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177Lu-DOTAGA-rhCCK-9
- Development stage
- Preclinical
- Lead developer
- Technical University of Munich
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
177Lu-DOTAGA-rhCCK-9 is a radiohybrid (rh) minigastrin analogue labeled with Lutetium-177 (177Lu) designed for targeting the cholecystokinin-2 receptor (CCK-2R, also known as cholecystokinin B receptor). Developed by researchers at the Technical University of Munich and the University Hospital Augsburg, it incorporates a silicon-based fluoride acceptor (SiFA) moiety into the D-glutamate chain of the minigastrin peptide backbone, allowing for either fluorine-18 (18F) or lutetium-177 (177Lu) labeling within the same molecular scaffold. Preclinical evaluations in AR42J tumor-bearing mice demonstrated that 177Lu-DOTAGA-rhCCK-9 exhibits enhanced tumor retention and decelerated blood clearance compared to reference ligands like [177Lu]Lu-DOTA-PP-F11N, although it also shows elevated kidney retention.
- Other names
- (R)-DOTAGA-rhCCK-9DOTAGA-rhCCK-9DOTAGA-rhCCK9DOTAGA-rhCCK 9[177Lu]Lu-(R)-DOTAGA-D-Dap(SiFA)-(D-Glu)8-Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH2rhCCK-9rhCCK9rhCCK 9
02
Targets
CCK2R (Cholecystokinin 2 Receptor)
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