Accession Number:



Development of a Radioligand to Detect Glucocorticoid Receptor Expression in Enzalutamide-Resistant Prostate Cancer with Positron Emission Tomography

Personal Author(s):

Corporate Author:

University of California San Francisco United States

Report Date:



The purpose of this project is to develop radioligands to measure glucocorticoid receptor GR expression in enzalutamide resistant prostate cancer. GR was recently identified in a preclinical model of acquired resistance to enzalutamide, and its expression was confirmed in drug resistant patient specimens. As spontaneous GR overexpression is one of several potential mechanisms of resistance to enzalutamide, we are leading an effort to develop a translational imaging assay to detect those patients with resistance due to GR overexpression. A small library of two steroidal and one non-steroidal radioligand to GR have been developed. All three are potent and selective GR ligands in vitro. Moreover, we have shown that one steroidal radioligand is stable in vivo and can specifically target GR in normal and cancerous tissues.

Descriptive Note:

Technical Report,30 Sep 2015,29 Sep 2017



Subject Categories:

Distribution Statement:

Approved For Public Release;

File Size: