Drug intelligence / Profile preview

68Ga-GRPR

Development stage
Unknown
Lead developer
Advanced Accelerator Applications
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Peptides
Administration
Intravenous
01

Overview

68Ga-GRPR refers to a class of Gallium-68 labeled radiopharmaceuticals that target the gastrin-releasing peptide receptor (GRPR), which is overexpressed in various cancers, including prostate, breast, and gastrointestinal stromal tumors (GIST). These agents function as diagnostic imaging tracers for positron emission tomography (PET) or PET/computed tomography (PET/CT) and PET/magnetic resonance imaging (PET/MRI). The class includes several specific GRPR antagonists and agonists, such as 68Ga-RM2, 68Ga-RM26, 68Ga-SB3, and 68Ga-NeoBOMB1. Upon administration, the peptide moiety of the tracer binds with high affinity to GRPR on tumor cells, allowing for high-contrast visualization of primary tumors and metastatic lesions. 68Ga-GRPR imaging is particularly valuable as a complementary diagnostic tool to PSMA-targeted imaging in prostate cancer, especially for low-grade or PSMA-negative tumors, and for staging estrogen receptor-positive (ER+) breast cancer.

Other names
68Ga-GRPR antagonist68Ga-GRPR ligand68Ga-GRPR tracer68Ga-labeled gastrin-releasing peptide receptor antagonist68Ga-labeled GRPR antagonist68Ga-labeled GRPR ligandGa-68 GRPRGa68 GRPRGa 68 GRPR
02

Targets

GRPR (Gastrin-releasing peptide receptor)

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