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Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

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Abstract

In this study, 177Lu-(4-{[(bis(phosphonomethyl))carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid (177Lu-BPAMD) was successfully prepared. The quality control, partition coefficient, hydroxyapatite binding assay and stability of the complex were determined. For better comparison, biodistribution patterns of 177Lu-BPAMD and 177Lu-EDTMP complexes were compared in same animal model. 177Lu-BPAMD was prepared with high radiochemical purity (>93 %) and specific activity of 534 GBq/mmol at the optimal conditions. Comparative study between 177Lu-BPAMD and 177Lu-EDTMP indicated higher bone uptake and lesser accumulation in the other organs for 177Lu-BPAMD. 177Lu-BPAMD can be considered as a promising agent for bone pain palliation in the near future.

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References

  1. Kufe DW, Pollock RE, Weichselbaum RR, Bast RC, Gansler TS, Holland JF, Frei E (2003) Holland-Frei Cancer Medicine. 6th edn. Hamilton (ON), BC Decker

  2. IAEA-TECDOC-1549 (2007) Criteria for palliation of bone metastases—clinical applications, IAEA, Austria, Vienna

  3. Lipton A (2004) Pathophysiology of bone metastases: how this knowledge may lead to therapeutic intervention. J Support Oncol 2:205–220

    Google Scholar 

  4. Chow E, Harris K, Fan G, Tsao M, Sze WM (2007) Palliative radiotherapy trials for bone metastases: a systematic review. J Clin Oncol 25:1423–1436

    Article  Google Scholar 

  5. Eary JF, Collins C, Stabin M, Vernon C, Petersdorf S, Baker M, Hartnett S, Ferency S, Addison SJ, Appelbaum F, Gordon EE (1993) 153Samarium-EDTMP biodistribution and dosimetry estimation. J Nucl Med 34:1031–1036

    CAS  Google Scholar 

  6. Rajendran JG, Eary JF, Bensinger W, Durack LD, Vernon C, Fritzberg A (2002) High-dose 166Ho-DOTMP in myeloablative treatment of multiple myeloma: pharmacokinetics, biodistribution, and absorbed dose estimation. J Nucl Med 43:1383–1390

    CAS  Google Scholar 

  7. Farhanghi M, Holmes RA, Volkert WA, Logan KW, Singh A (1992) 153Samarium-EDTMP: pharmacokinetic, toxicity and pain response using an escalating dose schedule in treatment of metastatic bone cancer. J Nucl Med 33:1451–1458

    CAS  Google Scholar 

  8. Kálmán FK, Király R, Brücher E (2008) Stability constants and dissociation rates of the EDTMP complexes of samarium(III) and yttrium(III). Eur J Inorg Chem 30:4719–4727

    Article  CAS  Google Scholar 

  9. Beyer GJ, Offord R, Künzi G, Aleksandrova Y, Ravn U, Jahn S, Barker J, Tengblad O, Lindroos M (1997) The influence of EDTMP concentration on the biodistribution of radio-lanthanides and 225Ac in tumor-bearing mice. Nucl Med Biol 24:367–372

    Article  CAS  Google Scholar 

  10. Fellner M, Riss P, Loktionova N, Zhernosekov KP, Thews O, Geraldes CFGC, Kovacs Z, Lukeš I, Rösch F (2011) Comparison of different phosphorus-containing ligands complexing 68Ga for PET-imaging of bone metabolism. Radiochim Acta. 99:43–51

    Article  CAS  Google Scholar 

  11. 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  CAS  Google Scholar 

  12. Fellner M, Baum RP, Kubícek V, Hermann P, Lukeš I, Prasad V, Rösch F (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 

  13. Yuan J, Liu C, Liu X, Wang Y, Kuai D, Zhang G, Zaknun JJ (2013) Efficacy and safety of 177Lu-EDTMP in bone metastatic pain palliation in breast cancer and hormone refractory prostate cancer: a phase II study. Clin Nucl Med 38:88–92

    Article  Google Scholar 

  14. Fellner M, Baum R, Kubicek V, Hermann P, Roesch F (2010) 177Lu-BPAMD-From bone imaging to therapy with a macrocycle-bisphosphonate ligand. J Nucl Med 51:1164

    Google Scholar 

  15. Yousefnia H, Amraei N, Hosntalab M, Zolghadri S, Bahrami-samani A (2015) Preparation and biological evaluation of 166Ho-BPAMD as a potential therapeutic bone-seeking agent. J Radioanal Nucl Chem. doi:10.1007/s10967-014-3924-1

    Google Scholar 

  16. Bahrami-Samania A, Anvari A, Jalilian AR, Shirvani-Arania S, Yousefniaa H, Aghamiri MR, Ghannadi-Maragheh M (2012) Production, quality control and pharmacokinetic studies of 177Lu-EDTMP for human bone pain palliation therapy trials. Iran J Pharm Res 11:137–144

    Google Scholar 

  17. Neves M, Gano L, Pereira N, Costa MC, Costa MR, Chandia M, Rosado M, Fausto R (2002) Synthesis, characterization and biodistribution of bisphosphonates 153Sm complexes: correlation with molecular modeling interaction studies. Nucl Med Biol 29:329–338

    Article  CAS  Google Scholar 

  18. IAEA-TECDOC-1401. (2004) Quantifying uncertainty in nuclear analytical measurements, IAEA, Austria, Vienna

  19. Meckel M. (2014) Macrocyclic bisphosphonates for PET-diagnosis and endoradiotherapy of bone metastases. http://d-nb.info/1062595645/34

  20. Deligny CL, Gelsema WJ, Tji TG, Huigen YM, Vink HA (1990) Bone seeking radiopharmaceuticals. Nucl Med Biol 17:161–791

    CAS  Google Scholar 

  21. Agarwal KK, Singla S, Arora G, Bal C (2014) 177Lu-EDTMP for palliation of pain from bone metastases in patients with prostate and breast cancer: a phase II study. Eur J Nucl Med Mol Imaging 42:79–88

    Article  CAS  Google Scholar 

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Authors and Affiliations

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

    Hassan Yousefnia, Samaneh Zolghadri, Amir Reza Jalilian & Saeed Shanehsazzadeh

  2. Department of Medical Physics, School of Medicine, Hamadan University of Medical Sciences, Hamadan, Iran

    Hamid Reza Sadeghi

  3. Department of Chemistry, University of Zanjan, Zanjan, Iran

    Mojdeh Naderi

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  1. Hassan Yousefnia
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  2. Samaneh Zolghadri
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  3. Hamid Reza Sadeghi
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  4. Mojdeh Naderi
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  5. Amir Reza Jalilian
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  6. Saeed Shanehsazzadeh
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Correspondence to Samaneh Zolghadri.

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Yousefnia, H., Zolghadri, S., Sadeghi, H.R. et al. Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP. J Radioanal Nucl Chem 307, 1243–1251 (2016). https://doi.org/10.1007/s10967-015-4225-z

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  • DOI: https://doi.org/10.1007/s10967-015-4225-z

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