Skip to main content
Log in

Preclinical evaluation of 188 Re-HYNIC-PSMA as a novel therapeutic agent

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

Abstract

In this study, optimized preparation, quality control, cell assessments and biostribution of 188Re-HYNIC-PSMA in normal rats and tumor bearing mice are studied. Optimized conditions for radiolabeling were evaluated and radiochemical purity (> 99%) was investigated using ITLC and HPLC methods. 188Re-HYNIC-PSMA was stable both in PBS (4 °C) and in human serum (37 °C) even after 48 h. The results showed the complex was cleared from the blood very fast via urinary track. This new radiolabeled compound has a high potential to be considered as an agent for the treatment of patients with PSMA expressing tumors however more biological studies are still needed.

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

Access this article

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

Instant access to the full article PDF.

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7
Fig. 8
Fig. 9
Fig. 10

Similar content being viewed by others

References

  1. Bray F, Ferlay J, Soerjomataram I, Siegel RL, Torre LA, Jemal A (2018) Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin 68:394–424

    PubMed  Google Scholar 

  2. Emmett L, Willowson K, Violet J, Shin J, Blanksby A, Lee J (2017) Lutetium 177 PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy. J Med Radiat Sci 64:52–60

    Article  PubMed  PubMed Central  Google Scholar 

  3. Sharifi M, Yousefnia H, Bahrami-Samani A, Jalilian AR, Zolghadri S, Vaez-Tehrani M et al (2017) Optimized production assessment, compartmental modeling and dosimetric evaluation of 177Lu- PSMA-617 for clinical trials. Int J Nucl Med Res 4:19–29

    Article  Google Scholar 

  4. Sharifi M, Jalilian AR, Yousefnia H, Alirezapour H, Bahrami-Samani A, Zolghadri S (2018) Production, quality control, biodistribution and imaging studies of 177Lu-PSMA-617 in breast adenocarcinoma model. Radiochim Acta 106:507–513

    Article  CAS  Google Scholar 

  5. Carlucci G, Ippisch R, Slavik R, Mishoe A, Blecha J, Zhu Sh (2021) ) 68Ga-PSMA-11 NDA approval: a novel and successful academic partnership. J Nucl Med 62:149–155

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  6. Sgouros G, Bodei L, McDevitt MR, Nedrow JR (2020) Radiopharmaceutical therapy in cancer: clinical advances and challenges. Nat Rev Drug Discov 19:589–608

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  7. Clinical Departments (2021) Novartis receives FDA breakthrough therapy designation for 177Lu-PSMA-617 in mCRPC patients. App Rad Oncol. https://appliedradiationoncology.com/articles

  8. Maecke H (2005) Radiolabeled peptides in nuclear oncology: influence of peptide structure and labeling strategy on pharmacology. Mol Imaging 49:43–72

    Article  Google Scholar 

  9. Ahmadi N, Yousefnia H, Bahrami-Samani A, Zolghadri S, Alirezapour B, Ghazi FM (2021) Development of 186/188Re-Chitosan as an Effective Therapeutic Agent for Rheumatoid Arthritis. Curr Radiopharm 14:154–160

    Article  CAS  PubMed  Google Scholar 

  10. Lepareur N, Lacœuille F, Bouvry Ch, Hindré F, Garcion E, Chérel M et al (2019) Rhenium-188 labeled radiopharmaceuticals: current clinical applications in oncology and promising perspectives. Front Med (Lausanne) 6:132

    Article  Google Scholar 

  11. Edelman MJ, Clamon G, Kahn D, Magram M, Lister-James J, Line BR (2009) Targeted radiopharmaceutical therapy for advanced lung cancer: phase I trial of rhenium Re188 P2045, a somatostatin analog. J Thorac Oncol 4:1550–1554

    Article  PubMed  Google Scholar 

  12. Biological Council (1987) Guidelines on the use of living animals in scientific investigations. Biological Council, UK, 2nd edn

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

    Google Scholar 

  14. Karamivand M, Mohammadpour-Ghazi F, Alirezapour B, Kalantari B, Zolghadri S, Yousefnia H (2021) Characterization of 188 W/188Re generator and quality control of its Eluate. J Nucl Sci Tech (JONSAT). https://doi.org/10.24200/nst.2020.619.1426

    Article  Google Scholar 

  15. Benešová M, Bauder-Wüst U, Schäfer M et al (2015) linker modification strategies to control the prostate- specific membrane antigen (PSMA)-targeting and pharmacokinetic properties of DOTA-conjugated PSMA inhibitors. J Med Chem 59:1761–1775

    Article  Google Scholar 

  16. Yousefnia H, Jalilian AR, Zolghadri S, Bahrami-Samani A, Shirvani-Arani S, Ghannadi-Maragheh M (2010) Preparation and quality control of lutetium-177 bleomycin as a possible therapeutic agent. NUKLEONIKA 55:285–291

    CAS  Google Scholar 

  17. Sharifi M, Yousefnia H, Bahrami-Samani A, Jalilian AR, Zolghadri S et al (2017) Optimized production, quality control, biological evaluation and PET/CT imaging of 68Ga-PSMA-617 in breast adenocarcinoma model. Radiochim Acta 105:399–407

    Article  CAS  Google Scholar 

  18. Chang SS (2004) Overview of prostate-specific membrane antigen. Rev Urol 6:13–18

    Google Scholar 

  19. Sharifi M, Yousefnia H, Zolghadri S, Bahrami-Samani A, Naderi M, Jalilian A et al (2016) Preparation and biodistribution assessment of 68Ga-DKFZ-PSMA-617 for PET prostate cancer imaging. Nucl Sci Tech 27(6):142–150

    Article  Google Scholar 

  20. Kalidindi TM, Lee SG, Jou K, Chakraborty G, Skafida M, Tagawa ST et al (2021) A simple strategy to reduce the salivary gland and kidney uptake of PSMA-targeting small molecule radiopharmaceuticals. Eur J Nucl Med Mol Imaging 48:2642–2651

    Article  CAS  PubMed  Google Scholar 

  21. Kratochwil C, Giesel FL, Eder M, Afshar-Oromieh A, Benešová M, Mier W et al (2015) [177Lu] Lutetium-labelled PSMA ligand-induced remission in a patient with metastatic prostate cancer. Eur J Nucl Med Mol Imag 42:987–988

    Article  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Hassan Yousefnia.

Additional information

Publisher’s Note

Springer Nature remains neutral with regard to jurisdictional claims in published maps and institutional affiliations.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Hadisi, M., Vosoughi, N., Yousefnia, H. et al. Preclinical evaluation of 188 Re-HYNIC-PSMA as a novel therapeutic agent . J Radioanal Nucl Chem 331, 841–849 (2022). https://doi.org/10.1007/s10967-021-08173-1

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s10967-021-08173-1

Keywords

Navigation