Radiolabeling of Ibandronate with 188Re and its quality control as a bone-seeking radiopharmaceutical

Document Type : Original Article

Authors

1 Nuclear Fuel Cycle Research School, Nuclear Science and Technology Research Institute, Tehran, Iran

2 Radiation Applications Research School, Nuclear Science and Technology Research Institute, Tehran, Iran

Abstract

Skeletal metastases are prevalent complications related to patients with solid tumor cancer. Till now several boneseeking radiopharmaceuticals have been developed for bone metastases. Interesting features of bisphosphonates attracted attentions to them in the field of radiopharmaceutical therapy and studies on new generation of them have been doing too. The aim of this study was to produce and quality control of a radiopharmaceutical made with ibandronate as the third generation of bisphosphonates. For this purpose, Ibandronate was labeled with beta-emitting radionuclide of rhenium-188. Radionuclide purity was investigated using gamma spectrometry and radiochemical purity by thin layer chromatography. Finally, the biodistribution of this radiopharmaceutical was evaluated in mice. The results showed that the radiochemical purity of this compound is about 97%. the highest uptake (ID/g) was related to bone and the amount of this uptake was 7.11% at 12 hours after injection. The kidneys and stomach were the two organs that had the most activity after bone. Considering the possibility of producing the 188Re-IBA radiopharmaceutical, as well as the proper distribution of this radiopharmaceutical in target and non-target organs, it can be concluded that the ibandronate as the third generation of bisphosphonates this radiopharmaceutical can be useful in the bone metastases treatment. 

Keywords


  1. A. E. Bădilă, D. M. Rădulescu, A. -G. Niculescu, A. M. Grumezescu, M. Rădulescu, A. R. Rădulescu. Recent advances in the treatment of bone metastases and primary bone tumors: An up-to-date review. Cancers 13 (16) (2021) 4229.
  2. R. Zajączkowska, M. Kocot-Kępska, W. Leppert, J. Wordliczek. Bone pain in cancer patients: mechanisms and current treatment. Int. J. Mol. Sci. 20 (23) (2019) 6047.
  3. H. Ranjbar, A. Bahrami-Samani, D. Beiki, M. Ghannadi-Maragheh. Development of 153Sm/ 177Lu-EDTMP as a possible therapeutic complex. Iranian J. Nucl. Med. 25 (1) (2017) 11-16.
  4. C. Petit, B. Lacas, J. P. Pignon, Q. T. Le, V. Grégoire, C. Grau, A. Hackshaw, B. Zackrisson, M. K. B. Parmar, J. W. Lee, M. G. Ghi, G. Sanguineti, S. Temam, M. Cheugoua-Zanetsie, B. O'Sullivan, M. R. Posner, E. E. Vokes, J. J. Cruz Hernandez, Z. Szutkowski, E. Lartigau, V. Budach, R. Suwiński, M. Poulsen, S. Kumar, S. Ghosh Laskar, J. J. Mazeron, B. Jeremic, J. Simes, L. P. Zhong, J. Overgaard, C. Fortpied, P. Torres-Saavedra, J. Bourhis, A. Aupérin, P. Blanchard. MACH-NC and MARCH Collaborative Groups. Chemotherapy and radiotherapy in locally advanced head and neck cancer: an individual patient data network meta-analysis. Lancet Oncol. 22 (5) (2021) 727-736.
  5. Z. Pourhabib, H. Ranjbar, A. Bahrami Samani, A. A. Shokri. Appraisement of 186/188 Re-HEDP, a new compositional radiophar- maceutical. J. Radioanalytical Nucl. Chem. 322 (2019) 1133-1138.
  6. N. Salek, S. Vosoughi, A. Bahrami Samani, S. Shirvani Arani, M. Ghannadi Maragheh. Radiolabeled TPP with 166 Dy/166 Ho in vivo generator as a novel therapeutic agent. J. Radioanalytical Nucl. Chem. 326 (2020) 813-821.
  7. H. Ranjbar, Z. Pourhabib. Human Absorbed Dose Evaluation of [177Lu] Lu-IBA as a Bone Palliative Candidate. Nuklearmedizin Nucl. Med. 60 (5) (2021) 375-380.
  8. T. Xu, Y. Wang, Z. Chen, H. Liu, S. Yang, G. Liu, Y. Zhao, W. Fu, L. Liu, K. Xiang, D. Peng, Y. Chen. Preparation, characterization, and preliminary imaging study of [188Re] re-ibandronate as a novel theranostic radiopharmaceutical for bone metastasis. Contrast Media Mol. Imaging 2022 (2022) 7684076.
  9. L. Moghaddam-Banaem, S. Setayeshi, M. Ghannadi, S. Ahmadi, R. Gholipour, M. Firouz zareh, S. Mazidi, S. Mirfalah. Production and labeling of rhenium-186 and 188 via HEDP using natural rhenium and it’s biodistribution in rats. J. Nucl. Sci. Tech. (JonSat), 29 (4) (2009) 43-49.
  10. W. Y. Lin, C. P. Lin, S. J. Yeh, B. T. Hsieh, , Z. T. Tsai, G. Ting,  T. C. Yen, S. J. Wang, F. F. Knapp Jr, M. G. Stabin. Rhenium-188 hydroxyethylidene diphosphonate: a new generator-produced radiotherapeutic drug of potential value for the treatment of bone metastases. Eur. J. Nucl. Med. 24 (1997) 590-595.
  11. M. Erfani, N. Rahmani, A. Doroudi, M. Shafiei. Preparation and evaluation of rhenium-188-pamidronate as a palliative treatment in bone metastasis. Nucl. Med. Biol. 49 (2017) 1-7.
  12. B. L. Faintuch, S. Faintuch, E. Muramoto, Complexation of 188Re-phosphonates: in vitro and in vivo studies. Radiochimica Acta 91(10) (2003) 607-612.