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Total chemical synthesis of PSMA-617: an API for prostate cancer endotherapeutic applications

  • Kalangattu Sundaran Ajish Kumar EMAIL logo and Anupam Mathur
Published/Copyright: February 14, 2024
Radiochimica Acta
From the journal Radiochimica Acta Volume 112 Issue 7-8

Abstract

Synthesis of PSMA-617, a peptide based ligand used in the preparation of nuclear medicine, 177Lu-PSMA-617, for the treatment of prostate cancer, is demonstrated in 6 steps, starting from appropriately protected amino acid building blocks. A solution phase Boc-strategy was adopted for the synthesis of peptide, wherein deprotection of carbamate group using HCl (g), was employed as the key step. The synthesis furnished PSMA-617 in purity >99.5 % as confirmed by HPLC analysis. ESI-MS and NMR analysis supported the structural integrity of the compound. The synthesized ligand was radiolabelled using 177Lu to generate the desired radiopharmaceutical, 177Lu-PSMA-617, in radiochemical purity >98 %, as revealed by radio HPLC and TLC analysis. This establishes its potential as a nuclear medicine for therapeutic application.

Keywords: radiopharmaceutical; ligand; radionuclide; therapy
Corresponding author: Kalangattu Sundaran Ajish Kumar, Bio-Organic Division, Bhabha Atomic Research Centre, Mumbai 400085, India; and Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India, E-mail:

Acknowledgments

KSAK thankfully acknowledge Prof. B. S Patro, Head, Bio-Organic Division, Prof. T. K. Ghanty, Group Director, Bio Science Group, BARC and former Group Directors (Prof. S. K. Nayak, Prof. V. P. Venugopalan, Prof. S. K. Ghosh) for their constant support and encouragement throughout the course of this activity. We are grateful to the support from National NMR Facility, TIFR, Mumbai. KSAK is highly thankful to Dr. M. B. Mallia, Radiopharmaceutical Division, BARC for his enthusiasm and support towards the program.

  1. Research ethics: Not applicable.

  2. Author contributions: The authors have accepted responsibility for the entire content of this manuscript and approved its submission.

  3. Competing interests: The authors states no conflict of interest.

  4. Research funding: None declared.

  5. Data availability: The data can be obtained on request from the corresponding author.

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Received: 2023-07-27
Accepted: 2023-09-21
Published Online: 2024-02-14
Published in Print: 2024-08-27

© 2023 Walter de Gruyter GmbH, Berlin/Boston

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https://doi.org/10.1515/ract-2023-0205
Keywords for this article
radiopharmaceutical; ligand; radionuclide; therapy

Articles in the same Issue

  1. Frontmatter
  2. Preface
  3. NUCAR-2023: Foreword
  4. Research Articles
  5. Theoretical analysis of light and heavy-ion induced reactions: production of medically relevant 97Ru
  6. Excitation functions of alpha-particle induced nuclear reactions on nat Sn
  7. Non-destructive assay of plutonium in absence of gamma-ray spectrometry
  8. Catalytic destruction of oxalate in the supernatant stream generated during plutonium reconversion process
  9. Quantification of Zr in simulated dissolver solution of U–Zr fuel by laser-induced breakdown spectroscopy
  10. Radiochemical and chemical characterization of fuel, salt, and deposit from the electrorefining of irradiated U-6 wt% Zr in hot cells
  11. Zirconium sponge production: an integrated approach for chemical characterization of process intermediates using ICP-OES
  12. Determination of 10B/11B in boric acid and B4C using LA-ICPMS
  13. Evaluating sustainability of Bhuj aquifer system, Western India using nuclear dating techniques
  14. Nanocrystalline Ce(OH)4-based materials: ruthenium selective adsorbent for highly alkaline radioactive liquid waste
  15. Production and radiochemical separation of 68Ge from irradiated Ga–Ni alloy target in 30 MeV cyclotron
  16. Preparation of [64Cu]Cu–NOTA complex as a potential renal PET imaging agent using 64Cu produced via the direct activation route
  17. Total chemical synthesis of PSMA-617: an API for prostate cancer endotherapeutic applications
  18. Rapid screening technique for gross α and gross β estimations in aqueous samples during radiation emergency
  19. Development of Dy3+ doped lithium magnesium borate glass system for thermoluminescence based neutron dosimetry applications
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