Li Jiayi, Zhu Bo, Lu Jian, Dong Zheyi, Li Ping, Li Wenge, Zheng Chunfu, Chang Junbiao, Shang Shunlai
Pingyuan Laboratory, Xinxiang, China.
Department of Nephrology, China-Japan Friendship Hospital, Beijing, China.
Front Pharmacol. 2025 Apr 25;16:1524072. doi: 10.3389/fphar.2025.1524072. eCollection 2025.
The global impact of COVID-19 has highlighted the urgent need for effective therapeutic interventions against SARS-CoV-2. Azvudine, a dual-target nucleoside drug initially developed for human immunodeficiency virus (HIV), has gained attention for its potential in treating COVID-19. On 25 July 2022, Azvudine received conditional approval from the National Medical Products Administration (NMPA) of China, making it the first oral SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor for COVID-19 treatment. This review explores the pharmacological activity, antiviral mechanisms, and clinical effectiveness of azvudine in the context of COVID-19. Clinical trials have demonstrated its ability to reduce the viral load, shorten the time to nucleic acid negativity, and improve clinical outcomes in patients. Additionally, azvudine has shown excellent pharmacokinetic properties and a favorable safety profile with mild side effects. The review also addresses the importance of drug interactions and safety considerations, particularly in high-risk populations. Research should focus on optimizing second-generation inhibitors with enhanced effectiveness against SARS-CoV-2 variants, improving oral bioavailability, and minimizing adverse effects, ensuring more robust treatment options for COVID-19.
新冠病毒病(COVID-19)的全球影响凸显了针对严重急性呼吸综合征冠状病毒2(SARS-CoV-2)采取有效治疗干预措施的迫切需求。阿兹夫定是一种最初为治疗人类免疫缺陷病毒(HIV)而研发的双靶点核苷类药物,因其在治疗COVID-19方面的潜力而受到关注。2022年7月25日,阿兹夫定获得中国国家药品监督管理局(NMPA)的附条件批准,成为首个用于COVID-19治疗的口服SARS-CoV-2 RNA依赖性RNA聚合酶(RdRp)抑制剂。本综述探讨了阿兹夫定在COVID-19背景下的药理活性、抗病毒机制及临床疗效。临床试验已证明其能够降低病毒载量、缩短核酸转阴时间并改善患者的临床结局。此外,阿兹夫定还表现出优异的药代动力学特性和良好的安全性,副作用轻微。本综述还阐述了药物相互作用及安全性考量的重要性,尤其是在高风险人群中。研究应聚焦于优化第二代抑制剂,以增强对SARS-CoV-2变异株的有效性、提高口服生物利用度并将不良反应降至最低,从而确保为COVID-19提供更有效的治疗选择。