Peringatan Keamanan

The oral LD50 of umifenovir in mice and rats has been reported as 340-400 mg/kg and >3000 mg/kg, respectively.A191475 Chronic administration of doses 10-50 times the therapeutic human dose resulted in no pathological changes to animal subjects.

Further information regarding the management of umifenovir overdose is unavailable.

Umifenovir

DB13609

small molecule investigational

Deskripsi

Umifenovir is an indole-based, hydrophobic, dual-acting direct antiviral/host-targeting agent used for the treatment and prophylaxis of influenza and other respiratory infections.A191475 It has been in use in Russia for approximately 25 years and in China since 2006. Its invention is credited to a collaboration between Russian scientists from several research institutes 40-50 years ago, and reports of its chemical synthesis date back to 1993.A191475 Umifenovir's ability to exert antiviral effects through multiple pathways has resulted in considerable investigation into its use for a variety of enveloped and non-enveloped RNA and DNA viruses, including Flavivirus,A191388 Zika virus,A191391 foot-and-mouth disease,A191394 Lassa virus,A191403 Ebola virus,A191403 herpes simplex,A191409, hepatitis B and C viruses, chikungunya virus, reovirus, Hantaan virus, and coxsackie virus B5.A191475,A191412 This dual activity may also confer additional protection against viral resistance, as the development of resistance to umifenovir does not appear to be significant.A191475

Umifenovir is currently being investigated as a potential treatment and prophylactic agent for COVID-19 caused by SARS-CoV2 infections in combination with both currently available and investigational HIV therapies.A191385,A191550,L12012

Struktur Molekul 2D

Berat 477.42
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of umifenovir following oral administration has been estimated to be between 17-21 hours.[A191475,A191499] Serum half-lives of the M5, M6-1, and M8 metabolites were found to be 26.3 ± 5.9, 25.0 ± 5.4, and 25.7 ± 8.8, respectively.[A191499]
Volume Distribusi Data regarding the volume of distribution of umifenovir are currently unavailable.
Klirens (Clearance) In a study involving healthy male Chinese volunteers, the oral clearance of umifenovir was found to be 99 ± 34 L/h.[A191499]

Absorpsi

Umifenovir is rapidly absorbed following oral administration, with an estimated Tmax between 0.65-1.8 hours.A191499,A191508,A191475 The Cmax has been estimated as 415 - 467 ng/mL and appears to increase linearly with dose,A191499,A191508 and the AUC0-inf following oral administration has been estimated to be approximately 2200 ng/mL/h.A191499,A191508

Metabolisme

Umifenovir is highly metabolized in the body, primarily in hepatic and intestinal microsomess, with approximately 33 metabolites having been observed in human plasma, urine, and feces.A191499 The principal phase I metabolic pathways include sulfoxidation, N-demethylation, and hydroxylation, followed by phase II sulfate and glucuronide conjugation. In the urine, the major metabolites were sulfate and glucuronide conjugates, while the major species in the feces was unchanged parent drug (~40%) and the M10 metabolite (~3.0%). In the plasma, the principal metabolites are M6-1, M5, and M8 - of these, M6-1 appears of most importance given its high plasma exposure and long elimination half-life (~25h), making it a potentially important player in the safety and efficacy of umifenovir.A191499 Enzymes involved in the metabolism of umifenovir include members of the cytochrome P450 family (primarily CYP3A4), flavin-containing monooxygenase (FMO) family, and UDP-glucuronosyltransferase (UGT) family (specifically UGT1A9 and UGT2B7).A191499,A191454,A191424

Rute Eliminasi

The major route of elimination is via the feces. Approximately 40% of an ingested dose is excreted unchanged, of which 38.9% is excreted in the bile and 0.12% excreted through the kidneys.A191508 The total recovery of parent drug and metabolites in the urine accounts for less than 1% of an ingested dose.A191499

Interaksi Obat

179 Data
Pitolisant The serum concentration of Umifenovir can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Umifenovir can be increased when combined with Metreleptin.
Mefenamic acid The metabolism of Umifenovir can be decreased when combined with Mefenamic acid.
Diflunisal The metabolism of Umifenovir can be decreased when combined with Diflunisal.
Deferasirox The metabolism of Umifenovir can be decreased when combined with Deferasirox.
Eltrombopag The metabolism of Umifenovir can be decreased when combined with Eltrombopag.
Isavuconazole The metabolism of Umifenovir can be decreased when combined with Isavuconazole.
Troglitazone The metabolism of Troglitazone can be decreased when combined with Umifenovir.
Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Umifenovir.
Indomethacin The metabolism of Indomethacin can be decreased when combined with Umifenovir.
Entacapone The metabolism of Entacapone can be decreased when combined with Umifenovir.
Valdecoxib The metabolism of Valdecoxib can be decreased when combined with Umifenovir.
Diclofenac The metabolism of Diclofenac can be decreased when combined with Umifenovir.
Labetalol The metabolism of Labetalol can be decreased when combined with Umifenovir.
Mycophenolate mofetil The metabolism of Mycophenolate mofetil can be decreased when combined with Umifenovir.
Flurbiprofen The metabolism of Flurbiprofen can be decreased when combined with Umifenovir.
Nateglinide The metabolism of Nateglinide can be decreased when combined with Umifenovir.
Zileuton The metabolism of Zileuton can be decreased when combined with Umifenovir.
Etodolac The metabolism of Etodolac can be decreased when combined with Umifenovir.
Naproxen The metabolism of Naproxen can be decreased when combined with Umifenovir.
Propofol The metabolism of Propofol can be decreased when combined with Umifenovir.
Oxazepam The metabolism of Oxazepam can be decreased when combined with Umifenovir.
Buprenorphine The metabolism of Buprenorphine can be decreased when combined with Umifenovir.
Ethinylestradiol The metabolism of Ethinylestradiol can be decreased when combined with Umifenovir.
Formoterol The metabolism of Formoterol can be decreased when combined with Umifenovir.
Fenofibrate The metabolism of Fenofibrate can be decreased when combined with Umifenovir.
Ibuprofen The metabolism of Ibuprofen can be decreased when combined with Umifenovir.
Gemfibrozil The metabolism of Gemfibrozil can be decreased when combined with Umifenovir.
Lumiracoxib The metabolism of Lumiracoxib can be decreased when combined with Umifenovir.
Topiroxostat The metabolism of Topiroxostat can be decreased when combined with Umifenovir.
Ezogabine The metabolism of Ezogabine can be decreased when combined with Umifenovir.
Vadimezan The metabolism of Vadimezan can be decreased when combined with Umifenovir.
Dapagliflozin The metabolism of Dapagliflozin can be decreased when combined with Umifenovir.
Ambrisentan The metabolism of Ambrisentan can be decreased when combined with Umifenovir.
Ketobemidone The metabolism of Ketobemidone can be decreased when combined with Umifenovir.
Seratrodast The metabolism of Seratrodast can be decreased when combined with Umifenovir.
Gavestinel The metabolism of Gavestinel can be decreased when combined with Umifenovir.
Canagliflozin The metabolism of Canagliflozin can be decreased when combined with Umifenovir.
Dolutegravir The metabolism of Dolutegravir can be decreased when combined with Umifenovir.
Dexibuprofen The metabolism of Dexibuprofen can be decreased when combined with Umifenovir.
Propacetamol The metabolism of Propacetamol can be decreased when combined with Umifenovir.
Artenimol The metabolism of Artenimol can be decreased when combined with Umifenovir.
Glasdegib The metabolism of Glasdegib can be decreased when combined with Umifenovir.
Fostamatinib The metabolism of Fostamatinib can be decreased when combined with Umifenovir.
Darolutamide The metabolism of Darolutamide can be decreased when combined with Umifenovir.
Methylene blue The metabolism of Umifenovir can be decreased when combined with Methylene blue.
Dabigatran etexilate The metabolism of Dabigatran etexilate can be decreased when combined with Umifenovir.
Artesunate The metabolism of Artesunate can be decreased when combined with Umifenovir.
Vericiguat The metabolism of Vericiguat can be decreased when combined with Umifenovir.
Cabotegravir The metabolism of Cabotegravir can be decreased when combined with Umifenovir.
Febuxostat The metabolism of Febuxostat can be decreased when combined with Umifenovir.
Niflumic acid The metabolism of Umifenovir can be decreased when combined with Niflumic acid.
Cannabidiol The metabolism of Umifenovir can be decreased when combined with Cannabidiol.
Phenytoin The metabolism of Phenytoin can be decreased when combined with Umifenovir.
Sorafenib The metabolism of Umifenovir can be decreased when combined with Sorafenib.
Regorafenib The metabolism of Regorafenib can be decreased when combined with Umifenovir.
Valproic acid The metabolism of Valproic acid can be decreased when combined with Umifenovir.
Mycophenolic acid The metabolism of Mycophenolic acid can be decreased when combined with Umifenovir.
Enasidenib The metabolism of Enasidenib can be decreased when combined with Umifenovir.
Rubella virus vaccine The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Umifenovir.
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 Umifenovir.
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 Umifenovir.
Yellow fever vaccine The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Umifenovir.
Anthrax vaccine The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Umifenovir.
Typhoid Vaccine Live The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Umifenovir.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Umifenovir.
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 Umifenovir.
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 Umifenovir.
Adenovirus type 7 vaccine live The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Umifenovir.
Varicella zoster vaccine (live/attenuated) The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Umifenovir.
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 Umifenovir.
Cenobamate The serum concentration of Umifenovir can be decreased when it is combined with Cenobamate.
Ritonavir The serum concentration of Umifenovir can be increased when it is combined with Ritonavir.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Umifenovir.
Tucatinib The metabolism of Tucatinib can be decreased when combined with Umifenovir.
Abametapir The serum concentration of Umifenovir can be increased when it is combined with Abametapir.
Satralizumab The serum concentration of Umifenovir can be decreased when it is combined with Satralizumab.
Sotorasib The serum concentration of Umifenovir can be decreased when it is combined with Sotorasib.
Cyclosporine The metabolism of Umifenovir can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Umifenovir can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Umifenovir can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Umifenovir can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Umifenovir can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Umifenovir can be decreased when combined with Isradipine.
Diltiazem The metabolism of Umifenovir can be decreased when combined with Diltiazem.
Clozapine The metabolism of Umifenovir can be decreased when combined with Clozapine.
Ciprofloxacin The metabolism of Umifenovir can be decreased when combined with Ciprofloxacin.
Nicardipine The metabolism of Umifenovir can be decreased when combined with Nicardipine.
Verapamil The metabolism of Umifenovir can be decreased when combined with Verapamil.
Aprepitant The metabolism of Umifenovir can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Umifenovir can be decreased when combined with Isoniazid.
Primaquine The metabolism of Umifenovir can be decreased when combined with Primaquine.
Miconazole The metabolism of Umifenovir can be decreased when combined with Miconazole.
Fusidic acid The metabolism of Umifenovir can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Umifenovir can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Umifenovir can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Umifenovir can be decreased when combined with Milnacipran.
Simeprevir The metabolism of Umifenovir can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Umifenovir can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Umifenovir can be decreased when combined with Desvenlafaxine.

Referensi & Sumber

Synthesis reference: Trofimov, F.A., Tsyshkova, N.G., Zotova, S.A., Grinev, A.N., 1993. Synthesis of a new antiviral agent, arbidole. Pharm Chem J 27, 75–76.
Artikel (PubMed)
  • PMID: 31996494
    Lu H: Drug treatment options for the 2019-new coronavirus (2019-nCoV). Biosci Trends. 2020 Jan 28. doi: 10.5582/bst.2020.01020.
  • PMID: 29642580
    Haviernik J, Stefanik M, Fojtikova M, Kali S, Tordo N, Rudolf I, Hubalek Z, Eyer L, Ruzek D: Arbidol (Umifenovir): A Broad-Spectrum Antiviral Drug That Inhibits Medically Important Arthropod-Borne Flaviviruses. Viruses. 2018 Apr 10;10(4). pii: v10040184. doi: 10.3390/v10040184.
  • PMID: 29895962
    Fink SL, Vojtech L, Wagoner J, Slivinski NSJ, Jackson KJ, Wang R, Khadka S, Luthra P, Basler CF, Polyak SJ: The Antiviral Drug Arbidol Inhibits Zika Virus. Sci Rep. 2018 Jun 12;8(1):8989. doi: 10.1038/s41598-018-27224-4.
  • PMID: 31162013
    Herod MR, Adeyemi OO, Ward J, Bentley K, Harris M, Stonehouse NJ, Polyak SJ: The broad-spectrum antiviral drug arbidol inhibits foot-and-mouth disease virus genome replication. J Gen Virol. 2019 Sep;100(9):1293-1302. doi: 10.1099/jgv.0.001283. Epub 2019 Jun 4.
  • PMID: 28003465
    Kadam RU, Wilson IA: Structural basis of influenza virus fusion inhibition by the antiviral drug Arbidol. Proc Natl Acad Sci U S A. 2017 Jan 10;114(2):206-214. doi: 10.1073/pnas.1617020114. Epub 2016 Dec 21.
  • PMID: 30700611
    Hulseberg CE, Feneant L, Szymanska-de Wijs KM, Kessler NP, Nelson EA, Shoemaker CJ, Schmaljohn CS, Polyak SJ, White JM: Arbidol and Other Low-Molecular-Weight Drugs That Inhibit Lassa and Ebola Viruses. J Virol. 2019 Apr 3;93(8). pii: JVI.02185-18. doi: 10.1128/JVI.02185-18. Print 2019 Apr 15.
  • PMID: 27918208
    Zeng LY, Yang J, Liu S: Investigational hemagglutinin-targeted influenza virus inhibitors. Expert Opin Investig Drugs. 2017 Jan;26(1):63-73. doi: 10.1080/13543784.2017.1269170. Epub 2016 Dec 14.
  • PMID: 28890393
    Li MK, Liu YY, Wei F, Shen MX, Zhong Y, Li S, Chen LJ, Ma N, Liu BY, Mao YD, Li N, Hou W, Xiong HR, Yang ZQ: Antiviral activity of arbidol hydrochloride against herpes simplex virus I in vitro and in vivo. Int J Antimicrob Agents. 2018 Jan;51(1):98-106. doi: 10.1016/j.ijantimicag.2017.09.001. Epub 2017 Sep 7.
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Contoh Produk & Brand

Produk: 0 • International brands: 2
International Brands
  • Arbidol
  • Arbidole

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