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 3 In-vivo stability of [¹⁷⁷Lu]Lu-PP-F11N

Time p.i. (min)	Entresto^®	Stability (% of initial signal) in patients 1–8
Time p.i. (min)	Entresto^®	1	2	3	4	5	6	7	8	Median	IQR
5	w/o	71	95.5	n.a.^a	96.1	94.3	96.5	93.9	92.4	94.1	2.7
5	w	91.4	99.4	98.3	n.a.^b	99.6	99.9	100	98.3	99.5	1.5
15	w/o	69.9	80.3	91.4	90.5	88.8	90.2	71.4	68.1	80.3	19.3
15	w	92.2	96.7	92.1	n.a.^b	91.6	99.2	92	88.9	92.1	2.7
30	w/o	64.5	72.3	74.8	67.6	n.a.^a	60.3	50.1	n.a.^a	64.5	9.8
30	w	78.5	85.7	80.6	n.a.^b	85.5	77.9	75.3	79.9	78.5	4.9
60	w/o	37.9	47.1	44.3	34.3	n.a.^a	53.7	26	n.a.^a	41.1	11.2
60	w	63.5	70.3	64.8	n.a.^b	75.6	n.a.^b	54.8	58.8	64.15	10

In-vivo stability of [¹⁷⁷Lu]Lu-PP-F11N without (w/o) and with (w) Entresto^® premedication at 5, 15, 30 and 60 min p.i. Values with premedication are significantly higher (p < 0.001)
^aActivity rate too low for HPLC analysis
^bHPLC malfunction