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Zirconium-89 PET Imaging Agent for Cancer

Posted Apr 22 2013 8:00pm

Description of Invention:
This technology is a new generation of rationally designed chelating agents which improve the complexation of Zirconium-89 for PET imaging of cancers. The technology uses cyclic or acyclic chelators made of 4 hydroxamate donors groups for improved stability compared to the currently used natural product siderophore desferrioxamine B (DFB), a chelator that consists of only 3 hydroxamate donors that fails to saturate the coordination sphere of Zr(IV). DFB, which has been the object of many pre-clinical and clinical studies exhibits insufficient stability resulting in progressive radioisotope accumulation in bone once injected that can contribute to toxicity and increased background. The new chelators described in this invention have shown improved kinetic inertness compared to DFB with stability up to 90% after 7 days compared to 28% for DFB. In association with an adequate targeting agent such as an antibody, toxicity to the bone can be reduced and images with better contrast can be obtained with these new chelators.

  • Cancer imaging
  • PET imaging
  • ImmunoPET

  • High stability
  • Low toxicity
  • Better imaging contrast

Development Status:
  • Prototype
  • In vitro data available

Martin W Brechbiel (NCI)
Yong-Sok Lee (CIT)
Francois Guerard (NCI)

Patent Status:
HHS, Reference No. E-111-2013/0
US, Application No. 61/779,016 filed 13 Mar 2013

Related Technologies:
US, Application No. 12/667,790 filed 05 Jan 2010, Reference No. E-194-2007/0
US, Patent No. 8,288,530, Issued 16 Oct 2012, Reference No. E-226-2006/0
PCT, Application No. PCT/US91/01919 filed 22 Mar 1991, Reference No. E-067-1990/0
US, Application No. 60/864,503 filed 06 Nov 2006, Reference No. E-226-2006/0
US, Application No. 60/929,913 filed 17 Jul 2007, Reference No. E-194-2007/0

Relevant Publication:
  1. Zhou Y, et al. [ PMID 23123291 ]
  2. Deri MA, et al. [ PMID 22998840 ]
  3. Vosjan MJ, et al. [ PMID 20360768 ]
  4. Nayak TK, et al. [ PMID 22213822 ]
  5. Evans MJ, et al. [ PMID 23236019 ]
  6. Guerard F, et al. [ PMID 23250287 ]

Collaborative Research Opportunity:
The Radioimmune & Inorganic Chemistry Section, ROB, CCR, NCI, is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize Zirconium-89 chelation technology for ImmunoPET imaging and other applications. For collaboration opportunities, please contact John D. Hewes, Ph.D. at .

For Licensing Information Please Contact:
Michael Shmilovich Esq.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-5019
Fax: 301-402-0220

Ref No: 2552

Updated: 04/2013

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