Translation. Region: Russian Federal

Source: Peter the Great St Petersburg Polytechnic University – Peter the Great St Petersburg Polytechnic University –

Polytechnic University scientists have developed a new chemical composition with increased anti-cancer activity and virtually zero toxicity.

Malignant neoplasms are one of the most serious problems of modern healthcare. Globally, about 20 million new cases of the disease are registered annually, and global mortality from cancer reaches 9-10 million people per year. In Russia, more than 640 thousand new cases of cancer are detected annually. At the same time, about 40% of patients seek medical help when the disease has already reached stage III-IV, which significantly reduces the effectiveness of treatment and worsens survival. The most common types are breast cancer, lung cancer and colorectal cancer.

High morbidity and a significant proportion of cases of late diagnosis require the introduction of new, effective and affordable methods of therapy, which scientists in all countries are working on. Over the past ten years, a breakthrough has been achieved in the treatment of malignant neoplasms after the approval of tyrosine kinase inhibitors and immune checkpoint inhibitors, which have significantly changed approaches to the treatment of patients with cancer tumors. Small-molecule inhibitors of poly(ADP-ribose) polymerase (PARP) are a promising group of new antitumor agents that can selectively inhibit the enzyme responsible for the restoration of genotoxic damage in cells, which ultimately leads to apoptosis and death of tumor cells.

In Russia, under the conditions of sanctions pressure and the rising cost of modern foreign medicines, the creation of domestic antitumor drugs with high efficiency and low toxicity is especially relevant. This is the task that a group of scientists from Peter the Great St. Petersburg Polytechnic University is solving. They have selected chemical substances and invented a method for obtaining a new compound that has not only high anticancer activity, but also low toxicity.

Standard tests using resazurin revealed that the obtained compound has more than 50 times the anti-cancer activity of its FDA-approved analogue. We determined the toxicity of the compound using the method of G. N. Pershin on mice. The results of the experiments showed that, according to the current classification, the compound belongs to class V of virtually non-toxic drugs. The obtained characteristics make it possible to use this compound to create new targeted drugs with low toxicity to healthy tissues, – said one of the authors of the invention, head of the Laboratory of Nano- and Microencapsulation of Biologically Active Substances of the Institute of Cardiovascular and Biological Problems of St. Petersburg Polytechnic University Alexander Timin.

The potential of the drug for further production of anti-cancer drugs is highly appreciated by specialists participating in testing the new compound, in accordance with the agreement concluded between the N. N. Petrov National Medical Research Center of Oncology of the Ministry of Health of Russia and SPbPU.

Currently, there are no registered inhibitors of domestic development in Russia. Therefore, it is especially important that the compound created by the scientists of the Polytechnic University of Petrovsky already demonstrates encouraging results at the early stages. This is an original molecule with characteristics comparable to foreign drugs. We continue research on biological models and are preparing for preclinical trials in accordance with international standards in order to provide patients with an effective and affordable antitumor agent in the future. Now we are waiting for the decision of the Ministry of Health on financing the project within the framework of the State assignment – the first stage of expert evaluation has already been successfully completed, – said Artem Poltoratsky, Head of the Department of Organization of Preclinical and Clinical Research, Leading Researcher and Oncologist at the N.N. Petrov National Medical Research Center of Oncology.

Conducting preclinical studies and, in general, bringing the drug to market will be significantly cheaper also because Polytechnic scientists use artificial intelligence technologies. They conduct retrosynthetic analysis of large data sets (Big Data), establishing the relationship between the structure and biological activity of the compounds being studied.

The neural network we trained generates potential structures with the required properties and predicts binding affinities with target molecules. The proposed approach allows us to calculate properties based on the structure, create training samples based on more than 40,000 molecules and predict the structures of leading compounds. These solutions and the developed neural network approach, which tracks the effect of molecules on the body, significantly reduce the time and material costs of preclinical studies, – said the leading researcher of the laboratory of nano- and microencapsulation of biologically active substances, one of the authors of the invention Sergey Shipilovskikh.

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