In-vivo inhibition of neutral endopeptidase 1 results in higher absorbed tumor doses of [177Lu]Lu-PP-F11N in humans: the lumed phase 0b study

EJNMMI Research

Table 5 Radiation doses

Patient	Mean tumor dose (Gy/GBq)		Kidney dose (Gy/GBq)		Stomach dose (Gy/GBq)		Bone marrow dose (Gy/GBq)
Entresto^®	Without	With	Without	With	Without	With	Without	With
1	n.a	n.a	0.04	0.07	0.3	0.48	0.02	0.02
2	n.a	n.a	0.05	0.13	0.26	0.43	0.04	0.04
3	n.a	n.a	0.05	0.12	0.03	0.05	0.03	0.04
4	0.03	0.05	0.05	0.12	0.23	0.50	0.03	0.05
4^a	0.05	0.07	0.05	0.12	0.23	0.50	0.03	0.05
5	n.a	n.a	0.03	0.07	1.15	1.53	0.02	0.03
6	0.99	1.26	0.05	0.11	0.19	0.30	0.04	0.06
7	0.22	0.75	0.04	0.10	0.17	0.88	0.03	0.04
7^a	0.47	1.12	0.04	0.10	0.17	0.88	0.03	0.04
8	0.33	0.73	0.03	0.09	0.2	0.39	0.03	0.04
Median	0.28	0.74	0.05	0.11	0.2	0.5	0.03	0.05
IQR	0.34	0.79	0.01	0.04	0.05	0.37	0.002	0.014
Wilcoxon’s signed rank test	0.03	0.01	0.01	0.01	0.22 NS	0.19 NS	0.44 NS

Patient	Tumor-to-kidney dose ratio		Tumor-to-stomach dose ratio		Tumor-to-bone marrow dose ratio
Entresto^®	Without	With	Without	With	Without	With
1	n.a	n.a	n.a	n.a	n.a	n.a
2	n.a	n.a	n.a	n.a	n.a	n.a
3	n.a	n.a	n.a	n.a	n.a	n.a
4	0.6	0.4	0.1	0.1	1.1	1
4^a	1.0	0.6	0.2	0.1	1.8	1.4
5	n.a	n.a	n.a	n.a	n.a	n.a
6	19.8	11.5	5.2	4.2	24.8	21.4
7	5.5	7.5	1.3	0.9	7.3	20.3
7^a	11.8	11.2	2.8	1.3	15.7	30.3
8	11.0	8.1	1.7	1.9	11	17.8
Median	8.3	7.8	1.5	1.1	9.2	19.1
IQR	9.5	8.1	2.1	1.5	11.4	15.7
Wilcoxon’s signed rank test

Radiation doses of tumors and organs and tumor-to-organ dose ratios without and with Entresto^® premedication. n.a. not applicable (no measurable tumor), NS not significant
^a2nd tumor in the same patient