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. 2021 Nov;31(11):1212-1214.
doi: 10.1038/s41422-021-00570-1. Epub 2021 Sep 28.

Design and development of an oral remdesivir derivative VV116 against SARS-CoV-2

Yuanchao Xie #  1 , Wanchao Yin #  1 , Yumin Zhang #  2 , Weijuan Shang  2 , Zhen Wang  1 , Xiaodong Luan  3   4   5 , Guanghui Tian  6 , Haji A Aisa  7   8 , Yechun Xu  1   7 , Gengfu Xiao  2   7 , Jia Li  1   7   9 , Hualiang Jiang  1   7   9 , Shuyang Zhang  3   4   5 , Leike Zhang  10   11 , H Eric Xu  12   13 , Jingshan Shen  14   15
Affiliations

Design and development of an oral remdesivir derivative VV116 against SARS-CoV-2

Yuanchao Xie et al. Cell Res. 2021 Nov.
No abstract available

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Conflict of interest statement

Y.Xie, L.Z., G.X., H.J., H.E.X., G.T. and J.S. filed a patent application on antiviral nucleoside analogs.

Figures

Fig. 1
Fig. 1. Discovery of VV116 as a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate.
a The chemical structures of RDV, GS-441524, GS-441524 derivatives A1–A11, the 7-deuterated GS-441524 analog X1, and the isobutyrate ester prodrugs X2–X6. b Inhibition of SARS-CoV-2 replication and cellular toxicity by RDV, GS-441524, X1 and X6 in Vero E6 cells. c Mean plasma concentrations of X1 following single intravenous (2.0 mg/kg X1 equivalent dose) and oral (10.0 mg/kg X1 equivalent dose) administration of X1, X2, X3 or X6 to SD rats (n = 3 per group). d Viral RNA levels and infectious virus titers in lung tissues of control (vehicle-treated), VV116- and EIDD-2801-treated mice on day 2 and day 5 p.i. For VV116, there were three dosage groups (25 mg/kg, 50 mg/kg and 100 mg/kg, mg/kg = mpk), and for EIDD-2801, there were two dosage groups (250 mg/kg and 500 mg/kg). Error bars indicate SEM.
See this image and copyright information in PMC

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