Table 14.
Composition of Studied Compounds - Metal Radionuclide - BFCA - Linker - Biomolecule |
Results and Findings - Phase of Trials - Cancer Type Studied - Imaging Technique Used - Benefits/Limitations/Conclusion |
Reference |
---|---|---|
- 111In - DOTA-ester - x - bis-ureidosulfonamide derivative |
- preclinical in vitro, in vivo - breast, colorectal - SPECT/CT - rapid clearance from blood and muscle, and selective accumulation within CAIX expressing colon cancer cells |
[240] |
- 99mTc - dipyridylamine, IDA - x - sulfonamide, sulfocoumarin |
- preclinical in vitro, initial in vivo - colorectal - x - significant limitations in very low tumor uptake and much higher liver uptake |
[241] |
- 68Ga - CBT, NODA, pyridine, DOTA-NHS, NODAGA-NHS - Asp-Arg-Asp, PEG2 linker - acetazolamide |
- synthesis, initial in vitro - x - useful CBT/1,2-aminothiol click reaction for CAIX ligands with in vitro stability developed |
[113] |
- 99mTc - hydroxamamide (Ham), methyl-substituted-Ham (MHam) - x - sulfonamide, ureidosulfonamide |
- synthesis, initial in vitro, in vivo - renal and colorectal - gamma counter - [99mTc]Tc-MHam-bivalent conjugate with the highest tumor specificity useful for further studies |
[242] |
- 111In -DOTA-bis(tBu)ester - x - imidazothiadiazole sulfonamide |
- preclinical in vitro, in vivo - breast and colorectal - SPECT/CT - favorable in vivo properties of [111In]In-DO3A-IS1 with selective binding and accumulation in CAIX-expressing colon cancer |
[243] |