Pilot Preclinical and Clinical Evaluation of (4S)-4-(3-[18F]Fluoropropyl)-L-Glutamate (18F-FSPG) for PET/CT Imaging of Intracranial Malignancies

• DOI: 10.1371/journal.pone.0148628
• Publication Date: 2016-02-18T21:25:55Z
• Authors: Erik S. Mittra; Norman Koglin; Camila Mosci; Meena Kumar; Aileen Hoehne; Khun Visith Keu; Andrei H. Iagaru; Andre Mueller; Mathias Berndt; Santiago Bullich; Matthias Friebe; Heribert Schmitt-...; Volker Gekeler; Lüder M. Fels; Claudia Bacher-Stier; Dae Hyuk Moon; Frederick T. Chin; Andrew W. Stephens; Ludger M. Dinkelborg; Sanjiv S. Gambhir
• Keywords: PET Imaging

Purpose (S)-4-(3-[18F]Fluoropropyl)-L-glutamic acid (18F-FSPG) is a novel radiopharmaceutical for Positron Emission Tomography (PET) imaging. It glutamate analogue that can be used to measure xC- transporter activity. This study was performed assess the feasibility of 18F-FSPG imaging orthotopic brain tumors in small animals and translation this approach human subjects with intracranial malignancies. Experimental Design For animal study, GS9L glioblastoma cells were implanted into brains Fischer rats studied 18F-FSPG, 18F-labeled glucose derivative 18F-FDG amino 18F-FET. five either primary or metastatic cancer recruited (mean age 50.4 years). After injection 300 MBq 3 whole-body PET/Computed (CT) scans obtained safety parameters measured. The three metastases also had an PET/CT scan. Quantitative qualitative comparison kinetics, biodistribution, relative efficacy tracers. Results In animals, visualized well 18F-FSPG. high tumor uptake model absence background signal led good visualization contrast (tumor/brain ratio: 32.7). 18F-FET showed T/B ratios 1.7 2.8, respectively. pilot tolerated there similar distribution all patients. All malignant lesions positive except one low-grade tumor. 18F-FSPG-PET-positive ratio observed as model. Conclusions PET demonstrates both studies Future on larger numbers wider array are planned. Trial Registration ClinicalTrials.gov NCT01186601