Preclinical evaluation of [²²⁵Ac]Ac-DOTA-TATE for treatment of lung neuroendocrine neoplasms.

ABSTRACT:

Purpose

There is significant interest in the development of targeted alpha-particle therapies (TATs) for treatment of solid tumors. The metal chelator-peptide conjugate, DOTA-TATE, loaded with the β-particle emitting radionuclide ¹⁷⁷Lu ([¹⁷⁷Lu]Lu-DOTA-TATE) is now standard care for neuroendocrine tumors that express the somatostatin receptor 2 (SSTR2) target. A recent clinical study demonstrated efficacy of the corresponding [²²⁵Ac]Ac-DOTA-TATE in patients that were refractory to [¹⁷⁷Lu]Lu-DOTA-TATE. Herein, we report the radiosynthesis, toxicity, biodistribution (BD), radiation dosimetry (RD), and efficacy of [²²⁵Ac]Ac-DOTA-TATE in small animal models of lung neuroendocrine neoplasms (NENs).

Methods

[²²⁵Ac]Ac

SUBMITTER: Tafreshi NK 

PROVIDER: S-EPMC12866175 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature