Download Novel 18F Radiolabeled Tags For PET Imaging

Novel 18F Radiolabeled Tags for PET Imaging
Non-invasive Positron Emission Tomography imaging using Tri-fluoroborate tag
molecules that efficiently and readily fluorinate any bio-molecule of choice.
Advantages:
Technology Details:
Advantages of the tag-molecule strategy.
 Image a ligand or bio-molecule of choice
through binding to a tag molecule.
 The 18F radioisotope can be introduced in
one mild and quick “wash-in” step.
 A high radiochemical yield is obtained
 Allows for centralized manufacture and
local stockpiling of tag molecules or tag
molecule-biomolecule conjugates.
Applications in major clinical fields
including oncology, neurology, and
cardiology.
 Non-invasive, early diagnosis to
determine disease type and extent.
 Theranostic applications to tailor
treatment based on individual diagnosis.
 Non-invasive imaging in numerous
research applications.
Principal Inventor:
David Perrin
Positron Emission Tomography (PET), which involves the
injection of short-lived radionucleotide-labeled tracer
molecules into a patient, is the gold-standard of diagnostic
imaging techniques. PET allows for non-invasive visualization
of metabolic processes, such as cellular proliferation and
neurological disorders. There are currently very few
18
F-labeled
molecules
in
regular
clinical
use,
18-fluorodeoxyglucose (FDG), a sugar derivative used to
image cancer, is the imaging agent used in over 80% of PET
procedures. Currently the synthesis of 18F-labeled molecules
involves high radioactive exposure, and the synthetic
environment is incompatible with the labeling of most
diagnostically relevant bio-molecules.
Dr. David Perrin and co-workers have developed a platform
strategy by which an exceptionally broad range of potential
diagnostically relevant ligands (eg. small molecules, short
DNA or RNA fragments, proteins, and antibodies) can be
easily and quickly labeled with 18F and utilized for imaging
purposes.
The following scheme outlines the process of bio-molecule
attachment, to a boron containing tag-molecule, and
subsequent fluorination to create an individualized PET
imaging agent.
Publications/References:
Ting R, Adam MJ, Ruth TJ, Perrin DM. J Am
Chem Soc. 2005;127(38):13095-6.
Patent Status:
 PCT patent application WO05/077967.
 National phase in the US, Canada, Europe,
and Japan.
 Filed patents describing incremental
improvements to the chemistry.
Reference #:
04-077
Contact:
Brett Sharp, Ph.D.
Technology Transfer Manager
Tel: (604) 822-8588
Email:[email protected]
chemical
linker
OR
X
Y
B
OR
X
B
Y
F acceptor
18
F
OR
Bio-molecule of choice
eg. antibody
Bio-molecule
OR
18F
H 18 F
X
B
Y
18
F
Bio-molecule
reacts with
bio-molecule
tag molecule
Development Stage:
Proof of concept experiments have been successfully
undertaken. The novel tag molecule has been conjugated with
a range of ligands/bio-molecules and the stability of the
chemistry has been proven via PET imaging studies in mice.
Preliminary efficacy studies have visualized a murine tumour
with an 18F–marimastat-tag molecule. Marimastat is a matrix
metalloproteinase inhibitor that underwent clinical trials as a
cancer chemotherapeutic. Bio-distribution data confirms
heightened 18F uptake in the primary tumor with respect to
other organs.
Last Updated: December 2007