Journal of Nuclear Science, Engineering and Technology (JONSAT)
In cooperation with the Iranian Nuclear Society

Evaluation of carrier added (CA) and no carrier added (NCA) 177Lu radionuclide roles in radiolabeling of peptide groups

Document Type : Research Paper

Authors

S. Vosoughi 1
N. Salek 2
M. Ghannadi Maragheh 2

1 Radiation Application Research School, Nuclear Science and Technology Research Institute, AEOI, P.O.Box: 1339-14155, Tehran - Iran

2 Nuclear Fuel Cycle Research School, Nuclear Science and Technology Research Institute, AEOI, P.O.Box: 11365-8486, Tehran – Iran

https://doi.org/10.24200/nst.2020.1148
Abstract
The peptides radiolabeled with 177Lu are including a wide range of promising radiopharmaceuticals. The NCA form of 177Lu provides a high specific activity that is required in targeted receptor therapy in order to avoid saturation of the targeted receptors. In this study, the outstanding quality of NCA radionuclides especially in the case of 177Lu was evaluated by comparing with CA radionuclide for radiolabeling of DOTATATE peptide and. The NCA 177Lu and CA 177Lu were obtained by chromatography separation of irradiated 176Yb (enrichment: 96.4%) and irradiation of 176Lu (enrichment: 95%) respectively. Radiolabeling of DOTATE with CA and NCA 177Lu was carried out in the same conditions and time. Then, radiolabeling yield was calculated as a function of some parameters like the Ligand: metal ratio and stability of compound after production. The results showed the superiority of NCA 177Lu with respect to CA 177Lu. Not only the particle ratio showed the advantages of the NCA radionuclide, but also the long-term comparison over a period of 14 days revealed the inferior character of CA.177Lu with regard to the high requirements regarding the specific activity set by radio-immunotherapy.

Highlights

1. W.A. Volkert, et al., Therapeutic radionuclides: production and decay property considerations, Journal of nuclear medicine: official publication, Society of Nuclear Medicine, 32, 174 (1991).

 

2. M. Fani, H.R. Maecke, S.M. Okarvi, Radiolabeled peptides: valuable tools for the detection and treatment of cancer. Theranostics, 2, 481 (2012).

 

3. J.C. Reubi, Peptide receptors as molecular targets for cancer diagnosis and therapy, Endocr. Rev, 24, 389 (2003).

 

4. M.R.A. Pillai, Metallic Radionuclides and Therapeutic Radiopharmaceuticals, (2010).

 

5. T. Das, et al, On the preparation of a therapeutic dose of 177Lu-labeled DOTA–TATE using indigenously produced 177Lu in medium flux reactor, Appl. Radiat. Isot., 65, 301 (2007).

 

6. J. Gains, et al, 177Lu-DOTATATE molecular radiotherapy for childhood neuroblastoma, J. Nucl., 52, 1041 (2011).

 

7. L. Bodei, et al, Peptide receptor radionuclide therapy with 177Lu-DOTATATE: the IEO phase I-II study, Eur J Nucl Med Mol Imaging, 38, 2125 (2011).

 

8. N. Salek, et al., Comparative studies of extraction chromatography and electro-amalgamation separation to produce no-carrier added 177Lu by Tehran research reactor, Iran. J. Nucl. Med, 25, 23 (2017).

 

9. N. Salek, et al., Production of 177Lu in No Carrier Added (NCA) form by Irradiation of Natural and Enriched Target in Tehran Research Reactor for Nuclear Medicine Approch, Journal of Nuclear Science and Technology, 77, 1 )2016).

 

10. W.A.P. Breeman, et al, Optimising conditions for radiolabelling of DOTA-peptides with 90Y, 111In and 177Lu at high specific activities, Eur. J. Nucl. Med. Mol. Imag. 30, 917 (2003).

Keywords

177Lu
No carrier added
Carrier added
DOTATATE
1. W.A. Volkert, et al., Therapeutic radionuclides: production and decay property considerations, Journal of nuclear medicine: official publication, Society of Nuclear Medicine, 32, 174 (1991).
 
2. M. Fani, H.R. Maecke, S.M. Okarvi, Radiolabeled peptides: valuable tools for the detection and treatment of cancer. Theranostics, 2, 481 (2012).
 
3. J.C. Reubi, Peptide receptors as molecular targets for cancer diagnosis and therapy, Endocr. Rev, 24, 389 (2003).
 
4. M.R.A. Pillai, Metallic Radionuclides and Therapeutic Radiopharmaceuticals, (2010).
 
5. T. Das, et al, On the preparation of a therapeutic dose of 177Lu-labeled DOTA–TATE using indigenously produced 177Lu in medium flux reactor, Appl. Radiat. Isot., 65, 301 (2007).
 
6. J. Gains, et al, 177Lu-DOTATATE molecular radiotherapy for childhood neuroblastoma, J. Nucl., 52, 1041 (2011).
 
7. L. Bodei, et al, Peptide receptor radionuclide therapy with 177Lu-DOTATATE: the IEO phase I-II study, Eur J Nucl Med Mol Imaging, 38, 2125 (2011).
 
8. N. Salek, et al., Comparative studies of extraction chromatography and electro-amalgamation separation to produce no-carrier added 177Lu by Tehran research reactor, Iran. J. Nucl. Med, 25, 23 (2017).
 
9. N. Salek, et al., Production of 177Lu in No Carrier Added (NCA) form by Irradiation of Natural and Enriched Target in Tehran Research Reactor for Nuclear Medicine Approch, Journal of Nuclear Science and Technology, 77, 1 )2016).
 
10. W.A.P. Breeman, et al, Optimising conditions for radiolabelling of DOTA-peptides with 90Y, 111In and 177Lu at high specific activities, Eur. J. Nucl. Med. Mol. Imag. 30, 917 (2003).
Journal of Nuclear Science, Engineering and Technology (JONSAT)
Volume 41, Issue 3 - Serial Number 93
November 2020
Pages 107-112

Home