Determination of pharmacokinetics and tissue distribution of a novel lutetium-labeled PSMA-targeted ligand, ¹⁷⁷Lu-DOTA-PSMA-GUL, in rats by using LC-MS/MS.

ABSTRACT: Prostate specific membrane antigen (PSMA) is known to be overexpressed in prostate cancer cells, providing as a diagnostic and therapeutic target for prostate cancer. A lutetium-labeled PSMA targeted ligand, ¹⁷⁷Lu-DOTA-PSMA-GUL is a novel radiopharmaceutical, which has been developed for the treatment of prostate cancer. While the GUL domain of ¹⁷⁷Lu-DOTA-PSMA-GUL binds to the antigen, the beta-emitting radioisotope, ¹⁷⁷Lu-labeled DOTA, interacts with prostate cancer cells. However, the in vivo pharmacokinetics of intact ¹⁷⁷Lu-DOTA-PSMA-GUL has never been characterized. This study aimed to evaluate the pharmacokinetics and tissue distribution of the radiopharmaceutical in rats by using its stable isotope-labeled analog, ¹⁷⁵Lu-DOTA-PSMA

SUBMITTER: Song CH 

PROVIDER: S-EPMC9474474 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature