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Novel precursors for the PET radiotracer [18F]FAZA

总结: TEC Edmonton is seeking licensing partners for a novel precursor that simplifies synthesis of [18F]FAZA, a PET radiotracer that selectively accumulates in hypoxic cells. It was invented and developed at the Cross Cancer Institute of Alberta and is currently used in several medical centers to assess tumor hypoxia in cancer patients. [18F]FAZA shows improved tracer pharmacokinetics in comparison to other 'first generation' clinical hypoxia PET tracers, giving higher hypoxia tissue: background ratios resulting in superior visualization of hypoxic tissue.

One drawback to the use of [18F]FAZA is its existing synthesis precursor, which gives low radiochemical yields (RCY) of [18F]FAZA. This is in part due to the complexity of the final radiolabeled mixture which generates secondary chemical and radiochemical products and requires careful purification to produce sufficiently pure [18F]FAZA for use.

The inventors of [18F]FAZA have recently discovered novel precursors that can be labeled cleanly, simplifying the final purification stage and significantly improving the RCY for the overall process. The labeling conditions required for these new precursors are compatible with commonly used commercial automated synthesis units for PET radiotracer preparation, and can be easily transformed into kit-based automated production of [18F]FAZA PET tracer.

附加资料: Inventor: Borbély, János | Bodnár, Magdolna | Balogh, Lajos | Polyák, András
Priority Number: US20130302243A1
IPC Current: A61K005104 | A61K005106 | A61K005112
US Class: 42400137
Assignee Applicant: BBS NanoMedicina Zrt.brecen | BBS NANOMEDICINA ZRT.brecen
Title: RADIOLABELED NANOSYSTEM, PROCESS FOR THE PREPARATION THEREOF AND ITS USE
Usefulness: RADIOLABELED NANOSYSTEM, PROCESS FOR THE PREPARATION THEREOF AND ITS USE
Summary: The composition is useful in targeted radiopharmaceutical imaging for targeting tumor cells (all claimed), preferably during diagnostic therapies of the tumor.
Novelty: Scintigraphic imaging composition useful in targeted radiopharmaceutical imaging for targeting tumor cells, comprises self-assembled nanoparticles and radionuclide metal ions complexed to nanoparticles containing targeting agent

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