BALOXAVIR: ANTI-INFLUENZA VIRUS AGENT VIA INHIBITION OF CAP-DEPENDENT ENDRONUCLEASE

Authors

  • Roongrat Piyananjaruhsri Department of Pharmacy, Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok

DOI:

https://doi.org/10.69598/tbps.15.1.91-108

Keywords:

baloxavir, endonuclease, influenza, oseltamivir, neuraminidase

Abstract

Influenza is an acute respiratory infection caused by a virus. Influenza A and influenza B are the two main types of influenza viruses that cause seasonal influenza epidemics each year. Influenza can also cause illness and can lead to death, especially in those at-risk patients with flu-related severe complications, e.g., the older adults aged 65 years and over, and patients with either chronic lung disease, diabetes mellitus, or immune deficiency. Early treatment of influenza can reduce the risk of severe complications. Currently, there are many limitations for influenza medication, such as oseltamivir - a neuraminidase inhibitors which inhibits the release of newly replicated influenza virus. Moverover, the lengthy treatment duration of five days, and common drug-related adverse event such as nausea and vomiting are also limitations for oseltamivir. Baloxavia has been approved by the US Food and Drug Administration (FDA) since October 2018. Baloxavir, a novel drug, is indicated for the treatment of acute uncomplicated influenza in patients aged 12 years and older whose symptom has occurred for not more than 48 hours. Baloxavir inhibits the cap-dependent endonuclease (CEN), which is required for viral gene transcription, and effectively inhibit viral replication while oseltamivir inhibits the neuraminidase enzyme. Consequently, baloxavir is superior to oseltamivir in a reduction in the number of viruses. Clinical studies assessing the effectiveness of the drug in the reduction of influenza A and B viral titer revealed that the time required to alleviate the symptoms and adverse effect are similar between baloxavir and oseltamivir. Baloxavir is oral-administered, and it can reduce the level of influenza A and B on the first day. Baloxavir has a long half-life and used as a single-dose treatment. Consequently, baloxavir is an alternative option to current therapy for acute uncomplicated influenza.

References

Chow EJ, Doyle JD, Uyeki TM. Influenza virus-related critical illness: prevention, diagnosis, treatment. Crit Care. 2019;23:214.

Rolfes MA, Foppa IM, Garg S, Flannery B, Brammer L, Singleton JA, et al. Annual estimates of the burden of seasonal influenza in the United States: a tool for strengthening influenza surveillance and preparedness. Influenza Other Respir Viruses. 2018;12:132-7.

Ministry of Public Health (Thailand). Department of Disease Control. Bureau of General Communicable Diseases. Influenza situation [Internet]. Nonthaburi: The Bureau; 2018 [cited 2019 Aug 14]. Available from: https://ddc.moph.go.th/uploads/files/23061bd58a4728ff18eb6cfd7b06ffe1.pdf (in Thai)

Ministry of Public Health (Thailand). Department of Disease Control. Bureau of General Communicable Diseases. Influenza situation [Internet]. Nonthaburi: The Bureau; 2019 [cited 2019 Aug 14]. Available from: https://ddc.moph.go.th/uploads/files/3ed4dd1901ec8c73de52ee37f7dc342b.pdf (in Thai)

Ministry of Public Health (Thailand). Department of Disease Control. Bureau of Epidemiology. Surveillance of influenza virus [Internet]. Nonthaburi: The Bureau; 2020 [cited 2020 Jan 13]. Available from: https://www.thainihnic. org/influenza/files/Flulab/Flu%20lab%20sur%20Dec_WK53%202019.pdf (in Thai)

O'Hanlon R, Shaw ML. Baloxavir marboxil: the new influenza drug on the market. Curr Opin Virol. 2019;35:14-8.

de St Maurice A, Halasa N. Preparing for the 2019-2020 influenza season. Pediatr Transplant. 2020;24(1);e13645.

IBM MICROMEDEX® [Database on the internet]. Greenwood Village (CO): IBM Watson Health; c2020. DRUGDEX®, Zanamivir [cited 2020 Jan 14]. Available from: https://www.micromedexsolutions.com [Subscription required to view].

IBM MICROMEDEX® [Database on the internet]. Greenwood Village (CO): IBM Watson Health; c2020. DRUGDEX®, Peramivir [cited 2020 Jan 14]. Available from: https://www.micromedexsolutions.com [Subscription required to view].

IBM MICROMEDEX® [Database on the internet]. Greenwood Village (CO): IBM Watson Health; c2020. DRUGDEX®, Oseltamivir [cited 2020 Jan 14]. Available from: https://www.micromedexsolutions.com [Subscription required to view].

IBM MICROMEDEX® [Database on the internet]. Greenwood Village (CO): IBM Watson Health; c2020. DRUGDEX®, Baloxavir [cited 2020 Jan 14]. Available from: https://www.micromedexsolutions.com [Subscription required to view].

IBM MICROMEDEX® [Database on the internet]. Greenwood Village (CO): IBM Watson Health; c2020. DRUGDEX®, Amantadine [cited 2020 Jan 14]. Available from: https://www.micromedexsolutions.com [Subscription required to view].

IBM MICROMEDEX® [Database on the internet]. Greenwood Village (CO): IBM Watson Health; c2020. DRUGDEX®, Rimantadine [cited 2020 Jan 14]. Available from: https://www.micromedexsolutions.com [Subscription required to view].

Locke SC, Splawn LM, Cho JC. Baloxavir marboxil: a novel cap-dependent endonuclease (CEN) inhibitor for the treatment of acute uncomplicated influenza. Drugs Today. 2019;55(6):359-66.

Hayden FG, Sugaya N, Hirotsu N, Lee N, de Jong MD, Hurt AC, et al. Baloxavir marboxil for uncomplicated influenza in adults and adolescents. N Engl J Med. 2018;379(10):913–23.

Ministry of Public Health (Thailand).Food and Drug Administration. Xofluza tab 20 mg [Internet]. Nonthaburi: FDA; 2019 [cited 2020 Jan 13]. Available from:

https://pertento.fda.moph.go.th/FDA_SEARCH_DRUG/SEARCH_DRUG/pop-up_drug_ex.aspx?Newcode=U1DR1C10126 21504211C (in Thai)

Ministry of Public Health (Thailand). Food and Drug Administration. Xofluza tab 40 mg [Internet]. Nonthaburi: FDA; 2019 [cited 2020 Jan 13]. Available from: https://pertento.fda.moph.go.th/FDA_SEARCH_DRUG/SEARCH_DRUG/pop-up_drug_ex.aspx?Newcode=U1DR1C10 12621504311C (in Thai)

Xofluza® (baloxavir marboxil) tablets [Package Insert]. South San Francisco (CA): Genentech USA; 2019.

Noshi T, Kitano M, Taniguchi K, Yamamoto A, Omoto S, Baba K, et al. In vitro characterization of baloxavir acid, a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit. Antiviral Res. 2018; 160:109-17.

Omoto S, Speranzini V, Hashimoto T, Noshi T, Yamaguchi H, Kawai M, et al. Characterization of influenza virus variants induced by treatment with the endonuclease inhibitor baloxavir marboxil. Sci Rep. 2018;8:9633.

Credille CV, Dick BL, Morrison CN, Stokes RW, Adamek RN, Wu NC, et al. Structure-activity relationships in metal-binding pharmacophores for influenza endonuclease.J Med Chem. 2018;61:10206-17.

Poovorawan Y. What you should know about influenza in Thailand [Internet]. Bangkok: Wongkarnpat; 2019 [cited 2020 Mar 14]. Available from: https://www.wongkarnpat. com/upfilecme/CME-Influenza.pdf (in Thai)

Krol E, Rychlowska M, Szewczyk B. Antivirals--current trends in fighting influenza. Acta Biochim Pol. 2014;61(3):495-504.

Chamni S. Influenza virus and current anti-influenza drugs. Thai Sci Technol J 2014;22(2):258-71. (in Thai)

Hirotsu N, Sakaguchi H, Sato C, Ishibashi T, Baba K, Omoto S, et al. Baloxavir marboxil in Japanese pediatric patients with influenza: safety and clinical and virologic outcomes. Clin Infect Dis [Internet]. 2019 [cited 2020 Jan 14];ciz908. Available from: https://academic.oup.com/cid/ advance-article/doi/10. 1093/ cid/ciz908/5571979

Koshimichi H, Ishibashi T, Wajima T. Population pharmacokinetics of baloxavir marboxil in Japanese pediatric influenza patients. J Pharm Sci. 2019;108:3112-7.

Kakuya F, Haga S, Okubo H, Fujiyasu H, Kinebuchi T. Effectiveness of baloxavir marboxil against influenza in children. Pediatr Int. 2019;61:616-8.

Shah S, McManus D, Bejou N, Tirmizi S, Rouse G, Lemieux S, et al. 2645. Clinical outcomes of oseltamivir vs. baloxavir in patients hospitalized with influenza A. Open Forum Infect Dis. 2019;6 Suppl 2:S925.

Ison MG, Portsmouth S, Yoshida Y, Shishido T, Hayden F, Uehara T. LB16. Phase 3 trial of baloxavir marboxil in high-risk influenza patients (CAPSTONE-2 Study). Open Forum Infect Dis. 2018;5 Suppl 1:S764-5.

Taieb V, Ikeoka H, Ma FF, Borkowska K, Aballéa S, Tone K, et al. A network meta-analysis of the efficacy and safety of baloxavir marboxil versus neuraminidase inhibitors for the treatment of influenza in otherwise healthy patients. Curr Med Res Opin. 2019;35:1355-64.

Ministry of Health, Labour and Welfare (Japan). Pharmaceutical Safety and Environmental Health Bureau. Report on the deliberation results [Internet]. Tokyo: The Bureau; 2018 [cited 2019 Aug 29]. Available from: https://www.pmda.go.jp/files/000225380.pdf

Downloads

Published

2020-05-15

How to Cite

Piyananjaruhsri , R. . (2020). BALOXAVIR: ANTI-INFLUENZA VIRUS AGENT VIA INHIBITION OF CAP-DEPENDENT ENDRONUCLEASE. Thai Bulletin of Pharmaceutical Sciences, 15(1), 91–108. https://doi.org/10.69598/tbps.15.1.91-108

Issue

Section

Review Articles