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Challenges in the solution phase synthesis of PSMA-11 and PSMA-617: organic ligands for radiopharmaceutical preparations in prostate cancer medication

  • K. S. Ajish Kumar ORCID logo EMAIL logo and Anupam Mathur
Published/Copyright: May 1, 2024
Radiochimica Acta
From the journal Radiochimica Acta Volume 112 Issue 9

Abstract

Patient specific treatments for different cancers are currently being actively addressed through nuclear medicine. More recently, the identification of biomarker namely; prostate-specific membrane antigen (PSMA) expressed on the prostate cancer cell surface has been considered as a turning point in prostate cancer management using radiopharmaceuticals. In this treatment method, apart from radionuclide, organic ligands that target PSMA constitute an essential component. PSMA-11 and PSMA-617 are two important ligands that form the radiopharmaceuticals, [68Ga]Ga-PSMA-11, [177Lu]Lu-PSMA-617, which are currently powering the prostate cancer management, especially metastatic castration resistant prostate cancer (mCRPC) in most part of the world. Identification of efficient synthetic routes towards these highly expensive ligands is an important prerequisite to make this treatment modality more popular. In this account, the synthetic challenges that we circumvent during the solution phase synthesis of PSMA-11 and PSMA-617, through different chemical synthetic routes are demonstrated. Post-synthesis, both the ligands, PSMA-11 and PSMA-617 were successfully radiolabelled using 68Ga, and 177Lu, respectively, to generate corresponding labelled products [68Ga]Ga-PSMA-11, and [177Lu]Lu-PSMA-617, in good radiochemical purity.

Keywords: ligand; diagnosis; therapy; radionuclide; prostate
Corresponding author: K. S. Ajish Kumar, Bio-Organic Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400085, India; and Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India, E-mail:

Acknowledgements

 KSAK is thankful to Prof. B. S. Patro, Head, Bio-Organic Division, and Prof. P. A. Hassan, Associate Director, Bio-Science Group for their encouragement and support. Help and support from former Directors of Bio-Science Group, particularly, Prof. S. K. Nayak, Prof. V. P. Venugopalan, Prof. S. K. Ghosh, and Prof. S. Chattopadhyay are thankfully acknowledged. KSAK is highly thankful to Dr. Madhava B. Mallia (RPhD), for his help and enthusiasm 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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Supplementary Material

This article contains supplementary material (https://doi.org/10.1515/ract-2024-0280).

Received: 2024-01-26
Accepted: 2024-04-08
Published Online: 2024-05-01
Published in Print: 2024-09-25

© 2024 Walter de Gruyter GmbH, Berlin/Boston

Articles in the same Issue

  1. Frontmatter
  2. Review
  3. Phytoremediation of radium contaminated soils: recent advances and prospects
  4. Original Papers
  5. Kinetic evaluation of the uranyl peroxide synthetic route on morphology
  6. Fabrication and characterization of graphene oxide and reduced graphene oxide decorated diatomite composite materials and their adsorption performance for uranium ions
  7. The performance of iron-silicate-based biochar as a sorbent material towards 133Ba retention from radioactive liquid waste
  8. Challenges in the solution phase synthesis of PSMA-11 and PSMA-617: organic ligands for radiopharmaceutical preparations in prostate cancer medication
  9. Synthesis, MTT assay, 99m-Technetium radiolabeling, biodistribution evaluation of radiotracer and in vitro magnetic resonance imaging study of P,N-doped graphene quantum dots as a new multipurpose imaging nano-agent
  10. Assessment of radioactivity and radiological risk indices in the sediments of the Tam Giang-Cau Hai, Thi Nai, and Nai lagoons in the Center of Vietnam
  11. Study of gamma, neutron, and proton interaction parameters of some immunotherapy drugs using EpiXs, NGCal, and PSTAR software
  12. Gamma and neutron attenuation of SiO2–B2O3–BaO–Li2O glasses doped with CeO2
https://doi.org/10.1515/ract-2024-0280
Keywords for this article
ligand; diagnosis; therapy; radionuclide; prostate

Articles in the same Issue

  1. Frontmatter
  2. Review
  3. Phytoremediation of radium contaminated soils: recent advances and prospects
  4. Original Papers
  5. Kinetic evaluation of the uranyl peroxide synthetic route on morphology
  6. Fabrication and characterization of graphene oxide and reduced graphene oxide decorated diatomite composite materials and their adsorption performance for uranium ions
  7. The performance of iron-silicate-based biochar as a sorbent material towards 133Ba retention from radioactive liquid waste
  8. Challenges in the solution phase synthesis of PSMA-11 and PSMA-617: organic ligands for radiopharmaceutical preparations in prostate cancer medication
  9. Synthesis, MTT assay, 99m-Technetium radiolabeling, biodistribution evaluation of radiotracer and in vitro magnetic resonance imaging study of P,N-doped graphene quantum dots as a new multipurpose imaging nano-agent
  10. Assessment of radioactivity and radiological risk indices in the sediments of the Tam Giang-Cau Hai, Thi Nai, and Nai lagoons in the Center of Vietnam
  11. Study of gamma, neutron, and proton interaction parameters of some immunotherapy drugs using EpiXs, NGCal, and PSTAR software
  12. Gamma and neutron attenuation of SiO2–B2O3–BaO–Li2O glasses doped with CeO2
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