Gastrin-releasing peptide receptor (GRPR) as a novel biomarker and therapeutic target in prostate cancer

Figures & data

Table 1. Recent studies on GRPR antagonists in prostate cancer and their conclusions.

Radiolabeled antagonist	Purpose	Conclude	Author	Year
^177Lu-AMTG	treatments	Compared to ^177Lu-RM2, ^177Lu-AMTG demonstrates a slightly increased affinity for GRPR, similar internalization rates, a slight improvement in lipophilicity, and significantly enhanced stability both in vivo and in vitro.	Günther, T	2022
[(68)Ga]Ga-RM2	imaging	[(68)Ga]Ga-RM2 is considered a promising PET tracer, particularly suitable for prostate cancer patients at intermediate risk. Imaging methods based on GRPr can complement other PET/CT imaging approaches in certain patients, offering improved characterization of prostate cancer and guidance for biopsies.	Beheshti, M	2023
(68)Ga-SB3	imaging	(68)Ga-SB3 PET/CT is a safe imaging method and a promising tool for early PCa imaging.	Bakker, I.L	2021
[(99m)Tc]Tc-maSSS-PEG(2)-RM26	imaging	maSSS-PEG(2)-RM26 is a promising GRPR antagonist: This substance is considered a potential GRPR (Gastrin-Releasing Peptide Receptor) antagonist, demonstrating targeting capabilities towards prostate cancer with GRPR expression.	Abouzayed, A.	2021
[(68)Ga]Ga-DOTA-Ava-BBN2/[(44g)Sc]Sc-DOTA-Ava-BBN2	imaging	It exhibits similar tumor uptake and retention characteristics, as well as rapid blood and kidney clearance features.	Ferguson, S	2020
[(99m)Tc]Tc-DB15	imaging	It exhibits high and sustained GRPR-specific uptake in mouse PC-3 tumors, while being rapidly cleared.	Nock, B.A	2021
[(68)Ga]Ga-AMBA	imaging	PET imaging using [(68)Ga]Ga-AMBA reveals that GRPRcould represent a feasible alternative target for diagnosis or treatment in PCa with limited PSMA expression levels.	Zhang-Yin, J	2020
(177)Lu-JMV4168	treatments	Radioisotope therapy using (177) Lu-JMV4168 leads to a significant reduction in the size of PC-3 tumors.	Chatalic, K.L	2016
(68)Ga-ProBOMB2/(177)Lu-ProBOMB2	–	(68)Ga-ProBOMB2 and (177) Lu-ProBOMB2 are considered promising tracers suitable for imaging and treating tumors expressing GRPR. Additionally, they exhibit low uptake in pancreatic tissue.	Bratanovic, I.J	2022
(68)Ga-JMV5132/(68)Ga-JMV4168	imaging	Both (68) Ga-JMV5132 and (68) Ga-JMV4168 demonstrate significantly high and specific accumulation in GRP-positive PC-3 tumors. These novel PET tracers are promising candidates for future clinical translation.	Chatalic, K.L	2014

Data availability statement

Data sharing is not applicable to this article, given that no new data were created or analysed in this study.