| 词条 | Tecovirimat |
| 释义 |
| verifiedrevid = | IUPAC_name = N3,5-Dioxo-4-azatetracyclo[5.3.2.0{2,6}.0{8,10}]dodec-11-en-4- yl4-(trifluoromethyl)benzamide | ATC_prefix = J05 | ATC_suffix = AX24 | image = Tecovirimat.svg | width = 200 | tradename = Tpoxx | licence_EU = | licence_US = | pregnancy_US = | legal_status = Prescription only (US)[1] | routes_of_administration = By mouth | bioavailability = | metabolism = | excretion = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = | UNII_Ref = {{fdacite|correct|FDA}} | UNII = F925RR824R | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1242629 | synonyms = ST-246 | C=19 | H=15 | F=3 | N=2 | O=3 | smiles = FC(F)(F)c1ccc(cc1)C(=O)NN1C(=O)C2C(C3C=CC2C2CC32)C1=O | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C19H15F3N2O3/c20-19(21,22)9-3-1-8(2-4-9)16(25)23-24-17(26)14-10-5-6-11(13-7-12(10)13)15(14)18(24)27/h1-6,10-15H,7H2,(H,23,25) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = CSKDFZIMJXRJGH-UHFFFAOYSA-N }}Tecovirimat (ST-246 or Tpoxx)[2] is an antiviral with activity against orthopoxviruses such as smallpox and monkeypox. It is the only antipoxviral drug approved in the US.[3] The drug works by blocking cellular transmission of the virus, thus preventing the disease.[4] Tecovirimat has been effective in laboratory testing; it has been shown to protect animals from monkeypox and rabbitpox and causes no serious side effects in humans.[2] However, tecovirimat has never been used to treat a human with smallpox due to the disease's eradication. Two million doses of tecovirimat are stockpiled in the US Strategic National Stockpile should an orthopoxvirus-based bioterror attack occur.[5][6] Clinical studyThe results of clinical trials involving tecovirimat supports its use against smallpox and other related orthopoxviruses. It has shown potential for a variety of uses including prophylaxis, as a post-exposure therapeutic, as a therapeutic and an adjunct to vaccination.[7] Tecovirimat can be taken orally and has recently been granted permission to conduct Phase II trials by the U.S. Food and Drug Administration (FDA). In Phase I trials tecovirimat was generally well tolerated with no serious adverse events.[8] Due to its importance for biodefense, the FDA has designated tecovirimat for 'fast-track' status, creating a path for expedited FDA review and eventual regulatory approval. On July 13, 2018, the FDA announced approval of tecovirimat.[9] Mechanism of actionTecovirimat inhibits the function of a major envelope protein required for the production of extracellar virus. Thus the virus is prevented from leaving an infected cell and the spread of the virus within the body is prevented.[10] Society and cultureOriginally researched by the National Institute of Allergy and Infectious Diseases, the drug was previously owned by Viropharma and discovered in collaboration with scientists at USAMRIID. It is currently owned and manufactured by Siga Technologies, a pharmaceutical company in the biodefense arena that won a government contract to develop the drug. References1. ^{{cite web|url=https://investor.siga.com/news-releases/news-release-details/us-food-and-drug-administration-approves-siga-technologies|title=U.S. Food and Drug Administration Approves SIGA Technologies’ TPOXX (tecovirimat) for the Treatment of Smallpox - SIGA|website=SIGA}} 2. ^1 {{cite web |last1=McNeil Jr. |first1=Donald G. |title=Drug to Treat Smallpox Approved by F.D.A., a Move Against Bioterrorism |url=https://www.nytimes.com/2018/07/13/health/smallpox-drug-fda-bioterrorism.html |website=The New York Times |publisher=The New York Times |accessdate=16 July 2018}} 3. ^{{cite web |title=Press Announcements - FDA approves the first drug with an indication for treatment of smallpox |url=https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm613496.htm |website=www.fda.gov |accessdate=1 August 2018 |language=en}} 4. ^{{cite journal |last1=Grosenbach |first1=Douglas W. |last2=Honeychurch |first2=Kady |last3=Rose |first3=Eric A. |last4=Chinsangaram |first4=Jarasvech |last5=Frimm |first5=Annie |last6=Maiti |first6=Biswajit |last7=Lovejoy |first7=Candace |last8=Meara |first8=Ingrid |last9=Long |first9=Paul |last10=Hruby |first10=Dennis E. |title=Oral Tecovirimat for the Treatment of Smallpox |journal=N Engl J Med |date=5 July 2018 |volume=379 |pages=44-53 |doi=10.1056/NEJMoa1705688 |url=https://www.nejm.org/doi/full/10.1056/NEJMoa1705688 |accessdate=16 July 2018}} 5. ^{{cite journal | doi = 10.1371/journal.ppat.1004108| pmid = 24789223| title = Are We There Yet? The Smallpox Research Agenda Using Variola Virus| journal = PLoS Pathogens| volume = 10| issue = 5| pages = e1004108| year = 2014| last1 = Damon| first1 = Inger K.| last2 = Damaso| first2 = Clarissa R.| last3 = McFadden| first3 = Grant| pmc=4006926}} 6. ^{{cite web|url=https://www.sciencenews.org/article/first-smallpox-treatment-one-step-closer-fda-approval|title=FDA approves the first smallpox treatment|first=Aimee|last=Cunningham|date=13 July 2018|publisher=}} 7. ^Siga Technologies 8. ^{{cite journal | pmc = 2346641| year = 2008| author1 = Jordan| first1 = R| title = Single-Dose Safety and Pharmacokinetics of ST-246, a Novel Orthopoxvirus Egress Inhibitor| journal = Antimicrobial Agents and Chemotherapy| volume = 52| issue = 5| pages = 1721–1727| last2 = Tien| first2 = D| last3 = Bolken| first3 = T. C.| last4 = Jones| first4 = K. F.| last5 = Tyavanagimatt| first5 = S. R.| last6 = Strasser| first6 = J| last7 = Frimm| first7 = A| last8 = Corrado| first8 = M. L.| last9 = Strome| first9 = P. G.| last10 = Hruby| first10 = D. E.| doi = 10.1128/AAC.01303-07| pmid = 18316519}} 9. ^{{cite web|url=https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm613496.htm|title=Press Announcements - FDA approves the first drug with an indication for treatment of smallpox|first=Office of the|last=Commissioner|website=www.fda.gov}} 10. ^{{cite journal | pmc = 1235851| year = 2005| author1 = Yang| first1 = G| title = An Orally Bioavailable Antipoxvirus Compound (ST-246) Inhibits Extracellular Virus Formation and Protects Mice from Lethal Orthopoxvirus Challenge| journal = Journal of Virology| volume = 79| issue = 20| pages = 13139–13149| last2 = Pevear| first2 = D. C.| last3 = Davies| first3 = M. H.| last4 = Collett| first4 = M. S.| last5 = Bailey| first5 = T| last6 = Rippen| first6 = S| last7 = Barone| first7 = L| last8 = Burns| first8 = C| last9 = Rhodes| first9 = G| last10 = Tohan| first10 = S| last11 = Huggins| first11 = J. W.| last12 = Baker| first12 = R. O.| last13 = Buller| first13 = R. L.| last14 = Touchette| first14 = E| last15 = Waller| first15 = K| last16 = Schriewer| first16 = J| last17 = Neyts| first17 = J| last18 = Declercq| first18 = E| last19 = Jones| first19 = K| last20 = Hruby| first20 = D| last21 = Jordan| first21 = R| doi = 10.1128/JVI.79.20.13139-13149.2005| pmid = 16189015}} 8 : Antivirals|Poxviruses|Imides|Hydrazides|Trifluoromethyl compounds|Benzamides|Nitrogen heterocycles|Cyclopropanes |
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