6	Kidney	5.3 ± 0.5	6.3 ± 0.9	5.1 ± 1.7	5.8 ± 1.7	4.9 ± 0.4
Muscle	1.3 ± 0.5	0.9 ± 0.5	1 ± 0.5	0.8 ± 0.5	0.9 ± 0.5	Muscle	0.7 ± 0.2	0.8 ± 0.3	0.5 ± 0.1	0.4 ± 0.1	0.3 ± 0.1
Bone	4.1 ± 2	3.5 ± 0.4	2.8 ± 1	3.3 ± 0.5	1.4 ± 0.3	Bone	1 ± 0.3	0.9 ± 0.1	1.1 ± 0.4	0.9 ± 0.4	0.6 ± 0.2
Skin	10.8 ± 1.4	9.3 ± 1.4	7.2 ± 2.1	5.4 ± 1.2	3 ± 1.1	Skin	1.8 ± 0.4	2.1 ± 0.7	2.6 ± 0.1	1.7 ± 0.8	2.2 ± 0.8

¹⁷⁷Lu-octapa-trastuzumab						¹⁷⁷Lu-DOTA-trastuzumab
Organ	24 h	48 h	72 h	96 h	120 h	Organ	24 h	48 h	72 h	96 h	120 h

Blood	19.1 ± 1.5	9.1 ± 9.5	9.7 ± 5.2	8.9 ± 6.9	7.6 ± 5.7	Blood	20.4 ± 1.7	17.4 ± 1	18.1 ± 2.8	15 ± 0.8	14.7 ± 0.7
Tumor	50 ± 5.4	63.5 ± 15	62.4 ± 20	70.4 ± 25.8	56.6 ± 12.7	Tumor	18.3 ± 4.8	31.6 ± 2.9	32.1 ± 7.4	37 ± 9.5	37.4 ± 10.3
Heart	4.2 ± 0.7	3.2 ± 1.9	2.5 ± 0.9	2.3 ± 0.7	2.6 ± 1.4	Heart	7.2 ± 1	4.9 ± 3.3	5.8 ± 1.6	4.6 ± 1.1	5.4 ± 0.6
Lung	7.8 ± 3.6	3.9 ± 3.1	5 ± 2.3	4.4 ± 2.5	2.7 ± 1.8	Lungs	10 ± 1.5	6.7 ± 4.6	7.1 ± 2.3	6.3 ± 0.6	6 ± 2.1
Liver	10.1 ± 1.3	13.2 ± 4	9.5 ± 3.5	9.8 ± 1.7	8 ± 2.6	Liver	4.5 ± 2	5.7 ± 3.6	5.7 ± 2.5	2.8 ± 0.9	3.7 ± 1.9
Spleen	8.8 ± 2.3	11.5 ± 2.5	7.4 ± 2.8	9.2 ± 1.2	6.7 ± 2.4	Spleen	3.8 ± 0.5	3.1 ± 2.9	3.2 ± 1	3.5 ± 0.4	3.8 ± 1
Stomach	1.4 ± 0.3	1 ± 0.5	0.9 ± 0.4	1.1 ± 0.3	0.6 ± 0.2	Stomach	0.7 ± 0.2	1.3 ± 1.9	0.9 ± 0.2	0.8 ± 0.2	0.7 ± 0.2
Lg Intestine	1.3 ± 0.3	1 ± 0.3	1.1 ± 0.5	1.1 ± 0.2	0.8 ± 0.2	Lg Intestine	0.6 ± 0.1	0.5 ± 0.3	0.8 ± 0.2	0.5 ± 0.1	0.6 ± 0.2
Sm Intestine	1.9 ± 0.5	2.5 ± 1.1	2 ± 0.9	2.3 ± 0.4	1.6 ± 0.4	Sm Intestine	1.7 ± 0.2	1.5 ± 1	1.5 ± 0.4	1.4 ± 0.3	1.2 ± 0.1
Kidney	4.9 ± 0.9	3.8 ± 2	3.7 ± 1.2	3.8 ± 1.8	2.8 ± 1.2	Kidney	5.5 ± 1.7	7.3 ± 0.7	5.1 ± 0.8	4.4 ± 0.2	7.1 ± 5
Muscle	0.9 ± 0.2	0.7 ± 0.5	0.8 ± 0.5	0.5 ± 0.2	0.4 ± 0.2	Muscle	0.7 ± 0.2	0.5 ± 0.4	0.4 ± 0.1	0.5 ± 0.2	0.5 ± 0.1
Bone	3.2 ± 0.5	4 ± 0.6	3.1 ± 0.7	4.2 ± 1.5	3.6 ± 1.7	Bone	1.2 ± 0	1.3 ± 0.8	1.3 ± 0.3	0.9 ± 0.2	1.4 ± 0.3
Skin	8.4 ± 2	6.8 ± 2.9	6.9 ± 0.5	5.6 ± 1.2	4.1 ± 2.2	Skin	1.9 ± 0.9	2.4 ± 1.7	2.1 ± 0.2	2.1 ± 0.7	3.1 ± 1.3