TY  - JOUR
T1  - Preclinical Evaluation of the PSMA/GRPR-Targeting Heterodimer [68Ga]Ga-BQ7812 for PET Imaging of Prostate Cancer: Advancing Toward Clinical Translation
A1  - E. Tursunov
A1  - G. Karimova
A1  - D. Akbarov
JF  - Asian Journal of Current Research in Clinical Cancer
JO  - Asian J Curr Res Clin Cancer
SN  - 3062-4444
Y1  - 2024
VL  - 4
IS  - 1
DO  - 10.51847/HuPwltXO8d
SP  - 90
EP  - 100
N2  - Radioligands that target prostate-specific membrane antigen (PSMA) and gastrin-releasing peptide receptor (GRPR) have emerged as promising tools for both imaging and therapeutic strategies in prostate cancer. Yet, heterogeneous expression of these receptors in tumors and metastatic lesions can limit the effectiveness of single-target approaches. To address this limitation, dual-targeting radioligands capable of simultaneously binding PSMA and GRPR have been developed. In this study, we report the preclinical evaluation of [68Ga]Ga-BQ7812, a PSMA/GRPR heterodimer designed for PET-based diagnostic imaging of prostate cancer, with the goal of supporting its clinical translation. In vitro assays using PSMA/GRPR-positive PC3-pip cells demonstrated rapid and selective binding to both targets. Biodistribution studies in PC3-pip xenograft-bearing mice revealed highest uptake at 1 hour post-injection in tumor tissue (PSMA+/GRPR+, 10.4 ± 1.0% IA/g), kidneys (PSMA+, 45 ± 16% IA/g), and pancreas (GRPR+, 5.6 ± 0.7% IA/g). By 3 hours post-injection, tumor-to-background ratios improved, reflecting preferential retention of the radioligand in tumor tissue. Additionally, [68Ga]Ga-BQ7812 exhibited low toxicity and an acceptable estimated dosimetry (effective dose = 0.0083 mSv/MBq), supporting its potential for first-in-human studies and further clinical development.
UR  - https://galaxypub.co/article/preclinical-evaluation-of-the-psmagrpr-targeting-heterodimer-68gaga-bq7812-for-pet-imaging-of-pro-oxgsa8igji7h11h
ER  -