Blockbuster small molecule drugs officially announced the new crown treatment potential from 1 to 2 to take the new blue ocean

In this race against the new crown, another innovative pharmaceutical company, Ascentage Pharma (685HK), came to an end, bringing fresh blood and a turning point to this protracted batt.

01From 1 to 2: Listed drugs bring new opportunities for treatment

On May 18, Ascentage Pharma, which is deeply engaged in the development of new small molecule drug product pipelines and is at the forefront of the research and development of new drugs for apoptosis pathways, announced exciting news: the company's marketed product Orebatinib (Neric®) The latest preclinical study of ) found that this variety can effectively inhibit the production of cytokine storm in human peripheral blood mononuclear cells (PBMCs) induced by the new coronavirus variant strain Omicron (SARS-CoV-2-Omicron), and then It is suggested that orebatinib has the potential to treat novel coronavirus pneumonia (COVID-19), especially moderate to severe patien.

The research results have been published in the internationally renowned journal "The EMBO Journa.

In this race against the new crown, another powerful innovative pharmaceutical company came to an end, bringing fresh blood and turning points to this protracted batt.

Data show that although most COVID-19 patients have only mild to moderate symptoms, 15-20% of patients will still experience excessive inflammation caused by the production of a large number of cytokines, that is, "cytokine storm", and eventually lead to alveolar damage and alveolar dama.

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It is reported that orebatinib is an original class 1 new drug of Ascentage Pharma, which is used to treat any TKI-resistant chronic myeloid leukemia (CML) adults with chronic phase (CP) or accelerated phase (AP) with T315I mutation The patient is the first and only third-generation BCR-ABL tyrosine kinase inhibitor (TKI) approved in Chi.

To a certain extent, compared with the arduous and long process of developing new drugs from 0 to 1, the discovery of new crown treatment potential in marketed drugs represents a breakthrough and innovation from 1 to 2: its significance is not only to reduce research and development Time and clinical cost - more importantly, because orebatinib has shown excellent clinical efficacy and safety in the past few years; this time the great potential of this drug in the field of new crown treatment means that It will shorten the path to help patients survive and stay out of the intensive care unit, addressing a clinically urgent need for treatme.

02Join the lead: Competitive position takes the lead

Today, the frequency of epidemics has approached "influenza", but its lethality far exceeds that of influen.

Compared with macromolecular drugs and injectable preparations, small-molecule oral drugs are more convenient to administer and have better patient complian.

At the same time, the targets of small molecule drugs are relatively clear and highly conserved, because during the mutation process of the new coronavirus, the surface structural proteins are prone to change, while the intracellular process is not prone to mutation, so the small molecule drugs acting on the intracellular process are subject to mutation The strain has little impact and has the potential to be generally effecti.

Orebatinib, a small molecule protein tyrosine kinase inhibitor, is also an oral dr.

In this new crown drug test, for patients with mild to moderate symptoms of the new crown, 3 drugs have been approved overseas, and Paxlovid has been approved for marketing in Chi.

Compared with mild-to-moderate drugs, the competition pattern of small-molecule drugs for moderate-to-severe diseases is relatively modera.

Ascentage Pharma has been focusing on the research and development of small molecule drugs for many years, and has the sharpest sense of smell and the most cutting-edge strategy in the pharmaceutical industry: the company has established 8 new product pipelines of Class 1 small molecule drugs that have entered the clinical development stage, including inhibition of Bcl-2, IAP Or inhibitors of key proteins of apoptosis pathway such as MDM2-p53; a new generation of inhibitors for kinase mutants appearing in cancer treatment, e.

Ascentage Pharma already has innate technological advantages in the field of small molecule drugs, and has discovered the potential of its class of innovative drugs to treat severe patients with COVID-19, which means that the company has won the first right to run on the tra.

03 Take the lead in the layout: leading the progress means greater business value

Our battle against the new crown epidemic is not only a fight against the virus, but also a race against time; in this process, companies that really take the lead in layout and progress will gain more incremental and market opportuniti.

Remdesivir is the most obvious example: the Delta virus strain has led to a surge in the number of confirmed cas.

At the same time, with the spread of the new variant omicron, moderate and severe patients across the country and the world are once again showing signs of risi.

This has also directly led to an increase in the sales of remdesivir: sales of remdesivir will increase by 98% in 2021 to $56 billi.

Another well-known small molecule drug is the JAK inhibitor baricitinib, which was officially approved by the FDA in May this year for the treatment of severe COVID-19, and was previously granted emergency use in the field of COVID-1 In addition, baricitinib has also been recommended by the WHO guidelines for the treatment of new crow.

It is understood that Baricitinib has been in a good trend of step-by-step growth since its launch: it broke the 100 million (USD) mark in the second year, and its sales in 2021 will reach 1 billion USD, a year-on-year increase of 75
It is worth noting that since baricitinib was approved for sale in the Chinese market in 2019, it has become popular in 2021, and the sales in the hospital have exploded, exceeding 30 million; Global sales topped 4 billion (USD)… This shows the commercial potential behind the dr.

From the above research results, .

Gujral confirmed that SARS-CoV-2-Omicron variant NTD (Omicron-NTD) can also significantly stimulate PBMCs to release a variety of cytokines, including IL-1β, IL-6 and tumor necrosis factor (TNF) -α)e.

The study found: Orebatinib is a potent inhibitor of Omicron-NTD-mediated cytokine release from PBMCs, targeting the release of seven cytokines (GM-CSF, IL-1β, IL-10, IL-6, IL-
, CCL-2 and TNF-α) 50% inhibitory activity (EC50) between 7 and 56 nM, and the efficacy is better than baricitin.

This also shows the therapeutic potential of orebatinib to some exte.

At present, the epidemic situation is repeated, the spread of mutant strains has greatly increased, the prevention and control of the epidemic has become more difficult, and the clinical demand for more therapies and drugs has increas.

Oral drugs with convenient administration can complement the shortcomings of "prevention + treatment" and have greater commercial potential and clinical val.

However, even with the surge of moderate and severe patients, the approved drugs are extremely ra.

Targeted new drugs are urgently needed in clinical practice, and the companies that take the lead will quickly seize the mark.

This time Orebatinib has proved the potential of new crown treatme.

In the future, it may be able to seize the market gap, make up for the shortcomings, and achieve greater market prospec.

Ascentage Pharma is already looking forward to launching relevant clinical studies as soon as possible, striving to bring safer and more effective innovative treatments to COVID-19 patients around the wor.