Tecovirimat is a potent, selective and orally bioavailable antipoxvirus compound active against multiple orthopoxviruses, including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), and variola viruses, with EC50 value of 0.01μM for Vaccinia virus in CPE assays. It inhibited plaque formation, virus-induced CPE and extracellular virus production at 5μM. Treatment with oral administration of Tecovirimat, at dose of 50 mg/kg twice a day for 14 days, protected BALB/c mice from lethal infection by vaccinia virus strain IHD-J, A/NCr mice from lethal infection by ectromelia virus[4]. Tecovirimat is FDA-approved for the treatment of human smallpox disease caused by Variola virus in adults and children[5].
作用机制
Tecovirimat blocks interaction of p37 with Rab9 and TIP47. Thus, ST-246 prevents wrapping complex formation by inhibiting interaction of p37 with components of LE-transport vesicle biogenesis[3].
Tecovirimat 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Vero (African green monkey) cell lines
0.01-100 µM
1 hour
To test MPXV sensitivity to tecovirimat, results showed that MPXV isolates with the E353K mutation remained sensitive to tecovirimat
Emerg Infect Dis. 2023 Dec;29(12):2426-2432
HeLa cells
10 µM
24 hours
Assess the effect of Tecovirimat on F13 dimerization, showing a significant increase in F13 dimerization signal.
Nat Microbiol. 2025 Mar;10(3):734-748
Vero cells
17 nM
48 hours
Evaluate the inhibitory effect of Tecovirimat on MPXV clade IIb strain, showing an IC50 of 17 nM.
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