Peringatan Keamanan

In single-dose toxicity studies, no LD50 has been reached even when tecovirimat was given at very high doses (2000 mg/kg) in mice or non-human primates.L41840 There is no clinical experience with overdosage of tecovirimat. In case of overdosage, patients should be monitored for any signs or symptoms of adverse effects. Hemodialysis is not expected to effectively remove tecovirimat in overdosed patients.L41835

Tecovirimat

DB12020

small molecule approved investigational

Deskripsi

The World Health Organization declared smallpox, a contagious and sometimes fatal infectious disease, eradicated in 1980. However, there have been longstanding concerns that smallpox may be used as a bioweapon.A35133,L3614 Tecovirimat is an antiviral drug that was identified via a high-throughput screen in 2002.A35133 It is effective against all orthopoxviruses, including vaccinia, cowpox, ectromelia, rabbitpox, monkeypox, and Variola (smallpox) virus.A35131,A35143

Tecovirimat was approved by the FDA in July 2018 as the first drug ever approved to treat smallpox.L3626, L3614 Tecovirimat was later approved by Health Canada in December 2021,L39397 followed by the approval from the European Commission in January 2022.L40159 Other than smallpox, tecovirimat is also indicated to treat complications due to replication of the vaccinia virus following vaccination against smallpox, and to treat monkeypox and cowpox in adults and children.L40154 Tecovirimat is available as both oral and intravenous formulations.L41835

Struktur Molekul 2D

Berat 376.335
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life (CV%) was 21 (45%) hours following intravenous administration of 200 mg tecovirimat and 19 (29%) hours following oral administration of 600 mg tecovirimat.[L41835]
Volume Distribusi The volume of distribution was 383 L following intravenous administration of 200 mg tecovirimat and 1030 L following oral administration of 600 mg tecovirimat. The blood-to-plasma ratio ranges from 0.62 to 0.90.[L41835]
Klirens (Clearance) The clearance rate was 13 L/h following intravenous administration of 200 mg tecovirimat and 31 L/h following oral administration of 600 mg tecovirimat.[L41835]

Absorpsi

Tecovirimat is readily absorbed following oral administration.A35133 Following oral administration of 600 mg tecovirimat in healthy adults, the mean steady-state AUC0-24hr was 29816 hr x ng/mL and the Cmax was 2159 ng/mL. Following intravenous administration of 200 mg tecovirimat every 12 hours, the mean steady-state AUC0-24hr was 39405 hr x ng/mL and the Cmax was 2630 ng/mL. The Tmax is about six hours.L41835 The steady-state is achieved within four to six days.A35134,L41835 The oral bioavailability of tecovirimat is increased when taken with food. A moderate fat and calories meal increased the drug exposure (AUC) by 39% when tecovirimat was orally administered in conjunction with food.L40154

Metabolisme

Tecovirimat undergoes hydrolysis mediated by UGT1A1 and UGT1A4.L41835 Major metabolites are metabolites M4 (N-{3,5-dioxo-4-azatetracyclo5.3.2.0{2,6}.0{8,10}dodec-11-en-4-yl}amine), M5 (3,5-dioxo-4-aminotetracyclo5.3.2.0{2,6}.0{8,10}dodec-11-ene), and TFMBA (4 (trifluoromethyl) benzoic acid). None of the metabolites is pharmacologically active. None of the glucuronide conjugates was found as a major metabolite in plasma.L40154 The exact chemical structures of tecovirimat metabolites have not been fully characterized.

Rute Eliminasi

The major routes of elimination are through metabolism and renal elimination. Following oral administration, about 73% of the dose was excreted in urine, predominantly in the form of glucuronidated metabolites. About 23% of the dose was recovered in feces, predominantly as the unchanged parent drug.L41835,L40154 In urine, primary tecovirimat glucuronide conjugate and M4 glucuronide conjugate were the most abundant components accounting for means of 24.4% and 30.3% of dose, respectively.L40154

Interaksi Makanan

1 Data
  • 1. Take with food. Take tecovirimat within 30 minutes of eating a fatty meal containing approximately 25 grams of fat.

Interaksi Obat

400 Data
Rubella virus vaccine The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Tecovirimat.
Bacillus calmette-guerin substrain tice live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Tecovirimat.
Bacillus calmette-guerin substrain connaught live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Tecovirimat.
Yellow fever vaccine The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Tecovirimat.
Anthrax vaccine The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Tecovirimat.
Typhoid Vaccine Live The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Tecovirimat.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Tecovirimat.
Human adenovirus e serotype 4 strain cl-68578 antigen The therapeutic efficacy of Human adenovirus e serotype 4 strain cl-68578 antigen can be decreased when used in combination with Tecovirimat.
Vibrio cholerae CVD 103-HgR strain live antigen The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Tecovirimat.
Adenovirus type 7 vaccine live The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Tecovirimat.
Varicella zoster vaccine (live/attenuated) The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Tecovirimat.
Bacillus calmette-guerin substrain russian BCG-I live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain russian BCG-I live antigen can be decreased when used in combination with Tecovirimat.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Tecovirimat.
Midazolam The serum concentration of Midazolam can be decreased when it is combined with Tecovirimat.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Tecovirimat.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Tecovirimat.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Tecovirimat.
Perampanel The metabolism of Perampanel can be increased when combined with Tecovirimat.
Warfarin The metabolism of Warfarin can be increased when combined with Tecovirimat.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Tecovirimat.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Tecovirimat.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Tecovirimat.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Tecovirimat.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Tecovirimat.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Tecovirimat.
Segesterone acetate The metabolism of Segesterone acetate can be increased when combined with Tecovirimat.
Diethylstilbestrol The metabolism of Diethylstilbestrol can be increased when combined with Tecovirimat.
Etonogestrel The metabolism of Etonogestrel can be increased when combined with Tecovirimat.
Desogestrel The metabolism of Desogestrel can be increased when combined with Tecovirimat.
Megestrol acetate The metabolism of Megestrol acetate can be increased when combined with Tecovirimat.
Levonorgestrel The metabolism of Levonorgestrel can be increased when combined with Tecovirimat.
Progesterone The metabolism of Progesterone can be increased when combined with Tecovirimat.
Medroxyprogesterone acetate The metabolism of Medroxyprogesterone acetate can be increased when combined with Tecovirimat.
Norethisterone The metabolism of Norethisterone can be increased when combined with Tecovirimat.
Estradiol The metabolism of Estradiol can be increased when combined with Tecovirimat.
Ethynodiol diacetate The metabolism of Ethynodiol diacetate can be increased when combined with Tecovirimat.
Mifepristone The metabolism of Mifepristone can be increased when combined with Tecovirimat.
Norgestimate The metabolism of Norgestimate can be increased when combined with Tecovirimat.
Ethinylestradiol The metabolism of Ethinylestradiol can be increased when combined with Tecovirimat.
Mestranol The metabolism of Mestranol can be increased when combined with Tecovirimat.
Drospirenone The metabolism of Drospirenone can be increased when combined with Tecovirimat.
Estrone sulfate The metabolism of Estrone sulfate can be increased when combined with Tecovirimat.
Octylphenoxy polyethoxyethanol The metabolism of Octylphenoxy polyethoxyethanol can be increased when combined with Tecovirimat.
Cyproterone acetate The metabolism of Cyproterone acetate can be increased when combined with Tecovirimat.
Trestolone The metabolism of Trestolone can be increased when combined with Tecovirimat.
Norelgestromin The metabolism of Norelgestromin can be increased when combined with Tecovirimat.
Gestodene The metabolism of Gestodene can be increased when combined with Tecovirimat.
Hydroxyprogesterone caproate The metabolism of Hydroxyprogesterone caproate can be increased when combined with Tecovirimat.
Ulipristal The metabolism of Ulipristal can be increased when combined with Tecovirimat.
Dienogest The metabolism of Dienogest can be increased when combined with Tecovirimat.
Norethynodrel The metabolism of Norethynodrel can be increased when combined with Tecovirimat.
Norgestrel The metabolism of Norgestrel can be increased when combined with Tecovirimat.
Cloprostenol The metabolism of Cloprostenol can be increased when combined with Tecovirimat.
Gestrinone The metabolism of Gestrinone can be increased when combined with Tecovirimat.
Nomegestrol The metabolism of Nomegestrol can be increased when combined with Tecovirimat.
Lynestrenol The metabolism of Lynestrenol can be increased when combined with Tecovirimat.
Gossypol The metabolism of Gossypol can be increased when combined with Tecovirimat.
Ormeloxifene The metabolism of Ormeloxifene can be increased when combined with Tecovirimat.
Chlormadinone The metabolism of Chlormadinone can be increased when combined with Tecovirimat.
Norgestrienone The metabolism of Norgestrienone can be increased when combined with Tecovirimat.
Quingestanol The metabolism of Quingestanol can be increased when combined with Tecovirimat.
Demegestone The metabolism of Demegestone can be increased when combined with Tecovirimat.
Etynodiol The metabolism of Etynodiol can be increased when combined with Tecovirimat.
Testosterone enanthate The metabolism of Testosterone enanthate can be increased when combined with Tecovirimat.
Estradiol benzoate The metabolism of Estradiol benzoate can be increased when combined with Tecovirimat.
Estradiol cypionate The metabolism of Estradiol cypionate can be increased when combined with Tecovirimat.
Estradiol valerate The metabolism of Estradiol valerate can be increased when combined with Tecovirimat.
Nomegestrol acetate The metabolism of Nomegestrol acetate can be increased when combined with Tecovirimat.
Norethindrone enanthate The metabolism of Norethindrone enanthate can be increased when combined with Tecovirimat.
Azithromycin The metabolism of Azithromycin can be increased when combined with Tecovirimat.
Ziprasidone The metabolism of Ziprasidone can be increased when combined with Tecovirimat.
Methysergide The metabolism of Methysergide can be increased when combined with Tecovirimat.
Terfenadine The metabolism of Terfenadine can be increased when combined with Tecovirimat.
Meperidine The metabolism of Meperidine can be increased when combined with Tecovirimat.
Chlorpromazine The metabolism of Chlorpromazine can be increased when combined with Tecovirimat.
Albendazole The metabolism of Albendazole can be increased when combined with Tecovirimat.
Cephalexin The metabolism of Cephalexin can be increased when combined with Tecovirimat.
Doxazosin The metabolism of Doxazosin can be increased when combined with Tecovirimat.
Cisapride The metabolism of Cisapride can be increased when combined with Tecovirimat.
Astemizole The metabolism of Astemizole can be increased when combined with Tecovirimat.
Fenofibrate The metabolism of Fenofibrate can be increased when combined with Tecovirimat.
Atazanavir The metabolism of Atazanavir can be increased when combined with Tecovirimat.
Rosuvastatin The metabolism of Rosuvastatin can be increased when combined with Tecovirimat.
Pimozide The metabolism of Pimozide can be increased when combined with Tecovirimat.
Amiodarone The metabolism of Amiodarone can be increased when combined with Tecovirimat.
Fosphenytoin The metabolism of Fosphenytoin can be increased when combined with Tecovirimat.
Allylestrenol The metabolism of Allylestrenol can be increased when combined with Tecovirimat.
Zuclopenthixol The metabolism of Zuclopenthixol can be increased when combined with Tecovirimat.
Roflumilast The metabolism of Roflumilast can be increased when combined with Tecovirimat.
Pretomanid The metabolism of Pretomanid can be increased when combined with Tecovirimat.
Cobimetinib The metabolism of Cobimetinib can be increased when combined with Tecovirimat.
Pimavanserin The metabolism of Pimavanserin can be increased when combined with Tecovirimat.
Lacosamide The metabolism of Lacosamide can be increased when combined with Tecovirimat.
Fosaprepitant The metabolism of Fosaprepitant can be increased when combined with Tecovirimat.
Lomitapide The metabolism of Lomitapide can be increased when combined with Tecovirimat.
Linagliptin The metabolism of Linagliptin can be increased when combined with Tecovirimat.
Vorapaxar The metabolism of Vorapaxar can be increased when combined with Tecovirimat.
Suvorexant The metabolism of Suvorexant can be increased when combined with Tecovirimat.
Netupitant The metabolism of Netupitant can be increased when combined with Tecovirimat.
Idelalisib The metabolism of Idelalisib can be increased when combined with Tecovirimat.

Target Protein

Envelope protein F13

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29972742
    Grosenbach DW, Honeychurch K, Rose EA, Chinsangaram J, Frimm A, Maiti B, Lovejoy C, Meara I, Long P, Hruby DE: Oral Tecovirimat for the Treatment of Smallpox. N Engl J Med. 2018 Jul 5;379(1):44-53. doi: 10.1056/NEJMoa1705688.
  • PMID: 21837250
    Grosenbach DW, Jordan R, Hruby DE: Development of the small-molecule antiviral ST-246 as a smallpox therapeutic. Future Virol. 2011 May;6(5):653-671. doi: 10.2217/fvl.11.27.
  • PMID: 20385870
    Jordan R, Chinsangaram J, Bolken TC, Tyavanagimatt SR, Tien D, Jones KF, Frimm A, Corrado ML, Pickens M, Landis P, Clarke J, Marbury TC, Hruby DE: Safety and pharmacokinetics of the antiorthopoxvirus compound ST-246 following repeat oral dosing in healthy adult subjects. Antimicrob Agents Chemother. 2010 Jun;54(6):2560-6. doi: 10.1128/AAC.01689-09. Epub 2010 Apr 12.
  • PMID: 24100494
    Mucker EM, Goff AJ, Shamblin JD, Grosenbach DW, Damon IK, Mehal JM, Holman RC, Carroll D, Gallardo N, Olson VA, Clemmons CJ, Hudson P, Hruby DE: Efficacy of tecovirimat (ST-246) in nonhuman primates infected with variola virus (Smallpox). Antimicrob Agents Chemother. 2013 Dec;57(12):6246-53. doi: 10.1128/AAC.00977-13. Epub 2013 Oct 7.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Tecovirimat Siga
    Capsule • 200 mg • Oral • EU • Approved
  • Tpoxx
    Injection, solution, concentrate • 10 mg/1mL • Intravenous • US • Approved
  • Tpoxx
    Capsule • 200 mg/1 • Oral • US • Approved
  • Tpoxx
    Capsule • 200 mg • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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