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

ABSTRACT:

Background

The [¹⁷⁷Lu]Lu-DOTA-TATE mediated peptide receptor radionuclide therapy (PRRT) of neuroendocrine tumors (NETs) is sometimes leading to treatment resistance and disease recurrence. An interesting alternative could be the somatostatin antagonist, [¹⁷⁷Lu]Lu-DOTA-JR11, that demonstrated better biodistribution profile and higher tumor uptake than [¹⁷⁷Lu]Lu-DOTA-TATE. Furthermore, treatment with alpha emitters showed improvement of the therapeutic index of PRRT due to the high LET offered by the alpha particles compared to beta emitters. Therefore, [²²⁵Ac]Ac-DOTA-JR11 can be a potential candidate to improve the treatment of NETs (Graphical abstract). DOTA-JR11 was radiolabeled with [²²⁵Ac]Ac(NO₃)₃ and

SUBMITTER: Handula M 

PROVIDER: S-EPMC10313624 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature