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The world's first safe analgesic passed preclinical trials

Elena Fritz

The world's first analgesic with no side effects has successfully passed the preclinical trials. The innovative drug was created by a scientific group that included specialists from TSU, IPCET SB RAS, and the Research Institute of Pharmacology and Regenerative Medicine named after E.D. Goldberg. The basis for the analgesic, which has no analogs, was the modified molecule of the powerful explosive CL-20.

- CL-20 or hexanitrohexaazaisowurtzitane (HNIW) is well known as the strongest high-energy substance, and in 2003 they began to try to use it for medical purposes, - says Alexander Vorozhtsov, TSU Vice-Rector for Research and Innovation Activities, Chief Researcher, IPCET SB RAS. - Using a computer simulation, a new molecule with the proposed activity of the analgesic was created. Using directed synthesis, we obtained a first-in-class substance. Preclinical studies have confirmed its unique medicinal properties.

Three-year studies of the properties of the new drug, called thiowurcin, were carried out by specialists of the Goldberg Research Institute on mice, rats, rabbits, guinea pigs, and Drosophila. The strength and duration of exposure to thiowurcin were superior to many known analgesics and could effectively relieve pain of any etiology. Along with the effectiveness, the pharmacologists studied the degree of toxic effects in animals to predict side effects in humans.

- According to the results of preclinical studies, properties that could interfere with the further study of this analgesic in clinical trials have not been identified, - says Professor Svetlana Krylova, a leading researcher at the Goldberg Research Institute. - The data obtained indicate that thiowurcin does not cause effects characteristic of opioid analgesics—there is no negative effect on the gastrointestinal tract, central nervous system (does not cause the development of euphoria and sedative effect), and does not inhibit the respiratory center and hematopoietic system. The most important thing is that even after a long administration of an analgesic in the experiment, the development of drug dependence and withdrawal does not occur.

Along with this, the effect of thiowurcin on the immune system and reproductive function of animals after administration, which lasted from two weeks to three months, was studied. No genotoxic and mutagenic effects leading to DNA damage were detected. The data obtained indicate the safety of its use by men and women planning childbearing.

Now developers have to go through the last and most expensive stage—clinical trials of the drug. The cost of research, giving an objective picture, starts from half a billion rubles. That is why a considerable part of the new pharmacological developments simply does not reach the pharmacy. Currently, research organizations—the creators of thiowurcin—are negotiating with several pharmaceutical companies, including abroad, and are looking for an investor who will be ready to finance clinical trials.

According to the developers, an innovative drug may help solve the global problem facing the whole world, especially the United States—this is an opioid crisis caused by the intake of synthesized analgesics. Their consumers are primarily people with chronic pain who are forced to take powerful painkillers for several months or even constantly, which are highly addictive and can lead to death if overdosed.

- The US authorities are allocating a billion dollars to create an analgesic that will be very effective, but safe for people, in Russia this substance has already been synthesized by us. Moreover, we created the finished dosage form—capsules. Several patents have been received for development, - notes Alexander Vorozhtsov. - I am sure that in the foreseeable future we will be able to find a serious investor to support clinical trials and registration of an analgesic, and then Russia, firstly, will be able to more effectively solve the problems of patients who suffer from chronic pain, and secondly, with the help of thiowurcin it will provide itself an advantage in the global pharmaceutical market.


Provided by Tomsk State University