Title: 

Diagnostic radiopharmaceutical for imaging the level of cholinesterases, method of its preparation and its application. 

Protection status: 

Patent No. Pat.236172 

Subject: 

The invention is a diagnostic radiopharmaceutical based on the tacrine derivative N-(1,2,3,4-tetrahydroacridin-9-yl)nonane-1,9-diamine (Tac(9)), a compound characterized by better bioavailability than tacrine itself, used in Alzheimer’s disease therapy. This compound combined with an appropriate ligand (e.g. HYNIC, DOTA, DOTAGA, NOTA, NODAGA – a molecule that binds the radionuclide cation) creates a bioconjugate which, after labeling with a radionuclide, creates a diagnostic radiopharmaceutical. Such a preparation introduced into the body accumulates in disease foci, in the case of the presented invention in areas of the brain with an increased level of the AChE enzyme. The intensity of the emitted radiation during SPECT (Single-Photon Emission Computed Tomography, using a preparation containing a gamma radiation emitter) or PET (Positron Emission Tomography, using a preparation containing a beta plus radiation emitter) method allows precise localization of the radiation source (radionuclides) – location areas of the brain affected by neurodegeneration. 

Benefits: 

The diagnostic radiopharmaceutical allows for precise identification of brain areas affected by neurodegeneration. enabling the diagnosis of Alzheimer’s disease at a very early stage, several years before detectable morphological symptoms appear, that can be diagnosed using standard diagnostic methods. As a result, this will allow for earlier treatment, which directly translates into effectively slowing down the development of this disease. 

The resulting complex of a radiopharmaceutical molecule – radionuclide, after attachment to a selected biologically active molecule, does not change its biological properties. Moreover, administering nanogram amounts of a radiopharmaceutical to patients does not affect the normal functioning of the body, therefore there are no practical contraindications in terms of the toxicity of the preparation. The compound is practically 100% stable in human serum and cerebrospinal fluid, has high biological activity towards appropriate enzymes and has a sufficiently good ability to cross the blood-brain barrier. It is easy to synthesize and does not require relatively high costs, thereby it can be widely available. 

Stage of work: 

The work is at the preclinical study stage. 

Application: 

Early diagnosis of Alzheimer’s disease. 

Contact: 

@:  sylwia.grzelak@umed.lodz.pl, tel.: 502 447 575