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

Table 9.

Summary of radiolabeled CCK/minigastrin analogues for CCKR-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
- 68Ga, 89Zr
- fusarinine C (FSC)
- x
-MG11
- preclinical in vitro, in vivo
- epidermoid
- microPET/CT
- decreased hydrophilicity, increased metabolic stability and kidney retention for dimer and trimer, and reduced TBR of 89Zr-monomer and dimers
[160]
- 111In
- DOTA
- x
- minigastrins MGS1, MGS2, MGS3, MGS4
- preclinical in vitro, in vivo
- epidermoid, pancreatic
- nanoSPECT/CT
- modified C-terminal of [111In]In-DOTA-MGS4 led to high CCK2R affinity, an improved biodistribution profile and a promising in vivo stability, tumor targeting, and TBR
[161]
- 99mTc
- HYNIC, EDDA
- x
-MGS5, MGS11
- preclinical in vitro, in vivo
- epidermoid
- gamma counter, autoradiography
- [99mTc]Tc-HYNIC-MGS11 with high resistance against enzymatic degradation and useful targeting profile similar to DOTA-analogue; a promising kit development of for CCK2R-imaging and radioguided surgery
[162]
- 111In
- DOTA
- x
- (D-Glu1−6)minigastrin
- clinical, 16 patients
- advanced medullary thyroid
- SPECT/CT
- high uptake in lesions and favorable dosimetry confirmed, but increased calcitonin concentrations in blood; initiation of 177Lu-analogue assessment
[163]