Skip to main content
SpringerLink
Log in

Preparation and biological evaluation of 166Ho-BPAMD as a potential therapeutic bone-seeking agent

  • Published:
Journal of Radioanalytical and Nuclear Chemistry Aims and scope Submit manuscript

Abstract

In this work 166Ho-(4-{[(bis(phosphonomethyl))carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid (166Ho-BPAMD) complex was prepared successfully with sufficient radiochemical purity of >94 % and specific activity of 244 GBq/mmol at the optimized conditions. The complex demonstrated significant stability at room temperature and in human serum at least for 24 h. Hydroxyapatite (HA) binding assay demonstrated that even at the small amount of HA, >10 mg, above 98 % of the complex is bound to HA. At the pH 7.4, LogP0/w was −1.73 ± 0.02. Both planar imaging and biodistribution studies showed major accumulation of the labelled compound in the bone tissue.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Subscribe and save

Springer+ Basic
$34.99 /Month
  • Get 10 units per month
  • Download Article/Chapter or eBook
  • 1 Unit = 1 Article or 1 Chapter
  • Cancel anytime
Subscribe now

Buy Now

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7

Similar content being viewed by others

References

  1. Child AH (2003) High dose chemotherapy with hematopoietic stem-cell rescue for multiple myeloma. N Engl J Med 348:1875

    Article  CAS  Google Scholar 

  2. Alexanian R, Barlogie B (1990) New treatment strategies for multiple myeloma. Am J Hematol 35:194–198

    Article  CAS  Google Scholar 

  3. Rostom AY, O’Cathail SM, Folkes A (1984) Systemic irradiation in multiple myeloma: a report on nineteen cases. Br J Haematol 58:423–431

    Article  CAS  Google Scholar 

  4. Cavo M, Gobbi M, Tura S (1981) Peptichemio in multiple myeloma, (preliminary results). Haematologica 66:208–215

    CAS  Google Scholar 

  5. Giralt S, Bensinger W, Goodman M, Podoloff D, Eary J, Wendt R, Alexanian R, Weber D, Maloney D, Holmberg L et al (2003) 166Ho-DOTMP plus melphalan followed by peripheral blood stem cell transplantation in patients with multiple myeloma: results of two phase I/II trials. Blood 102:2684–2691

    Article  CAS  Google Scholar 

  6. Palma E, Correia JDG, Campello MPC, Santos I (2011) Bisphosphonates as radionuclide carriers for imaging or systemic therapy. Mol BioSyst 7:2950–2966

    Article  CAS  Google Scholar 

  7. Fellnera M, Biesalski B, Bausbacher N, Kubícek V, Hermann P, Rösch F, Thews O (2012) 68Ga-BPAMD: PET-imaging of bone metastases with a generator based positron emitter. Nucl Med Biol 39:993–999

    Article  Google Scholar 

  8. Fellner M, Baum RP, Kubícek V, Hermann P, Lukeš I, Prasad V et al (2010) PET/CT imaging of osteoblastic bone metastases with 68Ga-bisphosphonates: first human study. Eur J Nucl Med Mol Imaging 37:834

    Article  Google Scholar 

  9. Calhoun JM, Cessna JT, Coursey BM, Hoppes DD, Schima FJ, Unterweger MP (1992) Standardization of holmium-166 by the CIEMAT/NIST liquid scintillation efficiency-tracing method. Radioact Radiochem. 2:38–45

    Google Scholar 

  10. Breitz HB, Wendt RE III, Stabin MS, Shen S, Erwin WD, Rajendran JG, Eary JF, Durack L, Delpassand E, Martin W et al (2006) 166Ho-DOTMP radiation-absorbed dose estimation for skeletal targeted radiotherapy. J Nucl Med 47:534–542

    CAS  Google Scholar 

  11. Yousefnia H, Zolghadri S, Jalilian AR, Tajik M, Ghannadi-Maragheh M (2014) Preliminary dosimetric evaluation of 166Ho-TTHMP for human based on biodistribution data in rats. Appl Radiat Isot 94:260–265

    Article  CAS  Google Scholar 

  12. Pedraza-López M, Ferro-Flores G, de Murphy CA, Tendilla JI, Villanueva-Sánchez O (2004) Preparation of 166Dy/166Ho-EDTMP: a potential in vivo generator system for bone marrow ablation. Nucl Med Commun 25:615–621

    Article  Google Scholar 

  13. Zeevaart JR, Jarvis NV, Louw WK, Jackson GE (2001) Metal-ion speciation in blood plasma incorporating the tetraphosphonate, N, N-dimethylenephosphonate-1-hydroxy-4-aminopropilydenediphosphonate (APDDMP), in therapeutic radiopharmaceuticals. J Inorg Biochem 83:57–65

    Article  CAS  Google Scholar 

  14. Marques F, Gano L, Campello MP, Lacerda S, Santos I (2007) Biological evaluation of 153Sm and 166Ho complexes with tetraazamacrocycles containing methylcarboxylate and/or methylphosphonate pendant arms. Radiochim Acta 95:335–341

    Article  CAS  Google Scholar 

  15. IAEA-TECDOC-1340 (2003) Manual for reactor produced radioisotopes. ISBN 92-0-101103-2, ISSN 1011-4289, IAEA, Austria

  16. Neves M, Gano L, Pereira N, Costa MC, Costa MR, Chandia M et al (2002) Synthesis, characterization and bio-distribution of bisphosphonates 153Sm complexes: correlation with molecular modeling interaction studies. Nucl Med Biol 29:329–338

    Article  CAS  Google Scholar 

  17. Du XL, Zhang TL, Yuan L, Zhao YY, Li RC, Wang K, Yan SC, Zhang L, Sun H, Qian ZM (2002) Complexation of ytterbium to human transferrin and its uptake by K562 cells. Eur J Biochem 269:6082–6090

    Article  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Nuclear Science and Technology Research Institute (NSTRI), 14155-1339, Tehran, Iran

    Hassan Yousefnia, Samaneh Zolghadri & Ali Bahrami-Samani

  2. Faculty of Engineering, Science and Research Branch, Islamic Azad University (IAU), Tehran, Iran

    Naeimeh Amraei & Mohammad Hosntalab

Authors
  1. Hassan Yousefnia
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Naeimeh Amraei
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Mohammad Hosntalab
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Samaneh Zolghadri
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Ali Bahrami-Samani
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Hassan Yousefnia.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Yousefnia, H., Amraei, N., Hosntalab, M. et al. Preparation and biological evaluation of 166Ho-BPAMD as a potential therapeutic bone-seeking agent. J Radioanal Nucl Chem 304, 1285–1291 (2015). https://doi.org/10.1007/s10967-014-3924-1

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s10967-014-3924-1

Keywords

Search

Navigation