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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

Cardiology Unit involved in evaluation of drug for rare genetic disease
2013-01-04

Front from the left, are: Marinda Karsten (study coordinator and registered nurse),
Laumarie de Wet (clinical technologist), Charmaine Krahenbuhl (study coordinator and radiographer),
Lorinda de Meyer (administrator), Andonia Page (study coordinator and enrolled nurse);
back Dr Gideon Visagie (sub investigator), Dr Derick Aucamp (sub investigagtor),
Prof. Hennie Theron, (principal investigator) and Dr Wilhelm Herbst (sub investigator).
Photo: Supplied
09 January 2013


The Cardiology Research Unit at the University of the Free State (UFS) contributed largely to the evaluation of the drug Juxtapid (lomitapide), which was developed by the Aegerion pharmaceutical company and approved by the FDA (Federal Drug Administration). Together with countries such as die USA, Canada and Italy, the UFS’ Unit recruited and evaluated the most patients (5 of 29) for the study since 2008.  

The drug was evaluated in persons with so-called familial homozygous hypercholesterolemia (HoFH).  

Following its approval by the FDA, Juxtapid is now a new treatment option for patients suffering from HoFH. The drug operates in a unique way which brings about dramatic improvements in cholesterol counts.  

According to Prof. Hennie Theron, Associate Professor in the Department of Cardiology at the UFS and Head of the Cardiology Contract Research Unit, HoFH is a serious, rare genetic disease which affects the function of the receptor responsible for the removal of low-density lipoprotein cholesterol (LDL-C) (“bad” cholesterol) from the body. Damage to the LDL receptor function leads to extremely high levels of blood cholesterol. HoFH patients often develop premature and progressive atherosclerosis, which is a narrowing or blockage of the arteries.  

“HoFH is a genetically transmitted disease and the most severe form of hypercholesterolemia. Patients often need a coronary artery bypass or/and aortic valve replacement before the age of 20. Mortality is extremely high and death often occurs before the third decade of life. Existing conventional cholesterol-lowering medication is unsuccessful in achieving normal target cholesterol values in this group of patients.  

“The only modality for treatment is plasmapheresis (similar to dialysis in patients with renal failure). Even with this type of therapy the results are relatively unsatisfactory because it is very expensive and the plasmapheresis has to be performed on a regular basis.  

“The drug Juxtapid, as currently evaluated, has led to a dramatic reduction in cholesterol values and normal values were achieved in several people. No existing drug is nearly as effective.  

“The drug represents a breakthrough in the treatment of familial homozygous hypercholesterolemia. The fact that it has been approved by the FDA, gives further impetus to the findings,” says Prof. Theron.  

In future further evaluation will be performed in other forms of hypocholesterolemia.  

According to Prof. Theron, the findings of the study, as well as the recent successful FDA evaluation, once again confirms the fact that the UFS’ Cardiology Contract Research Unit is doing outstanding work.  

Since its inception in 1992, the Unit has already been involved in more than 60 multi-centre, international phase 2 and 3 drug studies. Several of these studies, including the abovementioned study, really affected the way in which cardiology functions.  

The UFS’ Cardiology Contract Research Unit is being recognised nationally and internationally for its high quality of work and is constantly approached for their involvement in new studies.  

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