Seminar: Theranostics for prostate cancer - Approaches to development of GRPR- and PSMA-targeted radionuclide probes for diagnostic imaging and therapy

  • Date: –13:00
  • Location: Zoom
  • Lecturer: Anna Orlova, Professor, Department of Medicinal Chemistry
  • Contact person: Britt Skogseid
  • Seminarium

There is a clinical need to improve further therapy of disseminated prostate cancer (PCa). The most promising therapies for disseminated cancer are based on molecular recognition of cancer-associated phenotype abnormalities (targeted therapy approaches). Overexpression of gastrin-releasing peptide receptor (GRPR) and prostate-specific membrane antigen (PSMA), receptors and antigens closely associated with PCa, can be used for targeted therapy of PCa. Radionuclide molecular imaging in PCa might serve as a non-invasive phenotyping method, crucial in the therapy selection.

We have developed several imaging probes for detection of GRPR overexpression both for PET and SPECT that in preclinical model of PCa demonstrated high contrast shortly after administration. Optimization of molecular design resulted in identification of several imaging probes PET and for SPECT. Labelled with therapeutic radiometal Lu-177, GRPR targeting peptide could efficiently inhibit tumour growth in preclinical model.

Combination of GRPR- and PSMA-targeting parts in one pseudo-peptide should provide an imaging probe that should improve sensitivity for PCa and diagnostic accuracy, as well as delivery of cytotoxic radionuclide/drugs to PCa lesions and thereby improve therapy outcome. We have developed several GRPR- and PSMA-targeting heterodimers that are capable to binding to both targets in vivo.

Phase I clinical studies of this probes are ongoing or in preparation.