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Novel Fluorinated Dmt-Tic Analogues for Use as PET Radiotracers

Description of Technology:

Researchers at the NIH have developed fluorine-18 (18F) labeled analogues specific for the delta- opioid receptors. These radioligands include analogues of the Dmt-Tic pharmacophore, containing a delta-opioid receptor antagonist that may be useful for imaging opioid receptors expressed in lung malignant tumors or other peripheral tumors that express delta-opioid receptors. This methodology might be readily applicable to Dmt-Tic pharmacophoric ligands that exhibit dual antagonism for delta-/mu-opioid receptors.

Studies by the inventors have shown that injected radioligand failed to cross the blood-brain barrier (BBB) of rats; therefore, these compounds could serve as radiotracers for assessing and locating certain carcinomas that contain high levels of delta-opioid receptors, such as lung, breast and/or colon cancers. Since there is an increasing demand of radioligands for in vivo imaging of peripheral opioid receptors, this technology has the potential of enhancing current practices of PET imaging in oncology.

Available for licensing are compositions and methods of locating delta- and/or mu-opioid receptors located in peripheral cancers, such as in lung, breast, and/or colorectal cancer, using opiate radioligands.

Applications:
  • Non-invasive tool for screening lung, breast, and/or colorectal cancers
  • Diagnostic tool for use in PET imaging
Market:
  • For 2007, it was projected that close to 1.5 million Americans would develop cancer.
  • PET imaging is steadily becoming a technique of choice in oncology so many of these patients will likely undergo scans several times during their treatment to assess the stage of their disease. This is supported by rising sales of FDG, which are expected to reach $933 million by 2012.
Development Status:

Early stage

Inventors:

Lawrence H. Lazarus (NIEHS) et al.

Publication:

KA Roth and JD Barchas. Small cell carcinoma cell lines contain opioid peptides and receptors. Cancer 1986 Feb 15;57(4):769-773. [PubMed abs]

Patent Status:

DHHS Reference No. E-317-2007/0 --
U.S. Provisional Application No. 60/970,143 filed 05 Sep 2007

Licensing Status:

Available for licensing

Collaborative Research Opportunity:

The NIEHS Laboratory of Pharmacology, Medicinal Chemistry Group, is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize this technology. Please contact Elizabeth Denholm, Ph.D., Director, NIEHS Office of Technology Transfer, at 919-541-0981 or denholme@mail.nih.gov for more information.

Portfolios:

Cancer - Diagnostics, in vivo, other
Internal Medicine - Diagnostics, imaging, agents

For additional information, please contact:

Charlene A. Sydnor, Ph.D.
Office of Technology Transfer
National Institutes of Health
6011 Executive Boulevard, Suite 325
Rockville MD 20852
Phone: 301/435-4689
Fax: 301/402-0220
Email: sydnorc@mail.nih.gov




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