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Gastrin Releasing Peptide Receptors-targeted PET Diagnostics and Radionuclide Therapy for Prostate Cancer Management Preclinical and Clinical Developments of the Past 5 Years
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DOI：10.1016/j.cpet.2024.03.004.png)
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Abstract
En 中文
The field of theragnostics is ever growing with active research in novel targets, continuous development of new compounds with improved pharmacokinetics, and their translation into clinics. GRPR has emerged as a pan -cancer target as it is overexpressed in several human cancers. For PC theragnostics, significant progress has been made in the improvement of GRPR-targeting peptides with structural modifications to the GRPR backbone and the use of different linkers and chelators to improve stability and pharmacokinetics. These compounds have been radiolabeled to the well -researched theragnostic pair 68 Ga and 177 Lu as well as true matched theragnostic pairs such as 64 Cu and 67 Cu and 203 Pb and 212 Pb. Preclinical studies have shown promising results with favorable pharmacokinetics and tumor -to -background ratios. Clinical trials are currently underway and their results are highly anticipated. The dual interrogation of GRPR and PSMA in a single radiopharmaceutical is an exciting development to further improve diagnostic accuracy of PC which is characterized by high tumor heterogeneity, and the expression of GRPR and PSMA is on a spectrum throughout the different disease stages. Continued efforts in optimizing peptides and radionuclide selection are laying the foundation for their successful clinical translation. A GRPR TRT holds the potential to improve clinical management of not only patients with PC but all GRPR-expressing cancers and ultimately offer precision and personalized medicine.
Keywords:
Gastrin-releasing peptide receptor
GRPR
Bombesin
Theragnostics
Preclinical
Clinical
Prostate cancer
Journal
IF:
2.3
Papers:
360
Citations:
1.1K