First preclinical evaluation of [225Ac]Ac-DOTA-JR11 and comparison with [177Lu]Lu-DOTA-JR11, alpha versus beta radionuclide therapy of NETs

EJNMMI Radiopharmacy and Chemistry

Table 2 RCYs, RCPs and stability studies in PBS and mouse serum of [²²⁵Ac]Ac-DOTA-JR11 prepared following different radiochemical conditions: 1, 2 (without l-melatonin) and 3 (with l-melatonin)

	RCY (%)*	RCP (%)*	PBS (%)^†	Mouse serum (%)^†
Condition 1	95.1 ± 0.3	92.5 ± 3.8	76.9^a	80.9^a
Condition 2	86.9 ± 13.2	76.5 ± 14.7	56.6^b	81.4^b
Condition 3	98.4 ± 0.5	83.3 ± 7.5	81.0^c	81.0^c

*RCYs and RCPs are presented as percentage of radiolabeled peptide (n = 4, 3 and 4 for conditions 1, 2 and 3 respectively)
^†Results are expressed as percentage (%) of intact radiolabeled peptide after incubation at 37 °C (n = 1)
^aStability studies performed at 22 h
^bStability studies performed at 24 h
^cStability studies performed at 27 h