详情页 - 云南省第一人民医院机构库

当前位置：首页 > 详情页

Azvudine is a thymus-homing anti-SARS-CoV-2 drug effective in treating COVID-19 patients

文献详情

资源类型：

Pubmed体系：

收录情况： ◇ 统计源期刊 ◇ CSCD-C ◇ 卓越：领军期刊

作者：

机构： [1]State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China [2]lnstitute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China [3]lnstitute of Medical Biology, Chinese Academy of Medical Science and Peking Union Medical College, Kunming 650031 Yunnan, China [4]Genuine Biotech. Inc., Pingdingshan 467000 Henan, China [5]Department of Respiratory Medicine, Zhongnan Hospital of Wuhan University, Wuhan Research Center for Infectious Diseases and Cancer, Wuhan 430071 Hubei, China [6]the First Affiliated Hospital of Henan University of Chinese Medicine, Zhengzhou 450000 Henan, China [7]Department of Internal Medicine, Henan Provincial Peoples Hospital, Zhengzhou 450003 Henan, China [8]Henan Key Laboratory of Organic Functional Molecule and Drug Innovation, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007 Henan, China [9]National Clinical Research Center for Respiratory Diseases, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100005, China [10]School of Chemistry, Zhengzhou University, Zhengzhou 450001 Henan, China

出处：

DOI：

ISSN：

摘要：

Azvudine (FNC) is a nucleoside analog that inhibits HIV-1 RNA-dependent RNA polymerase (RdRp). Recently, we discovered FNC an agent against SARS-CoV-2, and have taken it into Phase III trial for COVID-19 patients. FNC monophosphate analog inhibited SARS-CoV-2 and HCoV-OC43 coronavirus with an EC50 between 1.2 and 4.3 μM, depending on viruses or cells, and selective index (SI) in 15-83 range. Oral administration of FNC in rats revealed a substantial thymus-homing feature, with FNC triphosphate (the active form) concentrated in the thymus and peripheral blood mononuclear cells (PBMC). Treating SARS-CoV-2 infected rhesus macaques with FNC (0.07 mg/kg, qd, orally) reduced viral load, recuperated the thymus, improved lymphocyte profiles, alleviated inflammation and organ damage, and lessened ground-glass opacities in chest X-ray. Single-cell sequencing suggested the promotion of thymus function by FNC. A randomized, single-arm clinical trial of FNC on compassionate use (n = 31) showed that oral FNC (5 mg, qd) cured all COVID-19 patients, with 100% viral ribonucleic acid negative conversion in 3.29 ± 2.22 days (range: 1-9 days) and 100% hospital discharge rate in 9.00 ± 4.93 days (range: 2-25 days). The side-effect of FNC is minor and transient dizziness and nausea in 16.12% (5/31) patients. Thus, FNC might cure COVID-19 through its anti-SARS-CoV-2 activity concentrated in the thymus, followed by promoted immunity.© 2021. The Author(s).

基金：

语种：

PubmedID：

中科院(CAS)分区：

出版当年[2021]版：

大类 | 1 区

医学

小类 | 1 区生化与分子生物学 1 区细胞生物学

最新[2023]版：

大类 | 1 区

医学

小类 | 1 区生化与分子生物学 1 区细胞生物学

第一作者：

第一作者机构： [1]State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China

共同第一作者：

通讯作者：

通讯机构： [1]State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China [2]lnstitute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China [8]Henan Key Laboratory of Organic Functional Molecule and Drug Innovation, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007 Henan, China [10]School of Chemistry, Zhengzhou University, Zhengzhou 450001 Henan, China

推荐引用方式(GB/T 7714)：

APA：

MLA：