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Since the relaxation of the control of the new crown epidemic, the number of positive infections in various places has increased exponentially, and many cities may reach the peak of infection in the near future, and as the number of people returning to their hometowns increases near the Spring Festival, each city will usher in the first wave of
new crown infections.
Today, although the annual north-south migration has not yet fully arrived, the new crown seems to have spread rapidly and will pose a serious threat
to the lives and health of vulnerable people with underlying diseases and severe disease risk factors.
A number of studies have shown that the decline in the fatality rate of the new crown is not only because of the reduction in Omicron pathogenicity and viral load, but also because the new crown vaccination rate in China has increased
significantly.
The vaccine may not be effective in preventing infection, but real-world data shows that vaccination can largely prevent severe disease and death, so vaccination is necessary
.
However, if the virus escapes immunity, infection will still occur even if vaccinated, and in this case, how to deal with the threat of the new coronavirus to human health is a major
issue that major pharmaceutical companies should consider.
Prevention should be followed by a focus on new crown treatment, so the development of new crown treatment drugs should be a top priority
.
In the field of new crown treatment drugs, pharmaceutical companies continue to be active, and in the process of targeting new crown virus replication, 3CL is a necessary key protease, which blocks viral replication
by inhibiting viral protein cleavage.
Based on this, 3CL protease inhibitors or effective new crown virus treatment drugs, in recent days, many pharmaceutical companies have made new progress in developing new crown drug 3CL protease inhibitors
.
The world's first 3CL protease PROTAC was granted by the U.
S.
Patent Office
S.
Patent Office
On December 21, Panlong Pharmaceutical issued an announcement announcing that its "Coronavirus 3CL Protease Inhibitor Development" project with the team of Dr.
Liang Chengyuan of Shaanxi University of Science and Technology has granted two patents authorized by the United States Patent and Trademark Office
.
Liang Chengyuan's team at Shaanxi University of Science and Technology has been granted two patents authorized by the United States Patent and Trademark Office
Figure 1 Relevant announcement notice (Source: [1])
These two patents are based on the PROTACs designed and synthesized by Panlong Pharmaceutical's novel coronavirus 3CL protease inhibitor candidate PLC-01, and cell and animal experiments have shown that they have excellent 3CL protease degradation ability, and are the first batch of authorized anti-coronavirus PROTACs patents in the world
.
Figure 2 Basic situation of patent authorization (Source: [1])
The above-mentioned US patent authorization is the result of the research stage progress of the cooperation project between Panlong Pharmaceutical and Shaanxi University of Science and Technology "Development of Coronavirus 3CL Protease Inhibitor", which is conducive to enhancing the company's comprehensive strength in innovation and R&D, thereby enhancing the company's core competitiveness
.
At present, many pharmaceutical companies around the world have deployed 3CL protease inhibitors, and as far as the domestic track is concerned, 4 drugs are at the forefront of progress, including RAY1216 of Zhongsheng Pharmaceutical, GST-HG171 of Guangshengtang, Forbutevir of Frontier Pharmaceutical, and Xiannoxin
of Simcere Pharmaceutical.
In addition to the 3CL protease inhibitor project, Panlong Pharmaceutical is also actively promoting the progress of the Qingwen lung protection particle project, hoping that these two projects can contribute to the treatment of the new coronavirus in the future
.
The clinical trial application of Salubris new crown drug 3CL protease inhibitor was accepted
The clinical trial application of Salubris new crown drug 3CL protease inhibitor was acceptedOn December 20, Salubris announced that its clinical trial application for the new crown treatment 3CL protease inhibitor SAL0133 was accepted
.
SAL0133 is a powerful, broad-spectrum anti-novel coronavirus 3CL protease inhibitor independently innovated and developed by Salubris with independent intellectual property rights, and currently intends to develop clinical indications for the treatment of mild/common novel coronavirus pneumonia
in adults.
in adults.
3CL protease plays an important role in the RNA replication of the new coronavirus, mainly acting on the initial replication stage after the virus enters the host cell, so as to inhibit the activity of 3CL protease, thereby effectively blocking the virus replication and achieving the effect
of anti-new coronavirus.
In addition, 3CL protease is highly conservative in beta-coronavirus, SARS-CoV-2 and SARS-CoV 3CL protease homology is greater than 96%, the structure of the two is basically the same, many 3CL protease inhibitors have been reported to have broad-spectrum anti-coronavirus ability [2].
Since there are no proteases in humans that are similar to the cleavage site of 3CL protease, highly specific inhibitors can be screened and have a good
safety profile.
Preclinical studies have shown that SAL0133 shows strong inhibitory activity against 3CL protease at the enzyme level, and has strong antiviral activity against wild-type new coronavirus and five new crown variants Alpha (B.
1), Beta, Delta, Omicron (BA.
2, BA.
5), and the current circulating strain Omicron
The antiviral activity EC90 value of BA.
5 strain is 10 times that of nematevir[2].
1), Beta, Delta, Omicron (BA.
2, BA.
5), and the current epidemic strain Omicron The antiviral activity EC90 value of BA.
5 strain is 10 times that of nematevir
In animal models infected with the new coronavirus, SAL0133 can significantly reduce the viral load of lung tissue and significantly improve lung inflammation, and its significantly lower viral load dose is lower than that of nematevir
.
In addition, SAL0133 has been shown to exhibit good oral absorption characteristics, good permeability, high oral bioavailability, long half-life, good metabolic stability, and high
oral exposure.
Overall, SAL0133 has a clear mechanism of action, has a potent, broad-spectrum anti-novel coronavirus effect, and is not expected to require the combination of CYP3A4 inhibitor ritonavir, and the potential risk of drug interactions is low
.
It is expected that Salubris can successfully develop SAL0133 and be approved for marketing to be used in the treatment of new crown infected patients in a timely manner to meet the clinical needs
that have not yet been met.
Simcere Pharmaceutical's 3CL protease inhibitor completed the enrollment of all patients in the registration phase II.
/III.
clinical trial
/III.
clinical trial
On December 18, Simcere Pharmaceutical announced that its anti-new coronavirus drug Xiannuoxin ™ co-developed with the Shanghai Institute of Materia Medica, Chinese Academy of Sciences and Wuhan Institute of Virology has completed the enrollment of all 1208 patients in a randomized, double-blind, placebo-controlled phase II.
/III.
clinical study of adult patients with mild and moderate disease, becoming the first domestic 3CL-targeted oral small molecule drug Phase II.
/III.
clinical study to be completed
.
/III.
clinical study of all 1208 patients in adult patients with mild and moderate new crown disease, becoming the first domestic 3CL target oral small molecule drug Phase II.
/III.
clinical study to complete the project
Synoxin ™ is a small molecule anti-new crown innovative drug candidate for 3CL protease and ritonavir combination packaged drug
.
In preclinical trials, Synoxin ™ showed highly potent, broad-spectrum anti-coronavirus activity
.
This study is the first clinical study
in China to enter the registration phase III trial for Chinese patients infected with the new crown Omicron strain and complete the total number of planned cases.
The clinical dosing regimen was Xenoxin ™ versus placebo for 5 consecutive days, and the study endpoints included the time required until the recovery of new crown symptoms, and the decrease in viral load
.
.
In preclinical trials, Synoxin ™ showed highly potent, broad-spectrum anti-coronavirus activity
.
On November 17, 2021, Simcere Pharmaceutical entered into technology transfer contracts with Shanghai Institute of Materia Medica, Chinese Academy of Sciences and Wuhan Institute of Virology, and obtained exclusive rights
for the global development, production and commercialization of Sinoxin.
On March 28, 2022 and May 13, 2022, Synoxin ™ received two drug clinical trial approval notices issued by the National Medical Products Administration, respectively, for the treatment of mild to moderate new crown infection and the exposure to preventive treatment
of close contacts of people who have been exposed to new crown positive infection.
Although many domestic pharmaceutical companies have deployed 3CL target anti-new coronavirus drugs, no products have been launched so far, and so far only one drug developed by Pfizer has been approved for marketing, and there are no other products
.
It is expected that domestic pharmaceutical companies will accelerate the progress of R&D and trials, so that these new coronavirus treatment drugs can be used for the treatment of new crown infection as soon as possible, benefiting the majority of infected people
.
Resources:
Resources:
[1]http://notice.
10jqka.
com.
cn/api/pdf/e240552f0feef4a7.
pdf
10jqka.
com.
cn/api/pdf/e240552f0feef4a7.
[2]https://finance.
sina.
com.
cn/roll/2022-12-21/doc-imxxkrak0735717.
shtml
sina.
com.
cn/roll/2022-12-21/doc-imxxkrak0735717.
shtml
[3]
[3]
