The secret of prostaglandins: how Gurus BioPharm uses biotechnology to treat asthma and limb ischemia

When it all began: from consulting to medicine

The history of Gurus began in 2005, when Igor Teterin,

at that time the director of marketing at the companyon freezing products, founded the consulting company Gurus Capital, which subsequently sharply changed its direction towards financing startups in the pharmaceutical field - the most interesting and promising area, according to the founder of the company. Teterin explains the decision to change course solely by personal interests.

"The two fastest growing and profitableThe industry now is IT and biotech. IT simply did not interest me, but medicine attracted by its social significance, Igor Teterin recalls. - Each discovery in this area is either someone’s life saved or a significant contribution to people's health. I wanted not only to earn money, but also to leave something really great behind me, to contribute to the development of national science. It is no secret that many talented scientists are leaving, but I would like the works of Russian scientists not to remain in the table, as is usually the case, but would be of practical use. All these motives attracted me to the medical field. ”

Igor Teterin. Photo: Vlad Shatilo / Hi-Tech

The pharmaceutical industry in Russia, which isOne of the most important elements of the healthcare system is on the verge of fundamental changes. To the greatest extent, these changes are associated with the formation of the innovation component, the development of import substitution and the growth of labor productivity. The domestic medical market is beginning to actively absorb innovative solutions and adapt to human needs. Biotech investors have higher returns than venture capital funds in other industries: 26.8% versus 21.8%. In 2017, investment in European biotechnology companies grew by 29%. All this draws close attention of potential investors to biomedicine. But there are also huge disadvantages, namely the long-term nature of the investment, usually exceeding five years, and the high risk: 90.4% of all phase 1 clinical trials do not achieve successful registration and market entry.

Return on investment in innovation from variousspheres (IT, medicine, new materials, etc.) - 400% growth in seven years. It is second only to biomedical innovations in terms of profitability, but by a wide margin compared to all other indices. Source: Thomson Reuters Venture Capital Indices

Initially, the company was engaged in the evaluation of innovativemedical projects. And Teterin himself specialized in raising financing for the development of enterprises, conducting marketing research on the pharmaceutical market, evaluating investment targets.

"By 2008, I had accumulated a goodhands-on marketing experience. I wanted to use it in more important, developing industries, ”says Igor Teterin. - In my opinion, medicine and pharmaceuticals were exactly like that.

With the future co-founder, Igor Lyubimov, wemet in April 2011 by chance - on the plane, on the way to Tomsk to the conference “Medicine of the Future”. We sat in neighboring places, talking about the development of medicine in our country and the world. And quickly found a common language. Since I was acutely aware that I was missing a partner in medicine, I suggested that Igor work together - to lead research, development, and later all the medical activities of the company. ”

Igor Teterin— co-founder of Gurus BioPharm.He received an economic education, an MBA in marketing, and graduated from the University of California. In 1991 he received a mathematical education. Since 2011, he has been an expert on biomedical technologies at the Skolkovo Foundation, leading over 100 examinations. He has held management positions for more than 20 years.

Igor Lyubimov— CEO and co-founder of Gurus BioPharm.He graduated from medical school with a degree in immunology. He completed graduate school in biology and received a PhD in biological sciences. With his participation, more than 100 examinations were carried out to create innovative medicines. The businessman has experience in management and scientific activities in the field of applied pharmacology. For a long time he participated in the development of biomedical projects. Before joining Gurus BioPharm, Lyubimov was an employee of a research institute (STS PMB).

At the end of 2011 in the work of Gurus BioPharmthere was a medical focus associated with the pharmaceutical industry. The first project was the development of an innovative medicine for the treatment of asthma in 2015, investments in which amounted to 44 million rubles. The next major development, a medicine for the treatment of critical limb ischemia, required as much investment in 2016. Both drugs are not yet ready for sale, and clinical trials are ongoing.

Igor Lyubimov. Photo: Vlad Shatilo / "Hightech"

Innovative projects

The company is a resident of the IC “Skolkovo”, onthe basis of which conducts research. The laboratory of the company with high-precision equipment purchased at its own expense is located in Skolkovo. The company employs about 15 people. The main staff consists of scientists - chemists and biologists, employees of various research institutes, which Teterin and Lyubimov selected individually for their projects. Research activities are conducted in two directions: the development of innovative products for aesthetic medicine and the creation of innovative medicines.

The company develops new molecules, conductspreclinical and clinical trials, which include tests for safety and efficacy. Such work may take more than eight years and includes the following steps:

  • Intelligent design.The company's scientists study a certain class of substances (for example, prostaglandins) and put forward hypotheses about what the chemical structure of the molecule must be in order for it to have a given therapeutic activity (in particular, for the treatment of asthma). Creation of a library of compounds - according to the hypothesis, 10-20 compounds are made.
  • Preclinical studies.This includes studies in cellular and biological models. In studies using cell models (the substance is dropped onto the cells), toxicity is tested and the mechanism of action is explored. Further studies are carried out on biological models. The cost of preclinical studies is 30–45 million rubles, duration is two years.
  • Clinical studies consisting of three phases. Substance is tested on humans (volunteers). The first phase is testing on healthy volunteers in order to understand how the substance affects the body (disintegration time and route of withdrawal). The second phase is testing for patient volunteers to identify the optimal effective and safe dose. The third phase - assessment of the effectiveness of patients with volunteers. Patients in the second or third phase can be invited to participate in clinical trials only by the attending physician, they do not participate in the first phase.
  • Commercialization and market entry.

Prostaglandins- physiologically active substances related toto the lipid group. They are formed in the body by fermentation from arachidonic acid. Contain a carbon chain of 20 members. Known since 1935, when they were first isolated from seminal fluid by the Swedish physiologist Ulf von Euler. The name comes from the Latin word prostata - “prostate gland”.

The precursor of all prostaglandins arepolyunsaturated fatty acids, in particular, arachidonic acid, which, after release from phosphoglycerins (phospholipids) of the biomembrane, gives rise to prostaglandins and leukotrienes.

Prostaglandins have a variedphysiological activity, active in low concentrations. They are involved in maintaining the homeostasis of the body, acting on pain receptors, regulating the immune response, in labor, keep the thoracic duct open during pregnancy, cause contraction (prostaglandins F) or expansion (prostaglandins E) of the bronchi and trachea. In addition, prostaglandins cause an increase in body temperature, have a sedative and tranquilizing effect, stimulate the secretion of pancreatic enzymes, inhibit gastric secretion, can mediate and modulate the action of other biological stimuli, act as synergists or antagonists.

Due to its wide distribution intissues and high and versatile biological activity of prostaglandins (and prostanoids in general) are becoming more widely used in medical practice as drugs. These circumstances stimulate further research both in the search for new prostanoids and in the chemical synthesis of their modified analogues with protected functional groups that are more active and stable when introduced into the body.

Prostaglandins are used in obstetrics, gynecology, treatment of peptic ulcer, rheumatoid arthritis and diseases of the blood coagulation system.

"The development was done by talented chemists -partners of the company, who have dedicated their lives to working with this group of substances, specifically with natural bioregulators, - said Igor Teterin. - They know prostaglandins very well, they have done thousands of experiments. Therefore, they obtained a substance that showed a very high activity in the treatment of asthma and critical ischemia. In any case, smooth muscle relaxation occurs. In the first case, these are smooth muscles of the trachea, which allow breathing air in a state of asthmatic spasm with a wide chest. And in the case of critical limb ischemia, the smooth muscles of the arteries and arterioles expand. This allows the tissues to receive blood, the lack of which is a sign of ischemia. "

Igor Lyubimov. Photo: Vlad Shatilo / "Hightech"

“All our developments are connected with one groupmolecules derived from arachidonic acid - prostaglandins. They are synthesized from it, and it turns out a whole set of different substances. Seven or eight key molecules are formed from this set. We work with three, ”adds Igor Lyubimov.

The hard way

Study of any drugalways causes difficulties: it is necessary to decide on the components and create a suitable study design for a specific dosage form. Activities are regulated by higher authorities; in Russia the Ministry of Health is also involved in this. The patenting process contains many pitfalls.

“Either they will give you a positive decision or not,- admits Igor Teterin. — For example, we were denied a patent in China. In this country, it was considered that the previous patent, obtained by chemical scientists before they came to Gurus BioPharm, duplicated an innovative medicine for asthma. Innovation was recognized all over the world, but not in China.”

China has its own patent policy. The Russian company sells its product in China, makes a profit, and taxes go to Russia. Oh wow! Any country does not want this. Any country resists granting patents to non-residents of their country. Simply, China is doing it especially aggressively.

Even payment of patent fees by many countries.rejected. Because sanctions. For example, we pay a fee in Brazil, but the money that is sent to a Brazilian bank is returned. They are not accepted by the bank. And it is clear that the internal financial policy is that they support sanctions against Russia. Do not even accept payments from here. Because they come from the side of our bank VTB. And we also came across this in Australia. ”

Igor Teterin. Photo: Vlad Shatilo / "Hightech"

Today, Gurus BioPharm already has tenpatents worldwide: in Russia, USA, Japan, Australia and European countries. The company has twice become a participant and winner of competitions from the Ministry of Education and Science - in 2016–2018 and in 2015–2017. These were programs of preclinical studies of drugs for the treatment of asthma and ischemia of the extremities. Thanks to the victory in the competition, the company received 33 million rubles for preclinical studies. This amount covered 75% of all costs. Another 11 million rubles were invested in preclinical studies from the company's own funds.

Ability to breathe

For people suffering from asthma, Gurus BioPharmis developing the drug GUR-501, the mechanism of action of which differs from the usual principle of operation of aerosols that relieve asthmatic symptoms. At the moment, GUR-501 is ready for clinical trials.

Old asthma drugs have a number of side effects.effects, as well as many of them are addictive. Currently, drugs for only two types of receptors involved in the regulation of bronchial tone have been developed to relieve acute attacks of bronchial asthma. These are β-adrenomimetics (alupent, ventolin, salbutamol, berotok and others), relaxing bronchi, and M-anticholinergic blockers (atropine and its analogs), blocking spasm. However, the use of β-adrenomimetics is often accompanied by serious side effects - severe tachycardia, headache, dizziness, muscle tremors, pulmonary edema, and others. And with prolonged use or overdose, loss of receptor sensitivity develops. This situation is deadly for the patient. M-holinoblokatory cause multiple side effects and do not apply independently, often with β-adrenomimetikami.

"There is a third, not used until nowtime type of receptors for regulating bronchial tone. This is the prostanoid receptor EP4 (for prostaglandin E2), which we develop and use to create drugs,” says Igor Lyubimov. — The relaxing effect of prostaglandin E2 on the smooth muscles of the bronchi is as strong as that of β-adrenergic agonists, but at the same time there are significantly fewer side effects, since it is a natural bioregulator of the body.

Use of natural prostaglandin E2(contained in the body of people and animals - "High-tech") for the relief of bronchospasm is impossible because of the strong cough it causes. This restriction is overcome in our proposed hybrid preparation containing only natural components: prostaglandin E2, glycerin and associated nitric oxide, which, when released, significantly enhances the bronchorelaxant effect. In the new structure, it was possible not only to eliminate the effect on cough receptors, but also to increase its activity by 20 times compared with natural prostaglandin. This led to a significant reduction in therapeutic dose and additional safety for patients: the impossibility of overdose and the absence of serious side effects.

Photo: Vlad Shatilo / "Hightech"

Significant expansion of the scopeThe proposed drug is possible with its complex use with β-adrenomimetics and inhalation glucocorticosteroids used in the clinic. Such complex drugs will be especially in demand for relief of severe attacks of asthma. The proposed drug may be the only effective means for patients with a long history of asthma, who have developed an addiction to existing bronchodilators. "

Ability to walk

Another drug, GUR-201, was created totreatment of critical limb ischemia. With currently existing methods of treating this disease, the number of patients undergoing leg amputation is 25%. The emergence of a new drug based on prostaglandins will help to avoid heavy surgery. This drug has also been preclinically tested and is ready for clinical studies.

Prostaglandin molecule, on the basis of whichA molecule was made for critical limb ischemia, it acts on vascular smooth muscle to improve blood supply. It happens that blood vessels suffer, namely smooth muscles and connective tissues. They begin to collapse, narrow, small vessels begin to suffer greatly, capillaries even more severely. And a condition such as hypoxia of peripheral tissues arises. To prevent necrotic phenomena from occurring, a substance is injected into people. It dilates capillaries and blood vessels, restores tissue nutrition. And a person’s leg or arm is actually saved. The Gurus BioPharm molecule is different in that it includes two components. The first acts as a foreign molecule, the second compensates for the function of damaged blood vessels.

“Our drug allows us to compensate for the functionendothelium, which can be completely destroyed in such pathologies,” notes Igor Lyubimov. “The difference between our substance is that it can act at more severe stages, when the vascular endothelium is already severely damaged. Old drugs are effective only in the early stages, when the functionality of the endothelium is still preserved.”

Hair Growth Serum

Another area that Gurus BioPharm is actively involved in is the development and production of products for aesthetic medicine.

“In the field of aesthetic medicine, we provide a full cycle: from the creation of a substance to mass production, market launch and sales,” says Igor Teterin.

Regeus serums that stimulate hair growth,eyelashes and eyebrows are finished products. Despite the fact that the idea of ​​such a serum came to the partners of the company in 1995, research continues to this day. The formula improves, interactions with other preparations are investigated. An innovative tool solves a difficult problem from the field of aesthetic medicine: hair loss, rare and weak eyelashes and eyebrows. Regeus is already available for purchase, and its cost is comparable with similar products in the industry.

Innovative moleculesnitrolipins- the active ingredient of Regeus serums. Nitrolipins are natural substances derived from arachidonic acid. Nitrolipins contain two components:

  • Prostaglandins. Prostaglandins E1, E2 and F2-alpha are contained in the human body and regulate many biological processes, including the activity of the hair follicle and its blood supply.
  • NO donors. NO is a small regulatory molecule found in the human body. Promotes vascular relaxation and better absorption of oxygen by tissue cells, which is necessary for hair growth.

Due to the unique chemical structure, nitrolipins penetrate deep into the dermis up to the level of the location of the vessels and hair follicles and act on them.

Nitrolipin E1 improves rheological propertiesblood in the growth papilla of the follicle by reducing platelet aggregation. Thus, nitrolipin E1 not only restores the narrowed diameter of the “pipeline system” of arterioles - capillaries to normal, but also cleans it from microthrombi. The restoration of the patency of the arteriole capillaries brings the blood supply to the hair follicles closer to the state of the blood supply to the young skin.

Nitrolipin E2 stimulates the division anddifferentiation of hair follicle stem cells, activates vascular endothelial growth factors (which leads to the formation of new microvessels), reduces the local activity of pro-inflammatory cytokines, prevents the transition of hair follicles to telogen (resting) phases.

Nitrolipin F activates a group of specialhair bulb receptors that promote the regeneration of hair follicle cells and their transition from the telogen phase (dormancy) to the anagen phase (active hair growth).

Normally, these molecules are produced in the bodyon their own. They act only locally - in the lower layers of the skin, where the hair bulbs are located, and do not penetrate deeper, because they are neutralized by special enzymes. Serum Regeus also functions in the same way: the active substances reach the follicles, physiologically and carefully affect them, then are removed from the body without causing adverse reactions. The serum contains no hormones. But tests have shown that serum prevents intense hair loss, activates the growth of hair, eyelashes, eyebrows and thickens hair, making it stronger and darker by several tones.

"Means for growth of hair, eyebrows, eyelashesdeveloped on the basis of prostaglandin derivatives. Active substances help solve the problem of baldness in men and women, - said Igor Teterin. “Serum is bought by women who have lost hair, and men who do not want to lose their hair with age.”

Photo: Vlad Shatilo / "Hightech"

The main channel to attract customers -Internet advertising and social networks. The serum based on nitrolipins was released in 2018, investment in products amounted to about 6 million rubles, but has not yet paid off. Sales of funds began six months ago.

Biomedical technology - new, but fasta growing industry that allows you to help a large number of people. The company's plans include preclinical studies on glaucoma and clinical studies on asthma and critical limb ischemia.

"We will continue to study serum forhair growth. Perhaps we will create new products in this area. For example, serum for beard growth, - adds Igor Lyubimov. - We are also working on bringing our products to new, foreign markets. Our principles are based on the use of mechanisms created by nature itself and already existing in our body. This is the most ideal thing we can have. We help the body to restore its own functions and thus get rid of pathologies. ”