JOURNAL OF THE CZECH PHARMACEUTICAL SOCIETY AND THE SLOVAK PHARMACEUTICAL SOCIETY

Čes. slov. farm. 2009, 58(5):208-211

Comparison of renal accumulation of [DOTA0, 1-Nal3]-octreotide labelled with selected radiometals

Z. Nový, J. Mandíková, F. Trejtnar*, A. Lázníčková
Charles University in Prague, Faculty of Pharmacy, Department of Pharmacology and Toxicology, Hradec Králové, Czech Republic

Radiolabelled somatostatin receptor-specific peptides are a useful tool in the diagnosis and/or radiotherapy of somatostatin-positive neuroendocrine tumours. However, significant renal uptake of the radiopeptides may result in radiotoxicological injure of the kidney. The aim of the study was to analyze the undesirable renal accumulation of a newly developed somatostatin receptor-specific peptide, [DOTA0, 1-Nal3]-octreotide (DOTA-NOC), labelled with 177Lu, 111In or 90Y. To quantify the accumulation rate of the radiopeptides, the renal uptake of 177Lu-DOTA-NOC, 111In-DOTA-NOC and 90Y-DOTA-NOC was compared with the accumulation of selected compounds known to be intensively concentrated in the renal cells, such as albumin or 99mTc-MAG3. The investigation studied the renal uptake in vitro at the cellular level using freshly isolated rat renal cells. The found results did not reveal a significant influence of the used radiolabel on the uptake in the rat renal cells. The studied radiopeptides exerted a lower renal uptake than the selected comparators. Nevertheless, the rate of accumulation of the studied radiopeptides in the renal rat cells seemed to be quantitatively relatively high. The results of the experiments confirmed that the used in vitro method might serve as a helpful tool for comparative studies or analyses of transport mechanisms in radiopharmaceuticals.

Keywords: somatostatin analogues; radiodiagnostic; radiotherapeutics; renal elimination
Grants and funding:

This study was supported by grant No. 124409/FaF/C-LEK of the Grant Agency of Charles University and performed in cooperation with COST Action BM0607.

Received: November 2, 2009; Accepted: November 11, 2009; Published: May 1, 2009  Show citation

ACS AIP APA ASA Harvard Chicago Chicago Notes IEEE ISO690 MLA NLM Turabian Vancouver
Nový Z, Mandíková J, Trejtnar F, Lázníčková A. Comparison of renal accumulation of [DOTA0, 1-Nal3]-octreotide labelled with selected radiometals. Čes. slov. farm. 2009;58(5-6):208-211.
Share...
Download citation
  • BibTeX (.bib)
  • Bookends (.ris)
  • EasyBib (.ris)
  • EndNote (.enw)
  • EndNote 8 (.xml)
  • ISI WoS (.isi)
  • Medlars (.medlars)
  • Mendeley (.ris)
  • MODS (.xml)
  • Papers (.ris)
  • RefWorks (.txt)
  • RefManager (.ris)
  • RIS (.ris)
  • MS Word (.xml)
  • Zotero (.ris)
    • Open full article

    References

    1. Signore, A., Annovazzi, A., Chianelli, M et al.: Eur. J. Nucl. Med., 2001; 28, 1555-1565. Go to original source... Go to PubMed...
    2. Weiner, R. E., Thakur, M. L.: Appl. Radiat. Isot., 2002; 57, 749-763. Go to original source... Go to PubMed...
    3. Forrer, F., Valkema, R., Kwekkeboom, D. J. et al.: Best Pract. Res. Clin. Endocrinol. Metab., 2007; 21, 111-129. Go to original source... Go to PubMed...
    4. Krenning, E. P., Kwekkeboom, D. J., Bakker, W. H. et al.: Eur. J. Nucl. Med., 1993; 20, 716-731. Go to original source... Go to PubMed...
    5. De Jong, M., Breeman, W. A., Bakker, W. H. et al.: Cancer Res., 1998; 58, 437-441.
    6. Storch, D., Behe, M., Walter, M. A. et al.: J. Nucl. Med., 2005; 46, 1561-1569.
    7. Wild, D., Schmitt, J. S., Ginj, M. et al.: Eur. J. Nucl. Med. Mol. Imaging, 2003; 30, 1338-1347. Go to original source... Go to PubMed...
    8. De Jong, M., Valdema, R., Jamar, F. et al.: Semin. Nucl. Med., 2002; 32, 133-140. Go to original source... Go to PubMed...
    9. Boerman, O. C., Wim, J. G., Corstens, F. H. M.: Eur. J. Nucl. Med., 2001; 28, 1447-1449. Go to original source... Go to PubMed...
    10. Cybulla, M., Weiner, S. M., Otte, A.: Eur. J. Nucl. Med., 2001; 28, 1552-1554. Go to original source... Go to PubMed...
    11. De Jong, M., Barone, R., Krenning, E. et al.: J. Nucl. Med., 2005; 46, 1696-1700.
    12. Melis, M., Krenning, E. P., Bernard, B. F. et al.: Eur. J. Nucl. Med. Mol. Imaging, 2005; 32, 1136-1143. Go to original source... Go to PubMed...
    13. Jones, D. P., Sundby, G. B., Ormstad, K. et al.: Biochem. Pharmacol., 1979; 28, 929-935. Go to original source... Go to PubMed...
    14. Trejtnar, F., Nový, Z., Petřík, M. et al.: Ann. Nucl. Med., 2008; 22, 859-867. Go to original source... Go to PubMed...
    15. Barone, R., Van Der Smissen, P., Devuyst, O. et al.: Kidney Int., 2005; 67, 969-976. Go to original source... Go to PubMed...
    16. Melis, M., Krenning, E. P., Bernard, B. F. et al.: Nucl. Med. Biol., 2007; 34, 633-641. Go to original source... Go to PubMed...
    17. Behr, T. M., Goldenberg, D. M., Becker, W.: Eur. J. Nucl. Med., 1998; 25, 201-212. Go to original source... Go to PubMed...
    18. Duncan, J. R., Behr, T. M., De Nardo, S. J.: J. Nucl. Med., 1997; 38, 829.
    19. Maina, T., Nock, B. A., Cordopatis, P., Bernard, B. F. et al.: Eur. J. Nucl. Med. Mol. Imaging, 2006; 33, 831-840. Go to original source... Go to PubMed...
    20. Balster, D. A., O'Dorisio, M. S., Summers, M. A. et al.: Am. J. Physiol. Renal Physiol., 2001; 280, F457-F465. Go to original source... Go to PubMed...
    21. Christensen, E. I., Nielsen, R.: Rev. Physiol. Biochem. Pharmacol., 2007; 158, 1-22.
    22. Blaufox, M. D.: J. Nucl. Med., 2004; 45, 86-88. Go to original source...

    Return to the content


    Czech and Slovak Pharmacy

    Madam, Sir,
    please be aware that the website on which you intend to enter, not the general public because it contains technical information about medicines, including advertisements relating to medicinal products. This information and communication professionals are solely under §2 of the Act n.40/1995 Coll. Is active persons authorized to prescribe or supply (hereinafter expert).
    Take note that if you are not an expert, you run the risk of danger to their health or the health of other persons, if you the obtained information improperly understood or interpreted, and especially advertising which may be part of this site, or whether you used it for self-diagnosis or medical treatment, whether in relation to each other in person or in relation to others.

    I declare:

    1. that I have met the above instruction
    2. I'm an expert within the meaning of the Act n.40/1995 Coll. the regulation of advertising, as amended, and I am aware of the risks that would be a person other than the expert input to these sites exhibited

    No
    Yes

    If your statement is not true, please be aware
    that brings the risk of danger to their health or the health of others.