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.
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].
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