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Fluorinated Fructose Derivatives for PET Imaging

Summary

TEC Edmonton is seeking collaborative development and licensing partners for a novel PET imaging agent. Dr. Chris Cheeseman and colleagues at the University of Alberta have recently designed and synthesized a new class of fluorinated fructose compounds with the potential to be used during in vivo PET imaging of breast cancer. One such compound, 6-deoxy-6-fluoro-D-fructose (6FDF), has been shown to be transported in vitro into two human, GLUT5 expressing breast cancer cell lines. Early in vivo trials using a GLUT 5 expressing murine breast cancer model have had promising results, with flank implanted tumors readily taking up [18F]6FDF.

Traditionally, tumor imaging with PET relies on the use of the glucose analogue 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) as the imaging agent, which takes advantage of the characteristic overexpression of GLUT1 (a member of the family of facilitative hexose transport proteins known as GLUTs) in many cancerous cells.

Unfortunately, [18F]FDG-PET is ineffective in the detection of small tumors and more differentiated subtypes, accumulates in areas of inflammation (due to the large uptake of [18F]FDG by immune cells), generating false-positives or poor resolution images. Additionally, certain tumors demonstrate low expression of GLUT1, leading to false negative results. In breast cancer, the glucose/fructose transporter GLUT2 and the fructose transporter GLUT5 have been shown to be over-expressed in many breast tumors, suggesting that fructose-based analogues would be useful for the improved imaging of breast cancer.

Supplementary Information

Patent Number: US8501154B2
Application Number: US13622599A
Inventor: Cheeseman, Chris | West, Frederick | Grant, Tina | Trayner, Brendan | Mercer, John | Manolescu, Andrei
Priority Date: 15 May 2009
Priority Number: US8501154B2
Application Date: 19 Sep 2012
Publication Date: 6 Aug 2013
IPC Current: A61K005100 | A61M003614
US Class: 42400173 | 42400111 | 42400161 | 42400185 | 42400189 | 536122 | 53600122
Assignee Applicant: The Governors of the University of Albertalgary, Alberta | The Governors of the University of Alberta,Edmonton
Title: Fluorinated fructose derivatives for PET imaging
Usefulness: Fluorinated fructose derivatives for PET imaging
Summary: (X) is useful for preparing (XI). (XI) is useful for diagnosing, treating or monitoring cancer in a subject, where the cancer brain cancer, lung cancer , breast cancer, pancreas cancer, kidney cancer, colon cancer, rectum cancer, ovary cancer, prostate cancer, head cancer, neck cancer, thyroid cancer, bladder cancer, bone cancer, endometrial cancer, testicular cancer, gastric cancer or neuroblastoma (all claimed). Tests details are described but no results given.
Novelty: New fructose derivatives useful for preparing (18F)-6-deoxy-6-fluoro-D-fructose, which is useful for diagnosing, treating or monitoring cancer e.g. brain cancer, lung cancer , breast cancer, pancreas cancer and kidney cancer

Industry

Disease Diagnostic/Treatment

Sub Category

Cancer/Tumor

Application No.

US Patent Nos. 8,293,208 and 8,501,154

ID No.

2008079

Country/Region

Canada