PURPOSE: 18F-Fluoroestradiol [18F]FES has emerged as a valuable PET tracer to predict the response to hormone therapy in recurrent or metastatic breast cancer patients. A clinically acceptable product requires a rapid reliable synthesis and must be demonstrated to maintain chemical stability and receptor specific uptake during patient studies. [18F]FES then becomes a dependable tracer for the evaluation and management of breast cancer patients. METHODS: An improved automated radiosynthesis of [18F]FES was developed. Stability studies of the injectible form of [18F]FES were performed up to 24 h after dose formulation under normal storage conditions. A comparative FES/FDG PET imaging in ER+ breast cancer patients is reported. RESULTS: The improved synthesis procedure utilizes fewer hydrolysis steps and a single high performance liquid column chromatography (HPLC) purification of the labeled mixture affording [18F]FES in good yield with high radiochemical purity (>99%). Stability studies with purified [18F]FES in saline/ethanol (85:15 v/v) indicated no radiolytic or chemical degradation of this radiopharmaceutical when stored for 24 h at 20-24 degrees C. Positron Emission Tomography (PET) studies with [18F]FES and [18F]FDG in estrogen receptor positive (ER+) breast cancer patients indicated that while FDG accumulation was seen in all metabolically hyperactive sites, the uptake of FES clearly delineated the ER+ tissues regions. CONCLUSIONS: An improved automated synthesis of [18F]FES has been developed and the integrity of this product has been validated by long term stability studies and clinical PET imaging studies in ER+ breast cancer patients. A lack of concordance between FES and FDG uptake in a patient with metastatic breast cancer suggests specificity of the FES for tumors expressing estrogen receptors.
PURPOSE:18F-Fluoroestradiol [18F]FES has emerged as a valuable PET tracer to predict the response to hormone therapy in recurrent or metastatic breast cancerpatients. A clinically acceptable product requires a rapid reliable synthesis and must be demonstrated to maintain chemical stability and receptor specific uptake during patient studies. [18F]FES then becomes a dependable tracer for the evaluation and management of breast cancerpatients. METHODS: An improved automated radiosynthesis of [18F]FES was developed. Stability studies of the injectible form of [18F]FES were performed up to 24 h after dose formulation under normal storage conditions. A comparative FES/FDG PET imaging in ER+ breast cancerpatients is reported. RESULTS: The improved synthesis procedure utilizes fewer hydrolysis steps and a single high performance liquid column chromatography (HPLC) purification of the labeled mixture affording [18F]FES in good yield with high radiochemical purity (>99%). Stability studies with purified [18F]FES in saline/ethanol (85:15 v/v) indicated no radiolytic or chemical degradation of this radiopharmaceutical when stored for 24 h at 20-24 degrees C. Positron Emission Tomography (PET) studies with [18F]FES and [18F]FDG in estrogen receptor positive (ER+) breast cancerpatients indicated that while FDG accumulation was seen in all metabolically hyperactive sites, the uptake of FES clearly delineated the ER+ tissues regions. CONCLUSIONS: An improved automated synthesis of [18F]FES has been developed and the integrity of this product has been validated by long term stability studies and clinical PET imaging studies in ER+ breast cancerpatients. A lack of concordance between FES and FDG uptake in a patient with metastatic breast cancer suggests specificity of the FES for tumors expressing estrogen receptors.
Authors: Dong Zhou; Mai Lin; Norio Yasui; Mohammed H Al-Qahtani; Carmen S Dence; Sally Schwarz; John A Katzenellenbogen Journal: J Labelled Comp Radiopharm Date: 2014-02-17 Impact factor: 1.921
Authors: Michel Paquette; Éric Lavallée; Serge Phoenix; René Ouellet; Helena Senta; Johan E van Lier; Brigitte Guérin; Roger Lecomte; Éric E Turcotte Journal: J Nucl Med Date: 2017-08-10 Impact factor: 10.057
Authors: Michel Paquette; Serge Phoenix; René Ouellet; Réjean Langlois; Johan E van Lier; Eric E Turcotte; Francois Bénard; Roger Lecomte Journal: Mol Imaging Biol Date: 2013-10 Impact factor: 3.488
Authors: Mary L Gemignani; Sujata Patil; Venkatraman E Seshan; Michelle Sampson; John L Humm; Jason S Lewis; Edi Brogi; Steven M Larson; Monica Morrow; Neeta Pandit-Taskar Journal: J Nucl Med Date: 2013-08-22 Impact factor: 10.057