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Nucleosides for Imaging and Treatment Applications

Description of Invention:
The present application describes recently developed nucleosides that provide for 1) external imaging of tumor cell proliferation, 2) noninvasive determination of which tumors would be sensitive to drug therapy, and 3) potential utility as a novel antitumor treatment approach. No comparable procedures are available to determine, prior to treatment, which tumors are likely to respond to a given therapeutic approach. This invention also has the ability to rapidly evaluate the success or failure of treatment, during the course of therapy. As imaging agents, these nucleosides are directly targeted towards specific events, rather than broad measures of effect such as fluorodeoxyglucose. There is no currently available treatment for tumors with high levels of drug resistance, specifically due to overexpression of the key enzyme, thymidylate synthase. The utility of these inventions has been demonstrated in cultured human tumor cells, and preclinical toxicology studies have been conducted which permit entry into initial human testing.

Inventors:
Jerry M. Collins (FDA)
Raymond W. Klecker (FDA)
Aspandiar G. Katki (FDA)
Lawrence Anderson (FDA)

Patent Status:
DHHS Reference No. E-058-1997/0 --
U.S. Patent No. 6,677,314 issued 13 Jan 2004
U.S. Patent No. 6,677,315 issued 13 Jan 2004
U.S. Patent No. 6,753,309 issued 22 Jun 2004
U.S. Patent No. 6,682,715 issued 27 Jan 2004
U.S. Patent No. 6,683,045 issued 27 Jan 2004
U.S. Patent No. 6,703,374 issued 09 Mar 2004

Relevant Publication:
  1. JL Eiseman, C Brown-Proctor, P Kinahan, JM Collins, L Anderson, E Joseph, DR Hamburger, SSPan, CA Mathis, MJ Egorin, RW Klecker. Distribution of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) uracil in colorectal cancer xenografts: rationale for therapeutic use and as a positron emission tomography probe for thymidylate synthase. Clin Cancer Res. 2004 Oct 1;10(19):6669-6676. [PubMed abs]
  2. H Sun, A Sloan, TJ Mangner, U Viashampayan, O Muzik, JM Collins, K Douglas, AF Shields. Imaging DNA synthesis with [F-18]FMAU and positron emission tomography in patients with cancers. Eur J Nucl Med Mol Imaging. 2005 Jan;32(1):15-22. [PubMed abs]
  3. H Sun, TJ Mangner, JM Collins, O Muzik, K Douglas, AF Shields. Imaging DNA synthesis in vivo with [F-18]FMAU and PET. J Nucl Med. 2005 Feb;46(2):292-296. [PubMed abs]
  4. H Sun, JM Collins, TJ Mangner, O Muzik, AF Shields. Imaging the pharmacokinetics of [F-18]FAU in patients with tumors: PET studies. Cancer Chemother Pharmacol. 2006 Feb;57(3):343-348. [PubMed abs]



Portfolios:
Cancer

Cancer -Therapeutics


For Additional Information Please Contact:
Whitney Hastings
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: 301/451-7337
Email: hastingw@mail.nih.gov
Fax: 301/402-0220


Web Ref: 369

Updated: 6/99

 

 
 
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