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68Ga-NOTA-PEG2-RM26
- Development stage
- Unknown
- Lead developer
- Karolinska University Hospital
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous
01
Overview
[68Ga]Ga-NOTA-PEG2-RM26 is a radiolabeled peptide-based PET imaging agent that targets the gastrin-releasing peptide receptor (GRPR), which is overexpressed in several cancers, notably prostate cancer and breast cancer. The compound consists of the GRPR antagonist RM26, conjugated via a PEG2 linker to a NOTA chelator, which binds gallium-68 for PET imaging. Its mechanism of action involves specific binding to GRPR on tumor cells, enabling visualization of primary tumors and metastases through PET/CT scans. Preclinical and early clinical studies have demonstrated high affinity for GRPR, rapid clearance from non-target tissues, favorable biodistribution profiles for diagnostic imaging shortly after administration, and safety in human subjects. The drug was initially developed by Karolinska University Hospital as part of efforts to improve molecular oncologic diagnostics and potentially serve as a companion diagnostic in theranostic approaches targeting GRPR-positive malignancies[1][2][3][4][5].
- Other names
- [68Ga]Ga-NOTA-PEG2-RM26
02
Targets
GRPR (Gastrin-releasing peptide receptor)
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