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A chemical compound that has strong analgesic properties has been discovered at the University of Warsaw. If the next steps in clinical trials are successful, a drug that is 5000 times more effective than the strongest painkillers currently available will be released to the market.
In the photo: a team of scientists from the University of Warsaw – Beata Wileńska, Rafał Wieczorek, Bartłomiej Fedorczyk
This agent could be used in the relief of neuropathic pain, in acute traumatic conditions or in palliative treatment, i.e. in situations where the strongest drugs from the opioid family have already failed.
A new substance from the peptidomimetic family with strong analgesic properties was developed by a team led by Prof. Aleksandra Misicka-Kęsik at the Faculty of Chemistry, University of Warsaw, in cooperation with prof. Barbara Przewłocka from the Institute of Pharmacology of the Polish Academy of Sciences. A potential drug is the subject of an application for patent protection in Poland and in selected countries of the world. In parallel, after very promising animal tests, advanced work is underway to start the first phase of clinical trials.
Clinical trials and further research will begin
The project has just received significant funding from the Intelligent Development Operational Program Measure 1.1 (from the National Center for Research and Development, under the so-called fast track) in the amount of PLN 12,6 million. It is one of the highest-funded scientific and implementation projects submitted to this program, which also shows the promising nature and significant potential for discovery. The funds obtained will allow for the launch of the first phase of clinical trials and for further research on the new drug. – Our plan is to investigate how quickly the drug is distributed in the human body, what will be the optimal methods of its administration, what side effects it may have and, of course, whether it shows any toxicity – explains Dr. Rafał Wieczorek from the research group that developed the compound at the Faculty of Chemistry, University of Warsaw.
The nature of the drug – where does its effectiveness come from?
The discovered molecule belongs to the family of peptidomimetics, i.e. chemical compounds that imitate peptides present in living cells, e.g. hormones. There are a lot of peptides in the human body, and their low concentrations are constantly regulated by natural means. While working on new peptidomimetics, chemists try to create molecules that imitate hormones, which will be degraded more slowly by cellular enzymes, thanks to which it is possible to implement various types of treatments such as regulating the hormonal balance.
The compound discovered by a team of scientists has two functions. – We were very lucky because we created a bifunctional relationship. One part of our molecule acts on opioid receptors, which means extinguishing pain reactions, while the other part acts on the fourth melanocortic receptor, which is responsible for sending the signal that initiates pain. In other words, the administration of one compound causes the body to simultaneously send a signal that inhibits and relieves the already existing pain, and the second signal quenches the source of its induction. This is a huge advantage over the previously known painkillers, because they all work in one or the other way, but neither of them uses both at the same time – adds Rafał Wieczorek.
Animal studies have shown that the discovered compound shows about 5000 times greater analgesic effect than opioids available on the market. Such a big difference is probably due to the synergy of two methods of action of the discovered compound.
– The discovery has enormous potential for commercialization. Successful completion of subsequent phases of clinical trials would allow for the production of a universal, extremely effective drug that has not been available on the market so far. In practice, it would be a rescue for many people struggling with chronic pain, for which there is currently no effective rescue. A very good prognosis is that scientists will obtain significant funding for further research, which will allow them to enter the key phases of clinical trials. According to the calculations, apart from the funding from the National Center for Research and Development, about PLN 5 million is still needed to close the budget for the first stage of advanced tests. For this purpose, we are already conducting parallel talks with several interested companies. I trust that such an investor will be found very soon – said Dr. Robert Dwiliński, Director of the University Center for Technology Transfer at the University of Warsaw.
A new spin-off from the University of Warsaw
A few months ago, Dr. Rafał Wieczorek together with his colleagues founded a university spin-off company – Matariki Bioscience. One of its goals is to bring a revolutionary painkiller to the market. In addition, Matariki’s team has discovered compounds in its portfolio that can potentially be used in the design of various drugs used in cancer therapies. At the same time, as emphasized by Dr. Wieczorek, the team is ready to provide services to the order of individual investors interested in searching for molecules with specific chemical or biophysical properties.
Instead of morphine
Currently, drugs from the opioid family, such as, for example, morphine, are used as relievers of neuropathic pain. The disadvantages of these drugs, however, are addictive properties and severe side effects. In addition, along with the systematic intake of opioids in patients, the so-called ceiling effect – pain relief requires the administration of an increasing dose of the drug, and from a certain point of increasing it, the drug ceases to be effective. The introduction of a new drug based on a peptidomimetic gives hope for complete and long-term pain relief, because compared to morphine, a concentration of the drug is required several thousand less to obtain the result, and moreover, animal tests have shown that a sufficiently high dose completely eliminates pain, even if it is derived from damaged or irritated nerves.