2-(18)F-fluoropropionic acid as a PET imaging agent for prostate cancer Journal Article


Authors: Pillarsetty, N.; Punzalan, B.; Larson, S. M.
Article Title: 2-(18)F-fluoropropionic acid as a PET imaging agent for prostate cancer
Abstract: There is a high interest in developing an (18)F-labeled PET tracer that can aid in diagnosis and therapy monitoring of prostate cancer. In the current study, we have evaluated the potential of 2-(18)F- fluoropropionic acid ((18)F-FPA) as a PET tracer for imaging prostate cancer. Methods: (18)F-FPA was synthesized starting from methyl-2-bromopropionate. Small-animal PET studies were performed on mice with CWR22rv1, PC-3, DU-145, and LNCaP prostate xenografts, and comparison of imaging characteristics of (18)F-FPA with (18)F-FDG uptake is reported. Biodistribution studies with (18)F-FPA were performed on mice with CWR22rv1 xenografts and compared with (14)C-acetate. Results: (18)F-FPA was synthesized in 44% overall radiochemical yield (decay-corrected). Small-animal PET studies revealed that (18)FFPA can delineate both androgen-dependent and androgen-independent prostate xenografts with high tumor-to-background ratios. Comparative imaging studies demonstrate the superior performance of (18)F-FPA over (18)F-FDG for imaging prostate cancer, with excellent tumor-to-background contrast. Biodistribution studies show that tumor uptake of the tracer was 5.52 ± 0.35, 5.53 ± 0.42, 5.74 ± 0.54, and 5.34 ± 0.19 percentage injected dose (%ID) per gram at 1, 2, 3, and 4 h, respectively, after injection. The %ID/g values for (18)F-FPA and (14)C-acetate 1 h after tail vein injection were 7.08 ± 0.80 and 0.36 ± 0.08 in tumor, and the corresponding tumor-to-muscle ratios were 1.94 and 2.06, respectively. Conclusion: The data presented here indicate that (18)F-FPA accumulates in prostate cancers with high tumor-to-background ratios. (18)F-FPA has potential for use in the clinical diagnosis of prostate cancer in humans. Copyright © 2009 by the Society of Nuclear Medicine, Inc.
Keywords: unclassified drug; human cell; androgen; nonhuman; positron emission tomography; mouse; animal tissue; animal experiment; animal model; tumor xenograft; drug synthesis; prostate cancer; drug accumulation; drug distribution; diagnostic value; fluorodeoxyglucose f 18; tracer; pet; drug tumor level; quantum yield; 2-<sup>18</sup>f-fluoropropionic acid; <sup>11</sup>c-acetate; cwr22rv1; 2 fluoropropionic acid f 18; acetic acid c 14; radiochemistry
Journal Title: Journal of Nuclear Medicine
Volume: 50
Issue: 10
ISSN: 0161-5505
Publisher: Society of Nuclear Medicine  
Date Published: 2009-10-01
Start Page: 1709
End Page: 1714
Language: English
DOI: 10.2967/jnumed.109.064212
PROVIDER: scopus
PUBMED: 19759108
PMCID: PMC4429801
DOI/URL:
Notes: --- - "Cited By (since 1996): 2" - "Export Date: 30 November 2010" - "CODEN: JNMEA" - "Source: Scopus"
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  1. Steven M Larson
    958 Larson