Evans Blue Dye Derivatives for Serum Albumin Labeling

Description:
The invention is an imaging agent and method of use for imaging blood pools and the lymphatic system. The imaging agent binds with high affinity to serum albumin, the most abundant serum protein, and can be tagged with several isotopes making it suitable for magnetic resonance imaging or positron emission tomographic imaging. To date, only very few blood-pool tracers have been introduced for positron emission tomography. The existing ones have short half-lives (20.4 min for 11C and 2.05 min for 15O) and thus can only be used in centers with an in-house cyclotron. Compared with these radiometals, 18F has the advantages of being a pure position emitter with ideal half-life. It is the dominant radioisotope used for PET imaging for both clinical applications and preclinical investigations. Evans blue dye has been an important tool in many physiological and clinical investigations because of its high affinity for plasma albumin and has been used for a long time in clinical practice for determination of patient plasma volume. By taking advantage of the high in-vivo EB binding affinity to albumin, the current imaging agent is a NOTA conjugate of truncated form of Evans blue (NEB) for in vivo albumin labeling and then labeling with 18F labeling by the formation of 18F-aluminum fluoride complex. The NOTA also facilitates radiometal labeling of NEB with either 68Ga or 64Cu. The resulting imaging agent does not affect the in vivo behavior of serum albumin such as circulation, extra-vascularization, and turn-over; thus the imaging results will reflect the distribution and metabolism of serum albumin accurately.
Patent Information:
For Information, Contact:
Michael Shmilovich
Senior Licensing And Patenting Manager
NIH Technology Transfer
301-435-5019
shmilovm@nih.gov
Inventors:
Lixin Lang
Gang NIU
Xiaoyuan (Shawn) Chen
Keywords:
Albumin
BLUE
CA2BXX
Evans Blue
fluorene-18
IA4AXX
LABELED
LABELING
Listed LPM Fenn as of 4/15/2015
Magnetic Resonance
PET
Pet imaging
positron emission
Positron-Emitting
Post LPM Assignment Set 20150420
Pre LPM working set 20150418
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