Gastrin Releasing Peptide Receptors-targeted PET Diagnostics and Radionuclide Therapy for Prostate Cancer Management

Every tumor possesses a unique molecular fingerprint, and personalized treatment strategies are key to addressing these distinct cancer phenotypes. As prostate cancer is a heterogeneous disease, more biological targets are needed to show the full extent of the disease in order to provide better care and more tailored and personalized treatment solutions for our patients. Gastrin-releasing peptide receptor (GRPR) is a promising biological target that is overexpressed in several cancers, including prostate cancer.

Advancements in GRPR-targeted radiopharmaceuticals include preclinical improvement of the peptide compound for GRPR affinity and metabolic stability and their translation into clinical practice, both in the diagnostic and therapeutic arena. Recent studies have highlighted the diagnostic performance of GRPR-targeting compounds such as [68Ga]Ga-RM2 and [68Ga]Ga-NeoB, both demonstrating high sensitivity, specificity, and accuracy at initial staging and biochemical recurrence of prostate cancer. Clinical trials involving [177Lu]Lu-RM2 and [177Lu]Lu-NeoB for targeted radionuclide treatment of prostate cancer have reported promising safety profiles and dosimetric results; the pancreas, with the highest physiological radiotracer uptake, shows quick wash-out.

The field of GRPR-targeted theranostics is progressing rapidly through continued research and clinical trials and goes beyond prostate cancer as GRPR is also expressed in other cancer types such as breast cancer and gastrointestinal stromal tumors.

Written by: Simone Dalm,¹ Heying Duan,² and Andrei Iagaru²

Department of Radiology and Nuclear Medicine, Erasmus MC, Rotterdam, The Netherlands.
Department of Radiology, Division of Nuclear Medicine and Molecular Imaging, Stanford University, Stanford, CA

Read the Abstract

Login