Automated sulfur-[18F]fluoride exchange radiolabelling of a prostate specific membrane antigen (PSMA) targeted ligand using the GE FASTlab™ cassette-based platform

Review Oncology

Radiotheranostics in oncology: Making precision medicine possible

Eric O. Aboagye et al.

Summary: Theranostics is a rapidly evolving field of medicine that combines diagnosis and treatment using similar tools. It offers the potential for high therapeutic efficacy with minimal toxicity. In oncology, theranostics relies on the identification of unique proteins and factors expressed in cancer cells, advances in imaging technology, and targeted chemicals and nanodevices for imaging and therapy. Radiotheranostics, using radiopharmaceuticals, is becoming routine in prostate cancer and neuroendocrine tumors. Although not all patients benefit from radiotheranostics, those who do often show high response rates.

CA-A CANCER JOURNAL FOR CLINICIANS (2023)

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Article Chemistry, Medicinal

Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts

Nils Walter et al.

Summary: A protocol for radiolabeling of aryl fluorosulfates using ultrafast isotopic exchange has been developed and optimized. This method allows for efficient labeling of low nanomolar amounts of aryl fluorosulfates without the need for azeotropic drying, base addition, and HPLC purification. The labeled compounds demonstrated sufficient stability in vivo and showed promise as tracers for visualizing specific molecular expressions.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Article Chemistry, Multidisciplinary

Sulfur [18F]Fluoride Exchange Click Chemistry Enabled Ultrafast Late-Stage Radiosynthesis

Qinheng Zheng et al.

Summary: Efficient and target-specific fluorination processes remain the main challenge in fluorine-18 PET, but a new ultrafast isotopic exchange method has been developed for the synthesis of novel PET agent aryl [F-18]fluorosulfate. This method enables automated F-18-radiolabeling of diverse aryl fluorosulfates with high yield and molar activity in just 30 seconds at room temperature, without the need for time-consuming HPLC purification steps. Additionally, the imaging application of a designed PARP1-targeting aryl [F-18]fluorosulfate has been successfully demonstrated in vivo.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

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Review Chemistry, Medicinal

The aluminium-[18F]fluoride revolution: simple radiochemistry with a big impact for radiolabelled biomolecules

Stephen J. Archibald et al.

Summary: The [F-18]AlF radiolabelling method, which combines the favorable decay characteristics of fluorine-18 with the convenience of metal-based radiochemistry, has been widely implemented in the development of radiopharmaceuticals for the clinic. This review captures the current status of [F-18]AlF-based technology and reflects on its impact on nuclear medicine, providing insights into the future prospects of this unique radiolabelling method.

EJNMMI RADIOPHARMACY AND CHEMISTRY (2021)

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Article Chemistry, Multidisciplinary

Radiolabelling an 18F biologic via facile IEDDA click chemistry on the GE FASTLab™ platform

Louis Allott et al.

Summary: This study introduces an automated method for producing radiolabelled biologics via IEDDA click chemistry on a single GE FASTLab (TM) cassette. The specific example discussed here is the production of fluorine-18 labelled IL2 radioconjugate and its in vitro uptake in cells with differential receptor expression. The method may be adapted for the radiosynthesis of any TCO-modified protein via IEDDA chemistry.

REACTION CHEMISTRY & ENGINEERING (2021)

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Article Radiology, Nuclear Medicine & Medical Imaging