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Theranostics in the fight against cancer

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 most advanced chemical research apparatus in Africa

2005-11-23

Celebrating the inauguration of the NMR were from the left Prof Frederick Fourie (Rector and Vice-Chancellor of the UFS), Dr Detlef Müller (Development Scientist and Manager: Africa and Asia of Bruker in Germany, the supplier of the NMR), Prof Jannie Swarts (head of the head of the Division Physical Chemistry at the UFS) and Prof Herman van Schalkwyk (Dean: Faculty of Natural and Agricultural Sciences at the UFS). Photo: Lacea Loader

UFS boasts with most advanced chemical research apparatus in Africa

The University of the Free State’s (UFS) Department of Chemistry now boasts with some of the most advanced chemical research apparatus in Africa after the latest addition, a nuclear magnetic resonance (NMR) spectrometer, was inaugurated today by the Rector and Vice-Chancellor, Prof Frederick Fourie. The NMR is used to analyse molecular structures.

Last month the Department of Chemistry celebrated the installation of the most advanced single crystal X-ray diffractometer in Africa. The diffractometer provides an indispensable technique to investigate among others the solid state of compounds for medicinal application.

“Three years ago the UFS executive management realised that, if we want to build a university of excellence, we should invest in research. We started to think strategically about chemistry and decided to bring the apparatus at the Department of Chemistry on a more competitive standard. Strategic partnerships were therefore secured with companies like Sasol,” said Prof Fourie during the inauguration ceremony.

“The installation of the NMR symbolises the ability of the UFS to turn academic areas around. I hope that this is the beginning of a decade of excellence for chemistry at the UFS,” said Prof Fourie.

”The catalogue value of the Bruker 600 MHz NMR is approximately R11 million. With such an advanced apparatus we are now able to train much more post-graduate students,“ said Prof Jannie Swarts, head of the Division Physical Chemistry at the UFS.

”The NMR is the flagship apparatus of the UFS Department of Chemistry that enables chemists to look at compounds more easily at a molecular level. Research in chemistry is critically dependent on NMR, which is a technique that can determine the composition of reactants and products in complicated chemical reactions, with direct application is most focus areas in chemistry,“ said Prof Swarts.

”Parts of the spectrometer consists of non-commercial items that were specifically designed for the UFS Department of Chemistry to allow the study of unique interactions in e.g. rhodium and platinum compounds,” said Prof Swarts.

According to Prof Swarts the NMR enables chemists to conduct investigations on the following:

To evaluate for example the complex behaviour of DNA in proteins as well as the analysis of illegal drugs sometimes used by athletes.
It provides an indispensable technique to investigate compounds for medicinal application for example in breast, prostate and related bone cancer identification and therapy, which are currently synthesised in the Department of Chemistry.
It can also be applied to the area of homogeneous catalysis where new and improved compounds for industrial application are synthesized and characterised, whereby Sasol and even the international petrochemical industry could benefit. This analytical capacity is highly rated, especially in the current climate of increased oil prices.
The NMR can detect and identify small concentrations of impurities in feed streams in the petrochemical industry, e.g. at Sasol and also the international petrochemical industry. These minute amounts of impurities can result in metal catalyst deactivation or decomposition and can cause million of rands worth in product losses.
It is indispensable for studying the complexity of samples that is non-crystalline. These materials represent the vast majority of chemical compounds such as solvents, gasoline, cooking oil, cleaning agents and colorants as examples.

According to Prof Swarts the general medical technique of MRI (magnetic resonance imaging) in use at larger hospitals, is based on NMR technology.

”The NMR apparatus enabled the Department of Chemistry to characterise complex molecules that were synthesised for the multi-national company, FARMOFS-PAREXEL, and to negotiate research agreements with overseas universities,” said Prof Swarts.

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

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