IMAGING TUMORS USING PHOSPHOAMIDATE DERIVATIVES OF FAU

Case ID:
05-746

Technology

Phosphoramidate derivatives of a furanosylurical analog (FAU-PA) have been developed which can effectively deliver intracellular FAU monophosphate. This results in improved formation of nucleoside triphosphates and higher incorporation into DNA and can be used for imaging and to treat cancers. When labeled with F-18 it may function as a PET tracer either alone or in conjunction with other agents for imaging and monitoring cellular proliferation.

Background

There is a clinical need for a specific anti-neoplastic agent which provides information about a tumor’s response to treatment. The ultimate goal is to understand the response of cancer to therapy using measurements of DNA synthetic pathways as imaged by positron emission tomography (PET). A new series of FAU thymidine analogs have been developed for use as an anti-neoplastic as well as a Positron Emission Tomography (PET) imaging agents.

Stage of Development

WSU has conducted the first-in human phase 0 study of 18F-FAU to determine its suitability for imaging and to determine its potential as an antineoplastic agent. A phase I study using unlabeled FAU has started at Karmanos Cancer Institute and uses 18F-FAU and PET to monitor pharmacodynamics in tumors.

Patent status

Issued 7,888,330

References

“Simultaneous determination of 1-(2'-deoxy-2'-fluoro-β-D-arabinofuranosyl) uracil (FAU) and 1-(2'-deoxy-2'-fluoro-β-D-arabinofuranosyl) 5-methyluracil (FMAU) in human plasma by liquid chromatography/tandem mass spectrometry.” J Chromatogr B Analyt Technol Biomed Life Sci. 2012;891-892:64-70.

 

Patent Information:
For Information, Contact:
Nicole Grynaviski
Commercialization Principal
Wayne State University
nicole.grynaviski@wayne.edu
Inventors:
Anthony Shields
Jiri Zemlicka
Sridhar Nimmagadda
Keywords:
Anti-cancer
Compound
Imaging