Table 2.

Biodistribution data obtained in KB tumor-bearing mice at 1, 4, 24, 48, 72, and 120 h after injection of [¹⁷⁷Lu]Lu-6R-RedFol-1, [¹⁷⁷Lu]Lu-6S-RedFol-1, and [¹⁷⁷Lu]Lu-OxFol-1. Data are shown as percentage of the injected activity per gram of tissue [% IA/g], representing the average ± SD

	1 h p.i.	4 h p.i.	24 h p.i.	48 h p.i.	72 h p.i.	120 h p.i.
[177Lu]Lu-6R-RedFol-1
Blood	23 ± 3	17 ± 1	5.4 ± 0.9	3.0 ± 0.4	1.0 ± 0.3	0.20 ± 0.13
Kidneys	8.4 ± 0.8	12 ± 1	24 ± 4	18 ± 1	19 ± 5	11 ± 2
Liver	3.3 ± 0.3	3.0 ± 0.2	1.3 ± 0.2	1.1 ± 0.2	0.61 ± 0.14	0.32 ± 0.05
Muscle	1.6 ± 0.2	1.4 ± 0.1	0.82 ± 0.22	0.82 ± 0.06	0.28 ± 0.08	0.28 ± 0.15
Bone	2.1 ± 0.3	1.9 ± 0.2	0.91 ± 0.22	0.75 ± 0.17	0.37 ± 0.09	0.19 ± 0.01
KB tumor	11 ± 1	20 ± 2	47 ± 4	39 ± 5	41 ± 12	23 ± 7
[177Lu]Lu-6S-RedFol-1
Blood	19 ± 2	15 ± 2	3.8 ± 0.9	1.0 ± 0.5	0.27 ± 0.11	0.05 ± 0.01
Kidneys	18 ± 2	33 ± 2	69 ± 7	64 ± 6	60 ± 10	28 ± 2
Liver	2.6 ± 0.1	2.3 ± 0.2	0.81 ± 0.22	0.46 ± 0.16	0.28 ± 0.07	0.16 ± 0.03
Muscle	1.6 ± 0.2	1.3 ± 0.1	0.47 ± 0.15	0.21 ± 0.05	0.13 ± 0.06	0.10 ± 0.01
Bone	2.0 ± 0.2	1.7 ± 0.2	0.53 ± 0.08	0.28 ± 0.08	0.16 ± 0.05	0.11 ± 0.01
KB tumor	14 ± 3	26 ± 1	46 ± 3	51 ± 7	42 ± 10	29 ± 3
[177Lu]Lu-OxFol-11
Blood	7.9 ± 1.4	2.3 ± 0.5	0.49 ± 0.08	0.19 ± 0.00	0.10 ± 0.02	0.02 ± 0.01
Kidneys	23 ± 4	22 ± 3	28 ± 3	19 ± 1	17 ± 2	9.5 ± 0.4
Liver	5.0 ± 1.3	3.1 ± 0.4	3.1 ± 1.0	1.9 ± 0.4	1.8 ± 0.6	0.93 ± 0.12
Muscle	1.3 ± 0.1	1.1 ± 0.2	1.0 ± 0.2	0.58 ± 0.26	0.50 ± 0.21	0.19 ± 0.06
Bone	1.6 ± 0.1	1.3 ± 0.2	0.74 ± 0.31	0.50 ± 0.09	0.29 ± 0.09	0.20 ± 0.04
KB tumor	11 ± 1	14 ± 2	18 ± 3	10 ± 1	8.6 ± 0.6	6.0 ± 1.7

¹Data reproduced with permission from Siwowska et al. 2017, Mol Pharm 14:523 [18]. Copyright 2020 American Chemical Society