Obeldesivir (5-25 mg/kg; p.o. and i.v.; Sprague Dawley rats) has favorable pharmacokinetic profiles in rats with high oral bioavailability (F %) of 81.5% and maximum blood concentration (Cmax) of 8.2 μM[1].
Obeldesivir (250-500 mg/kg; p.o.; daily, for 4 days; hACE2 knock-in and Ad5-hACE2 mice) has antiviral activity and inhibits SARS-CoV-2 replication in mouse models[1].
Obeldesivir (100-250 mg/kg; p.o.; daily, for 10 days) reduces lung damage and protects K18-hACE2 mice[1].
Obeldesivir (10-150 mg/kg; p.o.; daily, for 3 days) reduces virus titers and lung damage caused by Delta variant infection in K18-hACE2 mice[1].
| Animal Model: | Sprague Dawley rats[1] |
| Dosage: | 5 and 25 mg/kg |
| Administration: | Oral administration (25 mg/kg) and intravenous injection (5 mg/kg) |
| Result: | 1.19|
| parameters | i.v. (5 mg/kg) | p.o. (25 mg/kg) | | AUClast (μM·h) | 5.6 | 22.8 | | T1/2 (h) | 1.5 | 1.2 | | Tmax (h) | | 0.5 | | Cmax (μM) | 8.7 | 8.2 | | F % | | 81.5 |
|
| Animal Model: | hACE2 knock-in and Ad5-hACE2 mice[1] |
| Dosage: | 250 and 500 mg/kg |
| Administration: | Oral administration; daily, for 4 days |
| Result: | Inhibited gRNA and sgRNA, which is Biomarkers of coronavirus replication. Reduced the viral load and pathological damage of the lung. |
| Animal Model: | K18-hACE2 mice[1] |
| Dosage: | 100 and 250 mg/kg |
| Administration: | Oral administration; daily, for 10 days |
| Result: | Reduced viral RNA and increased the survival rate of mice. Reduced evidence of lung pathology and the production of inflammatory cytokines and chemokines in the lung tissues. |
| Animal Model: | K18-hACE2 mice[1] |
| Dosage: | 10, 30, 80 and 150 mg/kg |
| Administration: | Oral administration; daily, for 3 days |
| Result: | Reduced viral load in a dose-dependent manner and alleviated the symptoms in the lung. |
![D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate) Structure](/CAS/20211123/GIF/2647441-36-7.gif)
