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Standardization of the [<sup>68</sup>Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer

dc.contributor.authorLeonardo L. Fuscaldi
dc.contributor.authorDanielle V. Sobral
dc.contributor.authorAna Claudia R. Durante
dc.contributor.authorFernanda F. Mendonça
dc.contributor.authorAna Cláudia C. Miranda
dc.contributor.authorMarcelo L. da Cunha
dc.contributor.authorLuciana Malavolta
dc.contributor.authorJorge Mejia
dc.contributor.authorMarycel F. de Barboza
dc.contributor.otherHospital Israelita Albert Einstein, Sao Paulo 05652-900, Brazil
dc.contributor.otherDepartment of Physiological Sciences, School of Medical Sciences, Santa Casa de Sao Paulo, Sao Paulo 01221-020, Brazil
dc.contributor.otherHospital Israelita Albert Einstein, Sao Paulo 05652-900, Brazil
dc.contributor.otherDepartment of Physiological Sciences, School of Medical Sciences, Santa Casa de Sao Paulo, Sao Paulo 01221-020, Brazil
dc.contributor.otherHospital Israelita Albert Einstein, Sao Paulo 05652-900, Brazil
dc.contributor.otherHospital Israelita Albert Einstein, Sao Paulo 05652-900, Brazil
dc.contributor.otherDepartment of Physiological Sciences, School of Medical Sciences, Santa Casa de Sao Paulo, Sao Paulo 01221-020, Brazil
dc.contributor.otherHospital Israelita Albert Einstein, Sao Paulo 05652-900, Brazil
dc.contributor.otherHospital Israelita Albert Einstein, Sao Paulo 05652-900, Brazil
dc.date.accessioned2025-10-09T05:30:26Z
dc.date.available2025-10-09T05:30:26Z
dc.date.issued01-04-2021
dc.identifier.urihttps://www.mdpi.com/1424-8247/14/5/385
dc.identifier.urihttp://digilib.fisipol.ugm.ac.id/repo/handle/15717717/41101
dc.description.abstractProstate-specific membrane antigen (PSMA) is a glycoprotein present in the prostate, that is overexpressed in prostate cancer (PCa). Recently, PSMA-directed radiopharmaceuticals have been developed, allowing the pinpointing of tumors with the Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging techniques. The aim of the present work was to standardize and validate an automatic synthesis module-based radiolabeling protocol for [<sup>68</sup>Ga]Ga-PSMA-11, as well as to produce a radiopharmaceutical for PET imaging of PCa malignancies. [<sup>68</sup>Ga]Ga-PSMA-11 was evaluated to determine the radiochemical purity (RCP), stability in saline solution and serum, lipophilicity, affinity to serum proteins, binding and internalization to lymph node carcinoma of the prostate (LNCaP) cells, and ex vivo biodistribution in mice. The radiopharmaceutical was produced with an RCP of 99.06 ± 0.10%, which was assessed with reversed-phase high-performance liquid chromatography (RP-HPLC). The product was stable in saline solution for up to 4 h (RCP > 98%) and in serum for up to 1 h (RCP > 95%). The lipophilicity was determined as −3.80 ± 0.15, while the serum protein binding (SPB) was <17%. The percentages of binding to LNCaP cells were 4.07 ± 0.51% (30 min) and 4.56 ± 0.46% (60 min), while 19.22 ± 2.73% (30 min) and 16.85 ± 1.34% (60 min) of bound material was internalized. High accumulation of [<sup>68</sup>Ga]Ga-PSMA-11 was observed in the kidneys, spleen, and tumor, with a tumor-to-contralateral-muscle ratio of >8.5 and a tumor-to-blood ratio of >3.5. In conclusion, an automatic synthesis module-based radiolabeling protocol for [<sup>68</sup>Ga]Ga-PSMA-11 was standardized and the product was evaluated, thus verifying its characteristics for PET imaging of PCa tumors in a clinical environment.
dc.language.isoEN
dc.publisherMDPI AG
dc.subject.lccMedicine
dc.titleStandardization of the [<sup>68</sup>Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer
dc.typeArticle
dc.description.keywordsPSMA-11
dc.description.keywordsgallium-68
dc.description.keywordsautomatic synthesis module
dc.description.keywordsPET imaging
dc.description.keywordsprostate cancer
dc.description.doi10.3390/ph14050385
dc.title.journalPharmaceuticals
dc.identifier.e-issn1424-8247
dc.identifier.oaioai:doaj.org/journal:a30c82443d6c47a2bb9cc83d0ca1186d
dc.journal.infoVolume 14, Issue 5


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