Technologies

Prostate cancer is the most prevalent non-skin cancer in men, with ~233,000 new cases diagnosed each year. Although prostate cancer can be slow growing, the disease still accounts for almost 10% of cancer-related deaths in men. Androgen deprivation therapy (ADT) is highly effective in treating prostate cancer, reaching 80%-90% initial response rates. However, even treated with the second-generation anti-androgen drugs, Abiraterone and Enzalutamide, the vast majority of patients will eventually develop aggressive castration-resistant prostate cancer (CRPC) within a median of 18-24 months. It was recently found that upregulation of glucocorticoid receptor (GR) can recapitulate androgen receptor (AR)-like signaling and induce AR-target genes, which might be responsible for resistance to Abir and Enz. The new technology described here allows direct detection of GR protein overexpression with PET imaging in prostate cancer, especially CRPC patients. It may also be applied to evaluate GR levels in other types of cancer, including breast, ovarian and lung cancers, in which GR upregulation is implicated in treatment resistance to chemotherapy.

The current invention provides the following advantages:

• The first metabolically stable PET radiotracers capable of accurately measuring GR expression in the clinic
• Allow imaging with probes of high-affinity and specific GR-bindingin vivo
• Probes are synthesized through an efficient and high-yielding radiolabeling process with chemistry that is safe for human use
• Non-invasive and fast detection method to evaluate the potential for resistance to standard of care therapy