Automated Production of [⁶⁸Ga]Ga-Desferrioxamine B on Two Different Synthesis Platforms

• Main Authors: Martin Kraihammer (Author), Miloš Petřík (Author), Christine Rangger (Author), Michael Gabriel (Author), Hubertus Haas (Author), Bernhard Nilica (Author), Irene Virgolini (Author), Clemens Decristoforo (Author)
• Format: Book
• Published: MDPI AG, 2024-09-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/pharmaceutics16091231; 1999-4923
• Keywords: desferrioxamine B; gallium-68; PET; infection; imaging; validation; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 16, Iss 9, p 1231 (2024)

<b>Background/Objectives:</b> PET imaging of bacterial infection could potentially provide added benefits for patient care through non-invasive means. [⁶⁸Ga]Ga-desferrioxamine B-a radiolabelled siderophore-shows specific uptake by human-pathogenic bacteria like <i>Staphylococcus aureus</i> or <i>Pseudomonas aeruginosa</i> and sufficient serum stability for clinical application. In this report, we present data for automated production of [⁶⁸Ga]Ga-desferrioxamine B on two different cassette-based synthesis modules (Modular-Lab PharmTracer and GRP 3V) utilising commercially obtainable cassettes together with a licensed ⁶⁸Ge/⁶⁸Ga radionuclide generator. <b>Methods:</b> Quality control, including the determination of radiochemical purity, as well as a system suitability test, was set up via RP-HPLC on a C18 column. The two described production processes use an acetic acid/acetate buffer system with ascorbic acid as a radical scavenger for radiolabelling, yielding ready-to-use formulations with sufficient activity yield. <b>Results:</b> Batch data analysis demonstrated radiochemical purity of >95% by RP-HPLC combined with ITLC and excellent stability up to 2 h after synthesis. Specifications for routine production were set up and validated with four masterbatches for each synthesis module. <b>Conclusions:</b> Based on this study, an academic clinical trial for imaging of bacterial infection was initiated. Both described synthesis methods enable automated production of [⁶⁸Ga]Ga-desferrioxamine B in-house with high reproducibility for clinical application.