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Volume 14
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10.3390/ph14050385
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Article

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

by
Leonardo L. Fuscaldi
1,
Danielle V. Sobral
2,
Ana Claudia R. Durante
1,
Fernanda F. Mendonça
2,
Ana Cláudia C. Miranda
1,
Marcelo L. da Cunha
1,
Luciana Malavolta
2,
Jorge Mejia
1 and
Marycel F. de Barboza
1,*
1
Hospital Israelita Albert Einstein, Sao Paulo 05652-900, Brazil
2
Department of Physiological Sciences, School of Medical Sciences, Santa Casa de Sao Paulo, Sao Paulo 01221-020, Brazil
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2021, 14(5), 385; https://doi.org/10.3390/ph14050385
Submission received: 28 January 2021 / Revised: 6 March 2021 / Accepted: 9 March 2021 / Published: 21 April 2021
(This article belongs to the Special Issue Targets, Tracers and Translation, Part 2 - New Horizons in Radiopharmaceutical Development)
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Abstract

Prostate-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 [68Ga]Ga-PSMA-11, as well as to produce a radiopharmaceutical for PET imaging of PCa malignancies. [68Ga]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 [68Ga]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 [68Ga]Ga-PSMA-11 was standardized and the product was evaluated, thus verifying its characteristics for PET imaging of PCa tumors in a clinical environment.
Keywords: PSMA-11; gallium-68; automatic synthesis module; PET imaging; prostate cancer PSMA-11; gallium-68; automatic synthesis module; PET imaging; prostate cancer

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MDPI and ACS Style

Fuscaldi, L.L.; Sobral, D.V.; Durante, A.C.R.; Mendonça, F.F.; Miranda, A.C.C.; da Cunha, M.L.; Malavolta, L.; Mejia, J.; de Barboza, M.F. Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer. Pharmaceuticals 2021, 14, 385. https://doi.org/10.3390/ph14050385

AMA Style

Fuscaldi LL, Sobral DV, Durante ACR, Mendonça FF, Miranda ACC, da Cunha ML, Malavolta L, Mejia J, de Barboza MF. Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer. Pharmaceuticals. 2021; 14(5):385. https://doi.org/10.3390/ph14050385

Chicago/Turabian Style

Fuscaldi, Leonardo L., Danielle V. Sobral, Ana Claudia R. Durante, Fernanda F. Mendonça, Ana Cláudia C. Miranda, Marcelo L. da Cunha, Luciana Malavolta, Jorge Mejia, and Marycel F. de Barboza. 2021. "Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer" Pharmaceuticals 14, no. 5: 385. https://doi.org/10.3390/ph14050385

APA Style

Fuscaldi, L. L., Sobral, D. V., Durante, A. C. R., Mendonça, F. F., Miranda, A. C. C., da Cunha, M. L., Malavolta, L., Mejia, J., & de Barboza, M. F. (2021). Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer. Pharmaceuticals, 14(5), 385. https://doi.org/10.3390/ph14050385

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