Extensive preclinical evaluation of lutetium-177-labeled PSMA-specific tracers for prostate cancer radionuclide therapy.

Eline A M RuigrokNicole van VlietSimone U DalmErik de BloisDik C van GentJoost HaeckCorrina de RidderDebra StuurmanMark W KonijnenbergWytske M van WeerdenMarion de JongJulie Nonnekens

Published in: European journal of nuclear medicine and molecular imaging (2020)

[177Lu]Lu-PSMA-617 has the most favorable biodistribution in mice as well as more favorable binding characteristics in vitro in PSMA-positive cells and human kidney and salivary gland specimens compared with [177Lu]Lu-PSMA-I&T and [177Lu]Lu-JVZ-007. Based on our preclinical evaluation, [177Lu]Lu-PSMA-617 is the best performing tracer to be taken further into clinical evaluation for PSMA-targeted radiotherapeutic development although with careful evaluation of the tracer binding to PSMA-expressing organs.

Keyphrases

pet imaging
pet ct
prostate cancer
positron emission tomography
endothelial cells
computed tomography
induced apoptosis
drug delivery
cell therapy
adipose tissue
cell cycle arrest
cell death
replacement therapy
pi k akt
chemotherapy induced