Double targeting ligands to identify and treat prostate cancer

September 7, 2017

Researchers have demonstrated a new, effective way to precisely identify and localize prostate cancer tumors while protecting healthy tissue and reducing side effects. The new approach utilizes a single molecule designed to bind two proteins with differing affinities in an effort to optimize specific tumor localization—prostate-specific membrane antigen (PSMA) and human serum albumin—thereby enhancing tumor localization for targeted alpha radionuclide therapy. The study is presented in the featured basic article of the September issue of The Journal of Nuclear Medicine. 

PSMA-targeted radiotherapy of prostate cancer is a promising approach to the treatment of disease that has spread. A small number of ligands have been evaluated in patients, and while early tumor response is encouraging, the relapse rate is high and these compounds can cause adverse side effects.

"We see now the pitfalls of PSMA targeting and have attempted to circumvent some of these by improved molecular design," explains John W. Babich, PhD, professor of radiopharmaceutical sciences in radiology at Weill Cornell Medicine, New York, New York. "We believe that our double targeting ligands are the first PSMA ligands designed to make use of the blood pool as a 'safe zone' reservoir to protect sensitive organs and tissues from off-target effects of alpha irradiation and, simultaneously, to reduce kidney localization while maintaining excellent tumor targeting."

Read the full article.