RM2 and DB15 analogues bearing [¹⁷⁷Lu]Lu-DOTAGA via different linkers, as radiotherapeutics: a head-to-head comparative study.

ABSTRACT:

Background

Bombesin analogues are gaining popularity as GRPR-targeting theranostic agents aiming to provide molecular tools for a patient-tailored management. We previously reported on two series of DOTAGA-bearing GRPR-antagonists, based on either [NMe-Gly¹¹]RM26 (DOTAGA-X-DPhe-Gln-Trp-Ala-Val-NMe-Gly-His-Sta-Leu-NH₂) or on DB15 (DOTAGA-X-SAR; SAR: DPhe-Gln-Trp-Ala-Val-NMe-Gly-His-Leu-NHEt) motifs, which were preclinically screened after labelling with In-111. In the current study, we aimed to evaluate in vitro and in vivo the four best-performing agents, AU-RM26-M2 (X: PEG2-Pip; Pip: 4-amino-1-carboxymethyl-piperidine), AU-RM26-M4 (X: Arg-Arg-Pip), AU-SAR-M1 (X: AMA-DIG; AMA: p-amino methylaniline, DIG: diglycolate) and AU-SAR-M2 (Arg-AMA-DIG), this time labe

SUBMITTER: Kanellopoulos P 

PROVIDER: S-EPMC12314183 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature