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. 2021 Feb 21;14(2):167. doi: 10.3390/ph14020167

Table 10.

Summary of radiolabeled exendin analogues for GLP-1 receptor-positive tumor imaging over past 3 years.

Composition of Studied Compounds
- Metal Radionuclide
- BFCA
- Linker
- Peptide
Results and Findings
- Phase of Trials
- Cancer Type Studied
- Imaging Technique Used
- Benefits/Limitations/Conclusion
Reference
- 111In
- DTPA
- lysine
- exendin-3
- preclinical in vitro, in vivo
- insulinoma
- SPECT
- hexendin40–45 conjugate (with 6 Lys and 6 DTPA residues) as the most useful due to the 7-fold higher specific activity than simpler conjugates and improved visualization of the pancreas
[67]
- 111In
- NODAGA
- albumin-binding moiety (ABM)
- exendin-4
- preclinical in vitro, in vivo
- insulinoma
- SPECT/CT
- significantly reduced kidney uptake and improved GLP1R targeting, but a further assessment of whole-body doses needed
[68]
- 68Ga
- NOTA
- methylaminolevulinate
- Cys39-exendin-4
- preclinical in vitro, in vivo
- pheochromocytoma (PCM)
- microPET
- specific GLP1R targeting in both poorly and highly differentiated PCM cells, but high accumulation in kidneys; more studies needed to establish association between GLP-1R PET and a risk stratification of PCM
[165]
- 64Cu
- NODAGA
x
- Lys40-exendin-4
- preclinical in vivo
- insulinoma
- PET/MRI
- high background signal from the exocrine pancreas observed during an early time points; the positive correlation between [64Cu]Cu-Ex4, reflecting β-cell mass, and Mn-retention demonstrated by a simultaneous PET/MRI
[166]