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Article

GMP-Compliant Radiosynthesis of [18F]GP1, a Novel PET Tracer for the Detection of Thrombi

1
Institute of Radiology, Nuclear Medicine and Molecular Imaging, Heart and Diabetes Center North Rhine-Westphalia, University Hospital Ruhr-University Bochum, Georgstr. 11, 32545 Bad Oeynhausen, Germany
2
Life Molecular Imaging GmbH, Tegeler Str. 6-7, 13353 Berlin, Germany
3
Heart Failure Department, Heart and Diabetes Center North Rhine-Westphalia, University Hospital Ruhr-University Bochum, Georgstr. 11, 32545 Bad Oeynhausen, Germany
4
Department of Thoracic and Cardiovascular Surgery, Heart and Diabetes Center North Rhine-Westphalia, University Hospital Ruhr-University Bochum, Georgstr. 11, 32545 Bad Oeynhausen, Germany
5
Department of Thoracic and Cardiovascular Surgery, Erich & Hanna Klessmann Institute, Heart and Diabetes Center North Rhine-Westphalia, University Hospital Ruhr-University Bochum, Georgstr. 11, 32545 Bad Oeynhausen, Germany
*
Author to whom correspondence should be addressed.
Academic Editor: Gerald Reischl
Pharmaceuticals 2021, 14(8), 739; https://doi.org/10.3390/ph14080739
Received: 30 June 2021 / Revised: 23 July 2021 / Accepted: 23 July 2021 / Published: 28 July 2021
Thrombus formation and thromboembolic events play important roles in various cardiovascular pathologies. The key receptor involved in platelet aggregation is the fibrinogen receptor glycoprotein IIb/IIIa. [18F]GP1, a derivative of the GPIIb/IIIa antagonist elarofiban, is a specific 18F-labeled small-molecule radiotracer that binds with high affinity to GPIIb/IIIa receptors of activated platelets. An improved, robust and fully automated radiosynthesis of [18F]GP1 has been developed. [18F]GP1 has been synthesized with decay corrected radiochemical yields of 38 ± 6%, with a radiochemical concentration up to 1900 MBq/mL, molar activities of 952–9428 GBq/µmol and a radio-chemical purity >98%. After determination of the optimal reaction conditions, in particular for HPLC separation, adaption of the reaction conditions to PET center requirements, validation of the manufacturing process and the quality control methods, the synthesis of [18F]GP1 was successfully implemented to GMP standards and was available for clinical application. We describe the GMP-compliant synthesis of the novel radiotracer [18F]GP1. Moreover, we provide some proof-of-concept examples for clinical application in the cardiovascular field. PET/CT with the novel small-molecular radiotracer [18F]GP1 may serve as a novel highly sensitive tool for visualizing active platelet aggregation at the molecular level. View Full-Text
Keywords: [18F]GP1; GMP compliant radiosynthesis; detection of thrombi; PET/CT imaging; BPVT; LVAD; thrombosis [18F]GP1; GMP compliant radiosynthesis; detection of thrombi; PET/CT imaging; BPVT; LVAD; thrombosis
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MDPI and ACS Style

Hugenberg, V.; Zerna, M.; Berndt, M.; Zabel, R.; Preuss, R.; Rolfsmeier, D.; Wegener, J.; Fox, H.; Kassner, A.; Milting, H.; Koglin, N.; Stephens, A.W.; Gummert, J.F.; Burchert, W.; Deutsch, M.-A. GMP-Compliant Radiosynthesis of [18F]GP1, a Novel PET Tracer for the Detection of Thrombi. Pharmaceuticals 2021, 14, 739. https://doi.org/10.3390/ph14080739

AMA Style

Hugenberg V, Zerna M, Berndt M, Zabel R, Preuss R, Rolfsmeier D, Wegener J, Fox H, Kassner A, Milting H, Koglin N, Stephens AW, Gummert JF, Burchert W, Deutsch M-A. GMP-Compliant Radiosynthesis of [18F]GP1, a Novel PET Tracer for the Detection of Thrombi. Pharmaceuticals. 2021; 14(8):739. https://doi.org/10.3390/ph14080739

Chicago/Turabian Style

Hugenberg, Verena, Marion Zerna, Mathias Berndt, Reinhard Zabel, Rainer Preuss, Dirk Rolfsmeier, Janet Wegener, Henrik Fox, Astrid Kassner, Hendrik Milting, Norman Koglin, Andrew W. Stephens, Jan F. Gummert, Wolfgang Burchert, and Marcus-André Deutsch. 2021. "GMP-Compliant Radiosynthesis of [18F]GP1, a Novel PET Tracer for the Detection of Thrombi" Pharmaceuticals 14, no. 8: 739. https://doi.org/10.3390/ph14080739

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