Imaging and radionuclide therapy agents specific for sodium-iodide symporter

The sodium-iodide symporter (NIS) is biologically important for accumulating iodide in thyroid follicles and anion transport by the human symporter (hNIS) is an established target for molecular imaging and radionuclide therapy.  At present the best radiotracers for PET imaging are limited to 124I- and 18F-BF4-.  King’s researchers have developed a number of fluoride-containing hNIS substrates, such as fluorosulphate (18F-SO3F).  It is a high-affinity substrate that is easily synthesized in high yield and very high specific activity and represents a promising candidate for clinical PET imaging.

 

The Problem

The sodium-iodide symporter (NIS) is biologically important for accumulating iodide in thyroid follicles.  Anion transport by the symporter is an established target for molecular imaging and radionuclide therapy.  Several radioactive substrates of human NIS (hNIS) are being used for radionuclide therapy and imaging of thyroid-related disorders.  Next-generation radiopharmaceuticals being evaluated for these purposes include 186/188ReO4- for therapy and 18F-BF4- for positron emission tomography (PET) imaging.  The radiotracers for PET imaging are limited to 124I- and 18F-BF4- at present. The inventors thus sought to develop new 18F-labeled hNIS substrates offering higher specific activity, higher affinity and simpler radiochemical synthesis than 18F-BF4-.

 

The Solution

Researchers at King’s have developed a number of fluoride-containing hNIS substrates.  Fluorosulphate (SO3F) is a high-affinity hNIS substrate and appears to be the most promising.  18F-SO3F is easily synthesized in high yield and very high specific activity and is a promising candidate for pre-clinical and clinical PET imaging of hNIS expression and thyroid-related disease.

 

Benefits

The radiotracer compounds may be produced in a composition with high specific activity and high radiochemical purity. The present inventors have also shown that such radiotracer compounds have a high and NIS-specific uptake in NIS-expressing cells in vitro and excellent specific uptake of the tracer in NIS expressing tissues (namely, the thyroid, stomach and salivary glands) in animal model in vivo studies.  Also, the agents can be used for imaging cells engineered to express NIS, for the purposes of imaging and monitoring of diseases related to NIS-expressing cells and tracking of cells engineered to express NIS after therapeutic administration of such engineered cells.

 

Opportunity

We are seeking a development partner wishing to take an option / evaluation licence over the technology to support pre-clinical and clinical development.  Exclusivity is available for a suitable partner.

 

 

 

IP Status

There is currently an international PCT application which published as WO2017/076879 A1 in May 2017. The sole applicant is King’s College London (Application number: PCT/EP2016/076385; Priority date: 6 November 2015).

 

Further Information

See Journal of Nuclear Medicine, January 2017, vol. 58: pp 156-161.

 

 

Patent Information:
For Information, Contact:
Ceri Mathews
IP & Licensing Manager
King's College London
ceri.mathews@kcl.ac.uk
Inventors:
Philip Blower
Alex Khoshnevisan
Keywords: