Factors Influencing the Therapeutic Efficacy of the PSMA Targeting Radioligand ²¹²Pb-NG001.

ABSTRACT: This study aimed to determine the influence of cellular PSMA expression, radioligand binding and internalization, and repeated administrations on the therapeutic effects of the PSMA-targeting radioligand ²¹²Pb-NG001. Cellular binding and internalization, cytotoxicity, biodistribution, and the therapeutic efficacy of ²¹²Pb-NG001 were investigated in two human prostate cancer cell lines with different PSMA levels: C4-2 (PSMA+) and PC-3 PIP (PSMA+++). Despite 10-fold higher PSMA expression on PC-3 PIP cells, cytotoxicity and therapeutic efficacy of the radioligand was only 1.8-fold better than for the C4-2 model, possibly explained by lower cellular internalization and less blood-rich stroma in PC-3 PIP xenografts. Mice bearing subcutaneous PC-3 PIP xenografts were treat

SUBMITTER: Stenberg VY 

PROVIDER: S-EPMC9179904 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature