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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

Africa's Black Rhino conservation strategy must change

2017-07-10

The black rhino is on the brink of extinction. The study that was
published in the Nature Scientific Reports reveals that the
species has lost an astonishing 69% of its genetic variation.
Photo: iStock

The conservation strategy of the black rhino in Africa needs to change in order to protect the species from extinction, a group of international researchers has found. The study that was published in the Nature Scientific Reports reveals that the species has lost an astonishing 69% of its genetic variation.

South African researchers took part
The researchers, which included local researchers from the National Zoological Gardens of South Africa (NZG), have highlighted the fact that this means the black rhino is on the brink of extinction. "We have found that there is a decline in genetic diversity, with 44 of 64 genetic lineages no longer existing," said Prof Antoinette Kotze, the Manager of Research and Scientific Services at the Zoo in Pretoria. She is also affiliate Professor in the Department of Genetics at the University of the Free State and has been involved in rhino research in South Africa since the early 2000s.

DNA from museums and the wild
The study compared DNA from specimens in museums around the world, which originated in the different regions of Africa, to the DNA of live wild animals. The DNA was extracted from the skin of museum specimen and from tissue and faecal samples from animals in the wild. The research used the mitochondrial genome.

"The rhino poaching ‘pandemic’
needs to be defeated, because
it puts further strain on the genetic
diversity of the black rhino.”

Ability to adapt
Dr Desire Dalton, one of the collaborators in the paper and a senior researcher at the NZG, said the loss of genetic diversity may compromise the rhinos’ ability to adapt to climate change. The study further underlined that two distinct populations now exists on either side of the Zambezi River. Dr Dalton said these definite populations need to be managed separately in order to conserve their genetic diversity. The study found that although the data suggests that the future is bleak for the black rhinoceros, the researchers did identify populations of priority for conservation, which might offer a better chance of preventing the species from total extinction. However, it stressed that the rhino poaching ‘pandemic’ needs to be defeated, because it puts further strain on the genetic diversity of the black rhino.

Extinct in many African countries
The research report further said that black rhino had been hunted and poached to extinction in many parts of Africa, such as Nigeria, Chad, Cameroon, Sudan, and Ethiopia. These rhino are now only found in five African countries. They are Tanzania, Zimbabwe, Kenya, Namibia, and South Africa, where the majority of the animals can be found.

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