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

EJNMMI Research

Table 1 Cumulative biodistribution data of [¹¹¹In-DOTA]MG11 in AR42J tumor-bearing SCID mice including controls and animals treated with NEP and/or ACE inhibitors

Organs	[¹¹¹In-DOTA]MG11 (%ID/g tissue ± SD at 4 h pi, n ≥ 4)
Organs	+DG2 + PA^a	Control	+Lis^b	+PA^c	+PA + Lis^d	+TO^e	+Race^f
Blood	0.02 ± 0.01	0.04 ± 0.01	0.05 ± 0.02	0.06 ± 0.04	0.05 ± 0.02	0.02 ± 0.01	0.20 ± 0.08
Liver	0.14 ± 0.02	0.13 ± 0.03	0.13 ± 0.01	0.15 ± 0.04	0.17 ± 0.09	0.17 ± 0.05	1.19 ± 0.03
Heart	0.02 ± 0.01	0.05 ± 0.02	0.05 ± 0.01	0.07 ± 0.03	0.07 ± 0.03	0.03 ± 0.02	0.13 ± 0.03
Kidneys	1.31 ± 0.03	1.86 ± 0.25	1.85 ± 0.30	2.26 ± 0.33	1.82 ± 0.06	2.95 ± 0.80	1.93 ± 0.46
Stomach	0.08 ± 0.01	1.53 ± 0.65	2.83 ± 0.68	5.13 ± 2.29	6.21 ± 2.73	2.90 ± 0.51	4.60 ± 1.09
Intestines	0.48 ± 0.08	0.89 ± 0.76	0.65 ± 0.25	0.69 ± 0.13	0.82 ± 0.26	2.16 ± 0.88	0.83 ± 0.12
Spleen	0.09 ± 0.02	0.17 ± 0.07	0.34 ± 0.30	0.20 ± 0.08	0.30 ± 0.13	0.14 ± 0.04	0.30 ± 0.06
Muscle	0.01 ± 0.01	0.04 ± 0.01	0.04 ± 0.01	0.09 ± 0.17	0.07 ± 0.04	0.02 ± 0.01	0.10 ± 0.03
Lung	0.05 ± 0.01	0.07 ± 0.02	0.07 ± 0.01	0.10 ± 0.01	0.28 ± 0.19	0.12 ± 0.05	0.12 ± 0.03
Femur	0.04 ± 0.01	0.09 ± 0.05	0.08 ± 0.01	0.12 ± 0.06	0.15 ± 0.04	0.05 ± 0.01	0.26 ± 0.22
Pancreas	0.08 ± 0.01	0.11 ± 0.03	0.18 ± 0.09	0.36 ± 0.17	0.53 ± 0.24	0.30 ± 0.16	0.30 ± 0.061
Tumor	0.34 ± 0.04	1.82 ± 1.25	1.80 ± 0.74	15.32 ± 4.71	14.51 ± 4.73	12.32 ± 3.66	6.81 ± 2.79

^aCoinjection of 50 nmol DG2 [25] and 300 μg PA to assess non-specific tumor uptake
^bCoinjection of 100 μg Lis
^cCoinjection with 300 μg PA
^dCoinjection with 300 μg PA and 100 μg Lis
^eCoinjection with 150 μg TO
^fRadiotracer injection 30–40 min after ip injection of 3 mg Race