[⁶⁸Ga]Ga-THP-tetrazine for bioorthogonal click radiolabelling: pretargeted PET imaging of liposomal nanomedicines.

ABSTRACT: Pretargeted PET imaging using bioorthogonal chemistry is a leading strategy for the tracking of long-circulating agents such as antibodies and nanoparticle-drug delivery systems with short-lived isotopes. Here, we report the synthesis, characterisation and in vitro/vivo evaluation of a new ⁶⁸Ga-based radiotracer [⁶⁸Ga]Ga-THP-Tetrazine ([⁶⁸Ga]Ga-THP-Tz) for bioorthogonal click radiochemistry and in vivo labelling of agents with slow pharmacokinetics. THP-tetrazine (THP-Tz) can be radiolabelled to give [^68/67Ga]Ga-THP-Tz at room temperature in less than 15 minutes with excellent radiochemical stability in vitro and in vivo. [⁶⁸Ga]Ga-THP-Tz was tested in vitro and in vivo for pretargeted im

SUBMITTER: Mishra A 

PROVIDER: S-EPMC11221536 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature