automation-positron-emission-tomography-pet-radiotracer-synthesis

Automation of a Positron-emission Tomography (PET) Radiotracer Synthesis Protocol for Clinical Production

The development of new positron-emission tomography (PET) tracers is enabling researchers and clinicians to image an increasingly wide array of biological ...

David Geffen School of Medicine, University of California, Los Angeles (UCLA)

University of California, Los Angeles (UCLA)

Due to its selective overexpression in prostate cancer (PCa), the prostate-specific membrane antigen (PSMA) has been recognized as a highly promising target for diagnostic and therapeutic applications. So far, various PSMA ligands have been developed for radiolabeling with radioisotopes such as Ga or F which can be used for specific visualization and diagnosis of PSMA-expressing PCa. In addition, PSMA ligands suitable for radiolabeling with I or Lu have become available to the clinics, allowing PSMA-based radioligand therapies. Here, we provide a comprehensive review of the most frequently used PSMA ligands, their structural modifications, and the impact of those on clinical applications.

PSMA ligands in prostate cancer - Probe optimization and theranostic applications.

Peptides labeled with positron-emitting isotopes are emerging as a versatile class of compounds for the development of highly specific, targeted imaging agents for diagnostic imaging via positron-emission tomography (PET) and for precision medicine via theranostic applications. Despite the success of peptides labeled with gallium-68 (for imaging) or lutetium-177 (for therapy) in the clinical management of patients with neuroendocrine tumors or prostate cancer, there are significant advantages of using fluorine-18 for imaging. Recent developments have greatly simplified such labeling: in particular, labeling of organotrifluoroborates via isotopic exchange can readily be performed in a single-step under aqueous conditions and without the need for HPLC purification. Though an automated synthesis has not yet been explored, microfluidic approaches have emerged for F-labeling with high speed, minimal reagents, and high molar activity compared to conventional approaches. As a proof-of-concept, we performed microfluidic labeling of an octreotate analog ([F]AMBF-TATE), a promising F-labeled analog that could compete with [Ga]Ga-DOTATATE with the advantage of providing a greater number of patient doses per batch produced.

Microscale radiosynthesis, preclinical imaging and dosimetry study of [F]AMBF-TATE: A potential PET tracer for clinical imaging of somatostatin receptors.

Article	Year
PSMA ligands in prostate cancer - Probe optimization and theranostic applications. Methods (San Diego, Calif.)\| PubMed ID: 28666778	2017
Microscale radiosynthesis, preclinical imaging and dosimetry study of [F]AMBF-TATE: A potential PET tracer for clinical imaging of somatostatin receptors. Nuclear medicine and biology\| PubMed ID: 29747035	2018

Roger Slavik

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