Technology Bundle ID
NCI-E-111-2013

Zirconium-89 PET Imaging Agent for Cancer

Applications
Research Materials
Lead Inventors
Martin Brechbiel Brechbiel (NCI)
Co-Inventors
Francois Guerard (NCI)
Yong Lee (CIT)
Development Status
Prototype
ICs
NCI
CIT

Researchers at the NCI Radiation Oncology Branch  and NIH CIT Center for Molecular Modeling developed a tetrahydroxamate chelation technology that provides a more-stable Zr-89 complex as an immuno-PET cancer imaging agent. In either the linear or the macrocyclic form, the tetrahydroxamate complexes exhibit greater stability as chelating agents compared to Zr-89 complexed to the siderophore desferrioxamine B (DFB), a trihydroxamate, which represents the current state of the art chemistry and the agent currently in clinical use. 

In the Zr-89-DFB imaging agents, Zr-89 dissociates from the chelate, resulting in an increasing radioisotope accumulation in the bone 2-3 days after injection. In vitro studies demonstrate the tetrahydroxamate-chelated Zr-89 remained kinetically inert for seven or more days, thereby reducing the amount of Zr-89 that is released compared to the complex containing DFB.

Commercial Applications
  • PET imaging, especially for cancer and in particular Immuno-PET imaging
Competitive Advantages
  • High stability  with low toxicity

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