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Current Radiopharmaceuticals

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ISSN (Print): 1874-4710
ISSN (Online): 1874-4729

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Research Article

A New Buffer for Gallium-68 Labeling Suitable for use in Nuclear Medicine; Triethanolamine (TEA)

Author(s): Ayşe Uğur*, Olga Yaylali and Doğangün Yüksel

Volume 16, Issue 4, 2023

Published on: 13 June, 2023

Page: [308 - 314] Pages: 7

DOI: 10.2174/1874471016666230522100024

Price: $65

Abstract

Background: Radiopharmaceuticals labeled with [68Ga] from positron emission tomography (PET) radionuclides are utilized in nuclear medicine for non-invasive in vivo molecular imaging. Buffer solutions for radiolabeling play an important role as choosing the right buffer for the reaction helps to obtain high yield radiopharmaceuticals. Zwitterionic organic buffer 4-(2- hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), sodium acetate (CH3COONa), sodium bicarbonate (NaHCO3) buffers are widely used for labeling of peptides with [68Ga]Cl3. They can be used for peptide labelings with the acidic [68Ga]Cl3 precursor of triethanolammonium (TEA) buffer. The cost and toxicity of TAE buffer are relatively low.

Method: For [68Ga]GaPSMA-HBED-CC and [68Ga]GaDOTA-TATE labeling, the effectiveness of TEA buffer without chemical impurities in radiolabeling reactions and QC parameters in successful labeling was investigated.

Results: The method used to label [68Ga]Cl3 with PSMA-HBED-CC peptide in the presence of TEA buffer was successful when applied at room temperature. High purity radiosynthesis suitable for clinical use was performed to obtain DOTA-TATE peptide with the addition of 363K temperature and radical scavenger. Quality control tests with R-HPLC have shown that this method is suitable for clinical use.

Conclusion: We present an alternative procedure for labeling PSMA-HBED-CC and DOTATATE peptides with [68GaCl3] to obtain high radioactive doses of final radiopharmaceutical products used in nuclear medicine clinical applications. We have provided a quality-controlled final product that can be used in clinical diagnostic procedures. With the use of an alternative buffer, these methods could be adapted to semi-automatic or automated modules routinely used in nuclear medicine laboratories to label [68Ga]-based radiopharmaceuticals.

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[1]
Banerjee, S.R.; Pomper, M.G. Clinical applications of Gallium-68. Appl. Radiat. Isot., 2013, 76, 2-13.
[http://dx.doi.org/10.1016/j.apradiso.2013.01.039]
[2]
Mu, L.; Hesselmann, R.; Oezdemir, U.; Bertschi, L.; Blanc, A.; Dragic, M.; Löffler, D.; Smuda, C.; Johayem, A.; Schibli, R. Identification, characterization and suppression of side-products formed during the synthesis of high dose 68Ga-DOTA-TATE. Appl. Radiat. Isot., 2013, 76, 63-69.
[http://dx.doi.org/10.1016/j.apradiso.2012.07.022] [PMID: 22939572]
[3]
Velikyan, I. 68Ga-Based radiopharmaceuticals: Production and application relationship. Molecules, 2015, 20(7), 12913-12943.
[http://dx.doi.org/10.3390/molecules200712913]
[4]
European Pharmacopeia9.8, European Directorate for the Quality of Medicines and Healthcare (EDQM) Germany. European Pharmacopeia: Strasburg, 2019.
[5]
Afshar-Oromieh, A.; Babich, J.W.; Kratochwil, C.; Giesel, F.L.; Eisenhut, M.; Kopka, K.; Haberkorn, U. The rise of PSMA ligands for diagnosis and therapy of prostate cancer. J. Nucl. Med., 2016, 57(S3), 79S-89S.
[http://dx.doi.org/10.2967/jnumed.115.170720] [PMID: 27694178]
[6]
Das, S.; Al-Toubah, T.; El-Haddad, G.; Strosberg, J. 177 Lu-DOTATATE for the treatment of gastroenteropancreatic neuroendocrine tumors. Expert Rev. Gastroenterol. Hepatol., 2019, 13(11), 1023-1031.
[http://dx.doi.org/10.1080/17474124.2019.1685381] [PMID: 31652074]
[7]
Virgolini, I.; Ambrosini, V.; Bomanji, J.B.; Baum, R.P.; Fanti, S.; Gabriel, M.; Papathanasiou, N.D.; Pepe, G.; Oyen, W.; De Cristoforo, C.; Chiti, A. Procedure guidelines for PET/CT tumour imaging with 68Ga-DOTA-conjugated peptides: 68Ga-DOTA-TOC, 68Ga-DOTA-NOC, 68Ga-DOTA-TATE. Eur. J. Nucl. Med. Mol. Imaging, 2010, 37(10), 2004-2010.
[http://dx.doi.org/10.1007/s00259-010-1512-3] [PMID: 20596866]
[8]
Velikyan, I.; Beyer, G.J.; Långström, B. Microwave-supported preparation of (68)Ga bioconjugates with high specific radioactivity. Bioconjug. Chem., 2004, 15(3), 554-560.
[http://dx.doi.org/10.1021/bc030078f] [PMID: 15149183]
[9]
Antuganov, D.; Nadporojskii, M.; Sysoev, D.; Shatik, S.; Kondratenko, Y. Alkanolammonium protic ionic liquids for low temperature 68Ga-radiolabeling of dota-functionalized compounds. ChemistrySelect, 2020, 5(35), 10953-10957.
[http://dx.doi.org/10.1002/slct.202002891]
[10]
Kondratenko, Y.A.; Kochina, T.A.; Fundamenskii, V.S. Protic alkanolammonium ionic liquids based on triethanolammonium salts of carboxylic acids. Glass Phys. Chem., 2016, 42(6), 621-626.
[http://dx.doi.org/10.1134/S1087659616060092]
[11]
Kondratenko, Y.A.; Makovskaya, O.N.; Antuganov, D.O.; Zolotarev, A.A.; Ugolkov, V.L.; Nadporojskii, M.A.; Kochina, T.A. Dicationic protic ionic liquids based on N,N,N′N′-tetrakis(2-hydroxyethyl)ethylenediamine. J. Mol. Liq., 2022, 363, 119891.
[http://dx.doi.org/10.1016/j.molliq.2022.119891]
[12]
European Pharmacopoeia 10.4; Monograph no. 3044 “Gallium (68Ga) PSMA-11 Injection”; Council of Europe: Strasbourg, France, 2021.
[13]
Monograph “Gallium (68Ga) Edotreotide Injection” (Monograph Number 2485), 9th ed; European Pharmacopeia, 2019.
[14]
European Directorate for the Quality of Medicines & Healthcare (EDQM) Gallium (68Ga) edotreotide injection. European Pharmacopoeia, 2013, 2482, 4847-4848.
[15]
Good, N.E.; Winget, G.D.; Winter, W.; Connolly, T.N.; Izawa, S.; Singh, R.M.M. Hydrogen ion buffers for biological research. Biochemistry, 1966, 5(2), 467-477.
[http://dx.doi.org/10.1021/bi00866a011] [PMID: 5942950]
[16]
European Pharmacopoeia (European Pharmacopoeia, 3rd ed. Council of Europe: Strasbourg, , 1997; p. 121.
[17]
Antuganov, D.; Timofeev, V.; Timofeeva, K.; Antuganova, Y.; Kondratenko, Y.A. Evaluation of protic ionic liquids based on triethanolammonium and tris(hydroxymethyl)methylammonium salts as buffers for 68 ga‐radiolabelling of PSMA‐HBED‐CC. ChemistrySelect, 2019, 4(43), 12524-12527.
[http://dx.doi.org/10.1002/slct.201902588]
[18]
Eder, M.; Neels, O.; Müller, M.; Bauder-Wüst, U.; Remde, Y.; Schäfer, M.; Hennrich, U.; Eisenhut, M.; Afshar-Oromieh, A.; Haberkorn, U.; Kopka, K. Novel preclinical and radiopharmaceutical aspects of [68Ga]Ga-PSMA-HBED-CC: A new PET tracer for imaging of prostate cancer. Pharmaceuticals., 2014, 7(7), 779-796.

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