Impact of clinically tested NEP/ACE inhibitors on tumor uptake of [111In-DOTA]MG11—first estimates for clinical translation

EJNMMI Research

Table 2 Comparative biodistribution data of [¹¹¹In-DOTA]MG11 in SCID mice bearing double A431-CCK2R(+/−) tumors at 4 h pi, including controls and animals coinjected with gradually increasing amounts of TO and PA; TO and PA injected doses were equimolar

Organs	[¹¹¹In-DOTA]MG11 (%ID/g tissue ± SD at 4 h pi, n ≥ 4)
	Control	+TO			+PA
	Control	1.5 μg	15 μg	150 μg	3 μg	30 μg	300 μg
Blood	0.01 ± 0.01	0.02 ± 0.01	0.03 ± 0.02	0.02 ± 0.01	0.02 ± 0.01	0.04 ± 0.01	0.02 ± 0.01
Liver	0.11 ± 0.02	0.16 ± 0.02	0.15 ± 0.02	0.16 ± 0.01	0.13 ± 0.03	0.13 ± 0.02	0.12 ± 0.01
Heart	0.02 ± 0.01	0.03 ± 0.00	0.03 ± 0.00	0.03 ± 0.01	0.02 ± 0.01	0.04 ± 0.01	0.03 ± 0.01
Kidneys	1.30 ± 0.29	2.67 ± 0.30	2.28 ± 0.21	2.22 ± 0.19	2.11 ± 0.45	2.81 ± 1.03	1.78 ± 0.37
Stomach	1.32 ± 0.26	2.59 ± 0.40	3.38 ± 0.20	4.01 ± 0.20	2.68 ± 0.67	3.19 ± 0.12	4.56 ± 1.16
Intestines	0.83 ± 0.53	0.43 ± 0.10	0.47 ± 0.04	0.48 ± 0.02	0.40 ± 0.17	0.32 ± 0.09	0.47 ± 0.20
Spleen	0.06 ± 0.01	0.12 ± 0.02	0.10 ± 0.01	0.14 ± 0.04	0.09 ± 0.04	0.10 ± 0.02	0.07 ± 0.01
Muscle	0.02 ± 0.01	0.03 ± 0.01	0.02 ± 0.01	0.03 ± 0.02	0.03 ± 0.01	0.04 ± 0.01	0.02 ± 0.01
Lung	0.03 ± 0.01	0.05 ± 0.00	0.05 ± 0.00	0.62 ± 0.02	0.07 ± 0.05	0.07 ± 0.01	0.07 ± 0.03
Femur	0.02 ± 0.01	0.05 ± 0.00	0.06 ± 0.00	0.09 ± 0.07	0.04 ± 0.03	0.05 ± 0.01	0.06 ± 0.01
Pancreas	0.05 ± 0.02	0.14 ± 0.03	0.12 ± 0.03	0.22 ± 0.04	0.14 ± 0.07	0.17 ± 0.02	0.20 ± 0.03
Tumor (−)	0.12 ± 0.02	0.18 ± 0.03	0.13 ± 0.01	0.17 ± 0.04	0.17 ± 0.0.13	0.18 ± 0.07	0.13 ± 0.02
Tumor (+)	2.50 ± 0.92	4.98 ± 0.58	6.10 ± 1.26	7.99 ± 1.12	10.55 ± 1.77	15.41 ± 2.28	16.05 ± 2.37