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

Table 14.

Summary of radiolabeled small ligands for CA IX-positive tumor hypoxia imaging over past 3 years.

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]