Boron Amino Acid Mimetics for PET Imaging of Cancer


Available for licensing and commercial development as imaging agents for positron emission tomography of cancer are boramino acid compounds. The inventors showed that mimetics created by substituting the carboxylate group (-COO-) of an amino acid with trifluoroborate (-BF3-) are metabolically stable and allow for the use of fluorene-18 (18F) as the radiolabel. Using boroamino acid for 18F-labeling allows for integrating the 18F radiolabel into the core molecular backbone rather than the side-chains thus increasing the agent's target specificity. There is a direct relationship between amino acid uptake and cancer cell replication, where the uptake is extensively upregulated in most cancer cells. This uptake increases as cancer progresses, leading to greater uptake in high-grade tumors and metastases. Amino acids act as signaling molecules for proliferation and may also reprogram metabolic networks in the buildup of biomass. This invention provides for an unmet need for traceable amino acid mimics, including those based on naturally-occurring amino acids, which may be non-invasively detected by imaging technology, including for clinical diagnosis and anti-cancer drug evaluation.

Potential Commercial Applications: Competitive Advantages:
  • Cancer imaging
  • Anti-cancer drug development
 
  • Fluorene-18 labeling
  • Metabolic stability


Development Stage:
  • Early-stage
  • In vitro data available
  • In vivo data available (animal)


Inventors:

Xiaoyuan Chen (NIBIB)  ➽ more inventions...

Zhibo Liu (NIBIB)  ➽ more inventions...


Intellectual Property:
PCT Application No. PCT/US2016/030106
US Application No. 15/570,546
US Application No. 62/155,085

Publications:
Liu Z, et al. PMID 24970911
Liu Z, et al. PMID 25629412

Collaboration Opportunity:

The National Institute of Biomedical Imaging and Bioengineering is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize Boramino Acid Mimetics for Use in Cancer Imaging. For collaboration opportunities, please contact Cecilia Pazman at pazmance@nih.gov.


Licensing Contact:
Michael Shmilovich, J.D.
Email: shmilovm@mail.nih.gov
Phone: 301-435-5019

OTT Reference No: E-135-2015-0
Updated: Jun 29, 2015