Computational screening of dual inhibitors from FDA approved antiviral drugs on SARS-CoV-2 spike protein and the main protease using molecular docking approach
Acta Virol. 2021;65(2):160-172. doi: 10.4149/av_2021_208.ABSTRACTThe deadly disease-causing novel coronavirus has recently swept across the world and endangered many human lives. Although, various research on therapeutic measures to solve this pandemic crisis has been published; no favourable results have been achieved. We propose the use of potential FDA-approved dual inhibitors which can inhibit two targets (either on entry-level or the main protease) for the effective treatment of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). We screened 12 FDA-approved antiviral inhibitors listed in Drug bank and analys...
Source: Acta Virologica - June 16, 2021 Category: Infectious Diseases Authors: Shanthi Sabarimurugan Indu Purushothaman Rajarajan Swaminathan Arun Dharmarajan Sudha Warrier Sangeetha Kothandan Source Type: research
An influenza A(H5N8) virus isolated during an outbreak at a poultry farm in Russia in 2017 has an N294S substitution in the neuraminidase and shows reduced susceptibility to oseltamivir
This study aimed to assess the antiviral susceptibility of influenza A(H5N8) viruses isolated in Russia in 2014-2018. Genetic analysis of 57 Russian isolates with full genome sequences did not find any markers of reduced susceptibility to baloxavir. Only one strain bore an amino acid substitution associated with adamantane resistance (M2-S31N). The neuraminidase of 1 strain had an NA-N293/294S (N8/N2 numbering) substitution associated with reduced inhibition by oseltamivir and normal inhibition by zanamivir, which was confirmed phenotypically. There were no other strains with reduced inhibition by oseltamivir and zanamivir...
Source: Antiviral Research - May 2, 2021 Category: Virology Authors: Svetlana V Svyatchenko Natalia I Goncharova Vasiliy Y Marchenko Natalia P Kolosova Alexander N Shvalov Valentina L Kovrizhkina Alexander G Durymanov Galina S Onkhonova Tatyana V Tregubchak Ivan M Susloparov Andrey S Gudymo Tatyana N Ilyicheva Alexander B Source Type: research
An influenza A(H5N8) virus isolated during an outbreak at a poultry farm in Russia in 2017 has an N294S substitution in the neuraminidase and shows reduced susceptibility to oseltamivir
This study aimed to assess the antiviral susceptibility of influenza A(H5N8) viruses isolated in Russia in 2014-2018. Genetic analysis of 57 Russian isolates with full genome sequences did not find any markers of reduced susceptibility to baloxavir. Only one strain bore an amino acid substitution associated with adamantane resistance (M2-S31N). The neuraminidase of 1 strain had an NA-N293/294S (N8/N2 numbering) substitution associated with reduced inhibition by oseltamivir and normal inhibition by zanamivir, which was confirmed phenotypically. There were no other strains with reduced inhibition by oseltamivir and zanamivir...
Source: Antiviral Research - May 2, 2021 Category: Virology Authors: Svetlana V Svyatchenko Natalia I Goncharova Vasiliy Y Marchenko Natalia P Kolosova Alexander N Shvalov Valentina L Kovrizhkina Alexander G Durymanov Galina S Onkhonova Tatyana V Tregubchak Ivan M Susloparov Andrey S Gudymo Tatyana N Ilyicheva Alexander B Source Type: research
[PERSPECTIVES] Influenza Therapeutics in Clinical Practice--Challenges and Recent Advances
In the last few years, several new direct-acting influenza antivirals have been licensed, and others have advanced in clinical development. The increasing diversity of antiviral classes should allow an adequate public health response should a resistant virus to one agent or class widely circulate. One new antiviral, baloxavir marboxil, has been approved in the United States for treatment of influenza in those at high risk of developing influenza-related complications. Except for intravenous zanamivir in European Union countries, no antivirals have been licensed specifically for the indication of severe influenza or hospita...
Source: Cold Spring Harbor perspectives in medicine - April 1, 2021 Category: Research Authors: Beigel, J. H., Hayden, F. G. Tags: Influenza: The Cutting Edge PERSPECTIVES Source Type: research
Drug-induced neuropsychiatric adverse events using post-marketing surveillance
CONCLUSION: Our results should raise physicians' awareness of drugs associated with abnormal behavior, but further investigation of these medications is warranted.PMID:33588740 | DOI:10.2174/1574884716666210215104540 (Source: Current Clinical Pharmacology)
Source: Current Clinical Pharmacology - February 16, 2021 Category: Drugs & Pharmacology Authors: Tomohito Wakabayashi Takahiro Nakatsuji Hiroko Kambara Iku Niinomi Saki Oyama Ayaka Inada Sayaka Ueno Mayako Uchida Kazunori Iwanaga Tatsuya Iida Keiko Hosohata Source Type: research
Drug-induced neuropsychiatric adverse events using post-marketing surveillance
CONCLUSION: Our results should raise physicians' awareness of drugs associated with abnormal behavior, but further investigation of these medications is warranted.PMID:33588740 | DOI:10.2174/1574884716666210215104540 (Source: Current Clinical Pharmacology)
Source: Current Clinical Pharmacology - February 16, 2021 Category: Drugs & Pharmacology Authors: Tomohito Wakabayashi Takahiro Nakatsuji Hiroko Kambara Iku Niinomi Saki Oyama Ayaka Inada Sayaka Ueno Mayako Uchida Kazunori Iwanaga Tatsuya Iida Keiko Hosohata Source Type: research
Drug-induced neuropsychiatric adverse events using post-marketing surveillance.
CONCLUSION: Our results should raise physicians' awareness of drugs associated with abnormal behavior, but further investigation of these medications is warranted.
PMID: 33588740 [PubMed - as supplied by publisher] (Source: Current Clinical Pharmacology)
Source: Current Clinical Pharmacology - February 14, 2021 Category: Drugs & Pharmacology Authors: Wakabayashi T, Nakatsuji T, Kambara H, Niinomi I, Oyama S, Inada A, Ueno S, Uchida M, Iwanaga K, Iida T, Hosohata K Tags: Curr Clin Pharmacol Source Type: research
Neuraminidase inhibitors are effective and safe in reducing influenza complications: meta-analysis of randomized controlled trials.
CONCLUSIONS: NAIs are effective in reducing time to clinical resolution, total influenza-related complications, otitis media, and need of antibiotic administration. Reductions on mortality, pneumonia, asthma exacerbations or hospitalization rates only did demonstrate a trend benefit in favor of NAIs. The only significant AE is the increased occurrence of nausea and vomiting.
PMID: 33358065 [PubMed - as supplied by publisher] (Source: European Journal of Internal Medicine)
Source: European Journal of Internal Medicine - December 21, 2020 Category: Internal Medicine Authors: Tejada S, Jansson M, Solé-Lleonart C, Rello J Tags: Eur J Intern Med Source Type: research
Baloxavir (Xofluza) for Post-Exposure Prophylaxis of Influenza
Date: January 11, 2021
Issue #:
1615Summary:
The oral polymerase acidic endonuclease inhibitor
baloxavir marboxil (Xofluza— Genentech) is now FDAapproved
for post-exposure prophylaxis of influenza
in patients ≥12 years old. Baloxavir was approved for
treatment of acute uncomplicated influenza in patients
≥12 years old in 2018.1 Two neuraminidase inhibitors
are FDA-approved for prophylaxis of influenza:
oseltamivi r(Tamiflu, and generics) in patients ≥1 year
old, and zanamivir(Relenza) in patients ≥5 years old.2
Unlike oseltamivir and zanamivir, baloxavir is not FDA-appr...
Source: The Medical Letter - December 18, 2020 Category: Drugs & Pharmacology Authors: admin Tags: baloxavir influenza Oseltamivir Relenza Tamiflu Xofluza Zanamivir Source Type: research
A Comparison of the Frequency of Prescription and Pharmacy Revisits between Baloxavir Marboxil and Neuraminidase Inhibitors in Influenza-Infected Pediatric Patients during the 2019-2020 Influenza Season.
In this study, we investigated the frequency of prescription and pharmacy revisits for baloxavir marboxil at an outpatient clinic compared with that of neuraminidase inhibitors in pediatric patients with influenza. A total of 475 pediatric patients who were infected with the influenza virus visited the pharmacy between December 2019 and March 2020. Baloxavir marboxil (n = 149), oseltamivir (n = 161) and laninamivir (n = 162) were mainly prescribed and only a few patients were treated with peramivir (n = 2) or zanamivir (n = 1). Baloxavir marboxil-, oseltamivir- and laninamivir-treated pediatric patients...
Source: Biological and Pharmaceutical Bulletin - December 4, 2020 Category: Drugs & Pharmacology Authors: Norikoshi Y, Ikeda T, Sasahara K, Hamada M, Torigoe E, Nagae M, Tashiro T, Horio F, Saruwatari J, Uchida Y, Anraku M Tags: Biol Pharm Bull Source Type: research
Efficacy of oseltamivir compared with zanamivir in COPD patients with seasonal influenza virus infection: a randomized controlled trial.
Abstract
Influenza viruses exacerbate chronic obstructive pulmonary disease (COPD) with considerable morbidity and mortality. Zanamivir and oseltamivir are effective in treating influenza. However, their efficacy in relieving influenza symptoms in COPD patients remains unknown, with the lack of controlled trials in this subject. Therefore, we conducted this randomized controlled trial to investigate the clinical efficacy of both interventions in this population. Patients were allocated to two groups (80 patients each): oseltamivir (OSELTA) and zanamivir (ZANA) groups. Oseltamivir (75 mg) was orally adminis...
Source: Braz J Med Biol Res - December 3, 2020 Category: Research Authors: Li M, Han GC, Chen Y, Du WX, Liu F, Chi YM, Du JF Tags: Braz J Med Biol Res Source Type: research
Efficacy of a cap-dependent endonuclease inhibitor and neuraminidase inhibitors against H7N9 highly pathogenic avian influenza virus causing severe viral pneumonia in cynomolgus macaques.
Abstract
H7N9 highly pathogenic avian influenza virus (HPAIV) infection in a human was first reported in 2017. A/duck/Japan/AQ-HE29-22/2017 (H7N9) (Dk/HE29-22) found in imported duck meat at an airport in Japan possessed hemagglutinin with a multi-basic cleavage site, indicating high pathogenicity in chickens as in the case of other H7 HPAIVs. In the present study, we examined the pathogenicity of Dk/HE29-22 and the effectiveness of a cap-dependent endonuclease inhibitor (baloxavir) and neuraminidase inhibitors (oseltamivir and zanamivir) against infection with this strain in a macaque model (n = 3 for eac...
Source: Antimicrobial Agents and Chemotherapy - November 30, 2020 Category: Microbiology Authors: Suzuki S, Nguyen CT, Ogata-Nakahara A, Shibata A, Osaka H, Ishigaki H, Okamatsu M, Sakoda Y, Kida H, Ogasawara K, Itoh Y Tags: Antimicrob Agents Chemother Source Type: research
Role of zanamivir is likely to end in Okinawa, Japan
Publication date: Available online 26 November 2020Source: Respiratory InvestigationAuthor(s): Satoko Sunagawa, Yoshikazu Iha, Takeshi Kinjo, Katsunori Nakamura, Jiro Fujita (Source: Respiratory Investigation)
Source: Respiratory Investigation - November 27, 2020 Category: Respiratory Medicine Source Type: research
Integrating molecular modelling methods to advance influenza A virus drug discovery.
Abstract
Since the discovery of the anti-influenza drugs oseltamivir and zanamivir using computer-aided drug design methods, there have been significant applications of molecular modelling methodologies applied to influenza A virus drug discovery, such as molecular dynamics (MD) simulation, molecular docking, and virtual screening (VS). In this review, we provide a brief general introduction to molecular modelling in the context of drug discovery and then focus on the advances and impact of integrating these methods with specific reference to potential influenza A antiviral drug targets. Teaser: Molecular ...
Source: Drug Discovery Today - November 18, 2020 Category: Drugs & Pharmacology Authors: Patel H, Kukol A Tags: Drug Discov Today Source Type: research
Efficacy and safety of baloxavir marboxil versus neuraminidase inhibitors in the treatment of influenza virus infection in high-risk and uncomplicated patients - a Bayesian network meta-analysis.
CONCLUSIONS: Baloxavir was significantly more effective than placebo regarding all outcomes except for the risk of pneumonia. Besides, baloxavir was associated with similar clinical efficacy and safety, and superior antiviral activity compared to other antivirals in HR patients, as well as in the entire population of uncomplicated patients with influenza.
PMID: 33079575 [PubMed - as supplied by publisher] (Source: Current Medical Research and Opinion)
Source: Current Medical Research and Opinion - October 22, 2020 Category: Research Tags: Curr Med Res Opin Source Type: research
