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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

Prestige Scholar hosts Prof John Helliwell of Manchester University
2015-12-08

From left is Prof John R. Helliwell (School of Chemistry, University of Manchester), Dr Madeleine Helliwell (School of Chemistry, University of Manchester), Prof Andre Roodt (Department of Chemistry, University of the Free State) and Dr Alice Brink (Department of Chemistry, University of the Free State).
Photo: Steven Collett

At the invitation of Dr Alice Brink of the Department of Chemistry, Prof John Helliwell, the 2015 Max Perutz Prize winner, and his wife, Dr Madeleine Helliwell, visited the University of the Free State (UFS).
The Helliwells, both chemists of note, took part in a series of lectures and exchanges on the Bloemfontein and Qwaqwa Campuses.
This visit from 9-19 November 2015 was the consequence of Dr Brink’s participation in the Vice-Chancellor’s Prestige Scholars Programme (PSP) initiative to encourage the broadening of the international footprint of the next generation of scholars in the academy.

Two year collaboration

Dr Brink and Prof Helliwell from Manchester University have a standing collaboration going back two years. Dr Brink, an NRF Thuthuka grant holder and a member of the PSP since 2013, has spent almost eight months in Manchester, collaborating with Prof Helliwell on her study of the successful interaction of rhenium tricarbonyl complexes with proteins determined via protein crystallography.
Their collaboration resulted from the close association of Prof Helliwell and Prof Andre Roodt from the UFS Department of Chemistry, both former presidents of the European Crystallographic Association.

Sharing academic expertise

Prof Helliwell, the 2014 American Crystallographic Association Patterson Award winner for his “pioneering contributions to the global development of the instrumentation, methods and applications of synchrotron radiation in macromolecular crystallography”, gave three lectures in the Department of Chemistry, two on the Boemfontein Campus, and the other on the Qwaqwa Campus on 13 November 2015.

Dr Helliwell, former co-editor of the Acta Crystallographica Section C: Crystal Structure Communications journal, consulted with postgraduate students from the Departments of Chemistry and Biochemistry.

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