Radioligand/Theranostic to Detect Glucocorticoid Receptor Expression

Technology Description

Dysregulation of glucocorticoid receptor (GR) signaling has been implicated in Cushing’s syndrome, Addison’s disease, mood disorders, glomerular diseases and cancers (e.g. prostate cancer), but non-invasive biomarkers to better understand GR biology are needed.

UCSF researchers have developed a small molecule radioligand with ~100-fold more affinity for GR vs. other nuclear hormone receptors in the same family. YJH08 has sub-nM affinity for GR and binds GR on all normal tissues, including the brain. Use of this radioligand/theranostic can help identify patients most likely to respond to GR antagonists and could help develop tissue-specific GR-targeting drugs.

¹¹C-YJH08 is currently in clinical trials at UCSF to evaluate GR expression in normal tissues and treatment resistant cancer cells (NCT04927663).

ADVANTAGES

·         Non-invasive biomarker for detecting GR expression in vivo

·         Quantitative assessment in real time and multiple tissues simultaneously

·         Selective for GR

APPLICATIONS

·         Clinical trials – to identify prostate cancer patients whose cancer is driven by GR activity

·         Clinical trials – for development of GR antagonists as therapeutics

·         Radiotracer to measure glucocorticoid receptor expression levels in vivo with PET

REFERENCE

Huang, Y., et al. (2020). A Novel Radioligand Reveals Tissue Specific Pharmacological Modulation of Glucocorticoid Receptor Expression with Positron Emission Tomography. ACS chemical biology, 15(6), 1381–1391. https://doi.org/10.1021/acschembio.9b01043

PATENT STATUS

Pending in the United States only

INVENTOR PROFILE

Michael Evans, PhD

Patent Status