Peringatan Keamanan

Oral LD50 is >2000 mg/kg in rats.L42910

There is limited clinical experience with baloxavir overdose. In one ascending single-dose study involving healthy volunteers, up to 80 mg dose of baloxavir was administered without notable safety concerns.A39894 Treatment of an overdose of baloxavir marboxil should consist of general supportive measures, including monitoring of vital signs and observation of the clinical status of the patient. There is no specific antidote for overdose with baloxavir marboxil. Baloxavir, the active ingredient, is unlikely to be significantly removed by dialysis due to high serum protein binding.L42855

Baloxavir marboxil

DB13997

small molecule approved investigational

Deskripsi

Baloxavir marboxil is an antiviral drug used to treat influenza. More specifically, it is a first-in-class cap-dependent endonuclease inhibitor that works to block influenza virus proliferation.A39895, A251755 It is a prodrug of baloxavir L42855 with an improved absorption profile than its active metabolite due to the addition of a phenolic hydroxyl group to its structure.A251760 Baloxavir marboxil was first globally approved in Japan in February 2018,A39895 followed by the US approval in October, 2018.L4779 It was also approved by the European Commission on January 7, 2021.L45241

Struktur Molekul 2D

Berat 571.55
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent terminal elimination half-life of baloxavir is 79.1 hours.[L42855]
Volume Distribusi The volume of distribution is 1180 L.[L42855]
Klirens (Clearance) Clearance of baloxavir is 10.3 L/h.[L42855]

Absorpsi

Following oral administration of 40 mg baloxavir marboxil in adolescents and adults aged 12 years and older, the AUC was 5520 ng x hr/mL and the Cmax was 68.9 ng/mL. Following a 80 mg dose, the the AUC was 6930 ng x hr/mL and the Cmax was 82.5 ng/mL. The Tmax is about four hours. Food decreased Cmax by 48% and AUC0-inf by 36%.L42855 In pediatric patients aged five to 12 years of age weighing less than 20 kg, the AUCinf was 5830 ng x hr/mL and the Cmax was 148 ng/mL following a 2 mg/kg dose. The AUCinf was 4360 ng x hr/mL and the Cmax was 81.1 ng/mL following a 40 mg dose in pediatric patients who weigh greater than or equal to 20 kg. The Tmax ranged from 3.5 to 4.5 hours.L42855

Metabolisme

Baloxavir predominantly undergoes UGT1A3-mediated metabolism to form glucuronic acid conjugate. It is subsequently metabolized by CYP3A4 to form sulfoxide.A39895, L42855

Rute Eliminasi

Baloxavir is primarily eliminated by biliary excretion. About 80.1% of the total dose is excreted in feces. About 14.7% of the dose is excreted in urine, where 3.3% of the recovered dose is the unchanged parent drug.L42855

Interaksi Makanan

4 Data
  • 1. Avoid antacids. Baloxavir may form a chelate with polyvalent cations in antacids, which may decrease plasma concentrations of baloxavir.
  • 2. Avoid milk and dairy products. Baloxavir may form a chelate with polyvalent cations such as calcium in dairy products, which may decrease plasma concentrations of baloxavir.
  • 3. Avoid multivalent ions. Multivalent ions such as magnesium, calcium, and aluminum can form a chelate with baloxavir, which can reduce the absorption of baloxavir.
  • 4. Take with or without food. Food reduces drug absorption, but not to a clinically significant extent.

Interaksi Obat

14 Data
Rubella virus vaccine The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Baloxavir marboxil.
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 Baloxavir marboxil.
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 Baloxavir marboxil.
Yellow fever vaccine The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Baloxavir marboxil.
Anthrax vaccine The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Baloxavir marboxil.
Typhoid Vaccine Live The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Baloxavir marboxil.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Baloxavir marboxil.
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 Baloxavir marboxil.
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 Baloxavir marboxil.
Adenovirus type 7 vaccine live The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Baloxavir marboxil.
Varicella zoster vaccine (live/attenuated) The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Baloxavir marboxil.
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 Baloxavir marboxil.
Chikungunya vaccine (live, attenuated) The therapeutic efficacy of Chikungunya vaccine (live, attenuated) can be decreased when used in combination with Baloxavir marboxil.
Smallpox (Vaccinia) Vaccine, Live The therapeutic efficacy of Smallpox (Vaccinia) Vaccine, Live can be decreased when used in combination with Baloxavir marboxil.

Target Protein

Polymerase acidic protein PA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30184455
    Hayden FG, Sugaya N, Hirotsu N, Lee N, de Jong MD, Hurt AC, Ishida T, Sekino H, Yamada K, Portsmouth S, Kawaguchi K, Shishido T, Arai M, Tsuchiya K, Uehara T, Watanabe A: Baloxavir Marboxil for Uncomplicated Influenza in Adults and Adolescents. N Engl J Med. 2018 Sep 6;379(10):913-923. doi: 10.1056/NEJMoa1716197.
  • PMID: 29623652
    Heo YA: Baloxavir: First Global Approval. Drugs. 2018 Apr;78(6):693-697. doi: 10.1007/s40265-018-0899-1.
  • PMID: 32601915
    Shirley M: Baloxavir Marboxil: A Review in Acute Uncomplicated Influenza. Drugs. 2020 Jul;80(11):1109-1118. doi: 10.1007/s40265-020-01350-8.
  • PMID: 32020174
    Abraham GM, Morton JB, Saravolatz LD: Baloxavir: A Novel Antiviral Agent in the Treatment of Influenza. Clin Infect Dis. 2020 Oct 23;71(7):1790-1794. doi: 10.1093/cid/ciaa107.

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Sekuens Gen/Protein (FASTA)

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