F-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management.

TitleF-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management.
Publication TypeJournal Article
Year of Publication2018
AuthorsKommidi H, Guo H, Nurili F, Vedvyas Y, Jin MM, McClure TD, Ehdaie B, Sayman HB, Akin O, Aras O, Ting R
JournalJ Med Chem
Volume61
Issue9
Pagination4256-4262
Date Published2018 05 10
ISSN1520-4804
KeywordsAnimals, Carbocyanines, Cell Line, Tumor, Contrast Media, Electrons, Fluorine Radioisotopes, Glutamate Carboxypeptidase II, Male, Mice, Mice, Inbred C57BL, Optical Imaging, Positron-Emission Tomography, Prostatic Neoplasms, Radiochemistry, Tissue Distribution
Abstract

[F]-4, an anionic GCPII/PSMA inhibitor for image-guided intervention in prostate cancer, is described. [F]-4 is radiolabeled with a radiochemical yield that is ≥27% and a molar activity of 190 ± 50 mCi/μmol in a <1 h, one-step, aqueous isotopic exchange reaction. [F]-4 allows PSMA expression to be imaged by fluorescence (FL) and [F]-PET. PC3-PIP (PSMA-positive, EC = 6.74 ± 1.33 nM) cancers are specifically delineated in mice that bear 3 million (18 mg) PC3-PIP and PC3 (control, PSMA-negative) cells. Colocalization of [F]-4 PET, fluorescence, scintillated biodistribution, and PSMA expression are observed.

DOI10.1021/acs.jmedchem.8b00240
Alternate JournalJ Med Chem
PubMed ID29676909
PubMed Central IDPMC6263152
Grant ListK99 EB013904 / EB / NIBIB NIH HHS / United States
P30 CA008748 / CA / NCI NIH HHS / United States
R00 EB013904 / EB / NIBIB NIH HHS / United States
R01 CA178007 / CA / NCI NIH HHS / United States
Related Institute: 
Molecular Imaging Innovations Institute (MI3)

Weill Cornell Medicine
Department of Radiology
525 East 68th Street New York, NY 10065