Improved radiosynthesis of ¹²³I-MAPi, an auger theranostic agent.

ABSTRACT:

Purpose

¹²³I-MAPi, a novel PARP1-targeted Auger radiotherapeutic has shown promising results in pre-clinical glioma model. Currently, ¹²³I-MAPi is synthesized using multistep synthesis that results in modest yields and low molar activities (MA) that limits the ability to translate this technology for human studies where high doses are administered. Therefore, new methods are needed to synthesize ¹²³I-MAPi in high activity yields (AY) and improved MA to facilitate clinical translation and multicenter trials.

Materials and methods

¹²³I-MAPi was prepared in a single step via ¹²³I-iododetannylation of the corresponding tributylstannane precursor. In vitro internalization assay, subcellular fractionation and confocal microsco

SUBMITTER: Wilson TC 

PROVIDER: S-EPMC7775866 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature