Get to Know Azvudine, the New Oral Antiviral COVID-19 Treatment Developed in China

Get to Know Azvudine, the New Oral Antiviral COVID-19 Treatment Developed in China

Q1: What is Azvudine?

Azvudine tablets is the first oral small-molecule antiviral drug for the treatment of COVID-19 developed in China with fully independent intellectual property. On Jul. 25, 2022, it was approved by NMPA for the treatment of common COVID-19 in adults. On Aug. 9, 2022, the General Office of the National Health Commission and the Office of the National Administration of Traditional Chinese Medicine included Azvudine tablets in the Diagnosis and Treatment Guideline for COVID-19 (9th Edition). On Dec. 7, 2022, Azvudine was included in the latest version of Clinical Pharmacy Guideline for Antiviral Treatment of COVID-19 published by Guangdong Pharmaceutical Association.

Q2: What is the mechanism of action of Azvudine in the treatment of SARS-CoV-2 infection?

Azvudine is a broad-spectrum RNA virus inhibitor. As a synthetic nucleoside analogue of the viral RNA-dependent RNA polymerase (RdRp), it is metabolized intracellularly into an active antiviral metabolite 5'-triphosphate (Azvudine triphosphate) that specifically targets the SARS-CoV-2 RdRp. It is incorporated into the viral RNA chain during SARS-CoV-2 virus RNA synthesis, thereby terminating the replication of SARS-CoV-2 virus and exerting therapeutic effects against SARS-CoV-2 infection.

To be brief, if we liken SARS-CoV-2 virus to a small house that is built with rebars and cements, then Azvudine would be the raw material connecting rebars to cements. To build a house, connection of rebars and cements is needed. However, Azvudine, playing the role of the raw material, interrupts the connection and prevents the house construction to be completed. That's how the virus dies due to replication failure.

Q3: What about the clinical effect of Azvudine tablets?

The results of international multicenter phase III clinical study of Azvudine tablets demonstrate its anti-SARS-CoV-2 efficacy and safety. The clinical trial results show that, Azvudine has significant efficacy of inhibiting the replication of SARS-CoV-2 virus, accelerating clearance of SARS-CoV-2 virus, alleviating symptoms, and shortening disease course, at a low dosage level that makes it safer. Furthermore, as the target SARS-CoV-2 RdRp is relatively conservative with a low mutation rate, Azvudine has the potential of fighting multiple variants efficiently.

Q4: What is the price of Azvudine tablets?

Azvudine tablets have been covered by the basic medical insurance and included in the basic medical insurance networks of 31 provinces, municipalities, and autonomous regions in China. The price is RMB 270 per bottle.

Q5: What are the dosage and administration of Azvudine tablets?

1 mg of Azvudine tablet is indicated for the treatment of common COVID-19 in adults. 5mg of Azvudine should be administered once a day. Azvudine should be administered on an empty stomach, and the tablets should be swallowed whole and not crushed.

Q6: What are the experts' opinions on Azvudine?

Jiang Jiandong, an academician of Chinese Academy of Engineering and the president of the Institute of Materia Medica of Chinese Academy of Medical Sciences, said, "An important therapeutic principle observed by China's medical community is to address both symptoms and root causes, namely the treatment of both symptoms and causes of any disease is emphasized. The antiviral drug Azvudine is characterized by the treatment of symptoms and the elimination of disease causes: antiviral effect is the treatment of symptoms while thymus protection is the elimination of the causes. “"Treating SARS-CoV-2 with Azvudine follows two pharmacology modes: one is antiviral effect to inhibit the function of SARS-CoV-2 RdRp, mainly focusing on the thymus that is actually an amplifier. As long as T-cells work efficiently, the treatment will go to the second mode, i.e., killing the viruses throughout the body via immune system."

Zhang Fujie, the Director of Clinical Research Center for Infectious Diseases, Beijing Ditan Hospital Capital Medical University, said, "Azvudine is a nucleoside analogue acting specifically on RdRp capable of blocking precisely the replication of SARS-CoV-2 RNA. Nonclinical studies show that, Azvudine efficiently inhibits SARS-CoV-2 virus strains, improves lung injury, boosts immunity, and significantly shortens the time to RNA clearance. Phase III clinical studies carried out in China and Russia also demonstrated the efficacy and safety of Azvudine in patients with mild and moderate COVID-19."

Professor Chang Junbiao, the inventor of Avudine and vice president of Zhengzhou University, said, "As a nucleoside analogue that inhibits viral RNA-dependent RNA polymerase (RdRp), Azvudine specifically acts on the RdRp of SARS-CoV-2 virus, thereby inhibiting the viral replication with strong long-acting drug targeting. Related trials show that, Azvudine has a broad-spectrum effect of inhibiting viral RNA replication. SARS-CoV-2 is also a virus with RNA as genetic material. As confirmed by clinical trials, this drug has good inhibitory effect on SARS-CoV-2 virus. Also, it is efficacious to virus variants likewise."

Q7: How should high-risk patients be treated immediately after being infected?

For seniors or special populations with underlying diseases and a weakened immune system, infection often leads to a risk of critical illness or even death due to insufficient autoimmune protection. For such patients, experts advise that, immediately after being infected, they should seek medical attention in time for medication in a scientific, safe, and reasonable manner, so as to reduce the risk of causing critical illness. Antiviral treatment is preferably started in the early phase of virus infection. The earlier the treatment starts, the more significant the effect will be. Early virus clearance minimizes virus infection-induced organ injuries and prevents complications from occurring, so as to enable rehabilitation as soon as possible.

Q8: What are the precautions for administration of Azvudine tablets?

Azvudine tablets should be administered in strict accordance with instructions for use under the guidance of a physician, and the contraindications and special notes for special populations are subject to the instructions for use.