⁸⁹Zr-labeled PSMA ligands for pharmacokinetic PET imaging and dosimetry of PSMA-617 and PSMA-I&T: a preclinical evaluation and first in man.

ABSTRACT:

Rationale

Prolonged in vivo evaluation of PSMA tracers could improve tumor imaging and patient selection for ¹⁷⁷Lu-PSMA-617 and ¹⁷⁷Lu-PSMA-I&T. In this study, we present the radiolabeling method of PSMA-617 and PSMA-I&T with the long-lived positron emitter ⁸⁹Zr to enable PET imaging up to 7 days post-injection. We compared the biodistribution of ⁸⁹Zr-PSMA-617 and ⁸⁹Zr-PSMA-I&T to those of ¹⁷⁷Lu-PSMA-617 and ¹⁷⁷Lu-PSMA-I&T, respectively, in a PSMA⁺ xenograft model. Moreover, we provide the first human ⁸⁹Zr-PSMA-617 images.

Materials and methods

PSMA ligands were labeled with 50-55 MBq [⁸⁹Zr]ZrCl₄ using a two-step labeling protocol. For biodistribution, BALB

SUBMITTER: Prive BM 

PROVIDER: S-EPMC12722385 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature