The high incidence and heavy disease burden of prostate
cancer
(PC) require accurate and comprehensive assessment for appropriate
disease management. Prostate-specific membrane antigen (PSMA) positron
emission tomography (PET) cannot detect PSMA-negative lesions, despite
its key role in PC disease management. The overexpression of gastrin-releasing
peptide receptor (GRPR) in PC lesions reportedly performs as a complementary
target for the diagnosis and therapy of PC. Radiopharmaceuticals derived
from the natural ligands of GRPR have been developed. These radiopharmaceuticals
enable the visualization and quantification of GRPR within the body,
which can be used for disease assessment and therapeutic guidance.
Recently developed radiopharmaceuticals exhibit improved pharmacokinetic
parameters without deterioration in affinity. Several heterodimers
targeting GRPR have been constructed as alternatives because of their
potential to detect tumor lesions with a low diagnostic efficiency
of single target detection. Moreover, some GRPR-targeted radiopharmaceuticals
have entered clinical trials for the initial staging or biochemical
recurrence detection of PC to guide disease stratification and therapy,
indicating considerable potential in PC disease management. Herein,
we comprehensively summarize the progress of radiopharmaceuticals
targeting GRPR. In particular, we discuss the impact of ligands, chelators,
and linkers on the distribution of radiopharmaceuticals. Furthermore,
we summarize a potential design scheme to facilitate the advancement
of radiopharmaceuticals and, thus, prompt clinical translation.