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25 April 2022 | Story Elsabé Brits
Andre Roodt and Alice Brink
Prof Andreas Roodt and Prof Alice Brink are two of the inventors of the ‘Multinuclear complexes and their preparation patent.

According to the World Health Organisation (WHO), cancer is a leading cause of death worldwide, accounting for nearly 10 million deaths in 2020, or nearly one in six. The most common cancers are breast, lung, colon, rectum, and prostate cancers. There is a constant need to provide methods to diagnose and treat cancer-related tumours.  Current research strategies focus on eliminating cancer cells with the minimum damage to surrounding healthy cells.

A limitation of current technologies is that they are mostly based on the separate identification of cancer (diagnostic), followed by treatment (therapy) using chemotherapy and/or radiotherapy. To fit both needs at the same time and with similar or identical compounds, the principle of theranostic medicine was identified. This concept employs both diagnosing (by imaging) cancer and delivering therapy (treatment) simultaneously, which has been receiving increased attention internationally.

Collaborating with the University of Zurich
A University of the Free State (UFS) team, together with a team from the University of Zürich, conducted exciting research in this area and filed a patent titled ‘Multinuclear complexes and their preparation’. The patent was granted in South Africa and by the European Patent Office. It is being validated in selected European countries. The patent is pending in the USA, Japan, Hong Kong, and India. The inventors from the UFS are Prof Andreas Roodt, Prof Alice Brink, Dr Pennie Mokolokolo, and Dr Vincent Dumisani Kama. The approach that their technology takes is to enable the synthesis of a multinuclear compound/s, which may contain different pre-selected radioisotopes, to allow both imaging and therapy to the cancer site(s) with one and the same metal-organic complex.

So far, high-yield production of compounds has been successfully innovated, which contain both an imaging (in particular the widely utilised imaging isotope Technetium-99m) and therapeutic (typically the therapeutic isotope Rhenium-186) radioactive isotope(s), optionally carrying an additional cytotoxic agent. (Chemotherapy uses anti-cancer [cytotoxic] drugs to destroy cancer cells.)

Nuclear medicine technologies
In the next phase of the research, a lead compound portfolio of four to five model pharmaceuticals containing these metal nuclides with appropriate directing groups to target cancer sites will be designed and constructed. A number of these entities are known and can be introduced through different techniques. These will then undergo full characterisation and efficacy evaluation in biological models (in vitro), followed by extensive animal and human trials.

The technology will be delivered as a product or service in the way that current nuclear medicine technologies are delivered.

The fact that this product(s) contains both imaging and therapeutic radionuclides or cytotoxic modalities, enables detailed tracking of the pharmaceutical and monitoring of the tumours' response to the therapy. Not directly related to the patent, but an asset to it, is the fact that the incorporation of rhenium with a high atomic number (Z = 75) opens the additional opportunity to utilise the multinuclear compounds also as radiosensitisers. Synergistic effects, enhancing the therapeutic efficacy, can thus be expected in combination with radiotherapy.

The UFS would like to partner with a pharmaceutical company working in the field of nuclear medicine to commercialise this technology. Interested parties can contact Ravini Moodley at MoodleyR5@ufs.ac.za

News Archive

UFS boasts with world class research apparatus
2005-10-20

 

 

At the launch of the diffractometer were from the left Prof Steve Basson (Chairperson:  Department of Chemistry at the UFS), Prof Jannie Swarts (Unit for Physical and Macro-molecular Chemistry at the UFS Department of Chemistry), Mr Pari Antalis (from the provider of the apparatus - Bruker SA), Prof Herman van Schalkwyk (Dean:  Faculty of Natural and Agricultural Sciences at the UFS), Prof André Roodt (head of the X-ray diffraction unit at the UFS Department of Chemistry) and Prof Teuns Verschoor (Vice-Rector:  Academic Operations at the UFS).

UFS boasts with world class research apparatus
The most advanced single crystal X-ray diffractometer in Africa has been installed in the Department of Chemistry at the University of the Free State (UFS).

“The diffractometer provides an indispensable technique to investigate compounds for medicinal application for example in breast, prostate and related bone cancer identification and therapy, currently synthesized in the Department of Chemistry.  It also includes the area of homogeneous catalysis where new compounds for industrial application are synthesised and characterised and whereby SASOL and even the international petrochemical industry could benefit, especially in the current climate of increased oil prices,” said Prof Andrè Roodt, head of the X-ray diffraction unit at the UFS Department of Chemistry.

The installation of the Bruker Kappa APEX II single crystal diffractometer is part of an innovative programme of the UFS management to continue its competitive research and extend it further internationally.

“The diffractometer is the first milestone of the research funding programme for the Department of Chemistry and we are proud to be the first university in Africa to boast with such advanced apparatus.  We are not standing back for any other university in the world and have already received requests for research agreements from universities such as the University of Cape Town,” said Prof Herman van Schalkwyk, Dean:  Faculty of Natural and Agricultural Sciences at the UFS.

The diffractometer is capable of accurately analysing molecules in crystalline form within a few hours and obtain the precise geometry – that on a sample only the size of a grain of sugar.   It simultaneously gives the exact distance between two atoms, accurate to less than fractions of a billionth of a millimetre.

“It allows us to investigate certain processes in Bloemfontein which has been impossible in the past. We now have a technique locally by which different steps in key chemical reactions can be evaluated much more reliable, even at temperatures as low as minus 170 degrees centigrade,” said Prof Roodt.

A few years ago these analyses would have taken days or even weeks. The Department of Chemistry now has the capability to investigate chemical compounds in Bloemfontein which previously had to be shipped to other, less sophisticate sites in the RSA or overseas (for example Sweden, Russia and Canada) at significant extra costs.

Media release
Issued by:Lacea Loader
Media Representative
Tel:   (051) 401-2584
Cell:  083 645 2454
E-mail:  loaderl.stg@mail.uovs.ac.za
19 October 2005   

 

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