Technology ID
TAB-4585

Radiotherapy and Imaging Agent-based on Peptide Conjugated to Novel Evans Blue Derivatives with Long Half-life and High Accumulation in Target Tissue

E-Numbers
E-150-2016-0
Lead Inventor
Chen, Xiaoyuan (Shawn) (NIBIB)
Co-Inventors
Jacobson weiss, Orit (NIBIB)
Applications
Research Materials
Diagnostics
Therapeutic Areas
Oncology
Development Stages
Pre-Clinical (in vitro)
Research Products
Research Equipment
Lead IC
NIBIB
ICs
NIBIB

This technology includes a newly designed, truncated Evans Blue (EB) form which allows labeling with metal isotopes for nuclear imaging and radiotherapy. Unlike previous designs, this new form of truncated EB confers site specific mono-labeling of desired molecules. The newly designed truncated EB form can be conjugated to various molecules including small molecules, peptides, proteins and aptamers to improve blood half-life and tumor uptake, and confer better imaging, therapy and radiotherapy. As a proof of concept, we chose to conjugate the new truncated EB to Arg-Gly-Asp (RGD) tripeptide, which binds to integrin avl33. lntegrin avl33 is a molecular marker for angiogenesis which is significantly upregulated in cancerous tissue and can be used as a target for therapy.

Commercial Applications
This product will be of use in nuclear imaging and radiotherapy of cancer as the EB derivative can be used for increasing the blood half-life of peptides and molecule.

Competitive Advantages
Compared to RGD alone, the EB-RGD has significantly higher half-life in the blood. Because RGD binding to avl33 induce peptide internalization into the cell, the higher half-life of EB-RGD in the blood result in about tenfold increase in peptide accumulation in target organ and low background.
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