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

作　　者：Bin Yu Junbiao Chang 

机构地区：[1]College of Chemistry & School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou,Henan,450001 China [2]Pingyuan Laboratory,State Key Laboratory of Antiviral Drugs,Henan Normal University,Xinxiang,Henan,453007 China

出　　处：《Chinese Journal of Chemistry》2023年第23期3349-3357,共9页中国化学（英文版）

基　　金：supported by the National Natural Science Foundation of China(Nos.82130103 and U1804283);the National Key R&D Program of China(Nos.2021YFC0864700 and 2022YFE0202700).

摘　　要：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,the 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 have revealed 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 5th,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.What is

关 键 词：NUCLEOSIDES Azvudine HIV COVID-19 Antiviral agents Infectious diseases Drug discovery 

分 类 号：R96[医药卫生—药理学]