Ensternivir has good efficacy, few side effects, and is widely applicable to people, or become the main force in the fight against the new crown
After the peak period of infection, the clinical demand for small molecule anti-new coronavirus drugs is becoming increasingly urgent, how to use such drugs reasonably and standardized? Today, Sun Yaoshi inventoried and sorted out such drugs from the aspects of drug action mechanism, adaptation to the population and medication precautions, hoping to benefit everyone.
At present, the small molecule anti-new coronavirus drugs approved for marketing mainly include nematevir/ritonavir, azvudine and monogravir, briefly introduce the mechanism of action of these three drugs:
Nematevir/ritonavir: The target is the 3CL protease of the virus, which is only present in the new coronavirus and not in the human body, which is a key substance in the replication process of the new coronavirus. Nirmatevir can inhibit 3CL protease, prevent it from working, and block viral replication. Ritonavir itself has no anti-coronavirus effect, but it can inhibit the metabolism of nematevir by liver enzymes, thereby increasing the blood concentration of nirmatevir and enhancing its antiviral effect.
Azvudine: The target is viral RNA-dependent RNA polymerase, which is metabolized into an active 5'-triphosphate metabolite (azvudine triphosphate) in cells after oral administration, which can specifically act on the new coronavirus RNA polymerase, embed viral RNA in the process of virus synthesis, inhibit viral replication, and kill viruses.
Monoravir: The target is also RNA-dependent RNA polymerase, that is, when the virus replicates almost ends and a new viral RNA is formed, the wrong component is added to make the virus die.
These 3 drugs are suitable for:
Nematevir/ritonavir: patients with mild to moderate COVID infection at high risk of severe disease.
Azvudine: medium-sized (common crown infection) new crown patients.
Monoravir: patients with mild to moderate COVID infection and at high risk of severe disease.
Precautions for taking these 3 medications:
nematevir/ritonavir:
1. There is liver and kidney toxicity, and patients with severe liver disease and kidney disease should not be used;
2. There are extensive drug-drug interactions, be sure to consult a doctor or pharmacist before taking the drug.
3. Animal experiments have shown that ritonavir has reproductive toxicity.
4. The safety and efficacy of this product in patients under 18 years of age have not been determined.
Azvudine:
1. Genotoxicity and reproductive toxicity.
2. It is not recommended to use during pregnancy and lactation, and patients with moderate and severe liver and kidney function impairment should be used with caution.
3. Pay attention to its liver toxicity and muscle toxicity. (The new version of the manual has not yet been revealed)
4. The risk of carcinogenicity needs to be evaluated by subsequent carcinogenicity test.
5. Elderly and children lack clear efficacy and safety research data, should be used with caution.
Monoravir:
1. There is a theoretical risk of mutagenicity.
2. There is genotoxicity, embryo-fetal toxicity, non-clinical trials show reproductive toxicity, there may be hypersensitivity reactions, and bone and cartilage growth may be affected.
3. Treatment is not recommended for pregnant women.
4. Women of childbearing potential take effective contraception during treatment and within 4 days after taking the last dose.
5. There is bone and cartilage toxicity, not recommended for children.
Ensternivir from Shionogi Corporation in Japan has 3 major advantages over the above 3 drugs:
1. Applicable to a wider range of people: nematevir/ritonavir and monoravir are for mild and moderate adult patients with the risk of severe disease, azvudine is for ordinary adult patients, and enstevir is for all new crown mild and moderate patients over 12 years old, the elderly and children can take it, there are no strict restrictions, and it has a wider audience, especially in the context of Omicron virus dominance, the proportion of mild and moderate patients accounts for the majority.
2. Better efficacy: Phase 2 and 3 clinical trials of entrevir have shown good efficacy, and it is the only oral anti-new coronavirus drug that shows both respiratory symptom improvement and antiviral effect, and has significantly improved the five typical symptoms of new coronavirus infection (nasal congestion/runny nose, sore throat, cough, fever and tiredness). Clinical data show that the viral load on the 4th day of treatment is reduced by 30 times, which can not only greatly shorten the time for patients to "turn negative", but also effectively reduce the infectivity of the virus.
3. Better safety: nematevir/ritonavir has a wide range of drug-drug interactions, azvudine and monogravir act on the RNA polymerase of the virus, and human cells themselves also have the process of synthesizing RNA, so these two drugs are considered to have potential harm to the human body, while entivir does not have the above risks and is safer.
In November 2022, Japan urgently approved the listing of Enstrevir. In view of the good effect of the drug in the treatment of the new crown, the governments of the United States and Japan each ordered 2 million copies of the drug from Shionogei. At present, data from Shionogi's official website shows that among the 4,000 patients in Japan who have taken the drug, the five major symptoms caused by the Omicron strain have obvious effects, and the safety has been confirmed again.
According to media reports, Shionogi new crown oral drug will not only be priced lower than Pfizer's Paxlovid in the United States, improve drug accessibility, but also willing to put the entire industrial chain in China, at present, Japan has set up a factory in China, and it is expected to be put into production as soon as mid-2023 to effectively ensure the supply of the huge Chinese market.
In view of the characteristics of China's large number of infected people, mainly patients with moderate and mild diseases, and limited affordability of drug prices, compared with the two new crown drugs that have been approved in China, entivir is not only guaranteed in efficacy and safety, but also more "close to the people" in price and more secure in supply.
In short, entrevir is currently the only oral drug with both symptom improvement and antiviral effects, more comprehensive and safe, more beneficial to "one old and one young", can be taken over 12 years old, elderly patients have good compliance, can quickly shorten the recovery time of cement nose, blade throat and other symptoms, the whole industry chain in China, to ensure stable supply. #How to choose new crown oral drugs# #Enstevir is more widely applicable# How to solve #新冠五大 "torture"# #Enstevir has small side effects# #老人小孩用药首选恩司特韦 #
