A Nearly 20‐Year Journey to Success of Azvudine for Antiviral Therapy

Comprehensive Summary

Modified nucleosides, particularly those with 4'‐modifications, are significant nucleosides used in antiviral treatments. The drug discovery campaign of Azvudine starts from 2′‐deoxynucleoside, followed by extensive modifications, such as introducing the 4’‐position substitutions, a 2’‐β‐fluoro atom, and changing the nucleobases. Azvudine acts potently toward various HIV‐1 strains by inhibiting HIV‐1 reverse transcription and preventing Vif‐induced A3G degradation, representing the first‐in‐class dual‐acting antiviral agent. In July 2021, NMPA conditionally approved Azvudine as an adjunct therapy for adult patients with high levels of HIV‐1 virus load when combined with NRTIs or NNRTIs. Azvudine is capable of inhibiting SARS‐CoV‐2, as well as its variants, including Alpha, Beta, Delta, and Omicron. Clinical trials reveal its real‐world effectiveness among hospitalized severely or critically ill COVID‐19 patients or those with pre‐existing conditions. On July 25th, 2022, the NMPA granted conditional authorization approving Azvudine as China's first domestic oral anti‐COVID‐19 agent. Generally, Azvudine at therapeutic doses is safe and well‐tolerated in clinical settings. Azvudine got approval from the National Health Commission and National Administration of Traditional Chinese Medicine on August 9th to be used in the "Diagnosis and Treatment Program for Novel Coronavirus Pneumonia (Ninth Edition)" for treating common COVID‐19 adult patients. On August 12th, 2022, it was also approved by the National Healthcare Security Administration to be added to the list of medical reimbursements. Of note, the achievements related to Azvudine were indexed in the China Basic Research Development Report in Thirty‐Five of 2022. Azvudine was also approved on January 5^th, 2023, to be used in the "Diagnosis and Treatment Program for Novel Coronavirus Pneumonia (Tenth Edition)" for treating COVID‐19 patients. In February 2023, the Ministry of Health of the Russian Federation approved the usage of Azvudine among individuals infected with SARS‐CoV‐2.

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