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. 2022 Apr 24;15(5):522.
doi: 10.3390/ph15050522.

Development and Validation of Analytical Methods for Radiochemical Purity of 177Lu-PSMA-1

Pauline Orhon  1 , Marie-Dominique Desruet  1   2 , Marie Piquemal  1 , Nicolas De Leiris  2   3 , Loïc Djaileb  2   3 , Jean-Philippe Vuillez  2   3 , Pierrick Bedouch  1   4 , Julien Leenhardt  1   2
Affiliations

Development and Validation of Analytical Methods for Radiochemical Purity of 177Lu-PSMA-1

Pauline Orhon et al. Pharmaceuticals (Basel). .

Abstract

Prostate Specific Membrane Antigen (PSMA) is a highly relevant target in nuclear medicine due to its overexpression in prostate cancer. The 68Ga/177Lu-PSMA-1 combination is a theranostic agent for the detection and treatment of tumors overexpressing the PSMA target. Specifically, 177Lu-PSMA-1 is used in the treatment of castration-resistant prostate cancer that is ineffective or intolerant to the latest generation of chemotherapy and/or hormone therapy. This radiopharmaceutical is manufactured in a radiopharmaceutical synthesizing unit and must pass a quality control where the radiochemical purity (RCP) is assessed prior to release of the batch. RCP evaluation is performed by high-performance liquid chromatography (HPLC) and thin-layer chromatography (TLC). Since there is no monograph for 177Lu-PSMA-1 in the European Pharmacopoeia, we validate the analytical methods according to the EANM recommendations adapted from ICH Q2. Specificity, linearity, accuracy, precision, intermediate precision, limit of quantification (LOQ) and robustness were described for HPLC and TLC in this study. The results obtained demonstrated the robustness and reliability of the HPLC and TLC analytical methods for the evaluation of the RCP of 177Lu-PSMA-1.

Keywords: 177Lu-PSMA-1; high-performance liquid chromatography (HPLC); prostate cancer; radiochemical purity; radioligand therapy; thin-layer chromatography (TLC); validation of analytical methods.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Retention time of the 175Lu-PSMA I/T standard.
Figure 2
Figure 2
Retention time of 177Lu-PSMA-1 complex.
Figure 3
Figure 3
Linearity in HPLC method.
Figure 4
Figure 4
Linearity in TLC method.
See this image and copyright information in PMC

References

    1. National Estimates of Cancer Incidence and Mortality in Metropolitan France between 1990 and 2018. [(accessed on 15 January 2022)]. Available online: https://www.santepubliquefrance.fr/content/download/190600/document_file....
    1. Carlsson S.V., Vickers A.J. Screening for Prostate Cancer. Med. Clin. N. Am. 2020;104:1051–1062. doi: 10.1016/j.mcna.2020.08.007. - DOI - PMC - PubMed
    1. Wilt T.J., Ullman K.E., Linskens E.J., MacDonald R., Brasure M., Ester E., Nelson V.A., Saha J., Sultan S., Dahm P. Therapies for Clinically Localized Prostate Cancer: A Comparative Effectiveness Review. J. Urol. 2021;205:967–976. doi: 10.1097/JU.0000000000001578. - DOI - PubMed
    1. Lowrance W.T., Breau R.H., Chou R., Chapin B.F., Crispino T., Dreicer R., Jarrard D.F., Kibel A.S., Morgan T.M., Morgans A.K., et al. Advanced Prostate Cancer: AUA/ASTRO/SUO Guideline PART I. J. Urol. 2021;205:14–21. doi: 10.1097/JU.0000000000001375. - DOI - PubMed
    1. Lowrance W.T., Breau R.H., Chou R., Chapin B.F., Crispino T., Dreicer R., Jarrard D.F., Kibel A.S., Morgan T.M., Morgans A.K., et al. Advanced Prostate Cancer: AUA/ASTRO/SUO Guideline PART II. [(accessed on 15 June 2021)];J. Urol. 2021 205:22–29. doi: 10.1097/JU.0000000000001376. Available online: https://www.auajournals.org/doi/10.1097/JU.0000000000001376. - DOI - DOI - PubMed

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