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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 to host one of three world summits on crystallography
2014-04-15

 
Prof André Roodt from the Department of Chemistry at the University of the Free State (UFS), co-unveiled a special plaque in Poznan, Poland, as president of the European Crystallographic Association, with prof Gautam Desiraju, president of the IUCr (front right) and others to commemorate the Nobel prize winner Max von Laue. (Photo's: Milosz Ruszkowski, Grzegorz Dutkiewicz)

Prof André Roodt from the Department of Chemistry at the University of the Free State (UFS), co-unveiled a special plaque in Poznan, Poland, as president of the European Crystallographic Association, to commemorate the Nobel prize winner Max von Laue at a special Laue Symposium organised by prof Mariusz Jaskolski from the A. Mickiewicz University in Poznan.

Max von Laue, who spent his early childhood in Poznan, was the first scientist to diffract X-rays with a crystal.

2014 has been declared by the United Nations as the International Year of Crystallography, and it was recently officially opened at the UNESCO headquarters in Paris, France, by the Secretary-General of the UN, Ban Ki-moon. The International Year of Crystallography celebrates the centennial of the work of Max von Laue and the father and son, William Henry and William Laurence Bragg.

As part of the celebrations, Prof Roodt, president of the European Crystallographic Association, one of the three regional affiliates (Americas, Europe and Africa; Asia and Australasia) of the International Union of Crystallography (IUCr), was invited by the president of the IUCr, Prof Gautam Desiraju, to host one of the three world summits, wherein crystallography is to showcase its achievements and strategise for the future.

The summit and conference will take place on the Bloemfontein Campus of the UFS from 12 to 17 October 2014 and is titled: 'Crystallography as vehicle to promote science in Africa and beyond.' It is an ambitious meeting wherein it is anticipated to bring the French-, English- and Arab-speaking nations of Africa together to strategise how science can be expanded, and to offer possibilities for this as nestled in crystallography. Young and established scientists, and politicians associated with science and science management, are the target audience to be brought together in Bloemfontein.

Dr Thomas Auf der Heyde, acting Director General of the South African Department of Science and Technology (DST), has committed some R500 000 for this effort, while the International Union of Crystallography provided R170 000.

“Crystals and crystallography form an integrated part of our daily lives, form bones and teeth, to medicines and viruses, new catalysts, jewellery, colour pigments, chocolates, electronics, batteries, metal blades in airplane turbines, panels for solar energy and many more. In spite of this, unfortunately, not many people know much about X-ray crystallography, although it is probably one of the greatest innovations of the twentieth century. Determining the structure of the DNA was one of the most significant scientific events of the 20th century. It has helped understand how genetic messages are being passed on between cells inside our body – everything from the way instructions are sent to proteins to fight infections, to how life is reproduced.

“At the UFS, crystallography finds application in Chemistry, Physics, Biology, Mathematics, Geology, Engineering and the Medical fields. Crystallography is used by the Curiosity Rover, analysing the substances and minerals on Mars!

“The UFS’s Departments of Chemistry and Physics, in particular, have advanced instruments and important research thrusts wherein X-ray crystallography has formed a central part for more than 40 years.

“Crystallography has produced some 28 Nobel prize winners over the past 100 years and continues to provide the means for fundamental and applied research,” said Prof Roodt.

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