
| 10.1038/s41392-021-00835-6
http://scihub22266oqcxt.onion/10.1038/s41392-021-00835-6
 34873151!8646019!34873151
free
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Signal+Transduct+Target+Ther 2021 ; 6 (1): 414 Nephropedia Template TP
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Azvudine is a thymus-homing anti-SARS-CoV-2 drug effective in treating COVID-19 patients #MMPMID34873151Zhang JL; Li YH; Wang LL; Liu HQ; Lu SY; Liu Y; Li K; Liu B; Li SY; Shao FM; Wang K; Sheng N; Li R; Cui JJ; Sun PC; Ma CX; Zhu B; Wang Z; Wan YH; Yu SS; Che Y; Wang CY; Wang C; Zhang Q; Zhao LM; Peng XZ; Cheng Z; Chang JB; Jiang JDSignal Transduct Target Ther 2021[Dec]; 6 (1): 414 PMID34873151show ga
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 EC(50) between 1.2 and 4.3 muM, 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.|*COVID-19 Drug Treatment[MESH]|*Thymus Gland/metabolism/virology[MESH]|Adult[MESH]|Aged[MESH]|Aged, 80 and over[MESH]|Animals[MESH]|Antiviral Agents/*administration & dosage[MESH]|Azides/*administration & dosage[MESH]|Coronavirus OC43, Human/metabolism[MESH]|Deoxycytidine/administration & dosage/*analogs & derivatives[MESH]|Female[MESH]|Humans[MESH]|Male[MESH]|Middle Aged[MESH]|Rats[MESH]
  
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