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

Table 7.

Summary of radiolabeled somatostatin analogues for SSTR-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 - DOTA - x - TOC, TATE	- clinical, 10 patients - metastatic NET - PET, PET/CT - reduced signal from the liver achieved; methodology improvement needed for implementation of parametric-based kinetic analysis	[142]
- ^99mTc, ¹⁷⁷Lu - DOTA, HYNIC, EDDA -6-carboxy-1,4,8,11-tetraazaundecane (N4) -p-Cl-Phe-cyclo(d-Cys-Tyr-d-Trp-Lys-Thr-Cys)d-Tyr-NH₂	- preclinical in vitro, in vivo - kidneys - SPECT/CT - more useful biodistribution results for a highly potent [^99mTc]Tc-N4-conjugate than with lutetium-177; HYNIC-conjugate with complete loss of SSTR-2 affinity	[143]
- ⁶⁸Ga - DOTA, NODAGA - x - JR11, TOC	- clinical, 12 patients - GEP-NET - PET/CT - very high TBR and image contrast of liver lesions for [⁶⁸Ga]Ga-NODAGA-JR11; studies in larger patient group proven	[60]
- ⁶⁸Ga - DOTA, fluorescein isothiocyanate - x -PA1, TATE	- preclinical in vitro, in vivo - lung, colorectal and gastric - microPET - effective tumor targeting and lower kidney accumulation of [⁶⁸Ga]Ga-DOTA-PA1; a potential for PET/CT of SSTR-positive tumors (especially lung) suggested	[144]
- ⁶⁴Cu - NODAGA, DOTA - x - JR11, TATE	- preclinical in vitro, in vivo - kidneys - microPET - more favorable in vivo pharmacokinetics, low levels in the liver, spleen and rapid blood clearance for [⁶⁴Cu]Cu-NODAGA-JR11 with further development for clinical translation	[145]
- ^99mTc - HYNIC, EDDA, tricine - x - TATE	- preclinical in vitro, in vivo; clinical, 6 patients - NET - SPECT/CT - reproducible kit with 2.96 GBq/6 mL formulated, but some differences in tumor uptake occurred	[146]
- ⁶⁸Ga - DOTA - x - TOC	- clinical, 4 patients - GEP-NET - PET/MRI - sensitive and accurate evaluation of the liver, but limited accuracy of MRI related to lung and bone diseases	[147]
- ⁶⁸Ga - DATA - x - TOC	- clinical, 53 patients - GEP-NET - PET/CT - comparable imaging profile of [⁶⁸Ga]Ga-DATA-TOC with DOTA-NOC; DATA-conjugate useful for instant kit labeling	[148]