Page last updated: 2024-11-06

zanamivir

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Description

Zanamivir is a neuraminidase inhibitor that is used to treat influenza A and B infections. It was first synthesized in the early 1990s and is a highly potent antiviral agent that works by preventing the release of new virus particles from infected cells. Zanamivir is available as an inhaled powder and is typically administered twice daily for 5 days. It is well tolerated and has a favorable safety profile. Zanamivir is effective in reducing the duration of influenza symptoms and preventing complications, such as pneumonia. It is particularly important for individuals at high risk of influenza complications, such as the elderly, young children, and those with underlying medical conditions. Zanamivir is studied extensively to understand its antiviral mechanism, optimize its use, and explore its potential in combination therapies. Research also investigates its efficacy against emerging influenza strains and its potential for use in pandemic preparedness.'

Zanamivir: A guanido-neuraminic acid that is used to inhibit NEURAMINIDASE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60855
CHEMBL ID222813
CHEBI ID50663
SCHEMBL ID9501
MeSH IDM0217195

Synonyms (123)

Synonym
BIDD:GT0349
bdbm4934
(2r,3r,4s)-4-carbamimidamido-3-acetamido-2-[(1r,2r)-1,2,3-trihydroxypropyl]-3,4-dihydro-2h-pyran-6-carboxylic acid
HY-13210
CHEMBL222813 ,
gr-121167
AKOS015841013
gr-121167x
gg-167
4-guanidino-neu5ac2en
5-(acetylamino)-4-{[amino(imino)methyl]amino}-2,6-anhydro-3,4,5-trideoxy-d-glycero-d-galacto-non-2-enonic acid
GNA ,
zmr ,
C08095
zanamivir
139110-80-8
gr121167x
gg167
4-guanidino-neueac2en
5-acetamido-2,6-anhydro-3,4,5-trideoxy-4-guanidino-d-glycero-d-galacto-non-2-enonic acid
relenza
(2r,3r,4s)-3-acetamido-4-guanidino-2-[(1r,2r)-1,2,3-trihydroxypropyl]-3,4-dihydro-2h-pyran-6-carboxylic acid
zanamavir
1A4G
4-guanidino-2,4-dideoxy-2,3-dehydro-n-acetylneuraminic acid
DB00558
5-(acetylamino)-2,6-anhydro-4-carbamimidamido-3,4,5-trideoxy-d-glycero-d-galacto-non-2-enonic acid
gana
(2r,3r,4s)-3-(acetylamino)-4-carbamimidamido-2-[(1r,2r)-1,2,3-trihydroxypropyl]-3,4-dihydro-2h-pyran-6-carboxylic acid
2QWE
zanamivir (usp/inn)
relenza (tn)
D00902
NCGC00164561-01
hsdb 7437
gr 121167x
5-acetylamino-2,6-anhydro-4-guanidino-3,4,5-trideoxy-d-galacto-non-enoic acid
gana (inhibitor)
d-glycero-d-galacto-non-2-enonic acid, 5-(acetylamino)-4-(aminoiminomethyl)amino)-2,6-anhydro-3,4,5-trideoxy-
2,3-didehydro-2,4-dideoxy-4-guanidino-n-acetyl-d-neuraminic acid
4-guanidino-2,4-dideoxy-2,3-didehydro-n-acetylneuraminic acid
zanamivir [usan:inn:ban]
2,3-didehydro-2,4-dideoxy-4-guanidinyl-n-acetylneuraminic acid
4-guanidino-2-deoxy-2,3-didehydro-n-acetylneuraminic acid
gg 167
CHEBI:50663 ,
5-acetamido-2,6-anhydro-4-carbamimidamido-3,4,5-trideoxy-d-glycero-d-galacto-non-2-enonic acid
(2r,3r,4s)-3-acetamido-4-(diaminomethylideneamino)-2-[(1r,2r)-1,2,3-trihydroxypropyl]-3,4-dihydro-2h-pyran-6-carboxylic acid
(2r,3r,4s)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1r,2r)-1,2,3-trihydroxypropyl]-3,4-dihydro-2h-pyran-6-carboxylic acid hydrate
A807485
bdbm50330326
(4s,5r,6r)-5-acetylamino-4-guanidino-6-((1r,3r)-1,2,3-trihydroxy-propyl)-5,6-dihydro-4h-pyran-2-carboxylic acid
(4s,5r,6r)-5-acetylamino-4-guanidino-6-((1r,2r)-1,2,3-trihydroxy-propy)-5,6-dihydro-4h-pyran-2-carboxylic acid
(4s,5r,6r)-5-acetamido-4-(diaminomethyleneamino)-6-((1r,2r)-1,2,3-trihydroxypropyl)-5,6-dihydro-4h-pyran-2-carboxylic acid
(4s,5r,6r)-5-acetylamino-4-guanidino-6-((1r,2r)-1,2,3-trihydroxy-propyl)-5,6-dihydro-4h-pyran-2-carboxylic acid
4-diaminomethylamino-3-methylcarboxamido-2-(1,2,3-trihydroxypropyl)-(3r)-3,4-dihydro-2h-6-pyrancarboxylic acid(zanamivir)
5-acetylamino-4-guanidino-6-(1,2,3-trihydroxy-propyl)-5,6-dihydro-4h-pyran-2-carboxylic acid(zanamivir)
(4s,5r,6r)-5-acetylamino-4-guanidino-6-((r)-1,2,3-trihydroxy-propyl)-5,6-dihydro-4h-pyran-2-carboxylic acid
(4s,5r,6r)-5-acetylamino-4-guanidino-6-(1,2,3-trihydroxy-propyl)-5,6-dihydro-4h-pyran-2-carboxylic acid
zanamivi
5-acetylamino-4-guanidino-6-(1,2,3-trihydroxy-propyl)-5,6-dihydro-4h-pyran-2-carboxylic acid
5-formylamino-4-guanidino-6-(1,2,3-trihydroxy-propyl)-5,6-dihydro-4h-pyran-2-carboxylic acid
dtxcid503749
tox21_112190
cas-139110-80-8
dtxsid0023749 ,
AKOS015994539
unii-l6o3xi777i
l6o3xi777i ,
d-glycero-d-galacto-non-2-enonic acid, 5-(acetylamino)-4-((aminoiminomethyl)amino)-2,6-anhydro-3,4,5-trideoxy-
zanamivir [mart.]
zanamivir [hsdb]
zanamivir [inn]
zanamivir [who-dd]
zanamivir [mi]
zanamivir [orange book]
zanamivir [usp monograph]
zanamivir [vandf]
zanamivir [usp-rs]
zanamivir [usan]
CS-0631
S3007
Z0023
551942-41-7
SCHEMBL9501
NCGC00164561-02
tox21_112190_1
BS-1017
5-acetylamino-4-guanidino-6-(1,2,3-trihydroxypropyl)-5,6-dihydro-4h-pyran-2-carboxylic acid
4 guanidino 2 deoxy 2,3 didehydro n acetylneuraminic acid
acid, 4-guanidino-2-deoxy-2,3-didehydro-n-acetylneuraminic
4 guanidino neu5ac2en
Q-201942
(2r,3r,4s)-3-acetamido-4-((diaminomethylene)amino)-2-((1r,2r)-1,2,3-trihydroxypropyl)-3,4-dihydro-2h-pyran-6-carboxylic acid
AB01566897_01
mfcd00866966
(2r,3r,4s)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1r,2r)-1,2,3-trihydroxypropyl]-3,4-dihydro-2h-pyran-6-carboxylic acid
zanamivir, united states pharmacopeia (usp) reference standard
zanamivir, >=98% (hplc)
zanamivir for assay, europepharmacopoeia (ep) reference standard
zanamivir for system suitability, european pharmacopoeia (ep) reference standard
139110-80-8 (free base)
zanamivirhydrate
zanamivir (relenza)
(2r,3r,4s)-3-acetamido-4-guanidino-2-((1r,2r)-1,2,3-trihydroxypropyl)-3,4-dihydro-2h-pyran-6-carboxylic acid
Q146075
d-glycero-d-galacto-non-2-enonic acid, 5-(acetylamino)-4-[(aminoiminomethyl)amino]-2,6-anhydro-3,4,5-trideoxy-
NCGC00164561-08
CCG-267828
C72554
NCGC00164561-11
dectova
gtpl12307
EN300-26991905
(2r,3r,4s)-3-(acetylamino)-4-{[amino(imino)methyl]amino}-2-[(1r,2r)-1,2,3-trihydroxypropyl]-3,4-dihydro-2h-pyran-6-carboxylic acid
j05ah01
zanamivir (usp-rs)
zanamivir (usp monograph)
5-acetamido-4-guanidino-2,3,4,5-tetradeoxy-d-glycero-d-galacto-non-2-enopyranosonic acid
(2r,3r,4s)-3-(acetylamino)-4-carbamimidamido-2-((1r,2r)-1,2,3-trihydroxypropyl)-3,4-dihydro-2h-pyran-6-carboxylic acid
zanamivirum
zanamivir (mart.)
5-(acetylamino)-4-

Research Excerpts

Overview

Zanamivir (ZA) is a potent anti-influenza drug, but it cannot be administrated orally because of the hydrophilic carboxylate and guanidinium groups. It is a neuraminidase inhibitor effective against influenza A and B viruses.

ExcerptReferenceRelevance
"Zanamivir (ZA) is a potent anti-influenza drug, but it cannot be administrated orally because of the hydrophilic carboxylate and guanidinium groups. "( Intramolecular ion-pair prodrugs of zanamivir and guanidino-oseltamivir.
Cheng, YS; Fang, JM; Lee, PS; Liu, KC; Wang, SY; Wong, CH, 2011
)
2.09
"Zanamivir is a neuraminidase inhibitor effective against influenza A and B viruses. "( Zanamivir aqueous solution in severe influenza: A global Compassionate Use Program, 2009-2019.
Jayabalan, T; Joshi, A; Miller, I; Oliver, A; Peppercorn, A; Wang-Jairaj, J; Zammit-Tabona, P, 2022
)
3.61
"Zanamivir is a potent and highly selective inhibitor of influenza neuraminidase in which the inhibition of this enzyme prevents the virus from infecting other cells and specifically prevents release of the new virion from the host cell membrane. "( Population Pharmacokinetic/Pharmacodynamic Analysis of Intravenous Zanamivir in Healthy Adults and Hospitalized Adult and Pediatric Subjects With Influenza.
Barth, A; Collins, J; Hossain, M; Okour, M; Peppercorn, A; Roberts, G; Shortino, D; Watson, HA; Yates, P; Zuo, P, 2020
)
2.24
"Zanamivir is a neuraminidase (NA) inhibitor used for the treatment of influenza. "( Evaluation of safety and efficacy of intravenous zanamivir in the treatment of hospitalized Japanese patients with influenza: an open-label, single-arm study.
Furukawa, H; Murayama, M; Soutome, T; Watanabe, A; Yates, PJ, 2015
)
2.11
"Zanamivir (Za) is a highly polar and hydrophilic antiviral drug used for the treatment of influenza A viruses. "( Online solid phase extraction liquid chromatography using bonded zwitterionic stationary phases and tandem mass spectrometry for rapid environmental trace analysis of highly polar hydrophilic compounds - Application for the antiviral drug Zanamivir.
Appelblad, P; Blum, KM; Fedorova, G; Gillman, A; Järhult, J; Lindberg, RH; Pulit-Prociak, J; Söderström, H, 2015
)
2.04
"Zanamivir is a potent inhibitor of H5N1, attains high lung concentrations immediately on administration, distributes into plasma at antiviral concentrations, has a low propensity for generating resistant virus, and retains activity against H275Y oseltamivir-resistant virus."( Treatment options for H5N1: lessons learned from the H1N1 pandemic.
Reece, PA, 2010
)
1.08
"Zanamivir is a potent competitive inhibitor of the neuraminidase glycoprotein, which is essential in the infective cycle of influenza A and B viruses. "( Spotlight on zanamivir in influenza.
Cheer, SM; Wagstaff, AJ, 2002
)
2.13
"Zanamivir is an appropriate alternative for influenza outbreak control among institutionalized vaccinated elderly."( Inhaled zanamivir versus rimantadine for the control of influenza in a highly vaccinated long-term care population.
Ambrozaitis, A; Binder, E; Daly, J; Drinka, P; Elliott, M; Flack, N; Gravenstein, S; Hammond, J; Kandel, R; Keene, O; Krause, P; McElhaney, J; Osterweil, D; Schilling, M; Shult, P,
)
1.29
"Zanamivir is a novel antiviral agent developed for the treatment and prevention of influenza when administered by the oral inhaled route."( Preclinical development of low toxicity drugs: focus on zanamivir, an anti-influenza drug.
Bethell, R; Daniel, M; Dines, GD, 1998
)
1.27
"Zanamivir is a potent inhibitor of influenza A and B virus neuraminidases and is active topically in experimental and natural human influenza. "( Safety and efficacy of intravenous zanamivir in preventing experimental human influenza A virus infection.
Calfee, DP; Cass, LM; Hayden, FG; Lobo, M; Peng, AW, 1999
)
2.02
"Zanamivir is a well tolerated drug. "( Pharmacokinetics of zanamivir after intravenous, oral, inhaled or intranasal administration to healthy volunteers.
Bye, A; Cass, LM; Efthymiopoulos, C, 1999
)
2.07
"Zanamivir is a novel inhibitor of the enzyme neuraminidase, a surface glycoprotein essential for the replication of type A and B influenza viruses. "( Zanamivir: a review of its use in influenza.
Dunn, CJ; Goa, KL, 1999
)
3.19
"Zanamivir is a highly selective neuraminidase (NA) inhibitor with demonstrated clinical efficacy against influenza A and B virus infections. "( Zanamivir susceptibility monitoring and characterization of influenza virus clinical isolates obtained during phase II clinical efficacy studies.
Barnett, JM; Cadman, A; Candlin, A; Claas, EC; De Groot, R; Dempsey, M; Fenton, RJ; Gor, D; Lewis, AP; Morley, PJ; Osterhaus, AD; Owens, IJ; Rimmelzwaan, GF; Tisdale, M; Walters, M, 2000
)
3.19
"Zanamivir is a potent and specific inhibitor of influenza A and B virus neuraminidase, that is now approved for the treatment, and is currently under development for the prophylaxis of influenza. "( Pulmonary function and airway responsiveness in mild to moderate asthmatics given repeated inhaled doses of zanamivir.
Bye, A; Cass, LM; Gunawardena, KA; Macmahon, MM, 2000
)
1.96
"Zanamivir is a minimal modification of the natural ligand (Neu5Ac) of the enzyme."( A novel approach to antiviral therapy for influenza.
Colman, PM, 1999
)
1.02
"Zanamivir is a neuraminidase inhibitor, the first of a new class of drugs with potent, specific antiviral activity against influenza A and B. "( Effect of zanamivir on duration and resolution of influenza symptoms.
Monto, AS; Moult, AB; Sharp, SJ, 2000
)
2.15
"Zanamivir is a potent competitive inhibitor of the neuraminidase glycoprotein, which is essential in the infective cycle of influenza A and B viruses. "( Zanamivir: an update of its use in influenza.
Cheer, SM; Wagstaff, AJ, 2002
)
3.2

Effects

Zanamivir has been shown to inhibit both human and avian influenza viral neuraminidases (NAs) It is approved in several countries for the treatment and prophylaxis of influenza infection.

ExcerptReferenceRelevance
"Zanamivir has not been shown to reduce the incidence of influenza complications, whether used as prevention or cure. "( Zanamivir: new indication. Influenza: in children as in adults, symptom relief or vaccination.
, 2008
)
3.23
"Zanamivir has been shown to inhibit both human and avian influenza viral neuraminidases (NAs) and has been approved in several countries for the treatment and prophylaxis of influenza infection. "( Assaying susceptibility of avian and other influenza A viruses to zanamivir: comparison of fluorescent and chemiluminescent neuraminidase assays.
Klimov, A; Mungall, BA; Xu, X, 2003
)
2
"Zanamivir has similar performance."( Neuraminidase inhibitors for preventing and treating influenza in healthy adults.
Demicheli, V; Di Pietrantonj, C; Jefferson, TO; Jones, M; Rivetti, D, 2006
)
1.06
"Zanamivir treatment has been shown to reduce the severity and duration of naturally occurring, uncomplicated influenza illness in adults."( New approaches to influenza chemotherapy. Neuraminidase inhibitors.
Calfee, DP; Hayden, FG, 1998
)
1.02

Treatment

Zanamivir treatment within 24 and 24 - 48 h of illness onset in index cases reduced the risk of household transmission to 0.57 (95% CI 0.44, 0.73) and 0.58 ( 95%CI 0.38,0.86) times that among those receiving the same treatment at > 48 h.

ExcerptReferenceRelevance
"Zanamivir treatment within 24 and 24 - 48 h of illness onset in index cases, respectively, reduced the risk of household transmission to 0.57 (95% CI 0.44, 0.73) and 0.58 (95% CI 0.38, 0.86) times that among those receiving the same treatment at > 48 h and those not receiving treatment."( Household transmission of influenza (H1N1-2009) in Japan: age-specificity and reduction of household transmission risk by zanamivir treatment.
Nishiura, H; Oshitani, H, 2011
)
1.3
"Zanamivir-treated patients had an excess of outpatient visits (16.9% vs 14.5%; RR, 1.16; 95% CI, 1.02-1.33) and antibiotic use (16.3% vs 14.8%; RR, 1.10; 95% CI, 0.97-1.26), although the RRs were modest."( The effect of zanamivir treatment on influenza complications: a retrospective cohort study.
Ajene, AN; Cole, JA; Cook, SE; Loughlin, JE; Rosenberg, DM; Walker, AM, 2002
)
1.4
"Zanamivir treatment has been shown to reduce the severity and duration of naturally occurring, uncomplicated influenza illness in adults."( New approaches to influenza chemotherapy. Neuraminidase inhibitors.
Calfee, DP; Hayden, FG, 1998
)
1.02
"Zanamivir-treated patients returned to normal activities significantly faster and took significantly fewer relief medications than placebo-treated patients."( Zanamivir for treatment of symptomatic influenza A and B infection in children five to twelve years of age: a randomized controlled trial.
Barzilai, A; Behre, U; Hammond, J; Hedrick, JA; Henderson, FW; Keene, O; Reilly, L, 2000
)
2.47
"Zanamivir treatment reduced absenteeism, improved patient productivity and well-being, and reduced the additional use of healthcare resources in patients with influenza."( Impact of zanamivir treatment on productivity, health status and healthcare resource use in patients with influenza. Zanamivir Study Group.
Aoki, FY; Edmundson, S; Fleming, DM; Griffin, AD; Lacey, LA, 2000
)
2.15
"Zanamivir treatment was also associated with a significant reduction in time to alleviation of symptoms with no use of relief medication."( Effect of zanamivir on duration and resolution of influenza symptoms.
Monto, AS; Moult, AB; Sharp, SJ, 2000
)
1.43
"Zanamivir-treated high-risk patients had a treatment benefit of 2.5 days compared with those given placebo (P = .015). "( Zanamivir for the treatment of influenza A and B infection in high-risk patients: a pooled analysis of randomized controlled trials.
Campion, K; Keene, O; Lalezari, J; Silagy, C, 2001
)
3.2
"Treatment with zanamivir prevented the infection and abrogated the local cytokine and chemokine responses."( Nasal cytokine and chemokine responses in experimental influenza A virus infection: results of a placebo-controlled trial of intravenous zanamivir treatment.
Alvord, WG; Calfee, DP; Cass, LM; Fritz, RS; Hayden, FG; Peng, AW; Straus, SE; Strober, W, 1999
)
0.85
"Treatment with zanamivir for this high risk population results in an incremental cost of $A14.20 per day of symptoms avoided in the base case. "( Cost effectiveness of zanamivir for the treatment of influenza in a high risk population in Australia.
Cates, SC; Griffin, AD; Lamb, SC; Mauskopf, JA; Neighbors, DM; Rutherford, C, 2000
)
0.97
"Treatment with zanamivir for this population is cost effective based on an $A78,000 per QALY benchmark."( Cost effectiveness of zanamivir for the treatment of influenza in a high risk population in Australia.
Cates, SC; Griffin, AD; Lamb, SC; Mauskopf, JA; Neighbors, DM; Rutherford, C, 2000
)
0.96

Toxicity

Zanamivir was well tolerated, with an adverse event profile similar to that of placebo. Drowsiness was the most frequent adverse event for both drugs.

ExcerptReferenceRelevance
"The current study evaluated whether intranasal administration of the sialic acid analog 4-guanidino-Neu5Ac2en (GG167), an inhibitor of influenza virus neuraminidase, was effective and safe in either preventing or treating experimental human influenza."( Safety and efficacy of the neuraminidase inhibitor GG167 in experimental human influenza.
Betts, RF; Esinhart, JD; Hayden, FG; Hussey, EK; Lobo, M; Treanor, JJ,
)
0.13
"Direct respiratory administration of the selective neuraminidase inhibitor GG167 appears safe and effective for both prevention and early treatment of experimental influenza."( Safety and efficacy of the neuraminidase inhibitor GG167 in experimental human influenza.
Betts, RF; Esinhart, JD; Hayden, FG; Hussey, EK; Lobo, M; Treanor, JJ,
)
0.13
"In adults with influenza A or B virus infections, direct administration of a selective neuraminidase inhibitor, zanamivir, to the respiratory tract is safe and reduces symptoms if begun early."( Efficacy and safety of the neuraminidase inhibitor zanamivir in the treatment of influenzavirus infections. GG167 Influenza Study Group.
Aoki, FY; Bohnen, AM; Fleming, DM; Hayden, FG; Hirst, HM; Keene, O; Nicholson, KG; Osterhaus, AD; Treanor, JJ; Wightman, K, 1997
)
0.76
" Systemic plasma concentrations 1336-fold those achieved in clinical use were not associated with significant adverse effects."( Preclinical development of low toxicity drugs: focus on zanamivir, an anti-influenza drug.
Bethell, R; Daniel, M; Dines, GD, 1998
)
0.55
" The adverse event profiles were similar for zanamivir and placebo."( Randomised trial of efficacy and safety of inhaled zanamivir in treatment of influenza A and B virus infections. The MIST (Management of Influenza in the Southern Hemisphere Trialists) Study Group.
, 1998
)
0.81
" Serious adverse events from an ongoing Japanese clinical programme are also reported."( Zanamivir: a review of clinical safety.
Elliott, M; Freund, B; Gravenstein, S; Miller, I, 1999
)
1.75
" Zanamivir was well tolerated, with an adverse event profile similar to that of placebo."( Clinical efficacy and safety of the orally inhaled neuraminidase inhibitor zanamivir in the treatment of influenza: a randomized, double-blind, placebo-controlled European study.
Fleming, DM; Keene, ON; Mäkelä, MJ; Man, CY; Pauksens, K; Rostila, T; Webster, A, 2000
)
1.45
" The incidence and pattern of adverse events was similar in zanamivir and placebo recipients."( Zanamivir: a review of clinical safety in individuals at high risk of developing influenza-related complications.
Gravenstein, S; Johnston, SL; Loeschel, E; Webster, A, 2001
)
2
" However, the data presented are somewhat limited by the paucity of good quality adverse event data available."( Safety of neuraminidase inhibitors for influenza.
Del Mar, C; Jones, M, 2006
)
0.33
" All adverse events (AEs) occurring after the first dose of study medication were recorded."( Efficacy and safety of inhaled zanamivir in the prevention of influenza in community-dwelling, high-risk adult and adolescent subjects: a 28-day, multicenter, randomized, double-blind, placebo-controlled trial.
Bettis, R; Hampel, FC; Harris, J; Henderson, FW; Kudule, L; LaForce, C; Man, CY; McElhaney, JE; Tisdale, M; Webster, A; Yates, P, 2007
)
0.63
"Randomized, placebo-controlled, double-blind human trials of extended-duration NAI chemoprophylaxis that reported outcomes of laboratory-confirmed influenza or adverse events."( Systematic review: safety and efficacy of extended-duration antiviral chemoprophylaxis against pandemic and seasonal influenza.
Bravata, DM; Gould, MK; Holty, JE; Khazeni, N; Stave, CD; Uyeki, TM, 2009
)
0.35
" No study was powered to detect rare adverse events, and none included diverse racial groups, children, immunocompromised patients, or individuals who received live attenuated influenza virus vaccine."( Systematic review: safety and efficacy of extended-duration antiviral chemoprophylaxis against pandemic and seasonal influenza.
Bravata, DM; Gould, MK; Holty, JE; Khazeni, N; Stave, CD; Uyeki, TM, 2009
)
0.35
" All the reported adverse events, such as rash, nasal ache, muscle ache, nausea, diarrhea, headache, occurred in less than 1% of subjects."( An uncontrolled open-label, multicenter study to monitor the antiviral activity and safety of inhaled zanamivir (as Rotadisk via Diskhaler device) among Chinese adolescents and adults with influenza-like illness.
Cao, B; Chen, BY; Dong, JP; Gao, Y; Hu, K; Li, XL; Pu, ZH; Shu, YL; Song, SF; Wang, C; Wang, DY; Wang, J; Wei, LQ; Xu, Q; Yu, XM; Yu, YS, 2012
)
0.59
" Drowsiness was the most frequent adverse event for both drugs (38% for the oseltamivir group, and 22% for the zanamivir group)."( Comparison of efficacy and safety of oseltamivir and zanamivir in pandemic influenza treatment.
Karabay, O; Tuna, N; Yahyaoğlu, M,
)
0.59
"Efficacy (in terms of symptom relief and duration to resumption of work) and adverse events were similar for zanamivir and oseltamivir, but temperature normalization was much more rapid in patients using zanamivir."( Comparison of efficacy and safety of oseltamivir and zanamivir in pandemic influenza treatment.
Karabay, O; Tuna, N; Yahyaoğlu, M,
)
0.59
" Adverse events of interest such as abnormal behavior/delirium, dizziness/vertigo, respiratory disorders, shock/syncope, and any other serious events were intensively reviewed by the Safety Evaluation Committee."( Safety evaluation of laninamivir octanoate hydrate through analysis of adverse events reported during early post-marketing phase vigilance.
Eda, H; Fukushima, M; Nakano, T; Niwa, S; Okumura, A; Tanabe, T; Tsutsumi, H; Yonemochi, R, 2013
)
0.39
" A total of 20 adverse events (AEs) were reported (all grade 1) by nine subjects, with no AE reported ≥1× in any treatment group."( Safety, tolerability and pharmacokinetics of orally inhaled zanamivir: a randomized study comparing Rotacap/Rotahaler and Rotadisk/Diskhaler in healthy adults.
Jones, LS; Lou, Y; Ng-Cashin, J; Peppercorn, A; Piscitelli, S; Weller, S, 2013
)
0.63
" Primary outcomes included adverse events (AEs), and clinical/laboratory parameters."( Safety and pharmacokinetics of intravenous zanamivir treatment in hospitalized adults with influenza: an open-label, multicenter, single-arm, phase II study.
Alvarez-Lerma, F; Brealey, D; Francois, B; Garot, D; Lorente, JA; Man, CY; Mánez, R; Marty, FM; Peppercorn, AF; Thamlikitkul, V; van der Horst, C; Weller, S; Yates, PJ; Zhao, HH, 2014
)
0.67
" Overall adverse events (AEs) and serious adverse events (SAEs) were reported in 13 (62%) and 4 (19%) subjects, respectively."( Evaluation of safety and efficacy of intravenous zanamivir in the treatment of hospitalized Japanese patients with influenza: an open-label, single-arm study.
Furukawa, H; Murayama, M; Soutome, T; Watanabe, A; Yates, PJ, 2015
)
0.67
" Limited, low-quality data suggest NIs are likely safe in general populations and may be safe in pregnant women and children."( Safety and effectiveness of neuraminidase inhibitors in situations of pandemic and/or novel/variant influenza: a systematic review of the literature, 2009-15.
Boikos, C; Caya, C; Delisle, G; Doll, MK; Dolph, M; Gore, G; Kraicer-Melamed, H; Quach, C; Winters, N, 2017
)
0.46
" Our evidence suggests NIs are likely safe to use in the general population; however, data for children and pregnant women are limited."( Safety and effectiveness of neuraminidase inhibitors in situations of pandemic and/or novel/variant influenza: a systematic review of the literature, 2009-15.
Boikos, C; Caya, C; Delisle, G; Doll, MK; Dolph, M; Gore, G; Kraicer-Melamed, H; Quach, C; Winters, N, 2017
)
0.46
"We undertook a survey to evaluate the compliance and the tolerability of oseltamivir and zanamivir when they were used as post-exposure prophylaxis among the medical staffs in the 2014-2015 seasons to understand a characteristic of adverse events caused by anti-influenza (flu) agents."( Adverse events of prophylactic anti-influenza agents in medical staffs.
Asai, N; Furui, T; Hagihara, M; Kato, H; Kato, Y; Koizumi, Y; Kurumiya, A; Mikamo, H; Nishiyama, N; Sakata, M; Takahashi, T; Yamagishi, Y, 2017
)
0.68
" The adverse events caused by oseltamivir were reported by 86 of 382 medical staffs (22."( Adverse events of prophylactic anti-influenza agents in medical staffs.
Asai, N; Furui, T; Hagihara, M; Kato, H; Kato, Y; Koizumi, Y; Kurumiya, A; Mikamo, H; Nishiyama, N; Sakata, M; Takahashi, T; Yamagishi, Y, 2017
)
0.46
"5% subjects experienced any adverse events due to oseltamivir."( Adverse events of prophylactic anti-influenza agents in medical staffs.
Asai, N; Furui, T; Hagihara, M; Kato, H; Kato, Y; Koizumi, Y; Kurumiya, A; Mikamo, H; Nishiyama, N; Sakata, M; Takahashi, T; Yamagishi, Y, 2017
)
0.46
" We recommend that decisions regarding NI use are made in consideration of potential adverse events, particularly for the general population at low risk of complications."( Safety and effectiveness of neuraminidase inhibitors for influenza treatment, prophylaxis, and outbreak control: a systematic review of systematic reviews and/or meta-analyses.
Boikos, C; Doll, MK; Gore, G; Kraicer-Melamed, H; Quach, C; Winters, N, 2017
)
0.46
"7%) participants in the NTZ and placebo groups, respectively, reported serious adverse events."( Efficacy and Safety of Nitazoxanide in Addition to Standard of Care for the Treatment of Severe Acute Respiratory Illness.
Araujo-Meléndez, J; Beigel, JH; Galindo-Fraga, A; Gamiño-Arroyo, AE; García-Andrade, LA; Guerrero, ML; Holley, HP; Hunsberger, S; Ibarra-González, V; Kapushoc, H; Llamosas-Gallardo, B; Martínez-López, J; McCarthy, S; Moreno-Espinosa, S; Ramírez-Venegas, A; Roldán-Aragón, Y; Ruiz-Palacios, GM; Smolskis, MC, 2019
)
0.51
" The aim of this study was to evaluate age-related clinical manifestations of adverse events (AEs) related to NAIs."( Assessment of adverse events related to anti-influenza neuraminidase inhibitors using the FDA adverse event reporting system and online patient reviews.
Han, N; Kim, IW; Oh, JM, 2020
)
0.56
"We performed a retrospective pharmacovigilance disproportionality analysis using the Japanese Adverse Drug Event Report database."( Drug-induced Neuropsychiatric Adverse Events Using Post-Marketing Surveillance.
Hosohata, K; Iida, T; Inada, A; Iwanaga, K; Kambara, H; Nakatsuji, T; Niinomi, I; Oyama, S; Uchida, M; Ueno, S; Wakabayashi, T, 2022
)
0.72

Pharmacokinetics

The time above the 50% effective concentration (time>EC(50) is the pharmacodynamic (PD) index predicting the inhibition of viral replication by intravenous zanamivir. The study was conducted to evaluate the pharmacokinetic and safety profiles in Japanese subjects.

ExcerptReferenceRelevance
" Serum and urine samples were obtained for determination of pharmacokinetic parameters, and nasal washes and throat gargles were performed to assess drug concentrations in the nose and throat."( Pharmacokinetics of zanamivir after intravenous, oral, inhaled or intranasal administration to healthy volunteers.
Bye, A; Cass, LM; Efthymiopoulos, C, 1999
)
0.63
" The elimination of zanamivir from the serum was a first-order process with a half-life of approximately 2 hours and, at 16 L, the volume of distribution was similar to that of extracellular water."( Pharmacokinetics of zanamivir after intravenous, oral, inhaled or intranasal administration to healthy volunteers.
Bye, A; Cass, LM; Efthymiopoulos, C, 1999
)
0.95
" No significant differences in pharmacokinetic parameters were observed when demographic variables, indices of infection, or concurrent medication use were considered in either phase I or phase II population analyses."( A population pharmacokinetic analysis of zanamivir in subjects with experimental and naturally occurring influenza: effects of formulation and route of administration.
Hussey, EK; Moore, KH; Peng, AW, 2000
)
0.57
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" CS-8958 disappeared from plasma with a half-life of about 2 hours, although laninamivir was slowly eliminated from the body, lasting for even up to 144 hours after administration with a half-life of about 3 days."( Clinical pharmacokinetics of laninamivir, a novel long-acting neuraminidase inhibitor, after single and multiple inhaled doses of its prodrug, CS-8958, in healthy male volunteers.
Ishizuka, H; Okabe, H; Yoshiba, S; Yoshihara, K, 2010
)
0.36
" After intratracheal administration of CS-8958, plasma R-125489 concentration was slowly eliminated, and its half-life (14."( Pharmacokinetics and disposition of CS-8958, a long-acting prodrug of the novel neuraminidase inhibitor laninamivir in rats.
Hoshi, M; Kobayashi, N; Koyama, K; Murai, T; Nakai, N; Okazaki, O; Takahashi, M; Takakusa, H; Yamamura, N, 2010
)
0.36
" The area under the concentration-time curve extrapolated to infinity (AUC(0-inf)), maximum concentration (C(max)), and time to C(max) of CS-8958 did not change with the degree of renal impairment, whereas the half-life (t(1/2)) of CS-8958 increased with increasing renal insufficiency."( Assessment of the effects of renal impairment on the pharmacokinetic profile of laninamivir, a novel neuraminidase inhibitor, after a single inhaled dose of its Prodrug, CS-8958.
Ishizuka, H; Okabe, H; Yoshiba, S; Yoshihara, K, 2011
)
0.37
" In a companion paper, we show that the time above the 50% effective concentration (time>EC(50)) is the pharmacodynamic (PD) index predicting the inhibition of viral replication by intravenous zanamivir."( Effect of half-life on the pharmacodynamic index of zanamivir against influenza virus delineated by a mathematical model.
Adams, JR; Brown, AN; Bulitta, JB; Drusano, GL; Kulawy, R; McSharry, JJ; Weng, Q, 2011
)
0.81
" It is not known if there is any pharmacokinetic interaction between the two drugs."( An open-label crossover study to evaluate potential pharmacokinetic interactions between oral oseltamivir and intravenous zanamivir in healthy Thai adults.
Chueasuwanchai, S; Day, NP; Fukuda, C; Hanpithakpong, W; Jittamala, P; Leowattana, W; Lindegardh, N; Pan-Ngum, W; Panapipat, S; Permpunpanich, S; Phakdeeraj, A; Pukrittayakamee, S; Singhasivanon, P; Stepniewska, K; White, NJ, 2011
)
0.58
" Each zanamivir regimen was administered to six healthy subjects with serial pharmacokinetic sampling."( Zanamivir pharmacokinetics and pulmonary penetration into epithelial lining fluid following intravenous or oral inhaled administration to healthy adult subjects.
Gauvin, J; Gould, E; Jones, L; Lovern, M; Ng-Cashin, J; Rodvold, KA; Shelton, MJ, 2011
)
2.29
" The laninamivir concentration in ELF decreased with a longer half-life than that in plasma, and it exceeded the 50% inhibitory concentrations for viral neuraminidases at all time points examined for 240 h after the inhalation."( Intrapulmonary distribution and pharmacokinetics of laninamivir, a neuraminidase inhibitor, after a single inhaled administration of its prodrug, laninamivir octanoate, in healthy volunteers.
Furuie, H; Ishizuka, H; Okabe, H; Toyama, K; Yoshiba, S, 2012
)
0.38
" This study was conducted to evaluate the pharmacokinetic and safety profiles of intravenous zanamivir, an influenza viral neuraminidase inhibitor, in Japanese subjects to further characterize these profiles particularly following relatively high-doses when compared with inhalation doses and to provide reassurance that there are no marked differences with profiles reported for other ethnically different populations."( The pharmacokinetic and safety profiles of zanamivir after single and repeat intravenous administration in healthy Japanese males.
Hara, K; Hirama, T; Nohda, S; Shida, Y; Soutome, T, 2013
)
0.87
" The pharmacokinetic profile of zanamivir after intravenous administration was consistent with previously reported findings in non-Japanese subjects."( The pharmacokinetic and safety profiles of zanamivir after single and repeat intravenous administration in healthy Japanese males.
Hara, K; Hirama, T; Nohda, S; Shida, Y; Soutome, T, 2013
)
0.94
" The population pharmacokinetic model also provides insight into the likely kinetics of drug disposition in the respiratory tract following inhaled administration."( Population pharmacokinetics of laninamivir and its prodrug laninamivir octanoate in healthy subjects and in adult and pediatric patients with influenza virus infection.
Ishizuka, H; Kubo, Y; Yoshihara, K, 2013
)
0.39
" Serial blood samples were collected up to 24 h after dose administration (48 h for the severe renal impairment group) to estimate zanamivir serum pharmacokinetic parameters."( Pharmacokinetics of zanamivir following intravenous administration to subjects with and without renal impairment.
Jones, LS; Lou, Y; Ng-Cashin, J; Peppercorn, A; Weller, S, 2013
)
0.92
" Serial blood samples for pharmacokinetic analysis were collected over a 12-h dose interval on day 5 of each treatment period."( Safety, tolerability and pharmacokinetics of orally inhaled zanamivir: a randomized study comparing Rotacap/Rotahaler and Rotadisk/Diskhaler in healthy adults.
Jones, LS; Lou, Y; Ng-Cashin, J; Peppercorn, A; Piscitelli, S; Weller, S, 2013
)
0.63
"The safety and pharmacokinetic results from this study support the use of the Rotacap/Rotahaler presentation, potentially allowing an increased number of zanamivir treatment courses to be supplied in the event of an influenza pandemic."( Safety, tolerability and pharmacokinetics of orally inhaled zanamivir: a randomized study comparing Rotacap/Rotahaler and Rotadisk/Diskhaler in healthy adults.
Jones, LS; Lou, Y; Ng-Cashin, J; Peppercorn, A; Piscitelli, S; Weller, S, 2013
)
0.83
" Pharmacokinetic data showed dose adjustments for renal impairment yielded similar zanamivir exposures."( Safety and pharmacokinetics of intravenous zanamivir treatment in hospitalized adults with influenza: an open-label, multicenter, single-arm, phase II study.
Alvarez-Lerma, F; Brealey, D; Francois, B; Garot, D; Lorente, JA; Man, CY; Mánez, R; Marty, FM; Peppercorn, AF; Thamlikitkul, V; van der Horst, C; Weller, S; Yates, PJ; Zhao, HH, 2014
)
0.89
"Safety, pharmacokinetic and clinical outcome data support further investigation of intravenous zanamivir."( Safety and pharmacokinetics of intravenous zanamivir treatment in hospitalized adults with influenza: an open-label, multicenter, single-arm, phase II study.
Alvarez-Lerma, F; Brealey, D; Francois, B; Garot, D; Lorente, JA; Man, CY; Mánez, R; Marty, FM; Peppercorn, AF; Thamlikitkul, V; van der Horst, C; Weller, S; Yates, PJ; Zhao, HH, 2014
)
0.88
" The current population pharmacokinetic model based on data from eight studies of subjects treated with the intravenous formulation (125 healthy adults and 533 hospitalized adult and pediatric subjects with suspected or confirmed influenza) suggested a decreased zanamivir clearance in pediatric and renal impairment adult subjects."( Population Pharmacokinetic/Pharmacodynamic Analysis of Intravenous Zanamivir in Healthy Adults and Hospitalized Adult and Pediatric Subjects With Influenza.
Barth, A; Collins, J; Hossain, M; Okour, M; Peppercorn, A; Roberts, G; Shortino, D; Watson, HA; Yates, P; Zuo, P, 2020
)
0.97

Compound-Compound Interactions

Zanamivir is a specific inhibitor of influenza A and B virus neuraminidase. Data suggest there is no theoretical basis for expecting metabolic interactions between zanamvir and other coadministered compounds.

ExcerptReferenceRelevance
"The objective of this study was to assess the potential of zanamivir, a specific inhibitor of influenza A and B virus neuraminidase, to interact with other coadministered therapies in the clinical setting."( The low potential for drug interactions with zanamivir.
Barnett, JM; Daniel, MJ; Pearson, BA, 1999
)
0.81
"These data suggest the following: (i) there is no theoretical basis for expecting metabolic interactions between zanamivir and other coadministered compounds; (ii) zanamivir is unlikely to interact with coadministered compounds that are protein bound; and (iii) commonly coadministered drugs will not interfere with the antiviral activity of zanamivir in vivo."( The low potential for drug interactions with zanamivir.
Barnett, JM; Daniel, MJ; Pearson, BA, 1999
)
0.77
" These mt-QSARs offer also a good opportunity to construct drug-drug Complex Networks (CNs) that can be used to explore large and complex drug-viral species databases."( Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks.
Chou, KC; González-Díaz, H; Martinez de la Vega, O; Prado-Prado, FJ; Ubeira, FM; Uriarte, E, 2009
)
0.35

Bioavailability

Less than 5% of drug was excreted unchanged in urine within 8 hours of inhalation. The absolute oral bioavailability of zanamivir was low, averaging 2%. The lower bioavailability may explain the lower toxicity of Zanamivirs compared to oseltamivIR.

ExcerptReferenceRelevance
" While readily bioavailable by systemic routes, it was poorly bioavailable by the oral route."( Inhibition of influenza virus replication in mice by GG167 (4-guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic acid) is consistent with extracellular activity of viral neuraminidase (sialidase).
Dempsey, MH; Penn, CR; Ryan, DM; Ticehurst, J, 1994
)
0.29
" The study of absolute oral bioavailability had an open design."( Pharmacokinetics of zanamivir after intravenous, oral, inhaled or intranasal administration to healthy volunteers.
Bye, A; Cass, LM; Efthymiopoulos, C, 1999
)
0.63
" The absolute oral bioavailability of zanamivir was low, averaging 2%."( Pharmacokinetics of zanamivir after intravenous, oral, inhaled or intranasal administration to healthy volunteers.
Bye, A; Cass, LM; Efthymiopoulos, C, 1999
)
0.9
" Less than 5% of drug was excreted unchanged in urine within 8 hours of inhalation, confirming the low bioavailability of zanamivir after pulmonary delivery."( Pharmacoscintigraphic evaluation of lung deposition of inhaled zanamivir in healthy volunteers.
Brown, J; Bye, A; Cass, LM; Fayinka, S; Johansson, CJ; Newman, SP; Pickford, M, 1999
)
0.75
" This may be attributed to the low systemic bioavailability of zanamivir, which is given by oral inhalation, direct to the primary site of viral replication."( Zanamivir: a review of clinical safety.
Elliott, M; Freund, B; Gravenstein, S; Miller, I, 1999
)
1.99
" Zanamivir is delivered by inhalation because of its low oral bioavailability whereas oseltamivir is administered by mouth."( Influenza virus neuraminidase inhibitors.
Gubareva, LV; Hayden, FG; Kaiser, L, 2000
)
1.22
" Poor bioavailability of zanamivir in the peripheral lungs might have been limiting treatment efficacy in such an immunocompromised patient."( Failure of zanamivir therapy for pneumonia in a bone-marrow transplant recipient infected by a zanamivir-sensitive influenza A (H1N1) virus.
Lorin, V; Manuguerra, JC; Medeiros, R; Naffakh, N; Rameix-Welti, MA; Ribaud, P; Scieux, C; Socie, G; van der Werf, S, 2007
)
1.03
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" On the basis of these results, liposomes are able to improve permeability of zanamivir across the Caco-2 monolayers, thereby possibly enhancing oral bioavailability of zanamivir."( Characterization and in vitro evaluation of intestinal absorption of liposomes encapsulating zanamivir.
Boonyapiwat, B; Kunastitchai, S; Sarisuta, N, 2011
)
0.82
" The poor oral bioavailability is attributed to the high polarity (cLogP ∼ -5) resulting from the polar and zwitterionic nature of zanamivir."( Enhancing the intestinal membrane permeability of zanamivir: a carrier mediated prodrug approach.
Amidon, GL; Dahan, A; Gupta, D; Gupta, SV; Hilfinger, J; Lee, KD; Sun, J; Tsume, Y, 2011
)
0.83
" The absolute oral bioavailability of these compounds was lower than 12%."( Development of oseltamivir phosphonate congeners as anti-influenza agents.
Chen, CA; Chen, CL; Cheng, TJ; Cheng, YS; Fang, JM; Hsieh, WC; Hu, OY; Huang, PW; Jan, JT; Lin, WH; Shie, JJ; Tarbet, EB; Wang, SY; Weinheimer, S; Wong, CH, 2012
)
0.38
"We have demonstrated that simple formulations composed of the parent drug in combination with generally regarded as safe (GRAS) permeability enhancers are capable of dramatically increasing the absolute bioavailability of zanamivir."( Permeability enhancers dramatically increase zanamivir absolute bioavailability in rats: implications for an orally bioavailable influenza treatment.
Devalapally, H; Holmes, EH; Li, L; Ostrander, GK; Perdue, ML, 2013
)
0.83
" Among different prodrug strategies pursued, a simple amidoxime ethyl ester (9) exhibited a superior PK profile with an oral bioavailability of 31% (rats), which is comparable to oseltamivir (36%)."( Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
Clement, B; Koch, O; Kotthaus, J; Müller-Fielitz, H; Raasch, W; Riebling, L; Schade, D; Schmidtke, M; Seidel, N, 2014
)
0.4
" The lower bioavailability may explain the lower toxicity of zanamivir compared to oseltamivir."( Neuraminidase inhibitors for preventing and treating influenza in adults and children.
Del Mar, CB; Doshi, P; Hama, R; Heneghan, CJ; Howick, J; Jefferson, T; Jones, MA; Mahtani, KR; Nunan, D; Onakpoya, I; Spencer, EA; Thompson, MJ, 2014
)
0.64
"For the treatment of seasonal flu and possible pandemic infections the development of new anti-influenza drugs that have good bioavailability against a broad spectrum of influenza viruses including the resistant strains is needed."( From neuraminidase inhibitors to conjugates: a step towards better anti-influenza drugs?
Cheng, CK; Fang, JM; Shie, JJ; Tsai, CH, 2014
)
0.4
" Unfortunately, low oral bioavailability precludes their development as second generation neuraminidase inhibitors for treating influenza as this leaves them unsuitable for use in an oral formulation."( Assessing the oral bioavailability of difluorosialic acid prodrugs, potent viral neuraminidase inhibitors, using a snapshot PK screening assay.
Arns, S; Bourque, E; Dercho, S; Galey, A; Gusti, V; Liggins, R; Paquette, J; Ross, F; Sun, S; Tan, J; Udechukwu, J; Webb, M; Withers, SG; Zisman, N, 2015
)
0.42
" The most promising prodrug candidates, amidoxime ester 7 and N-hydroxyguanidine ester 8, were subjected to in vivo bioavailability studies."( Zanamivir Amidoxime- and N-Hydroxyguanidine-Based Prodrug Approaches to Tackle Poor Oral Bioavailability.
Clement, B; Hoffmann, A; Kotthaus, J; Müller-Fielitz, H; Raasch, W; Riebling, L; Schade, D; Schmidtke, M, 2015
)
1.86
" The bioavailability was 116% relative to Relenza®."( Preparation, characterization and pulmonary pharmacokinetics of a new inhalable zanamivir dry powder.
Cai, X; Mei, X; Xie, X; Yang, Y; Yang, Z; Yu, F; Zhang, T, 2016
)
0.66
" The lipophilic acyl substituents were verified to improve cell permeability, and may also improve the bioavailability of acylguanidine compounds."( Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
Cheng, TJ; Cheng, YE; Chiu, DC; Fang, JM; Hsu, PH; Jan, JT; Lee, PS; Tsai, KC; Wu, KL, 2018
)
0.77
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The current Food and Drug Administration-approved inhaled dosage of zanamivir is insufficient to achieve desired outcomes in humans.

ExcerptRelevanceReference
" Other measures of illness were reduced by approximately 50% to 70% in the GG167 dosing groups."( Safety and efficacy of the neuraminidase inhibitor GG167 in experimental human influenza.
Betts, RF; Esinhart, JD; Hayden, FG; Hussey, EK; Lobo, M; Treanor, JJ,
)
0.13
" In the absence of dose-limiting toxicity in animal studies and in an attempt to identify target-organ toxicity, the high dosage level in all repeat dose studies was selected to be the maximum practicable."( Preclinical development of low toxicity drugs: focus on zanamivir, an anti-influenza drug.
Bethell, R; Daniel, M; Dines, GD, 1998
)
0.55
" Compliance with the once-daily dosage was high."( Zanamivir in the prevention of influenza among healthy adults: a randomized controlled trial.
Crisp, A; Elliott, MJ; Herlocher, ML; Hinson, JM; Monto, AS; Robinson, DP, 1999
)
1.75
"The proposed total daily dosage of zanamivir by oral inhalation is 20 mg."( Effect of renal impairment on the pharmacokinetics of intravenous zanamivir.
Bye, A; Cass, LM; Efthymiopoulos, C; Marsh, J, 1999
)
0.82
" In addition, these data may be useful in the design of prophylactic protocols for humans, in that the dosing schedule may only need to be intermittent to provide protection."( Chemoprophylaxis of influenza A virus infections, with single doses of zanamivir, demonstrates that zanamivir is cleared slowly from the respiratory tract.
Crossman, L; Fenton, RJ; Gower, D; Morley, PJ; Owens, IJ; Parry, S; Wong, T, 1999
)
0.54
" Furthermore there was no apparent treatment difference over the 14 day dosing period in FEV1 data (90% CI: -0."( Pulmonary function and airway responsiveness in mild to moderate asthmatics given repeated inhaled doses of zanamivir.
Bye, A; Cass, LM; Gunawardena, KA; Macmahon, MM, 2000
)
0.52
" Oral administration of a dosage of 1 mg/kg of body weight/day of RWJ-270201 for 5 days (beginning 4 h preinfection) showed efficacy in the murine model of influenza virus infection as determined by lethality and weight loss protection."( Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir.
Ananth, SL; Andries, K; Babu, YS; Bantia, S; Chand, P; Dehghani, A; El-Kattan, Y; Horn, LL; Hutchison, TL; Kellog, DL; Kotian, PL; Lin, T; Montgomery, JA; Parker, CD, 2001
)
0.53
" We conducted two studies to assess the pharmacokinetics and protective efficacy of a reduced frequency dosing regimen of topical zanamivir."( Safety and efficacy of once daily intranasal zanamivir in preventing experimental human influenza A infection.
Calfee, DP; Hayden, FG; Hussey, EK; Lobo, M; Peng, AW, 1999
)
0.77
"Randomised controlled, double blind trials that were published in English, had data available before 31 December 2001, evaluated treatment or prevention of naturally occurring influenza with zanamivir or oseltamivir (if given using the formulation and dosage licensed for clinical use), and reported at least one end point of relevance."( Effectiveness of neuraminidase inhibitors in treatment and prevention of influenza A and B: systematic review and meta-analyses of randomised controlled trials.
Abrams, KR; Cooper, NJ; Nicholson, KG; Sutton, AJ; Turner, D; Wailoo, A, 2003
)
0.51
" Because no prospective data exist on the efficacy of these agents in humans for H5N1 strains, the dosage and duration of therapy in adults and children may differ from those documented to be effective for epidemic influenza strains."( Antiviral therapy and prophylaxis for influenza in children.
, 2007
)
0.34
" Factors which might contribute to this apparently limited efficacy include suboptimal dosing or routes of administration, suboptimal timing of treatment and the inability of antiviral drugs to interfere with immunopathology, and the development of drug resistance."( Neuraminidase inhibitors and their role in avian and pandemic influenza.
Crusat, M; de Jong, MD, 2007
)
0.34
" The paper describes mechanism of action of neuraminidase inhibitors (oseltamivir and zanamivir), their main pharmacokinetic features, dosing and side effects."( [Neuraminidase inhibitors in prophylaxis and treatment of influenza].
Brydak, LB; Nitsch-Osuch, A; Wardyn, AK, 2008
)
0.57
" The clinical and laboratory parameters and plasma and urinary concentrations of CS-8958 and laninamivir for 144 hours post dosing were measured."( Clinical pharmacokinetics of laninamivir, a novel long-acting neuraminidase inhibitor, after single and multiple inhaled doses of its prodrug, CS-8958, in healthy male volunteers.
Ishizuka, H; Okabe, H; Yoshiba, S; Yoshihara, K, 2010
)
0.36
" Further animal studies and human clinical trials are necessary to optimize neuraminidase inhibitor dosing strategies for the treatment of influenza A(H5N1) infections."( Assessing the development of oseltamivir and zanamivir resistance in A(H5N1) influenza viruses using a ferret model.
Barr, IG; Hurt, AC; Lowther, S; Middleton, D, 2010
)
0.62
" Therefore, we performed studies using the in vitro hollow-fiber infection model system to predict optimal dosing regimens for zanamivir against an oseltamivir-sensitive and an oseltamivir-resistant virus."( Zanamivir, at 600 milligrams twice daily, inhibits oseltamivir-resistant 2009 pandemic H1N1 influenza virus in an in vitro hollow-fiber infection model system.
Adams, JR; Brown, AN; Drusano, GL; Kulawy, R; McSharry, JJ; Weng, Q, 2011
)
2.02
" administration of 100 mg, 200 mg, and 600 mg zanamivir, the median zanamivir concentrations in ELF collected 12 h after dosing were 74, 146, and 419 ng/ml, respectively, each higher than the historic mean 50% inhibitory concentrations for the neuraminidases of wild-type strains of influenza A and B viruses."( Zanamivir pharmacokinetics and pulmonary penetration into epithelial lining fluid following intravenous or oral inhaled administration to healthy adult subjects.
Gauvin, J; Gould, E; Jones, L; Lovern, M; Ng-Cashin, J; Rodvold, KA; Shelton, MJ, 2011
)
2.07
" Maoto granules, a commercial medical dosage form, are made from four plants: Ephedra Herb, Apricot Kernel, Cinnamon Bark, and Glycyrrhiza Root."( A randomized, controlled trial comparing traditional herbal medicine and neuraminidase inhibitors in the treatment of seasonal influenza.
Ajisaka, K; Ikematsu, H; Kashiwagi, K; Kashiwagi, S; Masui, S; Nabeshima, S; Takeoka, H, 2012
)
0.38
" Intranasal administration of low dosage (<1."( Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
Cheng, TJ; Cheng, YS; Fang, JM; Jan, JT; Liu, KC; Wang, SY; Wong, CH; Yang, ST, 2012
)
0.38
"Single and 5-day BID repeat dosing of 600 mg were safely administered in Japanese healthy subjects."( The pharmacokinetic and safety profiles of zanamivir after single and repeat intravenous administration in healthy Japanese males.
Hara, K; Hirama, T; Nohda, S; Shida, Y; Soutome, T, 2013
)
0.65
" These results suggest that optimal human oral dosage forms of zanamivir should be enteric-coated gelcaps or softgels for intraduodenal release."( Permeability enhancers dramatically increase zanamivir absolute bioavailability in rats: implications for an orally bioavailable influenza treatment.
Devalapally, H; Holmes, EH; Li, L; Ostrander, GK; Perdue, ML, 2013
)
0.89
" The processed SPR data was analysed to determine 50% inhibitory concentrations (IC50-spr ), using a log dose-response curve fit."( A surface plasmon resonance assay for measurement of neuraminidase inhibition, sensitivity of wild-type influenza neuraminidase and its H274Y mutant to the antiviral drugs zanamivir and oseltamivir.
Fairbanks, AJ; Fee, CJ; Fredericks, R; Hall, RJ; Somasundaram, B; Watson, AJ, 2015
)
0.61
" Hits were evaluated in direct and orthogonal dose-response counterscreens using a standard recRSV reporter strain expressing Renilla luciferase."( Replication-Competent Influenza Virus and Respiratory Syncytial Virus Luciferase Reporter Strains Engineered for Co-Infections Identify Antiviral Compounds in Combination Screens.
Chung, HK; Lamb, K; Lin, MZ; Plemper, RK; Weisshaar, M; Yan, D, 2015
)
0.42
"Time to clinical response to intravenous zanamivir dosed at 600 mg was not superior to oseltamivir or 300 mg intravenous zanamivir."( Intravenous zanamivir or oral oseltamivir for hospitalised patients with influenza: an international, randomised, double-blind, double-dummy, phase 3 trial.
Chapman, MJ; Clark, C; Garot, D; Gupta, SK; Husa, P; Jacobs, F; Marty, FM; Merino, E; Peppercorn, AF; Rodriguez-Noriega, E; Shortino, D; Vidal-Puigserver, J; Watson, HA; Yates, PJ, 2017
)
1.1
" A single-center, open-label study was conducted to evaluate the plasma and intrapulmonary pharmacokinetics (PK) of laninamivir after a single nebulized administration of LO in healthy male Japanese subjects for identifying a safe and effective dosage regimen for a nebulizer."( Intrapulmonary Pharmacokinetics of Laninamivir, a Neuraminidase Inhibitor, after a Single Nebulized Administration of Laninamivir Octanoate in Healthy Japanese Subjects.
Furuie, H; Ishizuka, H; Toyama, K, 2018
)
0.48
" dosing is necessary to keep the exposure in influenza infected subjects above the 90% inhibitory concentration values of recently circulating viruses over the dosing interval."( Population Pharmacokinetic/Pharmacodynamic Analysis of Intravenous Zanamivir in Healthy Adults and Hospitalized Adult and Pediatric Subjects With Influenza.
Barth, A; Collins, J; Hossain, M; Okour, M; Peppercorn, A; Roberts, G; Shortino, D; Watson, HA; Yates, P; Zuo, P, 2020
)
0.79
"Limited data exist for dosing of zanamivir in the setting of CVVH in the intensive care unit (ICU)."( Pharmacokinetics of zanamivir in critically ill patients undergoing continuous venovenous hemofiltration.
Haringman, JJ; Koch, BC; Ter Horst, PG; Wagenvoort, GH; Wieringa, A, 2023
)
1.52
" These results highlight the potential of neuraminidase inhibition for ameliorating endothelial dysfunction in T2D and suggest the current Food and Drug Administration-approved inhaled dosage of zanamivir is insufficient to achieve desired outcomes in humans."( Neuraminidase inhibition improves endothelial function in diabetic mice.
Aroor, AR; Augenreich, MA; Bender, SB; Burr, K; Foote, CA; Ghiarone, T; Manrique-Acevedo, C; Martinez-Lemus, LA; McMillan, NJ; Morales-Quinones, M; Padilla, J; Power, G; Ramirez-Perez, FI; Smith, JA, 2023
)
1.1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
EC 3.2.1.18 (exo-alpha-sialidase) inhibitorAn antiviral drug targeted at influenza viruses. Its mode of action consists of blocking the function of the viral neuraminidase protein (EC 3.2.1.18), thus preventing the virus from budding from the host cell.
antiviral agentA substance that destroys or inhibits replication of viruses.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
guanidinesAny organonitrogen compound containing a carbamimidamido (guanidino) group. Guanidines have the general structure (R(1)R(2)N)(R(3)R(4)N)C=N-R(5) and are related structurally to amidines and ureas.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (39)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GALC proteinHomo sapiens (human)Potency0.707928.183828.183828.1838AID1159614
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency28.18380.01237.983543.2770AID1346984
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, NeuraminidaseInfluenza B virus (STRAIN B/BEIJING/1/87)IC50 (µMol)0.00400.00400.00400.0040AID977608
Chain A, NeuraminidaseInfluenza B virus (STRAIN B/BEIJING/1/87)IC50 (µMol)0.00400.00400.00400.0040AID977608
Chain A, NeuraminidaseInfluenza A virusIC50 (µMol)0.00400.00400.00400.0040AID977608
Chain A, NeuraminidaseInfluenza A virusKi0.03300.033098.0110280.0000AID977610
Chain A, NeuraminidaseInfluenza A virusKi0.03300.033098.0110280.0000AID977610
Chain A, NeuraminidaseInfluenza A virusKi0.03300.033098.0110280.0000AID977610
Chain A, NEURAMINIDASEInfluenza A virusKi0.03300.033098.0110280.0000AID977610
Chain A, NeuraminidaseInfluenza A virusKi0.03300.033098.0110280.0000AID977610
Neuraminidase Influenza A virus (A/Turkey/651242/2006(H5N1))IC50 (µMol)0.00540.00030.31032.8247AID1409417; AID1494239; AID1494240; AID560872
Neuraminidase Influenza A virus (A/Turkey/651242/2006(H5N1))Ki0.00100.00100.00440.0079AID560877
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))IC50 (µMol)41.70260.00000.503510.0000AID1064127; AID1064128; AID1064131; AID1064132; AID1071472; AID1071474; AID1071475; AID1071476; AID1071477; AID1071481; AID1071482; AID1071483; AID1241697; AID1241698; AID1241699; AID1308299; AID1308300; AID1308301; AID1308302; AID1308303; AID1308304; AID1308305; AID1308306; AID1308307; AID1308308; AID1308309; AID1308310; AID1308311; AID1308312; AID1308313; AID1308314; AID1308642; AID1308645; AID1308647; AID1308648; AID1308649; AID1308650; AID1308651; AID1308652; AID1355761; AID1355762; AID1355763; AID1355764; AID1355765; AID1355766; AID1355767; AID1355768; AID1355770; AID1360171; AID1494229; AID1494230; AID1494231; AID1494232; AID1494233; AID1494234; AID1494235; AID1494236; AID1494237; AID1494238; AID1494251; AID1494252; AID1604728; AID343686; AID384920; AID420935; AID420936; AID488375; AID532116; AID542945; AID542946; AID542947; AID542948; AID542949; AID542950; AID542951; AID542952; AID542953; AID542954; AID542955; AID542956; AID542957; AID542958; AID542959; AID542960; AID542961; AID542962; AID542963; AID542964; AID542965; AID542966; AID542967; AID542968; AID542969; AID542970; AID542971; AID542995; AID542996; AID542997; AID542998; AID542999; AID543000; AID543001; AID543002; AID543003; AID543004; AID543006; AID543007; AID543183; AID543184; AID543186; AID543187; AID560874; AID561142; AID561144; AID612400; AID636870; AID667460; AID667579; AID714642; AID722608; AID722609; AID722610
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))Ki0.00020.00011.78687.7000AID314411; AID488379; AID526403; AID560879
Neuraminidase Influenza A virus (A/duck/Laos/25/2006(H5N1))IC50 (µMol)0.00270.00011.10476.0950AID1355769; AID560875; AID561145
Neuraminidase Influenza A virus (A/duck/Laos/25/2006(H5N1))Ki0.00050.00050.00080.0011AID560880
Neuraminidase Influenza A virus (A/Brisbane/59/2007(H1N1))IC50 (µMol)0.02760.00340.14900.4510AID1494249; AID1494250
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))IC50 (µMol)0.00430.00050.976710.0000AID1355760; AID1368740; AID1368742; AID147346; AID147493; AID147504; AID1604725; AID1886446; AID1895906; AID203357; AID203359; AID203532; AID203533; AID203535; AID203537; AID532114
NeuraminidaseInfluenza A virus (A/Wilson-Smith/1933(H1N1))IC50 (µMol)0.00170.00040.13430.9930AID1331612; AID1360170; AID713858; AID714639; AID716614
NeuraminidaseInfluenza A virus (A/Memphis/1/1971(H3N2))IC50 (µMol)0.01470.00010.00910.0324AID1368741; AID1494241; AID1494242; AID1604726
NeuraminidaseInfluenza B virus (B/Lee/1940)IC50 (µMol)0.08090.00100.402810.0000AID147351; AID147494; AID1494247; AID1494248; AID203371; AID203373; AID203545; AID203546; AID203667
NeuraminidaseInfluenza B virus (B/Lee/1940)Ki0.00010.00010.00100.0025AID314410
NeuraminidaseInfluenza A virus (A/udorn/1972(H3N2))IC50 (µMol)0.01540.01540.36220.5813AID1626674
Acyl-CoA desaturase 1Mus musculus (house mouse)IC50 (µMol)0.00100.00100.68303.4000AID1064128
NeuraminidaseInfluenza B virus (STRAIN B/VICTORIA/3/85)IC50 (µMol)0.00450.00400.00450.0050AID1795717
Histamine H1 receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00770.00151.307210.0000AID1409417
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00740.00010.54948.4000AID1409416
Sialidase AStreptococcus pneumoniaeKi720.00000.10002.92839.4000AID1802683
NeuraminidaseInfluenza A virus (A/duck/Ukraine/1/1963(H3N8))IC50 (µMol)0.00740.00740.00820.0089AID1409416
Neuraminidase Influenza A virus (A/RI/5+/1957(H2N2))IC50 (µMol)1.40000.80001.76673.1000AID1129834
Neuraminidase Influenza A virus (A/udorn/1972(H3N2))IC50 (µMol)0.02290.00160.00910.0229AID714636
Neuraminidase Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1))IC50 (µMol)0.00070.00070.00250.0049AID560873; AID561143
Neuraminidase Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1))Ki0.00040.00040.00270.0049AID560878
Neuraminidase Influenza B virus (B/Perth/211/2001)IC50 (µMol)0.08820.00890.08820.1674AID1494245; AID1494246
Neuraminidase Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))IC50 (µMol)0.00240.00020.00130.0048AID560871; AID561141; AID714644
Neuraminidase Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))Ki0.00050.00010.00030.0005AID560876
NeuraminidaseInfluenza A virus (A/Singapore/1/1957(H2N2))IC50 (µMol)0.00700.00100.00500.0170AID1795717; AID1795726
NeuraminidaseInfluenza A virus (A/budgerigar/Hokkaido/1/1977(H4N6))IC50 (µMol)0.02280.01530.01900.0228AID1409413
NeuraminidaseInfluenza A virus (A/Aichi/2/1968(H3N2))IC50 (µMol)0.00270.00160.00210.0027AID532115
Integrase Human immunodeficiency virus 1IC50 (µMol)0.00250.00051.544310.0000AID1886450
Sialidase-4Homo sapiens (human)IC50 (µMol)350.00008.30008.30008.3000AID1308297; AID1308298; AID1405015; AID1490015; AID1619204; AID1889679; AID532109; AID532113
Sialidase-4Homo sapiens (human)Ki26.00001.00004.60005.8000AID1405019; AID1490011; AID1619220
Sialidase-3Homo sapiens (human)IC50 (µMol)5.66172.40005.99808.1700AID1308294; AID1405014; AID1490016; AID1619203; AID532112; AID539786
Sialidase-3Homo sapiens (human)Ki0.62000.62001.26572.2000AID1405018; AID1490012; AID1619219
Sialidase-2Homo sapiens (human)IC50 (µMol)9.79223.90006.73337.8000AID1308295; AID1405013; AID1490017; AID1619202; AID1889674; AID1889675; AID1889677; AID532107; AID748614
Sialidase-2Homo sapiens (human)Ki8.52505.00005.52505.7000AID1405017; AID1490013; AID1619218; AID473065
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
NeuraminidaseInfluenza A virus (A/udorn/1972(H3N2))Kd0.00470.00470.00470.0047AID1626683
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
viral release from host cellNeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))
glycoprotein catabolic processSialidase-4Homo sapiens (human)
ganglioside catabolic processSialidase-4Homo sapiens (human)
oligosaccharide catabolic processSialidase-4Homo sapiens (human)
negative regulation of neuron projection developmentSialidase-4Homo sapiens (human)
oligosaccharide catabolic processSialidase-1Homo sapiens (human)
ganglioside catabolic processSialidase-1Homo sapiens (human)
carbohydrate metabolic processSialidase-3Homo sapiens (human)
ganglioside catabolic processSialidase-3Homo sapiens (human)
oligosaccharide catabolic processSialidase-3Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwaySialidase-3Homo sapiens (human)
glycosphingolipid catabolic processSialidase-3Homo sapiens (human)
negative regulation of clathrin-dependent endocytosisSialidase-3Homo sapiens (human)
glycoprotein catabolic processSialidase-2Homo sapiens (human)
ganglioside catabolic processSialidase-2Homo sapiens (human)
oligosaccharide catabolic processSialidase-2Homo sapiens (human)
glycosphingolipid catabolic processSialidase-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
exo-alpha-sialidase activityNeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))
peptidase activator activityNeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))
exo-alpha-sialidase activitySialidase-4Homo sapiens (human)
protein bindingSialidase-4Homo sapiens (human)
exo-alpha-(2->3)-sialidase activitySialidase-4Homo sapiens (human)
exo-alpha-(2->6)-sialidase activitySialidase-4Homo sapiens (human)
exo-alpha-(2->8)-sialidase activitySialidase-4Homo sapiens (human)
exo-alpha-sialidase activitySialidase-1Homo sapiens (human)
protein bindingSialidase-1Homo sapiens (human)
alpha-sialidase activitySialidase-1Homo sapiens (human)
exo-alpha-(2->3)-sialidase activitySialidase-1Homo sapiens (human)
exo-alpha-(2->6)-sialidase activitySialidase-1Homo sapiens (human)
exo-alpha-(2->8)-sialidase activitySialidase-1Homo sapiens (human)
exo-alpha-sialidase activitySialidase-3Homo sapiens (human)
protein bindingSialidase-3Homo sapiens (human)
alpha-sialidase activitySialidase-3Homo sapiens (human)
exo-alpha-(2->3)-sialidase activitySialidase-3Homo sapiens (human)
exo-alpha-(2->6)-sialidase activitySialidase-3Homo sapiens (human)
exo-alpha-(2->8)-sialidase activitySialidase-3Homo sapiens (human)
exo-alpha-sialidase activitySialidase-2Homo sapiens (human)
protein bindingSialidase-2Homo sapiens (human)
exo-alpha-(2->3)-sialidase activitySialidase-2Homo sapiens (human)
exo-alpha-(2->6)-sialidase activitySialidase-2Homo sapiens (human)
exo-alpha-(2->8)-sialidase activitySialidase-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular regionNeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))
plasma membraneNeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))
lysosomeSialidase-4Homo sapiens (human)
mitochondrial outer membraneSialidase-4Homo sapiens (human)
mitochondrial inner membraneSialidase-4Homo sapiens (human)
lysosomeSialidase-4Homo sapiens (human)
endoplasmic reticulum membraneSialidase-4Homo sapiens (human)
plasma membraneSialidase-4Homo sapiens (human)
organelle inner membraneSialidase-4Homo sapiens (human)
neuron projectionSialidase-4Homo sapiens (human)
lysosomal lumenSialidase-4Homo sapiens (human)
lysosomeSialidase-4Homo sapiens (human)
cytoplasmSialidase-4Homo sapiens (human)
membraneSialidase-4Homo sapiens (human)
extracellular regionSialidase-1Homo sapiens (human)
lysosomeSialidase-1Homo sapiens (human)
lysosomal membraneSialidase-1Homo sapiens (human)
plasma membraneSialidase-1Homo sapiens (human)
cell junctionSialidase-1Homo sapiens (human)
specific granule lumenSialidase-1Homo sapiens (human)
lysosomal lumenSialidase-1Homo sapiens (human)
intracellular membrane-bounded organelleSialidase-1Homo sapiens (human)
extracellular exosomeSialidase-1Homo sapiens (human)
lysosomeSialidase-1Homo sapiens (human)
cytoplasmSialidase-1Homo sapiens (human)
membraneSialidase-1Homo sapiens (human)
lysosomal membraneSialidase-3Homo sapiens (human)
plasma membraneSialidase-3Homo sapiens (human)
caveolaSialidase-3Homo sapiens (human)
external side of plasma membraneSialidase-3Homo sapiens (human)
early endosome membraneSialidase-3Homo sapiens (human)
recycling endosome membraneSialidase-3Homo sapiens (human)
membraneSialidase-3Homo sapiens (human)
lysosomeSialidase-3Homo sapiens (human)
cytoplasmSialidase-3Homo sapiens (human)
cytosolSialidase-2Homo sapiens (human)
catalytic complexSialidase-2Homo sapiens (human)
lysosomeSialidase-2Homo sapiens (human)
membraneSialidase-2Homo sapiens (human)
cytoplasmSialidase-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (917)

Assay IDTitleYearJournalArticle
AID1813704Antiviral activity against Influenza A virus (A/California/07/2009 (H1NI)) harboring NA H275Y mutant infected in dog MDCK cells assessed as reduction in virus replication incubated for 72 hrs by CCK8 assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID1494246Inhibition of Influenza B virus (B/Perth/211/2001) neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1181484Cytotoxicity against MDCK cells assessed as reduction in cell viability after 72 hrs by MTS assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID716603Antiviral activity against Influenza A virus (A/California/07/2009(H1N1)) infected in BALB/c mouse assessed as protection from virus-induced death at 1.2 umol/kg/day, intranasally administered bid on days 1 to 4 and day 0 of infection measured after 12 da2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
AID131091Reduction in virus titre taken from mouse infected with Influenza A/Singapore/1/57 at 0.4 mg/kg dose in 7 day mouse influenza prevention assay2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID565048Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase H274Y mutant infected in MDCK cells selected at 6250 nM of oseltamivir after 7 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1813699Inhibition of Influenza A virus (A/California/07/2009 (H1N1)) neuraminidase N1 H275Y mutant using MUNANA as substrate preincubated for 30 mins followed by substrate addition by fluorescence method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID1308307Inhibition of Influenza A virus (A/duck/Tsukuba/28/2006(H3N8)) neuraminidase N8 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1355795Cytotoxicity against MDCK cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID352033Inhibition of Influenza A virus (A/Singapore/1/1957 (H2N2)) sialidase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID716610Antiviral activity against Influenza A virus (A/California/07/2009(H1N1)) infected in BALB/c mouse assessed as protection from virus-induced death at 12 umol/kg/day, intranasally administered bid on days 1 to 4 and day 0 of infection measured over 14 days2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
AID1903184Antiviral activity against influenza A virus H5N1 infected in dog MDCK cells assessed as inhibition of viral cytopathic effect incubated for 48 hrs by CCK-8 assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA-Dependent RNA Polymerase (RdRp).
AID133476Number of virus free mice from total 8 mice infected with Influenza A/Singapore/1/57 after 12.5 mg/kg of intranasal administration for 172 hr prior to viral infection2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID1405014Inhibition of MBP-fused recombinant human neuraminidase 3 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID542989Inhibition of Influenza B virus (B/Aichi/186/2005(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID667460Inhibition of Influenza A virus (A/Sydney/5/97(H3N2)) recombinant neuraminidase using 2'-(4- methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate after 1 hr by fluorescence assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
AID1308304Inhibition of Influenza A virus A/duck/Chiba/13/06(H12N5) neuraminidase N5 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1494238Inhibition of Influenza A virus (A/chicken/Vietnam/08/2004 (H5N1)) clade 1 neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID203371Compound was tested for inhibitory concentration against Influenza sialidase type B1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 2. Crystallographic and molecular modeling study of complexes of 4-amino-4H-pyran-6-carboxamides and sialidase from influenza virus types A and B.
AID523879Antiviral activity against sInfluenza A virus (A/Texas/12/2007 (H3N2)) with neuraminidase E119V mutant isolated from immunocompromized patient measured after X/CD2 additional passages in MDCK cells by NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID460210Antiviral activity against human influenza A virus A/TW/141/04 (H1N1) in MDCK cells assessed as reduction of virus-induced cytopathic effect2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.
AID761713Inhibition of influenza A virus A/California/04/2009 (pdm09 H1N1) N1 sialidase using fluorogenic substrate 4-methylumbelliferyl N-acetyl-alpha-D-neuraminide preincubated for 15 mins measured after 30 mins by spectrofluorometry2013Bioorganic & medicinal chemistry, Aug-15, Volume: 21, Issue:16
Novel 3,4-disubstituted-Neu5Ac2en derivatives as probes to investigate flexibility of the influenza virus sialidase 150-loop.
AID543000Inhibition of Influenza A virus (A/seal/Massachusetts/1/1980(H7N7)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID543205Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 166 ug/kg, itn administered 1 days pre-infection up to 20 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1405016Inhibition of recombinant His6-tagged human neuraminidase 1 expressed in HEK293 cells using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every 1 min for 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID567586Antiviral activity against influenza A (A/Washington/10/2008 (H1N1)) virus after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID567720Ratio of IC50 for influenza A (A/North Carolina/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/10/2008 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID92312Concentration required for reduction of plaque against influenza A2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID515130Inhibition of Influenza B virus B/Yamagata/186/05 neuraminidase N197 mutant expressed in Sf21 insect cells after 60 mins by MUNANA based assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID524856Antimicrobial activity against Influenza B virus (B/Malaysia/2506/2004) infected itn dosed Mustela putorius furo assessed as nasal viral titer treated after 4 hrs post infection measured after 3 days2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID567607Antiviral activity against influenza A (A/Singapore/57/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1903201Antiviral activity against Influenza A virus (A/PR/8/34) H1N1 infected in dog MDCK cells assessed as inhibition of viral cytopathic effect incubated for 48 hrs by CCK-8 assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA-Dependent RNA Polymerase (RdRp).
AID565478Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring wild type neuraminidase infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus (A/Vietnam/122009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1308301Inhibition of Influenza A virus (A/duck/Tsukuba/28/2005(H6N2)) neuraminidase N2 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID565259Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 3,125 nM of zanamivir after 6 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID542993Inhibition of Influenza B virus (B/Yamagata/1/2005(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID567709Ratio of IC50 for influenza A (A/Hong Kong/2369/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1472397Inhibition of Influenza A virus (A/Puerto Rico/8/34(H1N1)) neuraminidase using fetuin as substrate2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Aniline-Based Inhibitors of Influenza H1N1 Virus Acting on Hemagglutinin-Mediated Fusion.
AID542976Inhibition of Influenza B virus (B/Yamagata/15/2002(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1355760Inhibition of Influenza A virus (A/PuertoRico/8/1934(H1N1)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1626683Binding affinity to zanamivir/oseltamivir resistant recombinant Influenza A virus (A/Moscow/10/99(H3N2)) Neuraminidase N2 E119V/I222L double mutant expressed in baculovirus infected insect cells measured up to 400 sec by surface plasmon resonance analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID515126Fold resistance, ratio of IC50 for Influenza B virus (B/Perth/211/2001) wild type recombinant neuraminidase preincubated for 30 mins to IC50 for Influenza B virus (B/Perth/211/2001) neuraminidase E197 mutant preincubated for 30 mins2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1494232Inhibition of Influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase H274Y mutant using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1626673Inhibition of recombinant Influenza A virus (A/Moscow/10/99(H3N2)) Neuraminidase N2 expressed in baculovirus infected insect cells using 4-MU-NANA as substrate preincubated for 30 mins followed by substrate addition by microplate reader analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1485249Antiviral activity against Influenza A virus A/Ned/378/05(H1N1) infected in MDCK cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by formazan-based colorimetric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
AID667580Antiviral activity against Influenza A virus (A/Indonesia/5/2005(H5N1)) X-31 infected in MDCK cells assessed as protective rate against virus-induced cytopathic effect at 5 uM after 2 days by neutral red uptake assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
AID1494276Ratio of IC50 for Influenza B virus (B/Perth/211/2001) neuraminidase D197E mutant measured every min for 60 mins to IC50 for Influenza B virus (B/Perth/211/2001) neuraminidase D197E mutant preincubated for 60 mins followed by substrate addition measured e2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1308312Inhibition of Influenza A virus A/Kitakyushu/10/06(H1N1) neuraminidase N1 H274Y mutant activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID565051Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring hemagglutininin A45S, K156E, P210Q, L313F mutant gene and neuraminidase H274Y mutant infected in MDCK cells selected at 781 uM of oseltamivir after 10 passage after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1610156Antiviral activity against Influenza A virus (A/HK/7/87(H3N2)) infected in dog MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 7 days by microscopic analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID567703Ratio of IC50 for influenza A (A/New York/18/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/10/2008 (H1N1)) virus expressing wild type enzyme by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1490015Inhibition of human N-terminal MBP-fused NEU4 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Selective Inhibitors of Human Neuraminidase 3.
AID567726Ratio of IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID667593Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
AID565476Antiviral activity against Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase I222V and H274Y mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID567715Ratio of IC50 for influenza A (A/Montana/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1360170Inhibition of Influenza A virus (A/WSN/1933(H1N1)) wild type neuraminidase using MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured for 15 mins by fluorescence assay2018European journal of medicinal chemistry, Jun-25, Volume: 154Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
AID1895906Inhibition of Influenza A virus A/PR/8/1934 (H1N1) neuraminidase using 2(4-methylurnbellifery1)-a-u-acetyl neuraminic acid sodium salt hydrate (4-MUNANA) as substrate preincubated for 10 mins followed by substrate addition and measured after 40 mins by fl2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID667594Terminal half life in Sprague-Dawley rat at 2 mg/kg, iv2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
AID1368740Inhibition of Influenza A virus A/PR/8/34(H1N1) sialidase preincubated for 15 mins followed by MUNA substrate addition measured after 15 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Synthesis and anti-influenza virus evaluation of triterpene-sialic acid conjugates.
AID1731311Selectivity index, ratio of TC50 for MDCK cells to EC50 for antiviral activity against Influenza A virus A/Hebei Xinhua/SWL1106/2017 (H1N1) pdm09 infected in MDCK cells2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors.
AID20028Vss, volume of distribution at steady state at a dose of 50 mg/kg1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID543202Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 166 ug/kg, itn administered 10 days pre-infection up to 20 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID565256Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 25 nM of zanamivir after 3 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID722608Inhibition of influenza A virus (A/Guangdong/376/2001(H1N1)) neuraminidase infected in chick embryo using MUNANA as substrate after 1 hr by spectrophotometric analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID481717Inhibition of Influenza A PR/8/34 H1N1 virus neuraminidase activity by MUN-ANA substrate based fluorimetric assay2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
QSAR study of flavonoids and biflavonoids as influenza H1N1 virus neuraminidase inhibitors.
AID524843Antimicrobial activity against Influenza B virus (B/Hong Kong/05/1972) infected in BALB/c mouse assessed as increase in mouse survival at 1.1 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID565470Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase D198G mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus (A/Vietnam2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID352044Antiviral activity against Influenza B virus (B/Mie/1/93) assessed viral plaque reduction2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID567588Antiviral activity against influenza A (A/New York/18/2009 (H1N1)) virus after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1494245Inhibition of Influenza B virus (B/Perth/211/2001) neuraminidase activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID560874Inhibition of Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) neuraminidase by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID565050Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring hemagglutininin A45S, K156E, P210Q, L313F mutant gene and neuraminidase H274Y mutant infected in MDCK cells selected at 31 uM of oseltamivir after 9 passage after 48 hrs b2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID565269Ratio of IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase H274Y mutant to IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID203369Inhibitory concentration by Sialidase inhibitory assay; range- 11-29 ng/mL2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.
AID565477Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring wild type neuraminidase infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID565246Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 25 nM of zanamivir after 3 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1813703Antiviral activity against Influenza A virus (Avian A/Vietnam/1194/2004 (H5N1)) infected in dog MDCK cells assessed as reduction in virus replication incubated for 72 hrs by CCK8 assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID542945Inhibition of Influenza A virus (A/Puerto Rico/8/1934(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID352046Antiviral activity against Tamiflu-resistant influenza A virus (A/Yokohama/67/2006 (H1N1)) assessed viral plaque reduction2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID716601Antiinflammatory activity in mouse infected with Influenza A virus (A/VietNam/1194/2004(H5N1)) NIBRG-14 assessed as reduction in IL6 level in serum at 12 umol/kg/day, intranasally administered after 72 hrs by ELISA2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
AID1152623Cytotoxicity against MDCK cells after 72 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Design, synthesis and biological evaluation of small molecular polyphenols as entry inhibitors against H(5)N(1).
AID524830Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as increase in mouse survival at 3.3 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID1494233Inhibition of Influenza A virus (A/California/07/09 (H1N1)) neuraminidase activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1071469Cytotoxicity against MDCK cells assessed as cell viability after 72 hrs2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID283442Inhibition of Influenza A virus (A/gull/Pennsylvania/4175/83 (H5N1)) replication in MDCK cells by neutral red uptake assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID567618Antiviral activity against influenza A (A/Singapore/57/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1409414Inhibition of Influenza A virus A/goose/Guangdong/SH7/2013(H5N1) neuraminidase N1 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1071473Antiviral activity against Influenza A virus H3N22014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID1071466Antiviral activity against Oseltamivir-resistant Influenza A virus A/Berlin/55/08(H1N1) infected in MDCK cells assessed as reduction in virus yield after 48 hrs2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID203359Inhibitory activity against influenza A sialidase (Aichi)2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1355784Antiviral activity against Influenza A virus A/goose/Guangdong/SH7/2013(H5N1) infected in chicken embryo fibroblasts assessed as reduction in cytopathic effect after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID567711Ratio of IC50 for influenza A (A/North Carolina/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/10/2008 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1532046Selectivity index, ratio of CC50 for MDCK cells to IC50 for Influenza A virus (A/WSN/1933(H1N1))
AID524837Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as increase in mouse survival at 1.6 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID612400Inhibition of influenza A/WSN/1933 (H1N1) virus neuraminidase N1 using MUNANA substrate by fluorimetric assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Intramolecular ion-pair prodrugs of zanamivir and guanidino-oseltamivir.
AID1729968Inhibition of Influenza A virus (A/California/04/2009(H1N1)) neuraminidase using 4-MU-NANA as substrate preincubated for 5 mins followed by substrate addition and measured after 30 to 60 mins by fluorescence assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID1485247Antiviral activity against Influenza B virus B/Ned/537/05 infected in MDCK cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by formazan-based colorimetric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
AID542977Inhibition of Influenza B virus (B/Akita/9/2003(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID460206Antiviral activity against human influenza A virus A/WSN/33 (H1N1) in MDCK cells assessed as reduction of virus-induced cytopathic effect2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.
AID532109Inhibition of human NEU4 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using 4MU-NeuAc substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID1355783Cytotoxicity against chicken embryo fibroblasts after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID565466Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID560873Inhibition of Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) neuraminidase by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID567589Antiviral activity against influenza A (A/Washington/29/2009 (H1N1)) virus after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID543007Inhibition of Influenza A virus (A/Kawasaki/IMS22A-954/2003(H3N2)) neuraminidase R292K mutant after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID234904Relative potency in sialidase inhibitory assay and plaque reduction assay2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.
AID203533Compound was tested for its inhibitory activity against A/PR/8/34 (N1) sialidases.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID717280Antiviral activity against Influenza A virus (A/PR/8/34(H1N1)) infected in MDCK cells assessed as virus-induced cytopathic effect after 3 days by MTS assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
AID567594Antiviral activity against influenza A (A/Washington/29/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID92335Concentration required for reduction of plaque against influenza B2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides.
AID542991Inhibition of Influenza B virus (B/Sapporo/29/2005(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID542964Inhibition of Influenza A virus (A/Wisconsin/67/2005(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID542968Inhibition of Influenza A virus (A/Saitama/80/2003(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID565044Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 25 nM of oseltamivir after 3 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID515127Selectivity ratio of IC50 for Influenza B virus (B/Perth/211/2001) wild type recombinant neuraminidase to IC50 for Influenza B virus (B/Perth/211/2001) wild type recombinant neuraminidase preincubated for 30 mins2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID565460Ratio of IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase I222M and H274Y mutant to IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID24041t1/2, plasma elimination half life, the time taken for the plasma concentrations to fall by one half, once distribution is complete at a dose of 50 mg/kg1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID1355766Inhibition of Influenza A virus (A/goose/Jiangsu/1306/2014(H5N8)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID542961Inhibition of Influenza A virus (A/California/07/2004(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID352043Antiviral activity against Influenza A virus (A/Kitakyushu/159/93(H3N2)) assessed viral plaque reduction2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID1360172Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in MDCK cells expressing wild type neuraminidase assessed as protection against virus-induced cytopathic effect after 48 hrs by CellTiter96 aqueous non-radioactive cell proliferation2018European journal of medicinal chemistry, Jun-25, Volume: 154Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
AID524860Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as reduction in viral titer in lung at 0.17 mg/kg, itn administered 11 hrs post infection measured after 35 hrs post infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID718741Antiviral activity against Influenza A virus (A/Hong Kong/7/1987(H3N2)) H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Synthesis of isoindole and benzoisoindole derivatives of teicoplanin pseudoaglycon with remarkable antibacterial and antiviral activities.
AID565265Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222M and H274Y mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID565047Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase H274Y mutant infected in MDCK cells selected at 1250 nM of oseltamivir after 6 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID515121Inhibition of Influenza B virus (B/Perth/211/2001) recombinant wild type neuraminidase expressed in Sf21 insect cells after 60 mins by MUNANA based assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID561143Inhibition of Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) neuraminidase isolated from virus-infected BALB/c mouse by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID300564Antiviral activity against influenza B/Sichuan/83/2000 virus in MDCK cells by CPE assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir).
AID542962Inhibition of Influenza A virus (A/New York/55/2004(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID283443Inhibition of Influenza A virus (A/gull/Pennsylvania/4175/83 (H5N1)) replication in MDCK cells by virus yield reduction assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID565457Ratio of IC50 for Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase E119G mutant to IC50 for Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1889675Inhibition of NEU2 (unknown origin) using Neu5Acalpha2-6GalbetapNP as substrate incubated for 30 mins2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID1490011Inhibition of human N-terminal MBP-fused NEU4 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every minute for 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Selective Inhibitors of Human Neuraminidase 3.
AID1731306Inhibition of Influenza A virus A/Puerto Rico/8/1934(H1N1) neuraminidase using MUNANA as substrate measured after 60 mins by fluorescence assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors.
AID271157Antiviral activity against avian influenza virus H5N1 in MDCK cells measured as reduction in infected cells relative to control2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities.
AID1064132Inhibition of Influenza A virus H5N1 neuraminidase using MUNANA as substrate preincubated for 30 mins measured after 2 hrs2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Bifunctional thiosialosides inhibit influenza virus.
AID1626710Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) assessed as decrease in lung lesions at 10 mg/kg qd administered intranasally for 7 days starting from 1 day post infection by hematoxylin and eosin staining based microscopic analysi2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID532107Inhibition of human NEU2 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using 4MU-NeuAc substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID147314Fold resistance of R292K to compound against neuraminidase in a MUNANA-based enzyme inhibition assay, expressed as the ratio of IC50 of comp. with variant N9 to that of with wild-type N92002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Structural studies of the resistance of influenza virus neuramindase to inhibitors.
AID1485244Cytotoxicity against dog MDCK cells assessed as alterations in normal cell morphology measured after 5 to 6 days post infection by microscopic analysis2017European journal of medicinal chemistry, Jul-28, Volume: 135Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1360193Half life in human serum at 16 mg2018European journal of medicinal chemistry, Jun-25, Volume: 154Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
AID524839Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as reduction in viral titer in lung at 14 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID526403Inhibition of influenza A nuraminidase N12010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Carbocycles related to oseltamivir as influenza virus group-1-specific neuraminidase inhibitors. Binding to N1 enzymes in the context of virus-like particles.
AID352037Inhibition of Influenza A virus (A/R(duck/Mongolia/54/01-duck/Mongolia/47/01) (H5N1)) sialidase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID543001Inhibition of Influenza A virus (A/duck/Ukraine/1/1963(H3N8)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID524844Antimicrobial activity against Influenza B virus (B/Hong Kong/05/1972) infected in BALB/c mouse assessed as increase in mouse survival at 3.3 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID1308642Inhibition of oseltamivir-resistant Influenza A virus A/WSN/1933(H1N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate ad2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID565053Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 5 nM of oseltamivir after 2 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID718742Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Synthesis of isoindole and benzoisoindole derivatives of teicoplanin pseudoaglycon with remarkable antibacterial and antiviral activities.
AID561142Inhibition of Influenza A virus (A/Turkey/651242/2006(H5N1)) neuraminidase A119A mutant isolated from virus-infected BALB/c mouse by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID532116Inhibition of human influenza A virus A/DK/HK/313/4/78(H5N3) neuraminidase by fluorometric method using 4MU-NeuAc substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID567724Ratio of IC50 for influenza A (A/Montana/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID560880Inhibition of Influenza A virus (A/duck/Laos/25/2006(H5N1)) neuraminidase by Michaelis-Menten equation analysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID565461Ratio of IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase I222V mutant to IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1626699Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as protection against lethal virus challenge by measuring body weight at 20 mg/kg administered intranasally as single dose at 2 hrs post infection me2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1729971Inhibition of Influenza A virus (A/Chicken/Hebei/UR/2014(H5N2)) neuraminidase using 4-MU-NANA as substrate preincubated for 5 mins followed by substrate addition and measured after 30 to 60 mins by fluorescence assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID131092Reduction in virus titre taken from mouse infected with Influenza A/Singapore/1/57 at 1.0 mg/kg dose in 7 day mouse influenza prevention assay2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID1610159Antiviral activity against Influenza A virus (A/HK/7/87(H3N2)) infected in dog MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 7 days by MTS assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1485246Antiviral activity against Influenza B virus B/Ned/537/05 infected in MDCK cells assessed as host cell viability measured after 3 to 6 days post infection by MTS assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
AID1626676Inhibition of zanamivir/oseltamivir resistant recombinant Influenza A virus (A/Shanghai/2/2013(H7N9)) Neuraminidase N9 R294K mutant expressed in baculovirus infected insect cells using 4-MU-NANA as substrate preincubated for 30 mins followed by substrate 2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1626679Binding affinity to recombinant Influenza A virus (A/Moscow/10/99(H3N2)) Neuraminidase N2 expressed in baculovirus infected insect cells assessed as dissociation rate constant measured up to 400 sec by surface plasmon resonance analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1368741Inhibition of Influenza A virus A/Memphis/1/71(H3N2) sialidase preincubated for 15 mins followed by MUNA substrate addition measured after 15 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Synthesis and anti-influenza virus evaluation of triterpene-sialic acid conjugates.
AID1143481Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as increase in survival rate at 0.12 umol/kg/day administered on day 0 intranasally bid prior to viral infection continued for day 1 to day 4 measured on day2014European journal of medicinal chemistry, Jun-23, Volume: 81Tamiphosphor monoesters as effective anti-influenza agents.
AID1409411Antiviral activity against Influenza B virus (B/Lee/40) infected in MDCK cells after 3 days by plaque reduction assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID704188Inhibition of Influenza A virus sialidase N2 by fluorometric assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Exploring the interactions of unsaturated glucuronides with influenza virus sialidase.
AID524831Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as increase in mouse survival at 7 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID392530Antiviral activity against influenza H5N1 virus2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks.
AID1355765Inhibition of Influenza A virus (A/duck/Guangdong/674/2014(H5N6)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1409408Cytotoxicity against chicken embryo fibroblasts assessed as reduction in cell viability after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID561144Inhibition of Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) neuraminidase isolated from virus-infected BALB/c mouse by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID203374Inhibitory activity against sialidase of influenza B1999Bioorganic & medicinal chemistry letters, Feb-22, Volume: 9, Issue:4
Sialidase inhibitors related to zanamivir: synthesis and biological evaluation of 4H-pyran 6-ether and ketone.
AID1071467Antiviral activity against Influenza A virus A/Jena/5258/2009(H1N1) infected in MDCK cells assessed as reduction in virus yield after 48 hrs2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID1408332Cytotoxicity against MDCK cells assessed as reduction in cell viability after 3 days by MTS assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID1736919Antiviral activity against Influenza A virus (A/Duck/Guangdong/674/2014 (H5N6)) group-2 infected in chicken embryo fibroblast assessed as reduction in viral infection preincubated for 1 hrs followed by fibroblast infection and measured after 72 hrs by hem2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID1181478Antiviral activity against Influenza A virus (A/PR/8/34(H1N1)) infected in MDCK cells assessed as reduction in host cell viability after 72 hrs by MTS assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID130242Compound was tested for concentration of intranasally administered drug (0.5 mg/kg) which reduces virus titer by 90%1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID1071472Inhibition of neuraminidase in Influenza A virus A/Sachsen/6/02(H3N2) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID460214Antiviral activity against human influenza B virus B/TW/99/07 in MDCK cells assessed as reduction of virus-induced cytopathic2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.
AID565260Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase E119G mutant infected in MDCK cells selected at 16 uM of zanamivir after 7 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID567705Ratio of IC50 for influenza A (A/North Carolina/01/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1494254Inhibition of Influenza A virus (A/swine/Shepparton/6/2009 (H1N1)) neuraminidase activity using 4-MUNANA as substrate assessed as reactivation half life by measuring reaction rate to reach 50% of maximum rate of uninhibited control after removal of inhibi2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1626708Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as respiratory epithelium desquamation at 5 mg/kg qd administered intranasally for 7 days starting from 1 day post infection by hematoxylin and eosin2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID283441Inhibition of influenza A virus (A/duck/Minnesota/1525/1981 (H5N1)) replication in MDCK cells by virus yield reduction assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID131093Reduction in virus titre taken from mouse infected with Influenza A/Singapore/1/57 at 1.6 mg/kg dose in 7 day mouse influenza prevention assay2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID1494236Inhibition of Influenza A virus (A/swine/Shepparton/6/2009 (H1N1)) neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID515129Inhibition of Influenza B virus B/Gifu/11/2005 wild type neuraminidase expressed in Sf21 insect cells after 60 mins by MUNANA based assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID612398Octanol-water distribution coefficient, log D of the compound at pH 7.4 at 100 ug/mL2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Intramolecular ion-pair prodrugs of zanamivir and guanidino-oseltamivir.
AID565472Antiviral activity against Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase I222M mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus A/New Cal2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1736917Antiviral activity against Influenza A virus (A/goose/Guangdong/SH7/2013(H5N1)) group-1 infected in chicken embryo fibroblast assessed as reduction in viral infection preincubated for 1 hrs followed by fibroblast infection and measured after 72 hrs by hem2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID1813693Protection against Influenza A virus (A/Puerto Rico/8/34 (H1N1)) infected in Balb/c mouse at 4.2 uM/kg, IV administered once daily for 7 days starting from 24 hrs post viral infection2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID1494260Antiviral activity against Influenza A virus (A/Mississippi/03/01 (H1N1)) infected in MDCK cells assessed as reduction in plaque formation measured after 3 days post infection by neutral red staining-based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID300559Antiviral activity against influenza A/Jifang/15/90 (H3N2) virus in MDCK cells by CPE assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID532113Inhibition of human NEU4 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using ganglioside GM3 substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID542951Inhibition of Influenza A virus (A/Saitama/78/2003(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID532115Inhibition of human influenza A virus A/Aichi/2/1968(H3N2) neuraminidase by fluorometric method using 4MU-NeuAc substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID542984Inhibition of Influenza B virus (B/Shanghai/361/2002(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID16478Clp, plasma clearance at a dose of 50 mg/kg1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID352041Antiviral activity against Influenza A virus (A/Singapore/1/1957 (H2N2)) assessed viral plaque reduction2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID714635Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID567608Antiviral activity against influenza A (A/Washington/10/2008 (H1N1)) virus after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1181479Antiviral activity against Influenza A virus (A/PR/8/34(H1N1)) infected in MDCK cells assessed as virus-induced cytopathic effect after 72 hrs by microscopy2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID1626690Antiviral activity against Influenza A virus (A/Anhui/1/2013(H7N9)) expressing A/Puerto Rico/8/34(H1N1) genes infected in MDCK cells assessed as reduction in viral replication after 72 hrs by hemagglutination test2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID300561Antiviral activity against influenza A/Hanfang/359/95 (H3N2) virus in MDCK cells by CPE assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir).
AID565275Ratio of IC50 for Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase D198G mutant to IC50 for Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID716596Antiinflammatory activity in mouse infected with Influenza A virus (A/VietNam/1194/2004(H5N1)) NIBRG-14 assessed as reduction in IFN-gamma level in serum at 12 umol/kg/day, intranasally administered after 72 hrs by ELISA2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
AID1490018Inhibition of human CathA-IRES-6His-tagged NEU1 expressed in HEK293T cells using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Selective Inhibitors of Human Neuraminidase 3.
AID543002Inhibition of Influenza A virus (A/duck/Memphis/546/1974(H11N9)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID523884Antiviral activity against sInfluenza A virus (A/Texas/12/2007 (H3N2)) with neuraminidase E119(V/I) mutant isolated from immunocompromized patient measured after X/CD3 additional passages in MDCK cells by fluorescent NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID1532044Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect measured everyday
AID121248Number of survivors out of 8 tested mice at 10 days after infection with influenza A/PR/8/34 (H1N1) virus2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.
AID565458Ratio of IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase I222M mutant to IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID647177Selectivity index, ratio of CC50 for MDCK cells to IC50 for Influenza A virus (A/Vietnam/1194/2004(H5N1))2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Synthesis and antiviral activities of novel gossypol derivatives.
AID542947Inhibition of Influenza A virus (A/New Caledonia/20/1999(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID542972Inhibition of Influenza B virus (B/Brisbane/32/2002(Victoria) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1895908Inhibition of Influenza A virus A/Goose/Jiangsu/1306/2014 (H5N8) neuraminidase using using 2(4-methylurnbellifery1)-a-u-acetyl neuraminic acid sodium salt hydrate (4-MUNANA) as substrate preincubated for 10 mins followed by substrate addition and measured2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID133475Number of virus free mice from total 10 mice infected with Influenza A/Singapore/1/57 after 12.5 mg/kg of intranasal administration for 172 hr prior to viral infection2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID515124Inhibition of Influenza B virus (B/Perth/211/2001) wild type recombinant neuraminidase expressed in Sf21 insect cells preincubated for 30 mins measured after 60 mins by MUNANA based assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID488377Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathicity2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Analogs of zanamivir with modified C4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses.
AID714640Inhibition of Influenza B virus B/Taiwan/70641/2004 neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID567708Ratio of IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID717174Antiviral activity against Influenza A virus (A/X-31(H3N2)) infected in MDCK cells assessed as virus-induced cytopathic effect after 3 days by microscopic analysis2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
AID147493Inhibitory activity against influenza A neuraminidase2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity.
AID1813695Protection against Influenza A virus (A/Puerto Rico/8/34 (H1N1)) infected in Balb/c mouse at 84 uM/kg, IG administered once daily for 7 days starting from 24 hrs post viral infection2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID667595Clearance in Sprague-Dawley rat at 2 mg/kg, iv2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID133477Number of virus free mice from total 9 mice infected with Influenza A/Singapore/1/57 after 12.5 mg/kg of intranasal administration for 145 hr prior to viral infection2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID1409405Antiviral activity against Influenza A virus A/Chicken/Hebei/LZF/2014(H5N2) infected in chicken embryo fibroblasts assessed as reduction in cytopathic effect after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID283440Inhibition of influenza A virus (A/duck/Minnesota/1525/1981 (H5N1)) replication in MDCK cells by neutral red uptake assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID352040Antiviral activity against Influenza A virus (A/Yamagata/32/1989 (H1N1)) assessed viral plaque reduction2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID693525Antiviral activity against Influenza A/HK/7/87 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect measured on day 3 post infection by MTS assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis of fluorescent ristocetin aglycon derivatives with remarkable antibacterial and antiviral activities.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID717173Antiviral activity against Influenza A virus (A/X-31(H3N2)) infected in MDCK cells assessed as virus-induced cytopathic effect after 3 days by MTS assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
AID1886447Inhibition of Influenza A virus A/Goose/Guangdong/SH7/2013 (H5N1) neuraminidase using MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 mins by fluorescence based microplate reader method
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID283446Inhibition of viral replication of influenza A virus (A/Vietnam/1203/2004 (H5N1)) and influenza A virus (A/Ann Arbor/6/60(H2N2)) hybrid virus in MDCK cells by neutral red uptake assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID1308650Inhibition of oseltamivir-resistant Influenza A virus A/Vietnam/1194/2004(H5N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by sub2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID461109Selectivity index, ratio of CC50 for CEF cells to EC50 for Influenza A virus (A/Korea/KBNP-0028/2000(H9N2))2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Anti-influenza diarylheptanoids from the bark of Alnus japonica.
AID1405012Inhibition of recombinant His6-tagged human neuraminidase 1 expressed in HEK293 cells using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID300558Antiviral activity against influenza A/Yuefang/243/72 (H3N2) virus in MDCK cells by CPE assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir).
AID1308296Inhibition of human Neu1 expressed in HEK293T cells using 4MU-Neu5Ac as substrate incubated for 30 mins by HPLC analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID105771Inhibitory concentration against Influenza A virus (A/Yamagata/32/89) MDCK cells determined by plaque reduction assay2003Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir.
AID1071483Inhibition of neuraminidase in Influenza A virus A/Jena/5258/2009(H1N1) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID532119Inhibition of human influenza A virus A/DK/HK/313/4/78(H5N3) neuraminidase by fluorometric method using ganglioside GM3 substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID542973Inhibition of Influenza B virus (B/Malaysia/2506/2004(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1490014Inhibition of human CathA-IRES-6His-tagged NEU1 expressed in HEK293T cells using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every minute for 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Selective Inhibitors of Human Neuraminidase 3.
AID1494240Inhibition of Influenza A virus (A/chicken/Bangli/BBVD-563/2007(H5N1)) clade 2 neuraminidase activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID667596Volume of distribution in Sprague-Dawley rat at 2 mg/kg, iv2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
AID1409409Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells after 2 days by plaque reduction assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1308308Inhibition of Influenza A virus A/duck/Tsukuba/441/05(H11N9) neuraminidase N9 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1494257Inhibition of Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase activity using 4-MUNANA as substrate assessed as reactivation half life by measuring reaction rate to reach 50% of maximum rate of uninhibited control after removal of inhibitor preincuba2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1813701Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in dog MDCK cells assessed as reduction in virus replication incubated for 72 hrs by CCK8 assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID567603Antiviral activity against influenza A (A/Montana/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1731310Antiviral activity against Influenza A virus A/Hebei Xinhua/SWL1106/2017 (H1N1) pdm09 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect preincubated for 1 hr followed by viral infection and measured after 48 hrs by crystal vi2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors.
AID1610162Cytotoxicity against dog MDCK cells assessed as reduction in cell viability incubated for 3 days by coulter counter method2019European journal of medicinal chemistry, Dec-15, Volume: 184Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID1813708Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in dog MDCK cells assessed as inhibition of viral replication preincubated for 2 hrs followed by compound wash out and viral infection and measured after 72 hrs by CCK8 ass2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1813696Inhibition of Influenza A virus (A/Puerto Rico/8/34(H1N1)) neuraminidase N1 using MUNANA as substrate preincubated for 30 mins followed by substrate addition by fluorescence method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID1886448Inhibition of Influenza A virus A/Goose/Jiangsu/1306/2014 (H5N8) neuraminidase using MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 mins by fluorescence based microplate reader method
AID283448Cytotoxicity against MDCK cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID567718Ratio of IC50 for influenza A (A/Hong Kong/2369/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID718740Antiviral activity against Influenza B virus (B/Hong Kong/05/1972) H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Synthesis of isoindole and benzoisoindole derivatives of teicoplanin pseudoaglycon with remarkable antibacterial and antiviral activities.
AID523885Antiviral activity against Influenza A virus (A/Texas/12/2007 (H3N2)) clone 1 with neuraminidase E119V mutant isolated from immunocompromized patient measured after X/CD4 additional passages in MDCK cells by fluorescent NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID567609Antiviral activity against influenza A (A/North Carolina/02/2009 (H1N1)) virus after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID532110Inhibition of human NEU1 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using ganglioside GM3 substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID515137Fold resistance, ratio of Ki for Influenza B virus (B/Perth/211/2001) recombinant wild type neuraminidase to Ki for Influenza B virus (B/Perth/211/2001) recombinant neuraminidase E197 mutant2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1241703Cytotoxicity against MDCK cells by SRB assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.
AID567616Antiviral activity against influenza A (A/Washington/29/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1181482Antiviral activity against Influenza A virus (A/HK/7/1987(H3N2)) infected in MDCK cells assessed as virus-induced cytopathic effect after 72 hrs by microscopy2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID1626680Binding affinity to zanamivir/oseltamivir resistant recombinant Influenza A virus (A/Moscow/10/99(H3N2)) Neuraminidase N2 E119V/I222L double mutant expressed in baculovirus infected insect cells assessed as association rate constant measured up to 400 sec2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1360190Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as increase in mouse survival rate at 1.2 umol/kg/day administered intranasally for 5 days and measured at day 21 relative to control2018European journal of medicinal chemistry, Jun-25, Volume: 154Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
AID1604727Inhibition of Influenza A virus (A/Duck/Guangdong/674/2014(H5N6)) Neuraminidase N6 preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 mins by fluorescence method2020European journal of medicinal chemistry, Feb-01, Volume: 187Discovery of novel 1,2,3-triazole oseltamivir derivatives as potent influenza neuraminidase inhibitors targeting the 430-cavity.
AID1308324Antiviral activity against Influenza A virus A/duck/Tsukuba/441/05(H11N9) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID567604Antiviral activity against influenza A (A/Osaka/180/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID567601Antiviral activity against influenza A (A/Singapore/91/2009 (H1N1)) virus after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID539786Inhibition of human neuraminidase 3 assessed as inhibition of GM3 hydrolysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Inhibition of human neuraminidase 3 (NEU3) by C9-triazole derivatives of 2,3-didehydro-N-acetyl-neuraminic acid.
AID1604726Inhibition of Influenza A virus (A/Chicken/Hebei/LZF/2014(H5N2)) Neuraminidase N2 preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 mins by fluorescence method2020European journal of medicinal chemistry, Feb-01, Volume: 187Discovery of novel 1,2,3-triazole oseltamivir derivatives as potent influenza neuraminidase inhibitors targeting the 430-cavity.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1626675Inhibition of recombinant Influenza A virus (A/Anhui/1/2013(H7N9)) Neuraminidase N9 expressed in baculovirus infected insect cells using 4-MU-NANA as substrate preincubated for 30 mins followed by substrate addition by microplate reader analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID667585Terminal half life in Sprague-Dawley rat at 10 mg/kg, po2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
AID542970Inhibition of Influenza A virus (A/Tokushima/1/2005(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID561141Inhibition of Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) neuraminidase isolated from virus-infected BALB/c mouse by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID542980Inhibition of Influenza B virus (B/Yamagata/398/2003(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1409412Cytotoxicity against MDCK cells assessed as reduction in cell viability after 48 hrs by MTT assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID392529Antiviral activity against influenza H3N2 virus2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks.
AID1813698Inhibition of Influenza A virus (A/duck/Alberta/60/1976 (H12N5)) neuraminidase N5 using MUNANA as substrate preincubated for 30 mins followed by substrate addition by fluorescence method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID352049Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected mouse assessed as mouse survival at 0.3 umol/kg dosed intranasally 4 hrs before and 4 hrs, 17 hrs after viral infection measured 20 days post infection2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID567706Ratio of IC50 for influenza A (A/Montana/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID567723Ratio of IC50 for influenza A (A/North Carolina/01/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1626704Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as bronchial wall thickening in lungs at 5 mg/kg qd administered intranasally for 7 days starting from 1 day post infection by hematoxylin and eosin 2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID105808Plaque reduction in in influenza A (A/Yamagata/32/89) was determined using plaque reduction assay (relative to Zanamivir) in MDCK cells2003Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir.
AID620578Inhibition of influenza A virus A/PR/8/34(H1N1) neuraminidase assessed as fluorescent product using MUNANA as substrate after 60 mins by fluorescence analysis2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
3D QSAR and docking study of flavone derivatives as potent inhibitors of influenza H1N1 virus neuraminidase.
AID1813697Inhibition of Influenza A virus (A/Moscow/10/99(H3N2)) neuraminidase N2 using MUNANA as substrate preincubated for 30 mins followed by substrate addition by fluorescence method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID565254Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 1 nM of compound after 1 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID515132Inhibition of Influenza B virus B/Gifu/11/2005 wild type neuraminidase expressed in Sf21 insect cells preincubated for 30 mins measured after 60 mins by MUNANA based assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1494258Inhibition of Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase activity using 4-MUNANA as substrate assessed as reactivation half life by measuring reaction rate to reach 50% of maximum rate of uninhibited control after removal of inhibitor preincubated2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID524862Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as reduction in viral titer in lung at 0.17 mg/kg, itn administered 11 hrs post infection measured after 83 hrs post infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID392528Antiviral activity against influenza H2N2 virus2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks.
AID567714Ratio of IC50 for influenza A (A/North Carolina/01/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1308320Antiviral activity against Influenza A virus A/duck/Chiba/13/06(H12N5) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1626678Binding affinity to recombinant Influenza A virus (A/Moscow/10/99(H3N2)) Neuraminidase N2 expressed in baculovirus infected insect cells assessed as association rate constant measured up to 400 sec by surface plasmon resonance analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID722609Inhibition of Influenza A virus (A/Indonesia/5/2005(H5N1)) neuraminidase infected in chick embryo using MUNANA as substrate after 1 hr by spectrophotometric analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID722350Clearance in Sprague-Dawley rat at 10 mg/kg, iv2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID567600Antiviral activity against influenza A (A/Washington/29/2009 (H1N1)) virus after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID567722Ratio of IC50 for influenza A (A/Singapore/91/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1071474Inhibition of neuraminidase in Influenza A virus A/Rheinland-Pfalz/3911/03(H3N2) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID421013Antiviral activity against influenza A virus A/Vietnam/1194/2004 H5N1 infected in MDCK cells after 3 days by plaque reduction assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID1181494Antiviral activity against Influenza B virus (B/HK/05/1972) infected in MDCK cells assessed as reduction in host cell viability after 72 hrs by MTS assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID532108Inhibition of human NEU3 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using 4MU-NeuAc substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID595829Inhibition of viral Neuraminidase2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Inhibitor selectivity of a new class of oseltamivir analogs against viral neuraminidase over human neuraminidase enzymes.
AID1729967Inhibition of Influenza A virus (A/Puerto Rico/8/1934(H1N1)) neuraminidase using 4-MU-NANA as substrate preincubated for 5 mins followed by substrate addition and measured after 30 to 60 mins by fluorescence assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID1408326Antiviral activity against Influenza A virus A/HK/7/87(H3N2) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 3 days by microscopic method2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID523886Antiviral activity against Influenza A virus (A/Texas/12/2007 (H3N2)) clone 2 with neuraminidase E119I mutant isolated from immunocompromized patient measured after X/CD4 additional passages in MDCK cells by fluorescent NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID147346inhibitory concentration required to inhibit neuraminidase enzyme from different strains of influenza A virus2000Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19
BCX-1812 (RWJ-270201): discovery of a novel, highly potent, orally active, and selective influenza neuraminidase inhibitor through structure-based drug design.
AID1360699Cytotoxicity against MDCK cells assessed as reduction in cell viability measured after 3 to 6 days by MTS assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR).
AID567611Antiviral activity against influenza A (A/Washington/29/2009 (H1N1)) virus after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID565267Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222M mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1485250Antiviral activity against Influenza A virus A/Virginia/ATCC3/2009(H1N1) infected in MDCK cells assessed as host cell viability measured after 3 to 6 days post infection by MTS assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
AID542979Inhibition of Influenza B virus (B/Yamagata/145/2003(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID565475Antiviral activity against Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase I222V mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus A/New Cal2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID300563Antiviral activity against influenza B/Jingfang/76/98 in MDCK cells by CPE assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir).
AID352039Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) assessed viral plaque reduction2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID543194Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 0.3 umol/kg, itn administered 4 hrs pre-infection and at 4 hrs and 17 hrs post-infection up to 8 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID542949Inhibition of Influenza A virus (A/Yamagata/3/2002(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID565252Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring hemagglutininin K234N mutant gene and neuraminidase D198G and E119G mutant infected in MDCK cells selected at 31 uM of zanamivir after 9 passage after 48 hrs by hemaggluti2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1408322Antiviral activity against Influenza A virus A/PR/8/34(H1N1) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 3 days by microscopic method2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID203368Inhibition of sialidase activity2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Synthesis and anti-influenza virus activity of 4-guanidino-7-substituted Neu5Ac2en derivatives.
AID1494265Ratio of IC50 for Influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase measured every min for 60 mins to IC50 for Influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase preincubated for 60 mins followed by substrate addition measured every m2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1308297Inhibition of human Neu4 expressed in HEK293T cells using 4MU-Neu5Ac as substrate incubated for 30 mins by HPLC analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID716605Antiviral activity against Influenza A virus (A/VietNam/1194/2004(H5N1)) NIBRG-14 infected in BALB/c mouse assessed as protection from virus-induced death at 12 umol/kg/day, intranasally administered bid on days 1 to 4 and day 0 of infection measured over2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
AID542986Inhibition of Influenza B virus (B/Shizuoka/58/2004(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID543200Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 236 ug/kg, itn administered 4 days pre-infection up to 20 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID525093Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as increase in mouse survival at 1.7 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID421020Antiviral activity against influenza A virus A/WSN/1933 H1N1 infected in MDCK cells assessed as reduction of infectious viral titer at 100 nM incubated for 1 hr under laminar flow hood light before infection measured after 3 days2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID565469Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase H274Y mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus (A/Vietnam2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1626703Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) assessed as decrease in lung lesions at 20 mg/kg qd administered intranasally as single dose at 2 hrs post infection measured after 7 days post infection by hematoxylin and eosin stai2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1308294Inhibition of human Neu3 expressed in HEK293T cells using GM3 as substrate incubated for 30 mins by HPLC analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID147351inhibitory concentration required to inhibit neuraminidase enzyme from different strains of influenza B virus.2000Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19
BCX-1812 (RWJ-270201): discovery of a novel, highly potent, orally active, and selective influenza neuraminidase inhibitor through structure-based drug design.
AID565248Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 250 nM of zanamivir after 5 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1736921Cytotoxicity against chicken embryo fibroblast assessed as reduction in cell viability after 48 hrs by CCK8 assay2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID565046Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 250 nM of oseltamivir after 5 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID203516Inhibitory concentration against influenza A virus sialidase A/PR/8/342003Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir.
AID1241704Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect by SRB assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.
AID1895913Inhibition of Influenza A virus (A/California/07/2009 (H1N1)) neuraminidase H275Y mutant using 2(4-methylurnbellifery1)-a-u-acetyl neuraminic acid sodium salt hydrate (4-MUNANA) as substrate preincubated for 10 mins followed by substrate addition and meas2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID352036Inhibition of Influenza B virus (B/Mie/1/93) sialidase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID565479Antiviral activity against Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring wild type neuraminidase infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus A/New Caledo2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1813702Antiviral activity against Influenza A virus (A/Moscow/10/99 (H3N2)) infected in dog MDCK cells assessed as reduction in virus replication incubated for 72 hrs by CCK8 assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1368742Inhibition of Influenza A virus A/Duck/313/4/78(H5N3) sialidase preincubated for 15 mins followed by MUNA substrate addition measured after 15 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Synthesis and anti-influenza virus evaluation of triterpene-sialic acid conjugates.
AID1532045Cytotoxicity against MDCK cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
AID712807Antiviral activity against Influenza A virus (A/X-31(H3N2)) infected in MDCK cells assessed as virus-induced cytopathic effect measured 3 days post infection by microscopic analysis2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds.
AID1626688Antiviral activity against Influenza A virus (A/Moscow/10/99(H3N2)) expressing A/Puerto Rico/8/34(H1N1) genes infected in MDCK cells assessed as reduction in viral replication after 72 hrs by hemagglutination test2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID567612Antiviral activity against influenza A (A/Singapore/91/2009 (H1N1)) virus after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1355769Inhibition of Influenza A virus (A/Anhui/1/2005(H5N1)) neuraminidase H274Y mutant activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID532106Inhibition of human NEU1 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using 4MU-NeuAc substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID567617Antiviral activity against influenza A (A/Hong Kong/2369/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID542946Inhibition of Influenza A virus (A/Yamagata/32/1989(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1736918Antiviral activity against Influenza A virus (A/chicken/Hebei/LZF/ 2014(H5N2)) group-2 infected in chicken embryo fibroblast assessed as reduction in viral infection preincubated for 1 hrs followed by fibroblast infection and measured after 72 hrs by hema2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID524845Antimicrobial activity against Influenza B virus (B/Hong Kong/05/1972) infected in BALB/c mouse assessed as increase in mouse survival at 9.6 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID542952Inhibition of Influenza A virus (A/Aichi/193/2004(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1494262Antiviral activity against Influenza A virus (A/Victoria/503/06) infected in MDCK cells assessed as reduction in plaque formation measured after 3 days post infection by neutral red staining-based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1813700Inhibition of Influenza A virus (A/Moscow/10/99 (H3N2)) neuraminidase N2 E119V variant using MUNANA as substrate preincubated for 30 mins followed by substrate addition by fluorescence method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID561145Inhibition of Influenza A virus (A/duck/Laos/25/2006(H5N1)) neuraminidase isolated from virus-infected BALB/c mouse by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID565473Antiviral activity against Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase H274Y mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus A/New Cal2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1494249Inhibition of Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase E119V mutant activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID565474Antiviral activity against Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase I222M and H274Y mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1409415Inhibition of Influenza A virus A/Chicken/Hebei/LZF/2014(H5N2) neuraminidase N2 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1181483Antiviral activity against Influenza A virus (A/HK/7/1987(H3N2)) infected in MDCK cells assessed as reduction in host cell viability after 72 hrs by MTS assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID283445Inhibition of viral replication of influenza A virus (A/Hong Kong/213/03(H5N1)) and influenza A virus (A/Ann Arbor/6/60(H2N2)) hybrid virus in MDCK cells by virus yield reduction assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID1071482Inhibition of neuraminidase in Influenza A virus A/Jena/5555/09(H1N1) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID300562Antiviral activity against influenza B/Jifang/13/97 virus in MDCK cells by CPE assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir).
AID1409418Inhibition of Influenza A virus A/California/04/2009 neuraminidase N1 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID565263Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring hemagglutininin K205EQ mutant gene and neuraminidase E119G mutant infected in MDCK cells selected at 1950 uM of zanamivir after 10 passage after 48 hrs by hemagglutinini2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1494230Inhibition of Influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID271156Antiviral activity against avian influenza virus H5N1 measured as protective rate against MDCK cells at 50 uM by neutral red uptake assay2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities.
AID565266Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase H274Y mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID567587Antiviral activity against influenza A (A/North Carolina/02/2009 (H1N1)) virus after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID712814Antiviral activity against Influenza A virus (A/HK/7/87 (H3N2)) infected in MDCK cells assessed as virus-induced cytopathic effect measured 3 days post infection by microscopic analysis2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds.
AID565239Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222M mutant infected in MDCK cells selected at 3,125 nM of oseltamivir after 6 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID565045Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 50 nM of oseltamivir after 4 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID300560Antiviral activity against influenza A/Jingfang/262/95(H1N1) virus in MDCK cells by CPE assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir).
AID722351Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID565261Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase E119G mutant infected in MDCK cells selected at 78 uM of zanamivir after 8 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID121249Number of survivors out of 8 tested mice at 20 days after infection, with influenza A/PR/8/34 (H1N1) virus2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1889679Inhibition of human NEU42022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID147490Inhibitory concentration of compound against influenza viral coat protein neuraminidase; Range is 0.3-2.3 uM2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Investigation of neuraminidase-substrate recognition using molecular dynamics and free energy calculations.
AID1460742Inhibition of Influenza A virus (A/Puerto Rico/8/34(H1N1)) neuraminidase using MUNANA as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorescence assay relative to control2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Boronic Acid Modifications Enhance the Anti-Influenza A Virus Activities of Novel Quindoline Derivatives.
AID203537Compound was tested for its inhibitory activity against A/Victoria/3/75 (N2) sialidases.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID712808Antiviral activity against Influenza A virus (A/Ishikawa/7/82 (H3N2)) infected in MDCK cells assessed as virus-induced cytopathic effect measured 3 days post infection by microscopic analysis2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds.
AID565262Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring hemagglutininin K205EQ mutant gene and neuraminidase E119G mutant infected in MDCK cells selected at 390 uM of zanamivir after 9 passage after 48 hrs by hemagglutininin 2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID565273Ratio of IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase E119G mutant to IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID542983Inhibition of Influenza B virus (B/Mie/1/1993(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID523880Antiviral activity against Influenza A virus (A/Texas/12/2007 (H3N2)) with neuraminidase E119(V/I) mutant isolated from immunocompromized patient measured after X/CD3 additional passages in MDCK cells by NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID542998Inhibition of Influenza A virus (A/duck/Alberta/60/1976(H12N5)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID352045Antiviral activity against Influenza A virus (A/R(duck/Mongolia/54/01-duck/Mongolia/47/01) (H5N1)) assessed viral plaque reduction2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID1490016Inhibition of human N-terminal MBP-fused NEU3 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Selective Inhibitors of Human Neuraminidase 3.
AID647175Antiviral activity against Influenza A virus (A/Vietnam/1194/2004(H5N1)) infected in MDCK cells assessed as inhibition of viral replication by plaque reduction assay2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Synthesis and antiviral activities of novel gossypol derivatives.
AID567721Ratio of IC50 for influenza A (A/New York/18/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/10/2008 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID515135Selectivity ratio of IC50 for Influenza B virus B/Gifu/11/2005 wild type neuraminidase to IC50 for Influenza B virus B/Gifu/11/2005 wild type neuraminidase preincubated for 30 mins2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID203532Compound was tested for its inhibitory activity against A/Aichi/2/68 (N2) sialidases.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID352031Inhibition of Influenza A virus (A/Puerto Rico/8/34(H1N1)) sialidase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID524855Antimicrobial activity against Influenza B virus (B/Malaysia/2506/2004) infected itn dosed Mustela putorius furo assessed as nasal viral titer treated after 4 hrs post infection measured after 2 days2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID1308652Inhibition of Influenza A virus A/Shanghai/01/2014(H7N9) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measure2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID1736923Inhibition of Influenza A virus (A/chicken/Hebei/LZF/ 2014(H5N2)) group-2 Neuraminidase N2 preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 to 60 mins by fluorescence method2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID1736926Inhibition of Influenza A virus (A/Anhui/1/2005 (H5N1)) group-1 Neuraminidase N1 H274Y mutant preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 to 60 mins by fluorescence method2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID460213Antiviral activity against human influenza B virus B/TW/70325/05 in MDCK cells assessed as reduction of virus-induced cytopathic2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.
AID420929Inhibition of influenza A virus A/Vietnam/1194/2004 H5N1 neuraminidase at 10 nM using NA-STAR substrate after 15 mins incubation at room temperature by fluorescent assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID147494Inhibitory activity against influenza B neuraminidase2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID565243Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring hemagglutininin K234Q mutant gene and neuraminidase I222M and H274Y mutant infected in MDCK cells selected at 1950 uM of oseltamivir after 10 passage after 48 hrs by hem2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID203363Inhibitory activity against sialidase of influenza A1999Bioorganic & medicinal chemistry letters, Feb-22, Volume: 9, Issue:4
Sialidase inhibitors related to zanamivir: synthesis and biological evaluation of 4H-pyran 6-ether and ketone.
AID532117Inhibition of human Influenza A virus A/PR/8/34(H1N1) neuraminidase by fluorometric method using ganglioside GM3 substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID1494269Ratio of IC50 for Influenza A virus (A/chicken/Vietnam/08/2004 (H5N1)) clade 1 neuraminidase measured every min for 60 mins to IC50 for Influenza A virus (A/chicken/Vietnam/08/2004 (H5N1)) clade 1 neuraminidase preincubated for 60 mins followed by substra2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID524838Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as increase in mouse survival at 4.7 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID565274Ratio of IC50 for Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase H274Y mutant to IC50 for Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID543185Ratio of IC50 for Influenza A virus (A/Yokohama/IMS9A-2029/2003(H3N2)) neuraminidase E119V mutant to IC50 for Influenza A virus (A/Yokohama/IMS9A-2029/2003(H3N2)) wild type neuraminidase2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1494251Inhibition of Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase E119G mutant activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1494266Ratio of IC50 for Influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase H274Y mutant measured every min for 60 mins to IC50 for Influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase H274Y mutant preincubated for 60 mins followed by substrate2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID717281Antiviral activity against Influenza A virus (A/PR/8/34(H1N1)) infected in MDCK cells assessed as virus-induced cytopathic effect after 3 days by microscopic analysis2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
AID515125Inhibition of Influenza B virus (B/Perth/211/2001) recombinant neuraminidase E197 mutant expressed in Sf21 insect cells preincubated for 30 mins measured after 60 mins by MUNANA based assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID722354Terminal half life in Sprague-Dawley rat at 10 mg/kg, po2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID567606Antiviral activity against influenza A (A/Hong Kong/2369/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID717172Antiviral activity against Influenza B virus (B/HK/5/72) infected in MDCK cells assessed as virus-induced cytopathic effect after 3 days by microscopic analysis2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
AID1355768Inhibition of Influenza A virus (A/Anhui/1/2013(H7N9)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1903186Selectivity index, ratio of CC50 for cytotoxicity in dog MDCK cells assessed as reduction in cell viability to EC50 for antiviral activity against influenza A virus H5N1 infected in dog MDCK cells assessed as reduction in inhibition of viral cytopathic ef2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA-Dependent RNA Polymerase (RdRp).
AID1494235Inhibition of Influenza A virus (A/swine/Shepparton/6/2009 (H1N1)) neuraminidase activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID532118Inhibition of human influenza A virus A/Aichi/2/1968(H3N2) neuraminidase by fluorometric method using ganglioside GM3 substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID716613Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in MDCK cells assessed as inhibition of virus induced cytopathic effect2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
AID542988Inhibition of Influenza B virus (B/Yamagata/87/2004(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID515123Fold resistance, ratio of IC50 for Influenza B virus (B/Perth/211/2001) recombinant wild type neuraminidase to IC50 for Influenza B virus (B/Perth/211/2001) recombinant neuraminidase E197 mutant2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID283447Inhibition of viral replication of influenza A virus (A/Vietnam/1203/2004 (H5N1)) and influenza A virus (A/Ann Arbor/6/60(H2N2)) hybrid virus in MDCK cells by virus yield reduction assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID693526Antiviral activity against Influenza B/HK/5/72 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect measured on day 3 post infection by MTS assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis of fluorescent ristocetin aglycon derivatives with remarkable antibacterial and antiviral activities.
AID1494253Inhibition of influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase activity using 4-MUNANA as substrate assessed as reactivation half life by measuring reaction rate to reach 50% of maximum rate of uninhibited control after removal of inhibitor pr2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1889677Inhibition of human NEU22022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID421021Antiviral activity against influenza A virus A/WSN/1933 H1N1 infected in MDCK cells assessed as reduction of infectious viral titer at 500 nM incubated for 1 hr under laminar flow hood light before infection measured after 3 days2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID1494237Inhibition of Influenza A virus (A/chicken/Vietnam/08/2004 (H5N1)) clade 1 neuraminidase activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1857995Inhibition of influenza virus neuraminidase2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Sialidase Inhibitors with Different Mechanisms.
AID234903Relative potency against plaque formation and sialidase activity2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Synthesis and anti-influenza virus activity of 4-guanidino-7-substituted Neu5Ac2en derivatives.
AID1626697Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as protection against lethal virus challenge by measuring body weight at 5 to 10 mg/kg qd administered intranasally for 7 days starting from 1 day po2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID543199Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 236 ug/kg, itn administered 7 days pre-infection up to 20 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1494261Antiviral activity against Influenza A virus (A/Fukui/45/04(H3N2)) infected in MDCK cells assessed as reduction in plaque formation measured after 3 days post infection by neutral red staining-based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID567596Antiviral activity against influenza A (A/Singapore/57/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID92326Inhibition of plaque formation2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Synthesis and anti-influenza virus activity of 4-guanidino-7-substituted Neu5Ac2en derivatives.
AID1610157Antiviral activity against Influenza B virus (B/Ned/537/05) infected in dog MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 7 days by microscopic analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID1308326Antiviral activity against Influenza A virus (A/Narita/1/2009(H1N1)) infected in dog AX4 cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1731307Inhibition of Influenza A virus A/Minfang/151/2000 (H3N2) neuraminidase using MUNANA as substrate measured after 60 mins by fluorescence assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors.
AID717171Antiviral activity against Influenza B virus (B/HK/5/72) infected in MDCK cells assessed as virus-induced cytopathic effect after 3 days by MTS assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID543198Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 236 ug/kg, itn administered 10 days pre-infection up to 20 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1308313Inhibition of Influenza A virus (A/Aichi/75/2008(H3N2)) neuraminidase N2 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID560879Inhibition of Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) neuraminidase by Michaelis-Menten equation analysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID567592Antiviral activity against influenza A (A/Montana/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1308315Antiviral activity against Influenza A virus (A/duck/Tsukuba/67/2005(H1N1)) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID636870Inhibition of influenza A virus neuraminidase2011Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
The de-guanidinylated derivative of peramivir remains a potent inhibitor of influenza neuraminidase.
AID1485248Antiviral activity against Influenza A virus A/Ned/378/05(H1N1) infected in MDCK cells assessed as host cell viability measured after 3 to 6 days post infection by MTS assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
AID1490012Inhibition of human N-terminal MBP-fused NEU3 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every minute for 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Selective Inhibitors of Human Neuraminidase 3.
AID722611Terminal half life in Sprague-Dawley rat at 10 mg/kg, iv2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID1308316Antiviral activity against Influenza A virus (A/mallard/Hokkaido/24/2009(H5N1)) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID92327Inhibitory concentration by Plaque reduction assay; range- 13-27ng/mL2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.
AID565250Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring hemagglutininin K234N mutant gene and neuraminidase D198G mutant infected in MDCK cells selected at 6250 nM of compound after 7 passage after 48 hrs by hemagglutininin tit2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1736922Inhibition of Influenza A virus (A/goose/Guangdong/SH7/2013(H5N1)) group-1 Neuraminidase N1 preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 to 60 mins by fluorescence method2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID722355Tmax in Sprague-Dawley rat at 10 mg/kg, po2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID1408324Antiviral activity against Influenza A virus A/Virginia/ATCC3/2009(H1N1pdm) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 3 days by microscopic method2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID542985Inhibition of Influenza B virus (B/Shiga/31/2002(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1610160Antiviral activity against Influenza B virus (B/Ned/537/05) infected in dog MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 7 days by MTS assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID565055Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 125 nM of oseltamivir after 4 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID542971Inhibition of Influenza A virus (A/Saitama/07/2006(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID421012Antiviral activity against influenza A virus A/WSN/1933 H1N1 infected in MDCK cells after 3 days by plaque reduction assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID1889676Inhibition of human NEU12022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID92449Antiinfluenza activity of compound against Influenza B/Harbin/7/95 in influenza cytopathic effect (CPE) assay2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID1308322Antiviral activity against Influenza A virus (A/duck/Tsukuba/700/2007(H7N7)) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1355787Antiviral activity against Influenza A virus A/goose/Jiangsu/1306/2014(H5N8) infected in chicken embryo fibroblasts assessed as reduction in cytopathic effect after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1485245Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
AID525070Half life in human2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID524832Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as increase in mouse survival at 14 mg/kg, itn administered for 7 days before infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID1355794Antiviral activity against Influenza A virus (A/Wisconsin/67/2005(H3N2)) infected in MDCK cells assessed as reduction in plaque formation after 2 days by toluidine blue staining-based assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID460212Antiviral activity against human influenza B virus B/TW/710/05 in MDCK cells assessed as reduction of virus-induced cytopathic2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.
AID1308323Antiviral activity against Influenza A virus (A/duck/Tsukuba/28/2006(H3N8)) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1903185Cytotoxicity against dog MDCK cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA-Dependent RNA Polymerase (RdRp).
AID1408323Antiviral activity against Influenza A virus A/PR/8/34(H1N1) infected in MDCK cells after 3 days by MTS assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID515136Selectivity ratio of IC50 for Influenza B virus B/Yamagata/186/05 neuraminidase N197 mutant to IC50 for Influenza B virus B/Yamagata/186/05 neuraminidase N197 mutant preincubated for 30 mins2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1071481Inhibition of neuraminidase in Influenza A virus A/HH/1580/09(H1N1) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID567704Ratio of IC50 for influenza A (A/Singapore/91/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1626698Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as protection against lethal virus challenge by measuring mouse survival at 5 to 10 mg/kg qd administered intranasally for 7 days starting from 1 day2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID565463Drug level in sputum of healthy human between 6 to 24 hrs postdosing2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1360698Cytotoxicity against MDCK cells assessed as alterations in normal cell morphology measured after 3 to 6 days by microscopic analysis2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR).
AID1604725Inhibition of Influenza A virus (A/goose/Guangdong/SH7/2013(H5N1)) Neuraminidase N1 preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 mins by fluorescence method2020European journal of medicinal chemistry, Feb-01, Volume: 187Discovery of novel 1,2,3-triazole oseltamivir derivatives as potent influenza neuraminidase inhibitors targeting the 430-cavity.
AID1181493Antiviral activity against Influenza B virus (B/HK/05/1972) infected in MDCK cells assessed as virus-induced cytopathic effect after 72 hrs by microscopy2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID565272Ratio of IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222V and H274Y mutant to IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1731309Cytotoxicity against MDCK cells assessed as reduction in cell viability measured after 48 hrs by crystal violet staining based assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors.
AID567591Antiviral activity against influenza A (A/North Carolina/01/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID543184Inhibition of Influenza A virus (A/Yokohama/IMS9A-2029/2003(H3N2)) neuraminidase E119V mutant after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID567610Antiviral activity against influenza A (A/New York/18/2009 (H1N1)) virus after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID730333Inhibition of inactivated Influenza A virus (A/Puerto Rico/8/1934(H1N1)) neuraminidase using MUNANA as substrate incubated for 60 mins prior to substrate addition measured after 45 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Aspulvinones from a mangrove rhizosphere soil-derived fungus Aspergillus terreus Gwq-48 with anti-influenza A viral (H1N1) activity.
AID1494271Ratio of IC50 for Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase measured every min for 60 mins to IC50 for Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase preincubated for 60 mins followed by substrate addition measured every min for 60 mins2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID560876Inhibition of Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) neuraminidase by by Michaelis-Menten equation analysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID1355764Inhibition of Influenza A virus (A/Chicken/Hebei/LZF/2014(H5N2)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID565249Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring hemagglutininin K234N mutant gene and neuraminidase D198G mutant infected in MDCK cells selected at 1250 nM of compound after 6 passage after 48 hrs by hemagglutininin tit2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1626681Binding affinity to zanamivir/oseltamivir resistant recombinant Influenza A virus (A/Moscow/10/99(H3N2)) Neuraminidase N2 E119V/I222L double mutant expressed in baculovirus infected insect cells assessed as dissociation rate constant measured up to 400 se2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID761716Inhibition of influenza A virus A/R1/5+/1957 (H2N2) N2 sialidase using fluorogenic substrate 4-methylumbelliferyl N-acetyl-alpha-D-neuraminide preincubated for 15 mins measured after 30 mins by spectrofluorometry2013Bioorganic & medicinal chemistry, Aug-15, Volume: 21, Issue:16
Novel 3,4-disubstituted-Neu5Ac2en derivatives as probes to investigate flexibility of the influenza virus sialidase 150-loop.
AID1813715Protection against Influenza A virus (A/Puerto Rico/8/34 (H1N1)) infected in Balb/c mouse at 8.4 uM/kg, IN administered once daily for 7 days starting from 4 hrs prior to viral infection and measured after 14 days2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID1308647Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measure2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID543189Inhibition of Influenza B virus (B/Yokohama/UT2203/2005)) neuraminidase N294S mutant after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1355785Antiviral activity against Influenza A virus A/Chicken/Hebei/LZF/2014(H5N2) infected in chicken embryo fibroblasts assessed as reduction in cytopathic effect after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID567613Antiviral activity against influenza A (A/North Carolina/01/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1895909Inhibition of Influenza A virus A/Babol/36/2005 (H3N2) neuraminidase using using 2(4-methylurnbellifery1)-a-u-acetyl neuraminic acid sodium salt hydrate (4-MUNANA) as substrate preincubated for 10 mins followed by substrate addition and measured after 40 2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID515140Fold resistance, ratio of Ki for Influenza B virus B/Gifu/11/2005 wild type neuraminidase preincubated for 30 mins to Ki for Influenza B virus B/Yamagata/186/05 neuraminidase N197 mutant preincubated for 30 mins2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID542957Inhibition of Influenza A virus (A/Aichi/2/1968(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID147504Inhibitory activity was determined against Neuraminidase A from influenza virus A/Tokyo/3/672001Journal of medicinal chemistry, Apr-12, Volume: 44, Issue:8
Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores.
AID352032Inhibition of Influenza A virus (A/Yamagata/32/1989 (H1N1)) sialidase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID515133Inhibition of Influenza B virus B/Yamagata/186/05 neuraminidase N197 mutant expressed in Sf21 insect cells preincubated for 30 mins measured after 60 mins by MUNANA based assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID133474Number of virus free mice from total 10 mice infected with Influenza A/Singapore/1/57 after 12.5 mg/kg of intranasal administration for 117 hr prior to viral infection2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID1405018Inhibition of MBP-fused recombinant human neuraminidase 3 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every 1 min for 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID565244Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 1 nM of zanamivir after 1 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID352034Inhibition of Influenza A virus (A/Aichi/2/1968(H3N2)) sialidase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID1071468Antiviral activity against Oseltamivir-resistant Influenza A virus A/Berlin/55/08(H1N1) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID713858Inhibition of wild type Influenza A virus A/WSN/1933(H1N1) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID352047Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected mouse assessed as mouse survival at 0.2 umol/kg dosed intranasally 4 hrs before and 4 hrs, 17 hrs after viral infection measured 20 days post infection2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID203535Compound was tested for its inhibitory activity against A/USSR/90/77 (N1) sialidases.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID203518Relative potency against influenza A sialidase (A/PR/8/34) was determined using sialidase inhibitory assay (relative to Zanamivir)2003Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID667579Inhibition of Influenza A virus (A/Indonesia/5/2005(H5N1)) X-31 recombinant neuraminidase using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate after 1 hr by fluorescence assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
AID1494244Inhibition of Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1494268Ratio of IC50 for Influenza A virus (A/swine/Shepparton/6/2009 (H1N1)) neuraminidase measured every min for 60 mins to IC50 for Influenza A virus (A/swine/Shepparton/6/2009 (H1N1)) neuraminidase preincubated for 60 mins followed by substrate addition meas2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1308317Antiviral activity against Influenza A virus (A/duck/Tsukuba/28/2005(H6N2)) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID565043Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 5 nM of oseltamivir after 2 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1494248Inhibition of Influenza B virus (B/Perth/211/2001) neuraminidase D197E mutant activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1181481Antiviral activity against Influenza A virus A/Virginia/ATCC3/2009 infected in MDCK cells assessed as reduction in host cell viability after 72 hrs by MTS assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID515122Inhibition of Influenza B virus (B/Perth/211/2001) recombinant neuraminidase E197 mutant expressed in Sf21 insect cells after 60 mins by MUNANA based assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID532114Inhibition of human Influenza A virus A/PR/8/34(H1N1) neuraminidase by fluorometric method using 4MU-NeuAc substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID1308300Inhibition of Influenza A virus (A/mallard/Hokkaido/24/2009(H5N1)) neuraminidase N1 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID542953Inhibition of Influenza A virus (A/Okinawa/42/2004(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1308310Inhibition of Influenza A virus (A/Narita/1/2009(H1N1)) neuraminidase N1 V149I mutant activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1071475Inhibition of neuraminidase in Influenza A virus A/Berlin/10/04(H3N2) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID543004Inhibition of Influenza A virus (A/Yokohama/67/2006(clone 11)(H1N1)) neuraminidase H274Y mutant after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID565049Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase H274Y mutant infected in MDCK cells selected at 31 uM of oseltamivir after 8 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID560877Inhibition of Influenza A virus (A/Turkey/651242/2006(H5N1)) neuraminidase by Michaelis-Menten equation analysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID567597Antiviral activity against influenza A (A/Washington/10/2008 (H1N1)) virus after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1886450Inhibition of Influenza A virus A/California/04/2009 (H1N1) Neuraminidase H274Y mutant using MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 mins by fluorescence based microplate reader method
AID1895914Inhibition of Influenza A virus A/Anhui/1/2005 (H5N1) Neuraminidase H274Y mutant using 2(4-methylurnbellifery1)-a-u-acetyl neuraminic acid sodium salt hydrate (4-MUNANA) as substrate preincubated for 10 mins followed by substrate addition and measured aft2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID722610Inhibition of Influenza A virus (A/Sydney/5/1997(H3N2)) neuraminidase infected in chick embryo using MUNANA as substrate after 1 hr by spectrophotometric analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID1610158Antiviral activity against Influenza A virus (A/Ned/378/05(H1N1)) infected in dog MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 7 days by MTS assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID420936Inhibition of influenza A virus A/Vietnam/1194/2004 H5N1 neuraminidase using NA-STAR substrate after 15 mins incubation at room temperature by fluorescent assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID420928Inhibition of influenza A virus A/WSN/1933 H1N1 neuraminidase at 40 nM using NA-STAR substrate after 15 mins incubation at room temperature by fluorescent assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID1360171Inhibition of Influenza A virus (A/WSN/1933(H1N1)) neuraminidase H275Y mutant using MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured for 15 mins by fluorescence assay2018European journal of medicinal chemistry, Jun-25, Volume: 154Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
AID1409406Antiviral activity against Influenza A virus A/duck/Guangdong/674/2014(H5N6) infected in chicken embryo fibroblasts assessed as reduction in cytopathic effect after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1626691Antiviral activity against A/Puerto Rico/8/34(H1N1) genes expressing anamivir/oseltamivir resistant Influenza A virus (A/Shanghai/2/2013(H7N9)) harboring Neuraminidase N9 R294K mutant infected in MDCK cells assessed as reduction in viral replication after2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1626705Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as bronchial wall thickening in lungs at 20 mg/kg qd administered intranasally as single dose at 2 hrs post infection measured after 7 days post infe2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID565245Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 5 nM of zanamivir after 2 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID565258Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 625 nM of zanamivir after 5 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID693527Cytotoxicity against MDCK cells assessed as minimum concentration required to cause microscopically detectable alteration measured on day 3 post infection by MTS assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis of fluorescent ristocetin aglycon derivatives with remarkable antibacterial and antiviral activities.
AID567713Ratio of IC50 for influenza A (A/Singapore/91/2009 (H1N1))virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1308318Antiviral activity against Influenza A virus (A/duck/Tsukuba/394/2005(H5N3)) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID567716Ratio of IC50 for influenza A (A/Osaka/180/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1729978Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells as reduction in plaque formation2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID1813705Antiviral activity against Influenza A virus (A/Moscow/10/99 (H3N2)) harboring NA E119V mutant infected in dog MDCK cells assessed as reduction in virus replication incubated for 72 hrs by CCK8 assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID712796Cytotoxicity against dog MDCK cells assessed as cell morphology alterations2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds.
AID565471Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring neuraminidase E119G mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose to IC50 for Influenza A virus (A/Vietnam2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1408327Antiviral activity against Influenza A virus A/HK/7/87(H3N2) infected in MDCK cells after 3 days by MTS assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID542948Inhibition of Influenza A virus (A/Shiga/1/2002(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID460211Antiviral activity against human influenza A virus A/TW/3446/04 (H3N2) in MDCK cells assessed as reduction of virus-induced cytopathic effect2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.
AID567595Antiviral activity against influenza A (A/Hong Kong/2369/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID542987Inhibition of Influenza B virus (B/Yamagata/85/2004(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID543201Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 236 ug/kg, itn administered 1 days pre-infection up to 20 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1494256Inhibition of Influenza A virus (A/chicken/Bangli/BBVD-563/2007(H5N1)) clade 2 neuraminidase activity using 4-MUNANA as substrate assessed as reactivation half life by measuring reaction rate to reach 50% of maximum rate of uninhibited control after remov2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1308319Antiviral activity against Influenza A virus (A/duck/Tsukuba/20/2007(H8N4)) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1071480Antiviral activity against Influenza A virus H1N12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID1308311Inhibition of Influenza A virus A/Yamaguchi/20/06(H1N1) neuraminidase N1 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1532043Inhibition of Clostridium neuraminidase preincubated for 2 mins followed by neuraminidase fluorescent addition and measured after 30 mins by fluorescence assay
AID1494241Inhibition of Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1071477Inhibition of neuraminidase H274Y mutant in Oseltamivir-resistant Influenza A virus A/Berlin/55/08(H1N1) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID1355786Antiviral activity against Influenza A virus A/duck/Guangdong/674/2014(H5N6) infected in chicken embryo fibroblasts assessed as reduction in cytopathic effect after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1626707Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as immune cell infiltration in lungs at 20 mg/kg qd administered intranasally as single dose at 2 hrs post infection measured after 7 days post infec2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1241697Inhibition of recombinant Influenza A virus H1N1 neuraminidase2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.
AID1129834Inhibition of Influenza A virus (A/RI/5+/1957(H2N2)) recombinant neuraminidase using MUNANA as substrate after 30 mins2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Benzophenone C-glucosides and gallotannins from mango tree stem bark with broad-spectrum anti-viral activity.
AID352042Antiviral activity against Influenza A virus (A/Aichi/2/1968(H3N2)) assessed viral plaque reduction2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID523887Antiviral activity against Influenza A virus (A/Washington/01/2007 (H3N2)) measured in MDCK cells by fluorescent NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID542975Inhibition of Influenza B virus (B/Shiga/17/2002(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID140430Compound was tested for in vivo efficacy in mouse model of influenza A virus A/Singapore/1/57 at dose of 50 mg/kg (ip)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID567590Antiviral activity against influenza A (A/Singapore/91/2009 (H1N1)) virus after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID560871Inhibition of Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) neuraminidase by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID1494243Inhibition of Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1360697Antiviral activity against Influenza B virus B/Ned/537/05 infected in MDCK cells assessed as protection against virus-induced reduction in cell viability after 3 to 6 days by MTS assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR).
AID473065Inhibition of human neuraminidase 22010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Complexity in influenza virus targeted drug design: interaction with human sialidases.
AID1331612Competitive inhibition of MDCK infected Influenza A virus A/WSN/33(H1N1) neuraminidase using MU-NANA as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by spectrofluorometric method2016European journal of medicinal chemistry, Nov-10, Volume: 123Design and synthesis of 1,2,3-triazole-containing N-acyl zanamivir analogs as potent neuraminidase inhibitors.
AID1895907Inhibition of Influenza A virus A/Goose/Guangdong/SH7/2013 (H5N1) neuraminidase using 2(4-methylurnbellifery1)-a-u-acetyl neuraminic acid sodium salt hydrate (4-MUNANA) as substrate preincubated for 10 mins followed by substrate addition and measured afte2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID1494239Inhibition of Influenza A virus (A/chicken/Bangli/BBVD-563/2007(H5N1)) clade 2 neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID140427Compound was tested for in vivo efficacy in mouse model of influenza A virus A/Singapore/1/57 at dose of 0.5 mg/kg (in)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID1409416Inhibition of Influenza A virus A/goose/Jiangsu/1306/2014(H5N8) neuraminidase N8 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID714639Inhibition of oseltamivir-resistant Influenza A virus A/WSN/1933/H275Y(H1N1) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by 2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID488379Inhibition of Influenza A virus neuraminidase2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Analogs of zanamivir with modified C4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses.
AID567717Ratio of IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1355763Inhibition of Influenza A virus (A/goose/Guangdong/SH7/2013(H5N1)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1181480Antiviral activity against Influenza A virus A/Virginia/ATCC3/2009 infected in MDCK cells assessed as virus-induced cytopathic effect after 72 hrs by microscopy2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID565242Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring hemagglutininin K234Q mutant gene and neuraminidase I222M and H274Y mutant infected in MDCK cells selected at 390 uM of oseltamivir after 9 passage after 48 hrs by hemag2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID565468Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase E119G mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID542982Inhibition of Influenza B virus (B/Saitama/01/2006(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1490017Inhibition of human N-terminal MBP-fused NEU2 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Selective Inhibitors of Human Neuraminidase 3.
AID565462Ratio of IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase I222V and H274Y mutant to IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID567719Ratio of IC50 for influenza A (A/Singapore/57/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1308651Inhibition of oseltamivir-resistant Influenza A virus A/Vietnam/1194/2004(H5N1) recombinant neuraminidase H275Y mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by 2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1308309Inhibition of Influenza A virus (A/California/04/2009(H1N1)) neuraminidase N1 V149I mutant activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID565268Ratio of IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222M mutant to IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID420935Inhibition of influenza A virus A/WSN/1933 H1N1 neuraminidase using NA-STAR substrate after 15 mins incubation at room temperature by fluorescent assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID542960Inhibition of Influenza A virus (A/Wellington/1/2004(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID542992Inhibition of Influenza B virus (B/Tokushima/1/2005(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1626682Binding affinity to recombinant Influenza A virus (A/Moscow/10/99(H3N2)) Neuraminidase N2 expressed in baculovirus infected insect cells measured up to 400 sec by surface plasmon resonance analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID524861Antimicrobial activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as reduction in viral titer in lung at 0.17 mg/kg, itn administered 11 hrs post infection measured after 59 hrs post infection2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID1355770Inhibition of Influenza A virus (A/Babol/36/2005(H3N2)) neuraminidase E119V mutant activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1360174Cytotoxicity against MDCK cells after 48 hrs by CellTiter96 aqueous non-radioactive cell proliferation assay2018European journal of medicinal chemistry, Jun-25, Volume: 154Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
AID565247Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 50 nM of zanamivir after 4 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID352035Inhibition of Influenza A virus (A/Kitakyushu/159/93(H3N2)) sialidase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID565255Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 5 nM of zanamivir after 2 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1308328Antiviral activity against Influenza A virus A/Kitakyushu/10/06(H1N1) infected in dog AX4 cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID542997Inhibition of Influenza A virus (A/turkey/Ontario/6,118/1968(H8N4)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID283444Inhibition of viral replication of influenza A virus (A/Hong Kong/213/03(H5N1)) and influenza A virus (A/Ann Arbor/6/60(H2N2)) hybrid virus in MDCK cells by neutral red uptake assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID712809Antiviral activity against amantadine-sensitive Influenza A virus (A/FM/1/47 (H1N1)) infected in MDCK cells assessed as virus-induced cytopathic effect measured 3 days post infection by microscopic analysis2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds.
AID542955Inhibition of Influenza A virus (A/Yamagata/83/2006(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID523881Antiviral activity against Influenza A virus (A/Texas/12/2007 (H3N2)) clone 1 with neuraminidase E119V mutant isolated from immunocompromized patient measured after X/CD4 additional passages in MDCK cells by NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID567605Antiviral activity against influenza A (A/Washington/29/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID565042Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells selected at 1 nM of oseltamivir after 1 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID612401Antiviral activity against influenza A virus A/WSN/1933 (H1N1) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Intramolecular ion-pair prodrugs of zanamivir and guanidino-oseltamivir.
AID1494264Antiviral activity against Influenza B virus (B/Perth/211/2001) infected in MDCK cells assessed as reduction in plaque formation measured after 3 days post infection by neutral red staining-based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1494267Ratio of IC50 for Influenza A virus (A/California/07/09 (H1N1)) neuraminidase measured every min for 60 mins to IC50 for Influenza A virus (A/California/07/09 (H1N1)) neuraminidase preincubated for 60 mins followed by substrate addition measured every min2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1736925Inhibition of Influenza A virus (A/goose/Jiangsu/1306/2014 (H5N8)) group-1 Neuraminidase N8 preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 to 60 mins by fluorescence method2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID543006Inhibition of Influenza A virus (A/Kawasaki/IMS22A-954/2003(H3N2)) wild type neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1604728Inhibition of Influenza A virus H5N1 Neuraminidase N1 H274Y mutant preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 mins by fluorescence method2020European journal of medicinal chemistry, Feb-01, Volume: 187Discovery of novel 1,2,3-triazole oseltamivir derivatives as potent influenza neuraminidase inhibitors targeting the 430-cavity.
AID203546Compound was tested for its inhibitory activity against B/Lee/40 sialidases.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID1360173Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in MDCK cells expressing neuraminidase H275Y mutant assessed as protection against virus-induced cytopathic effect after 48 hrs by CellTiter96 aqueous non-radioactive cell proliferat2018European journal of medicinal chemistry, Jun-25, Volume: 154Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1626689Antiviral activity against A/Puerto Rico/8/34(H1N1) genes expressing anamivir/oseltamivir resistant Influenza A virus (A/Moscow/10/99(H3N2)) harboring Neuraminidase N2 E119V/I222L double mutant infected in MDCK cells assessed as reduction in viral replica2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID542974Inhibition of Influenza B virus (B/Ohio/01/2005(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID567712Ratio of IC50 for influenza A (A/New York/18/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/10/2008 (H1N1)) virus expressing wild type enzyme by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1494275Ratio of IC50 for Influenza B virus (B/Perth/211/2001) neuraminidase measured every min for 60 mins to IC50 for Influenza B virus (B/Perth/211/2001) neuraminidase preincubated for 60 mins followed by substrate addition measured every min for 60 mins2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID384920Inhibition of influenza virus neuraminidase2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
QSAR study of neuraminidase inhibitors based on heuristic method and radial basis function network.
AID748614Inhibition of human NEU2 using 4MU-NeuAc as substrate after 15 to 30 mins by fluorimetric analysis2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Identification of Selective Nanomolar Inhibitors of the Human Neuraminidase, NEU4.
AID1405011Selectivity index, ratio of IC50 for MBP-fused recombinant human neuraminidase 4 to IC50 for MBP-fused recombinant human neuraminidase 22018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID543195Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 0.3 umol/kg, itn administered 4 hrs pre-infection and at 4 hrs and 17 hrs post-infection up to 10 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID306105Inhibition of sialidase in Human parainfluenza virus 3 C2432007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Synthesis and evaluation of 4-O-alkylated 2-deoxy-2,3-didehydro-N-acetylneuraminic acid derivatives as inhibitors of human parainfluenza virus type-3 sialidase activity.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID524854Antimicrobial activity against Influenza B virus (B/Malaysia/2506/2004) infected itn dosed Mustela putorius furo assessed as nasal viral titer treated after 4 hrs post infection measured after 1 day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID1241698Inhibition of recombinant Influenza A virus H5N1 neuraminidase2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.
AID565465Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) infected in MDCK cells after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID565238Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 625 nM of oseltamivir after 5 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1071476Inhibition of neuraminidase in Influenza A virus A/Hong Kong/68(H3N2) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID532111Inhibition of human NEU2 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using ganglioside GM3 substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID1494259Inhibition of Influenza B virus (B/Perth/211/2001) neuraminidase activity using 4-MUNANA as substrate assessed as reactivation half life by measuring reaction rate to reach 50% of maximum rate of uninhibited control after removal of inhibitor preincubated2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1405019Inhibition of MBP-fused recombinant human neuraminidase 4 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every 1 min for 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID722349Volume of distribution at steady state in Sprague-Dawley rat at 10 mg/kg, iv2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID420930Inhibition of influenza A virus A/Vietnam/1194/2004 H5N1 neuraminidase at 40 nM using NA-STAR substrate after 15 mins incubation at room temperature by fluorescent assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID515128Selectivity ratio of IC50 for Influenza B virus (B/Perth/211/2001) recombinant neuraminidase E197 mutant to IC50 for Influenza B virus (B/Perth/211/2001) neuraminidase E197 mutant preincubated for 30 mins2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1736920Antiviral activity against Influenza A virus (A/goose/Jiangsu/1306/2014 (H5N8)) group-1 infected in chicken embryo fibroblast assessed as reduction in viral infection preincubated for 1 hrs followed by fibroblast infection and measured after 72 hrs by hem2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID1494273Ratio of IC50 for Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase measured every min for 60 mins to IC50 for Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase preincubated for 60 mins followed by substrate addition measured every min for 60 mins2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID523883Antiviral activity against Influenza A virus (A/Washington/01/2007 (H3N2)) measured in MDCK cells by NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID543005Ratio of IC50 for Influenza A virus (A/Yokohama/67/2006(clone 11)(H1N1)) neuraminidase H274Y mutant to IC50 for Influenza A virus (A/Yokohama/67/2006(clone 1)(H1N1)) wild type neuraminidase2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID730331Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 hrs by crystal violet staining method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Aspulvinones from a mangrove rhizosphere soil-derived fungus Aspergillus terreus Gwq-48 with anti-influenza A viral (H1N1) activity.
AID1886446Inhibition of Influenza A virus A/PR/8/1934 (H1N1) neuraminidase using MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 mins by fluorescence based microplate reader method
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID542995Inhibition of Influenza A virus (A/R(duck/Mongolia/54/01-duck/Mongolia/47/01)(H5H1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1405015Inhibition of MBP-fused recombinant human neuraminidase 4 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID1903202Antiviral activity against Influenza B virus (B/Lee/1940) H1N1 infected in dog MDCK cells assessed as inhibition of viral cytopathic effect incubated for 48 hrs by CCK-8 assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA-Dependent RNA Polymerase (RdRp).
AID203667Compound was tested for its inhibitory activity against B/Victoria/102/85 (N2) sialidases.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID1308329Antiviral activity against Influenza A virus (A/Aichi/75/2008(H3N2)) infected in dog AX4 cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID567728Ratio of IC50 for influenza A (A/Singapore/57/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID523882Antiviral activity against Influenza A virus (A/Texas/12/2007 (H3N2)) clone 2 with neuraminidase E119I mutant isolated from immunocompromized patient measured after X/CD4 additional passages in MDCK cells by NA inhibition assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.
AID1736924Inhibition of Influenza A virus (A/Duck/Guangdong/674/2014 (H5N6)) group-2 Neuraminidase N6 preincubated for 10 mins followed by MUNANA substrate addition and measured after 40 to 60 mins by fluorescence method2020European journal of medicinal chemistry, Apr-01, Volume: 191Discovery of novel "Dual-site" binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors.
AID1626674Inhibition of zanamivir/oseltamivir resistant recombinant Influenza A virus (A/Moscow/10/99(H3N2)) Neuraminidase N2 E119V/I222L double mutant expressed in baculovirus infected insect cells using 4-MU-NANA as substrate preincubated for 30 mins followed by 2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1494274Ratio of IC50 for Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase E119G mutant measured every min for 60 mins to IC50 for Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase E119G mutant preincubated for 60 mins followed by substrate addition measured e2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1355761Inhibition of Influenza A virus (A/California/04/2009(H1N1)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1626700Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as protection against lethal virus challenge by measuring mouse survival at 20 mg/kg administered intranasally as single dose at 2 hrs post infection2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1308303Inhibition of Influenza A virus (A/duck/Tsukuba/20/2007(H8N4)) neuraminidase N4 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1409407Antiviral activity against Influenza A virus A/goose/Jiangsu/1306/2014(H5N8) infected in chicken embryo fibroblasts assessed as reduction in cytopathic effect after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1308299Inhibition of Influenza A virus (A/duck/Tsukuba/67/2005(H1N1)) neuraminidase N1 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID543204Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 166 ug/kg, itn administered 4 days pre-infection up to 20 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID147312Fold resistance of E119G to compound against neuraminidase in a MUNANA-based enzyme inhibition assay, expressed as the ratio of IC50 of comp. with variant N9 to that of with wild-type N92002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Structural studies of the resistance of influenza virus neuramindase to inhibitors.
AID1355762Inhibition of Influenza A virus (A/Babol/36/2005(H3N2)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID542954Inhibition of Influenza A virus (A/Aichi/169/2005(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1729970Inhibition of Influenza A virus (A/goose/Guangdong/SH7/2013(H5N1)) neuraminidase using 4-MU-NANA as substrate preincubated for 5 mins followed by substrate addition and measured after 30 to 60 mins by fluorescence assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID716614Inhibition of Influenza A virus A/WSN/1933(H1N1)) neuraminidase in the presence of 2'-(4-methyl-umbelliferyl)-alphaD-N-acetylneuraminic acid substrate after 10 mins by fluorometric assay2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
AID542999Inhibition of Influenza A virus (A/duck/England/1/1956(H11N6)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID542959Inhibition of Influenza A virus (A/Wyoming/03/2003(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID560872Inhibition of Influenza A virus (A/Turkey/651242/2006(H5N1)) neuraminidase by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID1308295Inhibition of human Neu2 expressed in HEK293T cells using 4MU-Neu5Ac as substrate incubated for 30 mins by HPLC analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID542965Inhibition of Influenza A virus (A/Shiga/5/2002(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID542950Inhibition of Influenza A virus (A/Yamagata/57/2002(H1N1)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID722600Cmax in Sprague-Dawley rat at 10 mg/kg, po2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
AID567598Antiviral activity against influenza A (A/North Carolina/02/2009 (H1N1)) virus after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1308305Inhibition of Influenza A virus (A/duck/Shiga/8/2004(H4N6)) neuraminidase N6 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID515134Fold resistance, ratio of IC50 for Influenza B virus B/Gifu/11/2005 wild type neuraminidase preincubated for 30 mins to IC50 for Influenza B virus B/Yamagata/186/05 neuraminidase N197 mutant preincubated for 30 mins2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1626709Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as respiratory epithelium desquamation at 20 mg/kg qd administered intranasally as single dose at 2 hrs post infection measured after 7 days post inf2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1308643Antiviral activity against oseltamivir-resistant Influenza A virus A/WSN/1933(H1N1) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 hrs by CellTiter 96 AQueous Non-Radioactive cell proliferation assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID1729969Inhibition of Influenza A virus (A/Babol/36/2005 (H3N2)) neuraminidase using 4-MU-NANA as substrate preincubated for 5 mins followed by substrate addition and measured after 30 to 60 mins by fluorescence assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID515139Fold resistance, ratio of Ki for Influenza B virus B/Gifu/11/2005 wild type neuraminidase to Ki for Influenza B virus B/Yamagata/186/05 neuraminidase N197 mutant2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1626706Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Balb/c mouse assessed as immune cell infiltration in lungs at 5 mg/kg qd administered intranasally for 7 days starting from 1 day post infection by hematoxylin and eosin s2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID716598Cytotoxicity against MDCK cells at 100 uM2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Enhanced anti-influenza agents conjugated with anti-inflammatory activity.
AID1152624Selectivity index, ratio of CC50 for MDCK cells to IC50 for Influenza A virus (A/Vietnam/1194/2004(H5N1))2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Design, synthesis and biological evaluation of small molecular polyphenols as entry inhibitors against H(5)N(1).
AID543186Inhibition of Influenza A virus (A/Kawasaki/MS31A-1030/2002(H3N2)) wild type neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID567602Antiviral activity against influenza A (A/North Carolina/01/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1494242Inhibition of Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID525083Antimicrobial activity against Influenza B virus (B/Hong Kong/05/1972) infected in BALB/c mouse assessed as increase in mouse survival at 1.1 mg/kg, itn administered for 7 days before infection measured at day 202010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration.
AID1729980Cytotoxicity against MDCK cells assessed as reduction in cell viability by MTT assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID1494250Inhibition of Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase E119V mutant activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1408325Antiviral activity against Influenza A virus A/Virginia/ATCC3/2009(H1N1pdm) infected in MDCK cells after 3 days by MTS assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID1181485Cytotoxicity against MDCK cells assessed as change in cell morphology after 72 hrs by microscopy2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Semisynthetic teicoplanin derivatives as new influenza virus binding inhibitors: synthesis and antiviral studies.
AID488375Inhibition of Influenza A virus A/WSN/1933(H1N1) neuraminidase2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Analogs of zanamivir with modified C4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses.
AID714644Inhibition of Influenza A virus (A/reassortant/NIBRG-14(Viet Nam/1194/2004 x Puerto Rico/8/1934)(H5N1)) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prio2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID565240Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring hemagglutininin K234Q mutant gene and neuraminidase I222M mutant infected in MDCK cells selected at 16 uM of oseltamivir after 7 passage after 48 hrs by hemagglutininin 2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID543187Inhibition of Influenza A virus (A/Kawasaki/MS31A-1030/2002(H3N2)) neuraminidase N294S mutant after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1409417Inhibition of Influenza A virus A/Anhui/1/2005(H5N1) neuraminidase N1 H274Y mutant using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID92334Antiinfluenza activity of compound against Influenza A/Sydney/5/97 in influenza cytopathic effect (CPE) assay2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID565467Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222V and H274Y mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1064128Inhibition of Influenza A virus A/Hong Kong/8/1968 (H3N2) neuraminidase using MUNANA as substrate preincubated for 30 mins measured after 2 hrs2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Bifunctional thiosialosides inhibit influenza virus.
AID1626692Cytotoxicity against MDCK cells assessed as reduction in cell viability after 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID647176Cytotoxicity against MDCK cells by MTT assay2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Synthesis and antiviral activities of novel gossypol derivatives.
AID1889674Inhibition of NEU2 (unknown origin) using Neu5Acalpha2-3GalbetapNP as substrate incubated for 30 mins2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID565241Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring hemagglutininin K234Q mutant gene and neuraminidase I222M and H274Y mutant infected in MDCK cells selected at 78 uM of oseltamivir after 8 passage after 48 hrs by hemagg2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID542996Inhibition of Influenza A virus (A/duck/Hokkaido/84/2002(H5N3)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1308314Inhibition of Influenza A virus (A/Aichi/102/2008(H3N2)) neuraminidase N2 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID532112Inhibition of human NEU3 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using ganglioside GM3 substrate2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID1064127Inhibition of Influenza A virus A/California/07/2009 (H1N1) neuraminidase using MUNANA as substrate preincubated for 30 mins measured after 2 hrs2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Bifunctional thiosialosides inhibit influenza virus.
AID1886451Inhibition of Influenza A virus A/Anhui/1/2005 (H5N1) Neuraminidase H274Y mutant using MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 mins by fluorescence based microplate reader method
AID714636Inhibition of Influenza A virus A/Udorn/1972(H3N2) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID717169Cytotoxicity against dog MDCK cells assessed as cell viability by MTS assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1308330Antiviral activity against Influenza A virus (A/Aichi/102/2008(H3N2)) infected in dog AX4 cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1360696Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as protection against virus-induced reduction in cell viability after 3 to 6 days by MTS assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR).
AID1405013Inhibition of MBP-fused recombinant human neuraminidase 2 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID567710Ratio of IC50 for influenza A (A/Singapore/57/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1308321Antiviral activity against Influenza A virus (A/duck/Shiga/8/2004(H4N6)) infected in MDCK cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID565257Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 125 nM of zanamivir after 4 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1886449Inhibition of Influenza A virus A/Aichi/2/1968 (H3N2) neuraminidase using MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 mins by fluorescence based microplate reader method
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1813707Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in dog MDCK cells assessed as inhibition of viral replication preincubated for 2 hrs followed by viral infection and measured after 72 hrs by CCK8 assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Zanamivir-Cholesterol Conjugate: A Long-Acting Neuraminidase Inhibitor with Potent Efficacy against Drug-Resistant Influenza Viruses.
AID1409413Inhibition of Influenza A virus A/duck/Guangdong/674/2014(H5N6) neuraminidase N6 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID543190Inhibition of Influenza B virus (B/Yokohama/UT3318/2005)) neuraminidase N294S mutant after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1204714Total plasma concentration in CD1 mouse at 30 mg/kg, po measured at 20 mins by reversed-phase UPLC/MS analysis2015Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12
Assessing the oral bioavailability of difluorosialic acid prodrugs, potent viral neuraminidase inhibitors, using a snapshot PK screening assay.
AID567599Antiviral activity against influenza A (A/New York/18/2009 (H1N1)) virus after 30 mins by MUNANA substrate based fluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID543188Ratio of IC50 for Influenza A virus (A/Kawasaki/MS31A-1030/2002(H3N2)) neuraminidase N294S mutant to IC50 for Influenza A virus (A/Kawasaki/MS31A-1030/2002(H3N2)) wild type neuraminidase2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1064130Antiviral activity against Influenza A virus A/Hong Kong/8/1968 (H3N2) infected in MDCK cells assessed as reduction in virus plaque formation after 5 days2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Bifunctional thiosialosides inhibit influenza virus.
AID543191Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 66 ug/kg, itn administered 4 hrs pre-infection and at 4 hrs and 18 hrs post-infection up to 10 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID565054Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 25 nM of oseltamivir after 3 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID314411Inhibition of influenza A/N1/PR/8/34 neuraminidase2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
Synthesis of potent pyrrolidine influenza neuraminidase inhibitors.
AID543182Ratio of IC50 for Influenza A virus (A/Kawasaki/IMS22A-954/2003(H3N2)) neuraminidase R292K mutant to IC50 for Influenza A virus (A/Kawasaki/IMS22A-954/2003(H3N2)) wild type neuraminidase2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID717170Cytotoxicity against dog MDCK cells assessed as cell morphology alterations by microscopic analysis2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
AID1152622Antiviral activity against Influenza A virus (A/Vietnam/1194/2004(H5N1)) infected in MDCK cells assessed as inhibition of viral replication after 2 to 3 days by crystal violet staining-based plaque reduction assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Design, synthesis and biological evaluation of small molecular polyphenols as entry inhibitors against H(5)N(1).
AID542956Inhibition of Influenza A virus (A/Singapore/1/1957(H2N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID542969Inhibition of Influenza A virus (A/Osaka/56/2004(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID515131Fold resistance, ratio of IC50 for Influenza B virus B/Gifu/11/2005 wild type neuraminidase to IC50 for Influenza B virus B/Yamagata/186/05 neuraminidase N197 mutant2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID1308302Inhibition of Influenza A virus (A/duck/Tsukuba/394/2005(H5N3)) neuraminidase N3 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID567614Antiviral activity against influenza A (A/Montana/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID542958Inhibition of Influenza A virus (A/Kitakyushu/159/1993(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID567725Ratio of IC50 for influenza A (A/Osaka/180/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1494247Inhibition of Influenza B virus (B/Perth/211/2001) neuraminidase D197E mutant activity using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1308306Inhibition of Influenza A virus (A/duck/Tsukuba/700/2007(H7N7)) neuraminidase N7 activity using 4MU-Neu5Ac as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by fluorescence analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID203373Inhibitory activity against influenza B sialidase (Victoria)2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides.
AID1729979Antiviral activity against Influenza A virus (A/WSN/67/05(H3N2)) infected in MDCK cells as reduction in plaque formation2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID352038Inhibition of Tamiflu-resistant Influenza A virus (A/Yokohama/67/2006 (H1N1)) sialidase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en.
AID343686Inhibition of influenza virus neuraminidase2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Ensemble-based virtual screening reveals potential novel antiviral compounds for avian influenza neuraminidase.
AID1064129Antiviral activity against Influenza A virus A/California/07/2009 (H1N1) infected in MDCK cells assessed as reduction in virus plaque formation after 5 days2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Bifunctional thiosialosides inhibit influenza virus.
AID567615Antiviral activity against influenza A (A/Osaka/180/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 16 to 18 hrs by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID1409410Antiviral activity against Influenza A virus (A/Wisconsin/67/2005(H3N2)) infected in MDCK cells after 2 days by plaque reduction assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1071470Antiviral activity against Influenza A virus A/Jena/5258/2009(H1N1) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID1308325Antiviral activity against Influenza A virus (A/California/04/2009(H1N1)) infected in dog AX4 cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID712816Antiviral activity against amantadine-resistant Influenza A virus (A/PR/8/34 (H1N1)) infected in MDCK cells assessed as virus-induced cytopathic effect measured 3 days post infection by microscopic analysis2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds.
AID515138Fold resistance, ratio of Ki for Influenza B virus (B/Perth/211/2001) wild type recombinant neuraminidase preincubated for 30 mins to Ki for Influenza B virus (B/Perth/211/2001) neuraminidase E197 mutant preincubated for 30 mins2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses.
AID567707Ratio of IC50 for influenza A (A/Osaka/180/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID543003Inhibition of Influenza A virus (A/Yokohama/67/2006(clone 1)(H1N1)) wild type neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1308645Inhibition of Influenza A virus A/WSN/1933(H1N1) recombinant neuraminidase H275Y mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured aft2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID1731308Inhibition of Influenza B virus B/Sichuan/01/96 neuraminidase using MUNANA as substrate measured after 60 mins by fluorescence assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors.
AID1241701Competitive inhibition of recombinant Influenza A virus H1N1 neuraminidase using MU-NANA as substrate2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.
AID565251Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring hemagglutininin K234N mutant gene and neuraminidase D198G mutant infected in MDCK cells selected at 31 uM of compound after 8 passage after 48 hrs by hemagglutininin titer2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1409404Antiviral activity against Influenza A virus A/goose/Guangdong/SH7/2013(H5N1) infected in chicken embryo fibroblasts assessed as reduction in cytopathic effect after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID567593Antiviral activity against influenza A (A/Osaka/180/2009 (H1N1)) virus harboring neuraminidase H275Y mutant after 30 mins by NA-star substrate based chemiluminescent assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID542981Inhibition of Influenza B virus (B/Aichi/3/2006(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID314410Inhibition of influenza B/Memphis/3/89 neuraminidase2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
Synthesis of potent pyrrolidine influenza neuraminidase inhibitors.
AID1405010Selectivity index, ratio of IC50 for MBP-fused recombinant human neuraminidase 4 to IC50 for MBP-fused recombinant human neuraminidase 32018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID1494234Inhibition of Influenza A virus (A/California/07/09 (H1N1)) neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID565264Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222V mutant infected in MDCK cells assessed as inhibition of viral-induced cytopathogenicity after 4 days post dose2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1626696Half life in Sprague-Dawley rat at 6 umol/kg, iv by HPLC analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.
AID1494252Inhibition of Influenza A virus (A/NWS/G70C(H1N9)) neuraminidase E119G mutant activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID461108Antiviral activity against Influenza A virus (A/Korea/KBNP-0028/2000(H9N2)) infected in chicken egg after 5 days by hemagglutinination assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Anti-influenza diarylheptanoids from the bark of Alnus japonica.
AID718739Toxicity in MDCK cells assessed as induction of cell morphology changes2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Synthesis of isoindole and benzoisoindole derivatives of teicoplanin pseudoaglycon with remarkable antibacterial and antiviral activities.
AID1241705Therapeutic index, ratio of CC50 for MDCK cells to IC50 for Influenza A virus H1N12015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.
AID1494229Inhibition of Influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID704187Inhibition of Influenza A virus sialidase N22012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Exploring the interactions of unsaturated glucuronides with influenza virus sialidase.
AID420927Inhibition of influenza A virus A/WSN/1933 H1N1 neuraminidase at 10 nM using NA-STAR substrate after 15 mins incubation at room temperature by fluorescent assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synergistic effect of zanamivir-porphyrin conjugates on inhibition of neuraminidase and inactivation of influenza virus.
AID565271Ratio of IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222V mutant to IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID560875Inhibition of Influenza A virus (A/duck/Laos/25/2006(H5N1)) neuraminidase by fluorometric assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID133478Number of virus free mice from total 9 mice infected with Influenza A/Singapore/1/57 after 12.5 mg/kg of intranasal administration for 51 hr prior to viral infection2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
AID1494263Antiviral activity against Influenza A virus (A/NWS/G70C(H1N9)) infected in MDCK cells assessed as reduction in plaque formation measured after 3 days post infection by neutral red staining-based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID714642Inhibition of Influenza A virus A/Taiwan/3446/2002(H3N2) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID1308327Antiviral activity against Influenza A virus A/Yamaguchi/20/06(H1N1) infected in dog AX4 cells preincubated for 1 hr followed by infection measured after 19 to 20 hrs by galactosidase-based fluorescence assay and peroxidase-based chromogenic assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID1241699Inhibition of recombinant Influenza A virus H3N2 neuraminidase2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.
AID542966Inhibition of Influenza A virus (A/Yamagata/1/2002(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID560878Inhibition of Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) neuraminidase by Michaelis-Menten equation analysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidase inhibitor oseltamivir differs in vitro and in a mouse model.
AID203545Compound was tested for its inhibitory activity against B/Beijing/1/87 (N2) sialidases.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID1485251Antiviral activity against Influenza A virus A/Virginia/ATCC3/2009(H1N1) infected in MDCK cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by formazan-based colorimetric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1494270Ratio of IC50 for Influenza A virus (A/chicken/Bangli/BBVD-563/2007(H5N1)) clade 2 neuraminidase measured every min for 60 mins to IC50 for Influenza A virus (A/chicken/Bangli/BBVD-563/2007(H5N1)) clade 2 neuraminidase preincubated for 60 mins followed by2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1405017Inhibition of MBP-fused recombinant human neuraminidase 2 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every 1 min for 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 10-15, Volume: 26, Issue:19
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.
AID565253Antiviral activity against Influenza A virus (A/Vietnam/1203/2004 (H5N1)) harboring hemagglutininin K234N mutant gene and neuraminidase D198G mutant infected in MDCK cells selected at 781 uM of zanamivir after 10 passage after 48 hrs by hemagglutininin ti2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID542990Inhibition of Influenza B virus (B/Saitama/01/2005(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1494255Inhibition of Influenza A virus (A/chicken/Vietnam/08/2004 (H5N1)) clade 1 neuraminidase activity using 4-MUNANA as substrate assessed as reactivation half life by measuring reaction rate to reach 50% of maximum rate of uninhibited control after removal o2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID542967Inhibition of Influenza A virus (A/Yamagata/2/2002(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1204717Total plasma concentration in CD1 mouse at 30 mg/kg, po measured at 60 mins by reversed-phase UPLC/MS analysis2015Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12
Assessing the oral bioavailability of difluorosialic acid prodrugs, potent viral neuraminidase inhibitors, using a snapshot PK screening assay.
AID542963Inhibition of Influenza A virus (A/Hiroshima/52/2005(H3N2)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1610155Antiviral activity against Influenza A virus (A/Ned/378/05(H1N1)) infected in dog MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 7 days by microscopic analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID567727Ratio of IC50 for influenza A (A/Hong Kong/2369/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/29/2009 (H1N1)) virus expressing wild type enzyme by fetuin substrate based colorimetric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1129833Inhibition of Influenza A virus (A/RI/5+/1957(H2N2)) recombinant neuraminidase using MUNANA as substrate at 100 uM after 30 mins2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Benzophenone C-glucosides and gallotannins from mango tree stem bark with broad-spectrum anti-viral activity.
AID1408328Antiviral activity against Influenza B virus B/Ned/537/05 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 3 days by microscopic method2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID542994Inhibition of Influenza B virus (B/Yamagata/113/2005(Yamagata)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID565052Antiviral activity against Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) infected in MDCK cells selected at 1 nM of oseltamivir after 1 passage after 48 hrs by hemagglutininin titer assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID461110Cytotoxicity against CEF cells by MTT assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Anti-influenza diarylheptanoids from the bark of Alnus japonica.
AID567702Ratio of IC50 for influenza A (A/North Carolina/02/2009 (H1N1)) virus harboring neuraminidase H275Y mutant to IC50 for influenza A (A/Washington/10/2008 (H1N1)) virus expressing wild type enzyme expressing wild type enzyme by NA-star substrate based chemi2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Assessment of pandemic and seasonal influenza A (H1N1) virus susceptibility to neuraminidase inhibitors in three enzyme activity inhibition assays.
AID543183Inhibition of Influenza A virus (A/Yokohama/IMS9A-2029/2003(H3N2)) wild type neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1308298Inhibition of human Neu4 expressed in HEK293T cells using GM3 as substrate incubated for 30 mins by HPLC analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
A Novel Potent and Highly Specific Inhibitor against Influenza Viral N1-N9 Neuraminidases: Insight into Neuraminidase-Inhibitor Interactions.
AID203357Compound was tested for inhibitory concentration against Influenza sialidase type A1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 2. Crystallographic and molecular modeling study of complexes of 4-amino-4H-pyran-6-carboxamides and sialidase from influenza virus types A and B.
AID1490013Inhibition of human N-terminal MBP-fused NEU2 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every minute for 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Selective Inhibitors of Human Neuraminidase 3.
AID1308648Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant neuraminidase E119A mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition meas2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID1241707Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced change in cell morphology at 10 ug/ml after 2 days by microscopic analysis2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.
AID1355793Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in plaque formation after 2 days by toluidine blue staining-based assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID565270Ratio of IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring neuraminidase I222M and H274Y mutant to IC50 for Influenza A virus (A/Chicken/Laos/26/2006(H5N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1064131Inhibition of Influenza A virus H3N2 neuraminidase using MUNANA as substrate preincubated for 30 mins measured after 2 hrs2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Bifunctional thiosialosides inhibit influenza virus.
AID712810Antiviral activity against amantadine-sensitive Influenza A virus (A/Ned/378/05 (H1N1)) infected in MDCK cells assessed as virus-induced cytopathic effect measured 3 days post infection by microscopic analysis2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds.
AID1308649Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant neuraminidase R292K mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition meas2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID1308644Cytotoxicity against MDCK cells after 48 hrs by CellTiter 96 AQueous Non-Radioactive cell proliferation assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
AID565459Ratio of IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring neuraminidase H274Y mutant to IC50 for Influenza A virus A/New Caledonia/20/99 (H1N1)) harboring wild type neuraminidase2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro generation of neuraminidase inhibitor resistance in A(H5N1) influenza viruses.
AID1494231Inhibition of Influenza A virus (A/Mississippi/03/01 (H1N1)) neuraminidase H274Y mutant using 4-MUNANA as substrate measured every min for 60 mins by fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID543203Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in mouse infection model at 166 ug/kg, itn administered 7 days pre-infection up to 20 days2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID1729972Inhibition of Influenza A virus (A/Anhui/1/2005(H5N1)) neuraminidase H274Y mutant using 4-MU-NANA as substrate preincubated for 5 mins followed by substrate addition and measured after 30 to 60 mins by fluorescence assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.
AID542978Inhibition of Influenza B virus (B/Tokushima/1/2003(Victoria)) neuraminidase after 30 mins by fluorescence analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1494272Ratio of IC50 for Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase E119V mutant measured every min for 60 mins to IC50 for Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase E119V mutant preincubated for 60 mins followed by substrate addition meas2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.
AID1355767Inhibition of Influenza A virus (A/chicken/china/415/2013(H9N2)) neuraminidase activity using 4-MUNANA as substrate preincubated for 10 mins followed by substrate addition and measured after 40 to 60 mins by chemiluminescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1408333Cytotoxicity against MDCK cells assessed as alteration in cell morphology after 3 days by microscopic method2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID1408329Antiviral activity against Influenza B virus B/Ned/537/05 infected in MDCK cells after 3 days by MTS assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.
AID1610161Cytotoxicity against dog MDCK cells assessed as minimum cytotoxic concentration by observing alteration in cell morphology incubated for 3 days by microscopic analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID714634Terminal half life in Sprague-Dawley rat at 10 mg/kg, po2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID693524Antiviral activity against Influenza A/PR/8/34 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect measured on day 3 post infection by MTS assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis of fluorescent ristocetin aglycon derivatives with remarkable antibacterial and antiviral activities.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1795717Neuraminidase Inhibition Assay from Article 10.1021/jm970374b: \\Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.
AID1802683Sialidase Assay from Article 10.1186/1471-2091-13-19: \\Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases.\\2012BMC biochemistry, Oct-02, Volume: 13Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases.
AID1795726Neuraminidase Inhibition Assay from Article 10.1021/jm010277p: \\Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity.\\2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB1998Structure (London, England : 1993), Jun-15, Volume: 6, Issue:6
Drug design against a shifting target: a structural basis for resistance to inhibitors in a variant of influenza virus neuraminidase.
AID1811Experimentally measured binding affinity data derived from PDB1998Structure (London, England : 1993), Jun-15, Volume: 6, Issue:6
Drug design against a shifting target: a structural basis for resistance to inhibitors in a variant of influenza virus neuraminidase.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 2. Crystallographic and molecular modeling study of complexes of 4-amino-4H-pyran-6-carboxamides and sialidase from influenza virus types A and B.
AID1811Experimentally measured binding affinity data derived from PDB1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 2. Crystallographic and molecular modeling study of complexes of 4-amino-4H-pyran-6-carboxamides and sialidase from influenza virus types A and B.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,133)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's113 (9.97)18.2507
2000's397 (35.04)29.6817
2010's537 (47.40)24.3611
2020's86 (7.59)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 73.91

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index73.91 (24.57)
Research Supply Index7.13 (2.92)
Research Growth Index4.80 (4.65)
Search Engine Demand Index131.85 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (73.91)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials85 (7.28%)5.53%
Reviews215 (18.41%)6.00%
Case Studies57 (4.88%)4.05%
Observational7 (0.60%)0.25%
Other804 (68.84%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (25)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase I, Randomized, Placebo-Controlled, Four-Way Crossover Study to Evaluate the Effect of Intravenous (IV) Zanamivir on Cardiac Conduction as Assessed by 12-lead Electrocardiogram (ECG) With Moxifloxacin as a Positive Control in Healthy Volunteers [NCT01353729]Phase 140 participants (Actual)Interventional2011-05-19Completed
Role of Neuraminidase Activity on Endothelial Dysfunction in Type 2 Diabetes [NCT04867707]Phase 214 participants (Actual)Interventional2021-07-14Active, not recruiting
A Phase IV, Multi-center, Randomized, Partially Double Blinded, Placebo Controlled Study, to Evaluate the Safety of Daily Inhaled Zanamivir 10 mg Versus Placebo and Daily Oral Oseltamivir 75 mg Versus Placebo for Influenza Prophylaxis in Healthy Volunteer [NCT00980109]Phase 4390 participants (Actual)Interventional2009-09-30Completed
An Open-label, Multi-center, Single Arm Study to Evaluate the Safety and Tolerability of Intravenous Zanamivir in the Treatment of Hospitalized Adult, Adolescent and Pediatric Subjects With Confirmed Influenza Infection [NCT01014988]Phase 2202 participants (Actual)Interventional2009-11-30Completed
Efficacy and Safety of Combination Therapies With Oseltamivir & Zanamivir or Oseltamivir & Amantadine Versus Oseltamivir Monotherapy in the Treatment of Seasonal Influenza A Infection [NCT00830323]Phase 260 participants (Anticipated)Interventional2009-01-31Terminated
A Randomized, Double Blinded, Parallel Study to Evaluate the Pharmacokinetics of Zanamivir After Single and Repeated Dose (300 mg and 600 mg) Infusion Administration in Healthy Chinese Adults [NCT02377401]Phase 124 participants (Actual)Interventional2015-04-28Completed
Multicentre, Randomized, Controlled Clinical Trial Comparing Oseltamivir With Placebo And Zanamivir With Control As The First Line Treatment For Human Swine Influenza (H1N1) Infection In Designated Flu Clinics During The Pandemic Influenza in Hong Kong [NCT00979667]Phase 34 participants (Actual)Interventional2009-10-31Terminated(stopped due to Decreased Influenza activity; thus decrease/no eligible patient to recruit)
A Pilot Study for a Randomized Controlled Trial to Compare Trivalent Split Virus Influenza Vaccine to Seasonal Antiviral Prophylaxis in Healthcare and Other Healthy Adults: Assessment of Zanamivir Versus Vaccine (Stop-Flu-2) [NCT00784784]Phase 364 participants (Actual)Interventional2008-11-30Completed
Phase 1, Open-Label Study to Evaluate Potential Pharmacokinetic Interactions Between Orally-Administered Oseltamivir and Intravenous Zanamivir in Healthy Thai Adult Subjects [NCT00921726]Phase 117 participants (Actual)Interventional2009-07-31Completed
Randomised, Parallel Dose, Phase 1/2 Safety and Pharmacokinetics Study of Inhaled Laninamivir Octanoate TwinCaps® Dry Powder Inhaler in Children With Naturally Acquired Influenza A or B [NCT02014649]Phase 1/Phase 215 participants (Actual)Interventional2013-11-30Terminated(stopped due to Study was terminated as per BARDA decision to terminate contract.)
A Randomized, Placebo Controlled, 3-Way Crossover Study to Investigate the Safety, Tolerability, and Pharmacokinetics of Repeat Dose Zanamivir/Placebo 10mg Administered Twice Daily for 5 Days by a Rotahaler Compared to the Diskhaler in Healthy Subjects [NCT00989404]Phase 118 participants (Actual)Interventional2009-10-12Completed
Evaluation of Combination Therapy With Oseltamivir and Zanamivir Versus Monotherapy in the Treatment of Virologically Confirmed Influenza in Primary Care a Randomises Double Blind Controlled Trial Study [NCT00799760]Phase 3541 participants (Actual)Interventional2008-12-31Terminated(stopped due to Just Terminated for the end of the pandemia)
A Phase III International, Randomized, Double-blind, Double-dummy Study to Evaluate the Efficacy and Safety of 300 mg or 600 mg of Intravenous Zanamivir Twice Daily Compared to 75 mg of Oral Oseltamivir Twice Daily in the Treatment of Hospitalized Adults [NCT01231620]Phase 3626 participants (Actual)Interventional2011-01-15Completed
Special Drug Use Investigation for Relenza® (Zanamivir) (Prophylaxis) [NCT01390792]622 participants (Actual)Observational2007-01-31Completed
ADaptive ASsessment of TReatments for influenzA: A Phase 2 Multi-centre Adaptive Randomised Platform Trial to Assess Antiviral Pharmacodynamics in Early Symptomatic Influenza Infection (AD ASTRA) [NCT05648448]Phase 2250 participants (Anticipated)Interventional2023-02-22Recruiting
Phase 1, Open-Label Study to Evaluate Potential Pharmacokinetic Interactions Between Orally-Administered Oseltamivir and Intravenous Zanamivir in Healthy Thai Adult Subjects [NCT00540501]Phase 10 participants (Actual)Interventional2007-10-31Withdrawn(stopped due to Contract agreement not reached)
Zanamivir Treatment of Vascular Permeability in Dengue (ZAP-DENGUE): A Pilot Randomized Controlled Trial [NCT04597437]Early Phase 174 participants (Anticipated)Interventional2023-12-01Not yet recruiting
A Pilot, Randomized Study Comparing the Safety, Tolerability and Pharmacokinetics of Combination Therapy (Amantadine, Ribavirin, Oseltamivir) Versus Neuraminidase Inhibitor Monotherapy to Influenza Virus Infected Immunocompromised Patients [NCT00867139]Phase 1/Phase 27 participants (Actual)Interventional2009-03-31Completed
An Open-label, Multi-centre, Single Arm Study to Evaluate the Safety and Efficacy of Intravenous Zanamivir in the Treatment of Hospitalized Patients With Confirmed Influenza Infection (NAI115215) [NCT01527110]Phase 321 participants (Actual)Interventional2012-01-01Completed
Collection of Patients' Background InformationRelenza® Sentinel Site Monitoring Program in Japan [NCT01199744]1,575 participants (Actual)Observational2009-11-30Completed
Assessing the Safety of Inhaled Zanamivir Exposure in Pregnant Women [NCT01462487]1 participants (Actual)Observational2011-07-31Completed
Prophylactic Efficacy of Relenza Against Influenza A and B [NCT01156701]171,705 participants (Actual)Observational2009-07-31Completed
Randomised, Double-blind, Placebo-controlled Trial of Inhaled Zanamivir in Treatment of Influenza A and B Virus Infections in China [NCT01459081]Phase 3298 participants (Actual)Interventional2011-10-31Completed
A Phase 2 Randomized, Double Blind, Placebo Controlled, Parallel Arm Study to Investigate the Efficacy and Safety of Inhaled Laninamivir Octanoate TwinCaps® Dry Powder Inhaler in Adults With Symptomatic Influenza A or B Infection [NCT01793883]Phase 2639 participants (Actual)Interventional2013-05-31Completed
An Open Label, Single Arm Study to Evaluate Single and Multiple Dose Pharmacokinetics, Safety and Tolerability, and to Explore Clinical Outcomes of Treatment With Intravenous (IV) Zanamivir in Neonates and Infants Under 6 Months of Age With Confirmed Comp [NCT04494412]Phase 212 participants (Anticipated)Interventional2022-11-21Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00784784 (2) [back to overview]Number of Subjects Adhering to Long-term Zanamivir Prophylaxis
NCT00784784 (2) [back to overview]Number of Laboratory Confirmed Influenza Infections
NCT00867139 (12) [back to overview]Number of Participants With Adverse Events (AEs), Drug Specific AEs or AEs Resulting in Treatment Interruption
NCT00867139 (12) [back to overview]Days on Supplemental Oxygen
NCT00867139 (12) [back to overview]Duration of Hospitalization
NCT00867139 (12) [back to overview]Duration of Symptoms
NCT00867139 (12) [back to overview]Frequency of Confirmed Pneumonia
NCT00867139 (12) [back to overview]Number of Deaths
NCT00867139 (12) [back to overview]Number of Participants With ICU Admissions
NCT00867139 (12) [back to overview]Number of Participants With Intubations
NCT00867139 (12) [back to overview]Number of Participants With Viral Load Decrease as a Function of Time
NCT00867139 (12) [back to overview]Number of Participants With Viral Resistance as a Function of Drug Exposure
NCT00867139 (12) [back to overview]Pharmacokinetics (AUC0-last) of TCAD
NCT00867139 (12) [back to overview]Number of Patients Not Shedding Virus at Day 5 +/-1 and Day 10 +/- 1
NCT01014988 (33) [back to overview]Geometric Mean Terminal Half Life (t1/2) of Zanamivir
NCT01014988 (33) [back to overview]Geometric Mean Volume of Distribution (Vd) of Zanamivir
NCT01014988 (33) [back to overview]Mean Viral Susceptibility to Zanamivir at Baseline (Day 1) and All Post-Baseline Visits Collectively
NCT01014988 (33) [back to overview]Median Body Temperature at Baseline (Day 1) and Day 5
NCT01014988 (33) [back to overview]Median Time to Clinical Response (Sustained Resolution) of All Vital Signs (Composite)
NCT01014988 (33) [back to overview]Median Corrected QT Interval (QTc) for Heart Rate by Fridericia's Formula (QTcF) and Bazett's Formula (QTcB) at Baseline (Day 1) and Day 5
NCT01014988 (33) [back to overview]Median Duration of Hospitalization and Intensive Care Unit (ICU) Stays
NCT01014988 (33) [back to overview]Median Heart Rate at Baseline (Day 1) and Day 5
NCT01014988 (33) [back to overview]Median Oxygen Saturation Measured Via Transcutaneous Oximetry (TCPO2) at Baseline (Day 1) and Day 5
NCT01014988 (33) [back to overview]Median Respiration Rate at Baseline (Day 1) and Day 5
NCT01014988 (33) [back to overview]Median Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Baseline (Day 1) and Day 5
NCT01014988 (33) [back to overview]Number of Participants Assessed as Normal/Abnormal (Clinically Significant [CS] and Not Clinically Significant [NCS]) for 12-lead Electrocardiogram (ECG) at Baseline (Day 1)
NCT01014988 (33) [back to overview]Number of Participants With the Indicated Clinical Chemistry Values Relative to the Normal Range at Baseline (Day 1) and Day 5
NCT01014988 (33) [back to overview]Number of Participants With the Indicated Hematology Values Relative to the Normal Range at Baseline (Day 1) and Day 5
NCT01014988 (33) [back to overview]Number of Participants With the Indicated Mortality Status at Day 14 and Day 28
NCT01014988 (33) [back to overview]Number of Participants With the Indicated Treatment-emergent (TE) Grade 3/4 Clinical Chemistry Toxicities
NCT01014988 (33) [back to overview]Number of Participants With the Indicated Treatment-emergent (TE) Grade 3/4 Hematology Toxicities
NCT01014988 (33) [back to overview]Number of Participants With the Indicated Ventilation Status: Modality of Supplemental Oxygen Delivery and Mechanical Ventilation
NCT01014988 (33) [back to overview]Median Time to Resolution of Individual Vital Signs
NCT01014988 (33) [back to overview]Median Time to Return to Pre-morbid Functional Status
NCT01014988 (33) [back to overview]Median Change From Baseline (Influenza A or B Quantitative PCR, as Appropriate) in Viral Load at the Indicated Time Points
NCT01014988 (33) [back to overview]Median Time to Virologic Improvement
NCT01014988 (33) [back to overview]Number of Participants Who Permanently Discontinued the Study Treatment Due to an AE
NCT01014988 (33) [back to overview]Number of Participants Who Used Any Concomitant Antibiotic Medications for Complications of Influenza
NCT01014988 (33) [back to overview]Number of Participants Who Were Permanently Discontinued From the Study Due to an AE
NCT01014988 (33) [back to overview]Number of Participants With Any Adverse Event (AE) Considered to be Related to Study Treatment
NCT01014988 (33) [back to overview]Number of Participants With Treatment-emergent (TE) Mutations
NCT01014988 (33) [back to overview]Number of Participants With Any AE Categorized as an Influenza Complication
NCT01014988 (33) [back to overview]Number of Participants With Any Severe or Grade 3/4 AEs
NCT01014988 (33) [back to overview]Number of Participants With Any Severe or Grade 3/4 Treatment-related AE
NCT01014988 (33) [back to overview]Geometric Mean Area Under the Serum Drug Concentration-time Curve (AUC) Over a 12-hour Dosing Interval (AUC[0-tau]) and AUC Extrapolated to Infinity (AUC[0-inf]) of Zanamivir
NCT01014988 (33) [back to overview]Geometric Mean Maximum Serum Concentration (Cmax) of Zanamivir at the End of Infusion
NCT01014988 (33) [back to overview]Geometric Mean Serum Clearance of Zanamivir
NCT01156701 (7) [back to overview]Number of Patients With Respiratory Outcomes
NCT01156701 (7) [back to overview]Number of Participants Experiencing Hospitalization or Death Due to Influenza
NCT01156701 (7) [back to overview]Number of Patients With Any Respiratory Diagnosis
NCT01156701 (7) [back to overview]Number of Patients With Asthma
NCT01156701 (7) [back to overview]Number of Patients With Bronchitis
NCT01156701 (7) [back to overview]Number of Patients With Influenza
NCT01156701 (7) [back to overview]Number of Patients With Pneumonia
NCT01199744 (10) [back to overview]Number of Participants With Any Serious Adverse Drug Reaction (ADR)
NCT01199744 (10) [back to overview]Number of Male and Female Participants With Either a Serious or Non-serious Adverse Drug Reaction
NCT01199744 (10) [back to overview]Number of Participants in the Indicated Age Categories With Either a Serious or Non-serious Adverse Drug Reaction
NCT01199744 (10) [back to overview]Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Categorized by Either Having Complications or Having no Complications
NCT01199744 (10) [back to overview]Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Categorized by Either Having Risk Factors for Influenza or Having no Risk Factors
NCT01199744 (10) [back to overview]Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Categorized by Reason for the Use of Relenza
NCT01199744 (10) [back to overview]Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Who Were Also in the Indicated High-risk Categories
NCT01199744 (10) [back to overview]Number of Participants With Any Adverse Drug Reaction
NCT01199744 (10) [back to overview]Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Who Were Vaccinated for Influenza
NCT01199744 (10) [back to overview]Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Who Were Also Taking Concomitant Medications
NCT01231620 (36) [back to overview]Number of Participants With the Indicated Clinical Symptoms of Influenza
NCT01231620 (36) [back to overview]Number of Participants With the Indicated Hematology Values Shifts From Baseline (Day 1) and up to 42 Days
NCT01231620 (36) [back to overview]Number of Participants With the Indicated Treatment-emergent (TE) Grade (G) 3/4 Clinical Chemistry Toxicities
NCT01231620 (36) [back to overview]Number of Participants With the Indicated Treatment-emergent (TE) Grade 3/4 Hematology Toxicities
NCT01231620 (36) [back to overview]Number of Participants With the Indicated Ventilation Status: Modality of Invasive and Non-invasive Ventilator Support and Oxygen Supplementation
NCT01231620 (36) [back to overview]Serum Concentration of IV Zanamivir
NCT01231620 (36) [back to overview]Serum Concentration of IV Zanamivir
NCT01231620 (36) [back to overview]Median Time to Virologic Improvement
NCT01231620 (36) [back to overview]Median Time to Return to the Pre-morbid Level of Activity as Measured by the 3-point Scale
NCT01231620 (36) [back to overview]Number of Participants Who Permanently Discontinued the Study Treatment Due to an AE
NCT01231620 (36) [back to overview]Number of Participants Who Were Permanently Discontinued From the Study Due to an AE
NCT01231620 (36) [back to overview]Number of Participants With Any Adverse Event (AE) Considered to be Related to Study Treatment
NCT01231620 (36) [back to overview]Number of Participants With Any Severe or Grade 3/4 AE
NCT01231620 (36) [back to overview]Number of Participants With Any Severe or Grade 3/4 Treatment-related AE
NCT01231620 (36) [back to overview]Percentage of Participants With Respiratory Improvement
NCT01231620 (36) [back to overview]Time to Clinical Response (TTCR) in Participants With Confirmed Influenza
NCT01231620 (36) [back to overview]Change From Baseline in Quantitative Virus Culture From Nasopharyngeal Swabs Positive at Baseline
NCT01231620 (36) [back to overview]Change From Baseline in Quantitative Virus Culture From Nasopharyngeal Swabs Positive at Baseline
NCT01231620 (36) [back to overview]Change From Baseline in the Katz Activities of Daily Living (ADL) Score and Each ADL Activity Score
NCT01231620 (36) [back to overview]Change From Baseline Viral Load (Influenza A or B) by qPCR From Nasopharyngeal Swabs Positive at Baseline
NCT01231620 (36) [back to overview]Change From Baseline Viral Load (Influenza A or B) by qPCR From Nasopharyngeal Swabs Positive at Baseline
NCT01231620 (36) [back to overview]Median Time of Duration of Clinical Symptoms of Influenza
NCT01231620 (36) [back to overview]Median Time of Duration of Hospitalization and Intensive Care Unit (ICU) Stay
NCT01231620 (36) [back to overview]Median Time of Duration of Invasive and Non-invasive Ventilator Support and Oxygen Supplementation
NCT01231620 (36) [back to overview]Median Time to no Detectable Viral RNA and the Absence of Cultivable Virus in Any Obtained Sample (Upper and Lower Respiratory Samples)
NCT01231620 (36) [back to overview]Median Time to Return to Pre-morbid Functional Status as Measured by the Katz ADL Score and Each ADL Activity Score
NCT01231620 (36) [back to overview]Median Time to the Absence of Fever and Improved Respiratory Status, Oxygen Saturation, Heart Rate, and Systolic Blood Pressure
NCT01231620 (36) [back to overview]Number of Participants Assessed as Normal/Abnormal (Clinically Significant [CS] and Not Clinically Significant [NCS]) for 12-lead Electrocardiogram (ECG) at Baseline (Day 1) and Day 4
NCT01231620 (36) [back to overview]Number of Participants Who Returned to Their Pre-morbid Functional Status as Assessed Per the Katz ADL Score and Each ADL Activity Score at the End of the Study
NCT01231620 (36) [back to overview]Number of Participants With All Cause and Attributable Mortality at Day 14, at Day 28, and at the End of Study Visit
NCT01231620 (36) [back to overview]Number of Participants With Complications of Influenza and Associated Antibiotic Use
NCT01231620 (36) [back to overview]Number of Participants With no Detectable Viral RNA and the Absence of Cultivable Virus in Lower Respiratory Samples (Bronchoalveolar Lavage Sample [BAL], Endotracheal Aspirate)
NCT01231620 (36) [back to overview]Number of Participants With no Detectable Viral RNA and the Absence of Cultivable Virus in Lower Respiratory Samples (Bronchoalveolar Lavage Sample [BAL], Endotracheal Aspirate)
NCT01231620 (36) [back to overview]Number of Participants With no Detectable Viral RNA and the Absence of Cultivable Virus in Lower Respiratory Samples (Bronchoalveolar Lavage Sample [BAL], Endotracheal Aspirate)
NCT01231620 (36) [back to overview]Number of Participants With Resistance-associated Mutations Detected in the Neuraminidase (NA) and Hemagglutinin (HA) Gene of Influenza A and B Viruses in Nasopharyngeal Swabs and Endotracheal/BAL Samples
NCT01231620 (36) [back to overview]Number of Participants With the Indicated Chemistry Laboratory Values Shifts From Baseline (Day 1) and up to 42 Days
NCT01527110 (42) [back to overview]Mean Oxygen Saturation (OS) of Participants Over Period
NCT01527110 (42) [back to overview]Mean Respiratory Rate (RR) of Participants Over Period
NCT01527110 (42) [back to overview]Mean Systolic and Diastolic Blood Pressure (SBP and DBP) of Participants Over Period
NCT01527110 (42) [back to overview]Mean Temperature of Participants Over Period
NCT01527110 (42) [back to overview]Median Duration of Clinical Symptoms of Influenza Over Period
NCT01527110 (42) [back to overview]Median Duration of Use of Invasive and Non-invasive Ventilatory Support and Oxygen Supplementation Over Period
NCT01527110 (42) [back to overview]Median Time to Absence of Fever, Improved Respiratory Status, Improved OS, Improved HR and Improved SBP Over Period
NCT01527110 (42) [back to overview]Median Time to no Detectable Viral RNA by Quantitative RT-PCR and Viral Culture From Nasopharyngeal Samples Over Period
NCT01527110 (42) [back to overview]Median Duration of Hospital Stay for the Participants Over Period
NCT01527110 (42) [back to overview]Number of Participants of Treatment Emergent Toxicities in Clinical Chemistry and Hematology Over Period
NCT01527110 (42) [back to overview]Number of Participants With Abnormal Clinically Significant Electrocardiograph (ECG) Findings Over Period
NCT01527110 (42) [back to overview]Number of Participants With and Without Use of Modality of Invasive, Non-invasive Ventilatory Support and Oxygen Supplementation Over Period
NCT01527110 (42) [back to overview]Number of Participants With Any Adverse Event (AE), Drug-related AE, Grade 3 and Grade 4 AE, Grade 3 and 4 Drug-related AE , AE Leading to Discontinuation of Study Drug or From Study, Serious AE (SAE), Drug-related SAE, Fatal AE and Drug-related Fatal AE
NCT01527110 (42) [back to overview]Number of Participants With Clinical Chemistry Parameters of Alanine Amino Transferase (ALT), Alkaline Phosphatase (ALP), Creatine Kinase and Aspartate Amino Transferase (AST) Outside the Normal Reference Range at Any Time During Treatment
NCT01527110 (42) [back to overview]Number of Participants With Clinical Chemistry Parameters of Albumin and Total Protein Outside the Normal Reference Range at Any Time During Treatment
NCT01527110 (42) [back to overview]Number of Participants With Clinical Chemistry Parameters of Calcium, Carbon Dioxide Content/ Bicarbonate, Chloride, Magnesium, Potassium, Sodium and Urea/ Blood Urea Nitrogen (BUN) Outside the Normal Reference Range at Any Time During Treatment
NCT01527110 (42) [back to overview]Number of Participants With Clinical Chemistry Parameters of Creatinine, Direct Bilirubin and Total Bilirubin Outside the Normal Reference Range at Any Time During Treatment
NCT01527110 (42) [back to overview]Number of Participants With Complications of Influenza and Associated Use of Antibiotics Over Period
NCT01527110 (42) [back to overview]Number of Participants With Hematology Parameters of Basophiles, Eosinophils, Lymphocytes, Monocytes, Total Neutrophils, Platelet Count, White Blood Cell(WBC) Count, Hemoglobin and Hematocrit Outside the Normal Reference Range at Any Time During Treatment
NCT01527110 (42) [back to overview]Number of Participants With or Without Treatment Emergent Resistance or Suspected Treatment Emergent Resistance to Zanamivir Over Period
NCT01527110 (42) [back to overview]Number of Participants With Toxicity Shifts From Baseline in Clinical Chemistry Over Period
NCT01527110 (42) [back to overview]Number of Participants With Toxicity Shifts From Baseline in Hematology Parameters Over Period
NCT01527110 (42) [back to overview]Percentage of Participants With Abnormal Clinically Significant ECG Findings Over Period
NCT01527110 (42) [back to overview]Percentage of Participants With Undetectable Viral RNA and Absence Cultivable Virus From Samples Obtained From Nasopharyngeal Samples Over Period
NCT01527110 (42) [back to overview]Percentage of Participants With Undetectable Viral RNA and Absence of Cultivable Virus in Lower Respiratory Samples Over Period
NCT01527110 (42) [back to overview]Number of Participants of Clinical Symptoms of Influenza Over Period
NCT01527110 (42) [back to overview]Median Duration of Intensive Care Unit (ICU) Stay for the Participants Over Period
NCT01527110 (42) [back to overview]Median Time to Clinical Response Over Period
NCT01527110 (42) [back to overview]Median Time to Return to Pre-morbid Level of Activity Over Period
NCT01527110 (42) [back to overview]Median Time to Virologic Improvement Over Period
NCT01527110 (42) [back to overview]Mean 50% Inhibitory Concentration (IC50) for Phenotypes of Influenza for the Measure of Viral Susceptibility to Zanamivir at All Visits
NCT01527110 (42) [back to overview]Mean Change Baseline in Hematocrit at the Indicated Time Points
NCT01527110 (42) [back to overview]Mean Change From Baseline in Albumin and Total Protein at the Indicated Time Points
NCT01527110 (42) [back to overview]Mean Change From Baseline in ALT, ALP, Creatine Kinase and AST at the Indicated Time Points
NCT01527110 (42) [back to overview]Mean Change From Baseline in Counts of WBC and Platelets at the Indicated Time Points
NCT01527110 (42) [back to overview]Mean Change From Baseline in Creatinine, Direct Bilirubin and Total Bilirubin at the Indicated Time Points
NCT01527110 (42) [back to overview]Mean Change From Baseline in Hemoglobin at the Indicated Time Points
NCT01527110 (42) [back to overview]Mean Change From Baseline in Percentage of Basophils, Eosinophils, Lymphocytes, Monocytes and Total Neutrophils at the Indicated Time Points
NCT01527110 (42) [back to overview]Mean Change From Baseline in Quantitative Viral Load Measured by RT-PCR From Nasopharyngeal Swabs Positive at Baseline Over Period
NCT01527110 (42) [back to overview]Mean Change From Baseline in Quantitative Viral Load Measured by Viral Culture From Nasopharyngeal Swabs Over Period
NCT01527110 (42) [back to overview]Mean Change From Baseline in Sodium, Calcium, Potassium, Chloride, Magnesium, Carbon Dioxide Content/Bicarbonate and Urea/BUN at the Indicated Time Points
NCT01527110 (42) [back to overview]Mean Heart Rate (HR) of Participants Over Period
NCT01793883 (1) [back to overview]Time to Alleviation of Influenza Symptoms

Number of Subjects Adhering to Long-term Zanamivir Prophylaxis

Number of subjects taking 80% or more doses per week of zanamivir (10 mg once daily), as influenza prophylaxis, for 13 weeks or longer (as measured by weekly diary and dose counts at study visits). (NCT00784784)
Timeframe: 5 months

Interventionparticipants (Number)
Antiviral Prophylaxis34

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Number of Laboratory Confirmed Influenza Infections

Four-fold increase in antibody titer 2 weeks post injection and end of study or positive laboratory test for influenza during study (polymerase chain reaction [PCR] or culture) (NCT00784784)
Timeframe: 6 months

Interventioninfections (Number)
Influenza Vaccine2
Antiviral Prophylaxis1

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Number of Participants With Adverse Events (AEs), Drug Specific AEs or AEs Resulting in Treatment Interruption

"Abnormal lab data or newly appeared symptoms & signs were considered as AEs.~Examined lab data:~Blood cell count (WBC, differential count, Red Blood Cell (RBC), Hemoglobin, Hematocrit, Mean Corpuscular Volume (MCV), Mean Corpuscular Hemoglobin Concentration (MCHC), platelets), Chemistry (Cl, bicarbonate (HCO3), K, Na), Renal function test (BUN, Creatinine, Creatinine clearance), Liver function test (AST, Alanine aminotransferase(ALT), T.Bil, gamma-glutamyltransferase)" (NCT00867139)
Timeframe: 30 days after the final dose of study drug

Interventionnumber of participants with AEs (Number)
TCAD1
Neuraminidase Inihibitor Monotherapy1
Open-labeled TCAD1

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Days on Supplemental Oxygen

(NCT00867139)
Timeframe: 58 days

Interventiondays (Mean)
TCAD2
Neuraminidase Inihibitor Monotherapy0
Open-labeled TCAD0

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Duration of Hospitalization

(NCT00867139)
Timeframe: from baseline up to 58 days

Interventiondays (Mean)
TCAD6
Neuraminidase Inihibitor Monotherapy6
Open-labeled TCAD1

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Duration of Symptoms

"Calculated as the number of days (mean) any persistent symptom lasted per patient as listed below.~overall health, short of breath, chills, cough, diarrhea, ear pain, fatigue, fever, headache, hoarseness, muscle ache, phlegm, runny nose, sinus congestion, sneezing, sore throat, watery eyes, wheezing" (NCT00867139)
Timeframe: from baseline up to 28 days

Interventiondays (Mean)
TCAD4.5
Neuraminidase Inhibitor Monotherapy1
Open-label TCAD4.7

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Frequency of Confirmed Pneumonia

(NCT00867139)
Timeframe: 58 days

Interventionparticipants (Number)
TCAD0
Neuraminidase Inihibitor Monotherapy0
Open-labeled TCAD1

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Number of Deaths

(NCT00867139)
Timeframe: 58 days

Interventionparticipants (Number)
TCAD0
Neuraminidase Inihibitor Monotherapy0
Open-labeled TCAD0

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Number of Participants With ICU Admissions

The number of participants with ICU admissions was evaluated. (NCT00867139)
Timeframe: baseline and up to 58 days

Interventionparticipants (Number)
TCAD0
Neuraminidase Inihibitor Monotherapy0
Open-labeled TCAD1

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Number of Participants With Intubations

(NCT00867139)
Timeframe: 58 days

Interventionparticipants (Number)
TCAD0
Neuraminidase Inihibitor Monotherapy0
Open-labeled TCAD1

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Number of Participants With Viral Load Decrease as a Function of Time

Viral loads were measured by quantitative Polymerase Chain Reaction (PCR) on day 1, 3, 5, 7, 9, 15, 20 and 28, if applicable. (NCT00867139)
Timeframe: baseline and 28 days

Interventionnumber of participants (Number)
Neuraminidase Inhibitor Monotherapy0
Open-label TCAD2

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Number of Participants With Viral Resistance as a Function of Drug Exposure

Viral resistance was assessed within 28 days after drug administration by detecting resistance-conferring mutation genes and compared to the value at baseline. (NCT00867139)
Timeframe: 28 days

InterventionNumber of participants (Number)
TCAD0
Neuraminidase Inihibitor Monotherapy1
Open-labeled TCAD0

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Pharmacokinetics (AUC0-last) of TCAD

Only 5 patients had partial pharmacokinetic (PK) data available. Plasma concentration of oseltamivir was measured at several time points in one patient receiving neuraminidase inhibitor monotherapy. Plasma concentration of oseltamivir, amantadine, and ribavirin were measured at several time points in four patients receiving TCAD therapy. Area under the time-concentration curve up to the last measured time point (AUC0-last) was calculated from the plasma concentration-time profiles by non-compartmental analysis. (NCT00867139)
Timeframe: 5 days

Interventionng*hr/mL (Mean)
TCAD304
Neuraminidase Inhibitor Monotherapy1497
Open-lable TCAD2487

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Number of Patients Not Shedding Virus at Day 5 +/-1 and Day 10 +/- 1

(NCT00867139)
Timeframe: 10 days

,
Interventionparticipants (Number)
Day 5 +/-1Day 10 +/- 1
Neuraminidase Inihibitor Monotherapy00
Open-labeled TCAD01

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Geometric Mean Terminal Half Life (t1/2) of Zanamivir

"The t1/2 of zanamivir was evaluated. Terminal half life is defined as the time it takes for a substance to lose half of its pharmacologic, physiologic, or radiologic activity. Serial blood samples for PK analysis were collected if possible in conjunction with the initial dose on Day 1 (5-7 serial samples) and over a dosing interval during repeat dosing on Day 3, 4, or 5 (5 serial samples). PK data for all participants with available blood samples were analyzed. PK data for those participants with a CLcr>=80 mL/minutes (>=80 mL/minute/1.73m^2 for cohorts 1-4) and who received an ID and a MD of 14 mg/kg (6 months to <6 years of age), 12 mg/kg, not to exceed 600 mg (6 to <18 years of age) or 600 mg zanamivir (>=18 years of age) (represented by n=X in the category titles) were summarized. NA indicates that data are not available/analysis was not performed." (NCT01014988)
Timeframe: Day 1 and Days 3, 4, or 5

,,,,,
InterventionHours (Geometric Mean)
ID, 600 mg, CLcr>=80, n=67, 0, 0, 0, 0, 5ID, 12 mg/kg, CLcr>=80, n=0, 0, 0, 0, 8, 1ID, 14 mg/kg, CLcr>=80, n=0, 3, 5, 9, 0, 0MD, 600 mg, CLcr>=80, n=68, 0, 0, 0, 0, 2MD, 12 mg/kg, CLcr>=80, n=0, 0, 0, 0, 4, 0MD, 14 mg/kg, CLcr>=80, n=0, 0, 1, 4, 0, 0
Cohort 1: Infants (6 Months to <1 Year of Age)NANA1.84NANANA
Cohort 2: Children (1 to <2 Years of Age)NANA2.49NANA1.68
Cohort 3: Children (2 to <6 Years of Age)NANA1.60NANA1.76
Cohort 4: Children (6 to <13 Years of Age)NA2.57NANA1.81NA
Cohort 5: Adolescents (13 to <18 Years of Age)2.062.16NA1.73NANA
Cohort 6: Adults (18 Years and Older)2.39NANA2.56NANA

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Geometric Mean Volume of Distribution (Vd) of Zanamivir

"The Vd of zanamivir was evaluated. Volume of distribution is defined as the apparent volume in which zanamivir is distributed. Serial blood samples for PK analysis were collected if possible in conjunction with the initial dose on Day 1 (5-7 serial samples) and over a dosing interval during repeat dosing on Days 3, 4, or 5 (5 serial samples). PK data for all participants with available blood samples were analyzed. PK data for those participants with a CLcr >= 80 mL/minutes (>=80 mL/minute/1.73m^2 for cohorts 1-4) and who received an ID and a MD of 14 mg/kg (6 months to <6 years of age), 12 mg/kg, not to exceed 600 mg (6 to <18 years of age) or 600 mg zanamivir (>=18 years of age) (represented by n=X in the category titles) were summarized. NA indicates that data are not available/analysis was not performed." (NCT01014988)
Timeframe: Day 1 and Days 3, 4, or 5

,,,,,
InterventionLiters (L) (Geometric Mean)
ID, 600 mg, CLcr>=80, n=63, 0, 0, 0, 0, 5ID, 12 mg/kg, CLcr>=80, n=0, 0, 0, 0, 8, 1ID, 14 mg/kg, CLcr>=80, n=0, 3, 4, 9, 0, 0MD, 600 mg, CLcr>=80, n=65, 0, 0, 0, 0, 0MD, 12 mg/kg, CLcr>=80, n=0, 0, 0, 0, 8, 0MD, 14 mg/kg, CLcr>=80, n=0, 0, 1, 4, 0, 0
Cohort 1: Infants (6 Months to <1 Year of Age)NANA3.77NANANA
Cohort 2: Children (1 to <2 Years of Age)NANA3.94NANA3.77
Cohort 3: Children (2 to <6 Years of Age)NANA5.15NANA5.23
Cohort 4: Children (6 to <13 Years of Age)NA9.21NANA9.82NA
Cohort 5: Adolescents (13 to <18 Years of Age)18.5710.09NA23.20NANA
Cohort 6: Adults (18 Years and Older)24.89NANA24.61NANA

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Mean Viral Susceptibility to Zanamivir at Baseline (Day 1) and All Post-Baseline Visits Collectively

"Viral susceptibility to zanamivir at Baseline and at all post-Baseline visits collectively was assessed by neuraminidase (NA) enzyme inhibition assay. The mean IC50 data are summarized by subtype (A/H1N1, A/H3N2, B) and by visit. IC50 is defined as the concentration of zanamvir required to inhibit NA activity by 50%. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). NA indicates that data are not available/analysis was not performed. Please note: pediatric data are pending and will be updated when available." (NCT01014988)
Timeframe: Baseline and up to post-treatment (PT) + 23 days

InterventionNanomolar (nM) (Mean)
A/H1N1, Day 1, n=22, 2A/H1N1, All Post-Baseline, n=8, 1A/H3N2, Day 1, n=5, 16A/H3N2, All Post-Baseline, n=2, 3B, Day 1, n=2, 16B, All Post-Baseline, n=0, 10
Cohort 6: Adults (18 Years and Older)0.20910.18000.26600.23001.6100NA

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Median Body Temperature at Baseline (Day 1) and Day 5

Body temperature was recorded at Baseline (Day 1), Days 2, 3, 4, 5, 6, 7, 8, 9, and 10; and post-treatment +2 days, +5 days, +9 days, +16 days (assessments to be done if participant remained hospitalized), and +23 days. Body temperature was recorded once daily during inpatient or outpatient follow-up visits. Median body temperature at Baseline (Day 1) and Day 5 is summarized. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X, X in the category titles). (NCT01014988)
Timeframe: Baseline (Day 1) and Day 5

,,,,,,
InterventionDegrees centigrade (Median)
Day 1, n=87, 43, 7, 11, 12, 27, 14Day 5, n=73, 42, 7, 6, 9, 15, 10
Cohort 1: Infants (6 Months to <1 Year of Age)36.837.0
Cohort 2: Children (1 to <2 Years of Age)37.336.8
Cohort 3: Children (2 to <6 Years of Age)37.537.3
Cohort 4: Children (6 to <13 Years of Age)37.337.1
Cohort 5: Adolescents (13 to <18 Years of Age)37.537.1
Cohort 6: Adults (18 Years and Older); Zanamivir <=5 Days37.3037.00
Cohort 6: Adults (18 Years and Older); Zanamivir >5 Days37.3037.15

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Median Time to Clinical Response (Sustained Resolution) of All Vital Signs (Composite)

Sustained resolution of the following vital signs (composite) was assessed: afebrile status, normal oxygen saturation, normal respiratory status, normal HR, and normal BP. Clinical response is defined as the resolution of at least four of five vital signs within the following resolution criteria, maintained for 24 hours or hospital discharge, whichever occurred first: Temperature in degrees Centigrade (<=36.6 axilla, <=37.2 oral, <=37.7 rectal, core or tympanic); oxygen saturation (>=95%, without supplemental oxygen); respiratory status (return to pre-morbid oxygen requirement, or no need for supplemental oxygen, or respiratory rate <=60, <=40, <=34, <=30, <=24 or <=24 breaths/minute without supplemental oxygen for Cohorts 1-6 respectively); HR (<=160, <=150, <=140, <=120, <=100 or <=100 bpm for Cohorts 1-6 respectively); SBP (>=70, >=74, >=76, >=80, >=90 or >=90 mmHg for Cohorts 1-6 respectively). Only those participants available at the specified time points were analyzed. (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

InterventionDays (Median)
Cohort 6: Adults (18 Years and Older)9.0
Cohort 1: Infants (6 Months to <1 Year of Age)7.0
Cohort 2: Children (1 to <2 Years of Age)3.5
Cohort 3: Children (2 to <6 Years of Age)6.5
Cohort 4: Children (6 to <13 Years of Age)4.0
Cohort 5: Adolescents (13 to <18 Years of Age)5.0

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Median Corrected QT Interval (QTc) for Heart Rate by Fridericia's Formula (QTcF) and Bazett's Formula (QTcB) at Baseline (Day 1) and Day 5

"Twelve-lead ECGs were recorded for the parameters of QTcF and QTcB. The first set of pre-dose ECG values at Baseline (Day 1) and the pre-dose ECG values at Day 5 are presented. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X, X in the category titles). NA indicates that data are not available/analysis was not performed. Cohort 1 QTcF and QTcB minimum values of 0.0 were data entry errors that could not be addressed after Data Base Freeze." (NCT01014988)
Timeframe: Baseline (Day 1) and Day 5

,,,,,,
InterventionMilliseconds (Median)
QTcF, Baseline, n=87, 42, 6, 9, 11, 24, 13QTcF, Day 5, n=68, 40, 0, 1, 3, 3, 5QTcB, Baseline, n=87, 42, 6, 9, 11, 24, 13QTcB, Day 5, n=68, 40, 0, 1, 3, 3, 5
Cohort 1: Infants (6 Months to <1 Year of Age)356.00NA412.00NA
Cohort 2: Children (1 to <2 Years of Age)362.00373.00422.00416.00
Cohort 3: Children (2 to <6 Years of Age)365.00394.00410.00444.00
Cohort 4: Children (6 to <13 Years of Age)387.50353.00422.50380.00
Cohort 5: Adolescents (13 to <18 Years of Age)387.00389.00415.00399.00
Cohort 6: Adults (18 Years and Older); Zanamivir <=5 Days400.6406.6424.0422.0
Cohort 6: Adults (18 Years and Older); Zanamivir >5 Days413.5405.5432.0434.0

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Median Duration of Hospitalization and Intensive Care Unit (ICU) Stays

The duration of hospitalization (H) reflects the number of hospitalization days between the date of the first dose of investigational product and the date of discharge. ICU stay includes total duration in ICU and may include days in ICU before entry into the study. For participants with a missing discharge date who were not discharged at the end of the study, the date of discharge was imputed to the last follow-up visit (post-treatment +23 days). Only those participants available at the specified time points were analyzed (represented by n=X in the category titles). (NCT01014988)
Timeframe: Up to discharge from hospital

,,,,,
InterventionDays (Median)
Duration of H, n=130, 7, 11, 12, 27, 14Duration of H-ICU, n=108, 4, 6, 8, 19, 9
Cohort 1: Infants (6 Months to <1 Year of Age)7.07.5
Cohort 2: Children (1 to <2 Years of Age)4.05.0
Cohort 3: Children (2 to <6 Years of Age)6.55.5
Cohort 4: Children (6 to <13 Years of Age)6.08.0
Cohort 5: Adolescents (13 to <18 Years of Age)6.58.0
Cohort 6: Adults (18 Years and Older)15.011.50

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Median Heart Rate at Baseline (Day 1) and Day 5

Heart rate was measured at Baseline (Day 1); Days 2, 3, 4, 5, 6, 7, 8, 9, and 10; post-treatment +2 days, +5 days, +9 days, +16 days (assessments to be done if participant remained hospitalized), and +23 days. Heart rate was assessed once daily during inpatient or outpatient follow-up visits. Heart rate values at Baseline (Day 1) and Day 5 are summarized. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X, X in the category titles). (NCT01014988)
Timeframe: Baseline (Day 1) and Day 5

,,,,,,
InterventionBeats per minute (bpm) (Median)
Day 1, n=87, 43, 7, 11, 12, 27, 14Day 5, n=73, 42, 7, 6, 9, 15, 10
Cohort 1: Infants (6 Months to <1 Year of Age)119.0127.0
Cohort 2: Children (1 to <2 Years of Age)144.0122.5
Cohort 3: Children (2 to <6 Years of Age)115.5112.0
Cohort 4: Children (6 to <13 Years of Age)112.0102.0
Cohort 5: Adolescents (13 to <18 Years of Age)99.079.5
Cohort 6: Adults (18 Years and Older); Zanamivir <=5 Days93.0087.00
Cohort 6: Adults (18 Years and Older); Zanamivir >5 Days95.0093.50

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Median Oxygen Saturation Measured Via Transcutaneous Oximetry (TCPO2) at Baseline (Day 1) and Day 5

TCPO2 is a noninvasive test that directly measures the oxygen level of tissue beneath the skin. Because oxygen is carried to tissues by blood flow in the arteries, TCPO2 is an indirect measure of blood flow. The percent (%) oxygen saturation was measured at Baseline (Day 1), Days 2, 3, 4, 5, 6, 7, 8, 9, and 10; and post-treatment +2 days, +5 days, +9 days, +16 days (assessments to be done if participant remained hospitalized), and +23 days. Oxygen saturation was assessed once daily during inpatient follow-up visits. The median oxygen saturation values at Baseline (Day 1) and Day 5 are summarized. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X, X in the category titles). (NCT01014988)
Timeframe: Baseline (Day 1) and Day 5

,,,,,,
InterventionPercentage of oxygen level in blood (Median)
Day 1, n=87, 43, 7, 11, 12, 27, 14Day 5, n=70, 43, 7, 6, 9, 15, 9
Cohort 1: Infants (6 Months to <1 Year of Age)98.0100.0
Cohort 2: Children (1 to <2 Years of Age)100.095.5
Cohort 3: Children (2 to <6 Years of Age)98.097.0
Cohort 4: Children (6 to <13 Years of Age)98.097.0
Cohort 5: Adolescents (13 to <18 Years of Age)97.596.0
Cohort 6: Adults (18 Years and Older); Zanamivir <=5 Days97.0097.00
Cohort 6: Adults (18 Years and Older); Zanamivir >5 Days96.0096.00

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Median Respiration Rate at Baseline (Day 1) and Day 5

Respiration rate was measured at Baseline (Day 1), Days 2, 3, 4, 5, 6, 7, 8, 9, and 10; and post-treatment +2 days, +5 days, +9 days, +16 days (assessments to be done if participant remained hospitalized), and +23 days. Respiration rate was assessed once daily during inpatient or outpatient follow-up visits. The median respiration rate at Baseline (Day 1) and Day 5 is summarized. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X, X in the category titles). (NCT01014988)
Timeframe: Baseline (Day 1) and Day 5

,,,,,,
InterventionBreaths per minute (Median)
Day 1, n=87, 43, 7, 11, 12, 27, 14Day 5, n=67, 42, 7, 6, 9, 15, 10
Cohort 1: Infants (6 Months to <1 Year of Age)32.040.0
Cohort 2: Children (1 to <2 Years of Age)34.031.0
Cohort 3: Children (2 to <6 Years of Age)29.530.0
Cohort 4: Children (6 to <13 Years of Age)20.023.0
Cohort 5: Adolescents (13 to <18 Years of Age)21.019.0
Cohort 6: Adults (18 Years and Older); Zanamivir <=5 Days23.0020.00
Cohort 6: Adults (18 Years and Older); Zanamivir >5 Days22.0023.50

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Median Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Baseline (Day 1) and Day 5

SBP and DBP were measured at Baseline (Day 1), Days 2, 3, 4, 5, 6, 7, 8, 9, and 10; post-treatment +2 days, +5 days, +9 days, +16 days (assessments to be done if participant remained hospitalized), and +23 days. SBP and DBP were assessed once daily during inpatient or outpatient follow-up visits. SBP and DBP values at Baseline (Day 1) and Day 5 are summarized. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X, X in the category titles). (NCT01014988)
Timeframe: Baseline (Day 1) and Day 5

,,,,,,
InterventionMillimeters of mercury (mmHg) (Median)
SBP, Day 1, n=87, 43, 7, 11, 12, 27, 14SBP, Day 5, n=73, 43, 7, 5, 9, 15, 10DBP, Day 1, n=87, 43, 7, 11, 12, 27, 14DBP, Day 5, n=73, 43, 7, 5, 9, 15, 10
Cohort 1: Infants (6 Months to <1 Year of Age)102.0103.053.060.0
Cohort 2: Children (1 to <2 Years of Age)100.098.060.060.0
Cohort 3: Children (2 to <6 Years of Age)105.5117.058.067.0
Cohort 4: Children (6 to <13 Years of Age)108.0110.057.068.0
Cohort 5: Adolescents (13 to <18 Years of Age)107.0108.562.054.5
Cohort 6: Adults (18 Years and Older); Zanamivir <=5 Days126.00128.0068.0070.00
Cohort 6: Adults (18 Years and Older); Zanamivir >5 Days118.00132.0063.0066.00

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Number of Participants Assessed as Normal/Abnormal (Clinically Significant [CS] and Not Clinically Significant [NCS]) for 12-lead Electrocardiogram (ECG) at Baseline (Day 1)

The number of participants with an ECG status of normal and abnormal CS or NCS, as determined by the Investigator, is reported. Normal=all ECG parameters within the accepted normal ranges. Abnormal=ECG findings outside of normal ranges. CS=ECG with a CS abnormality that meets exclusion criteria. NCS=ECG with an abnormality that is not CS nor meets exclusion criteria, per Investigator, based on reasonable standards of clinical judgment. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X in the category titles). (NCT01014988)
Timeframe: Baseline (Day 1)

,,,,,
InterventionParticipants (Number)
Normal, n=128, 7, 10, 12, 25, 13Abnormal NCS, n=128, 7, 10, 12, 25, 13Abnormal CS, n=128, 7, 10, 12, 25, 13
Cohort 1: Infants (6 Months to <1 Year of Age)520
Cohort 2: Children (1 to <2 Years of Age)721
Cohort 3: Children (2 to <6 Years of Age)840
Cohort 4: Children (6 to <13 Years of Age)2050
Cohort 5: Adolescents (13 to <18 Years of Age)850
Cohort 6: Adults (18 Years and Older)68577

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Number of Participants With the Indicated Clinical Chemistry Values Relative to the Normal Range at Baseline (Day 1) and Day 5

Blood samples for laboratory assessments were collected at Baseline (Day [D] 1), Days 3 and 5, and on post-treatment +2 days (if hospitalized) and post-treatment +23 days. Clinical chemistry parameters included alanine aminotransferase (ALT), direct bilirubin (DB), total bilirubin (TB), and creatinine. The number of participants with values that were high (H)/normal (N)/low (L) relative to the normal range at Baseline (D 1) and D 5 for the indicated clinical chemistry parameters are summarized. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT01014988)
Timeframe: Baseline (Day 1) and Day 5

,
InterventionParticipants (Number)
D 1, H ALT, n=129, 71D 1, N ALT, n=129, 71D 1, L ALT, n=129, 71D 5, H ALT, n=102, 45D 5, N ALT, n=102, 45D 5, L ALT, n=102, 45D 1, H DB, n=83, 60D 1, N DB, n=83, 60D 1, L DB, n=83, 60D 5, H DB, n=70, 36D 5, N DB, n=70, 36D 5, L DB, n=70, 36D 1, H TB, n=128, 71D 1, N TB, n=128, 71D 1, L TB, n=128, 71D 5, H TB, n=102, 42D 5, N TB, n=102, 42D 5, L TB, n=102, 42D 1, H Creatinine, n=128, 71D 1, N Creatinine, n=128, 71D 1, L Creatinine, n=128, 71D 5, H Creatinine, n=111, 46D 5, N Creatinine, n=111, 46D 5, L Creatinine, n=111, 46
Cohort 6: Adults (18 Years and Older)4879141601176122046111110713854275051314634
Cohorts 1-5: Pediatrics/Adolescents (6 Months to <18 Years)21491162719453428113507632265697345

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Number of Participants With the Indicated Hematology Values Relative to the Normal Range at Baseline (Day 1) and Day 5

Blood samples for laboratory assessments were collected at Baseline (Day [D] 1), Days 3 and 5, and on post-treatment +2 days (if hospitalized) and post-treatment +23 days. Hematology parameters included hemoglobin, total neutrophils (TN), and white blood cell (WBC) count. The number of participants with values that were high (H)/normal (N)/low (L) relative to the normal range at Baseline (D 1) and D 5 for the indicated hematology parameters are summarized. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT01014988)
Timeframe: Baseline (Day 1) and Day 5

,
InterventionParticipants (Number)
D 1, H Hemoglobin, n=130, 71D 1, N Hemoglobin, n=130, 71D 1, L Hemoglobin, n=130, 71D 5, H Hemoglobin, n=114, 47D 5, N Hemoglobin, n=114, 47D 5, L Hemoglobin, n=114, 47D 1, H TN, n=123, 70D 1, N TN, n=123, 70D 1, L TN, n=123, 70D 5, H TN, n=106, 45D 5, N TN, n=106, 45D 5, L TN, n=106, 45D 1, H WBC Count, n=130, 71D 1, N WBC Count, n=130, 71D 1, L WBC Count, n=130, 71D 5, H WBC Count, n=114, 47D 5, N WBC Count, n=114, 47D 5, L WBC Count, n=114, 47
Cohort 6: Adults (18 Years and Older)048821258851591349498297130504915
Cohorts 1-5: Pediatrics/Adolescents (6 Months to <18 Years)130400163134297201879422012305

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Number of Participants With the Indicated Mortality Status at Day 14 and Day 28

The number of participants who died on or before Study Day 14 and Study Day 28 was summarized. Only those participants available at the specified time points were analyzed. (NCT01014988)
Timeframe: Day 14 and Day 28

,,,,,
InterventionParticipants (Number)
Died on or before Study Day 14, NoDied on or before Study Day 14, YesDied on or before Study Day 28, NoDied on or before Study Day 28, Yes
Cohort 1: Infants (6 Months to <1 Year of Age)7070
Cohort 2: Children (1 to <2 Years of Age)110101
Cohort 3: Children (2 to <6 Years of Age)120120
Cohort 4: Children (6 to <13 Years of Age)261261
Cohort 5: Adolescents (13 to <18 Years of Age)122113
Cohort 6: Adults (18 Years and Older)1131710822

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Number of Participants With the Indicated Treatment-emergent (TE) Grade 3/4 Clinical Chemistry Toxicities

A toxicity was considered to be TE if it was greater than the Baseline grade, and if it had developed or increased post-Baseline in intensity (and prior to the last dose of investigational product). Clinical chemistry parameters included ALT, TB, and creatinine. Per the DAIDS table for grading the severity of adult and pediatric AEs, Grade 3=severe and Grade 4=potentially life threatening. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

,
InterventionParticipants (Number)
ALT, Grade 3, n=128, 69ALT, Grade 4, n=128, 69TB, Grade 3, n=127, 69TB, Grade 4, n=127, 69Creatinine, Grade 3, n=129, 69Creatinine, Grade 4, n=129, 69
Cohort 6: Adults (18 Years and Older)1053365
Cohorts 1-5: Pediatrics/Adolescents (6 Months to <18 Years)101432

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Number of Participants With the Indicated Treatment-emergent (TE) Grade 3/4 Hematology Toxicities

A toxicity was considered to be TE if it was greater than the Baseline grade, and if it had developed or increased post-Baseline in intensity (and prior to the last dose of investigational product). The hematology parameters included hemoglobin, TN, and WBC count. Per the DAIDS table for grading the severity of adult and pediatric AEs, Grade 3=severe and Grade 4=potentially life threatening. Baseline is defined as the last pre-treatment value collected. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

,
InterventionParticipants (Number)
Hemoglobin, Grade 3, n=129, 69Hemoglobin, Grade 4, n=129, 69TN, Grade 3, n=122, 68TN, Grade 4, n=122, 68WBC count, Grade 3, n=129, 69WBC count, Grade 4, n=129, 69
Cohort 6: Adults (18 Years and Older)4090122
Cohorts 1-5: Pediatrics/Adolescents (6 Months to <18 Years)1223210

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Number of Participants With the Indicated Ventilation Status: Modality of Supplemental Oxygen Delivery and Mechanical Ventilation

"Ventilation status was measured at Baseline (Day 1); Days 2, 3, 4, 5, 6, 7, 8, 9, and 10; and post-treatment +2 days, +5 days, +9 days, +16 days (assessments to be done if participant remained hospitalized), and +23 days. Ventilation status was assessed once daily during inpatient follow-up visits. The number of participants reported for machine-assisted: extracorporeal membrane oxygenation (ECMO), endotracheal mechanical ventilation, and supplemental oxygen delivery (SOD) at any time (AT) on study and at Baseline (Day 1) are summarized." (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

,,,,,
InterventionParticipants (Number)
AT on Study, Machine-Assisted: ECMOAT on Study, Machine-Assisted: EndotrachealAT on Study, SODDay 1, Machine-Assisted: ECMODay 1, Machine-Assisted: EndotrachealDay 1, SOD
Cohort 1: Infants (6 Months to <1 Year of Age)033021
Cohort 2: Children (1 to <2 Years of Age)155133
Cohort 3: Children (2 to <6 Years of Age)047041
Cohort 4: Children (6 to <13 Years of Age)214132116
Cohort 5: Adolescents (13 to <18 Years of Age)145141
Cohort 6: Adults (18 Years and Older)4749136046

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Median Time to Resolution of Individual Vital Signs

Times to return to afebrile status (normal body temperature), normal respiratory status, normal heart rate, and normal systolic blood pressure were assessed. Afebrile status is defined as a temperature <=36.6 axilla, <=37.2 oral, or <=37.7 rectal, core or typanic, degrees Centigrade. A return to normal respiratory status is defined as either: (a) return to pre-morbid oxygen requirement; or (b) return to no need for supplemental oxygen; or (c) respiratory rate <=60, <=40, <=34, <=30, <=24 or <=24 breaths/minute (without supplemental oxygen) for Cohorts 1-6 respectively . A normal HR is defined as <=160, <=150, <=140, <=120, <=100 or <=100 bpm for Cohorts 1-6 respectively, and a normal SBP is defined as >=70, >=74, >=76, >=80, >=90 or >=90 mmHg for Cohorts 1-6 respectively. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X in the category titles). (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

,,,,,
InterventionDays (Median)
Afebrile Status, n=120, 7, 11, 7, 24, 13Respiratory Status, n=89, 7, 10, 12, 23, 9HR, n=121, 7, 11, 12, 27, 13SBP, n=128, 7, 11, 12, 27, 14
Cohort 1: Infants (6 Months to <1 Year of Age)4.05.02.02.0
Cohort 2: Children (1 to <2 Years of Age)2.02.02.02.0
Cohort 3: Children (2 to <6 Years of Age)25.03.52.02.0
Cohort 4: Children (6 to <13 Years of Age)3.03.02.02.0
Cohort 5: Adolescents (13 to <18 Years of Age)3.02.02.02.0
Cohort 6: Adults (18 Years and Older)3.08.02.02.0

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Median Time to Return to Pre-morbid Functional Status

Time to return to pre-morbid functional status was assessed on a 3-point scale (bed rest, limited ambulation, or unrestricted). Only those participants available at the specified time points were analyzed. (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

InterventionDays (Median)
Cohort 6: Adults (18 Years and Older)10.0
Cohort 1: Infants (6 Months to <1 Year of Age)8.0
Cohort 2: Children (1 to <2 Years of Age)3.0
Cohort 3: Children (2 to <6 Years of Age)5.0
Cohort 4: Children (6 to <13 Years of Age)5.5
Cohort 5: Adolescents (13 to <18 Years of Age)4.0

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Median Change From Baseline (Influenza A or B Quantitative PCR, as Appropriate) in Viral Load at the Indicated Time Points

"Change from Baseline in viral load was measured from nasopharyngeal swab samples, as determined by RT-PCR (PCR positive at Baseline). Nasopharyngeal swab samples were collected at Baseline (Day 1); Day 2, Day 3, Day 4, Day 5, Day 7, and Day 10; and, only if the participants had continued symptoms and were hospitalized, post-treatment (PT) samples were collected at +2 days, +5 days, +9 days, +16 days, and +23 days. 'PT +23 days' also comprises viral load values at early study withdrawal. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X, X, X in the category titles). NA indicates that data are not available/analysis was not performed." (NCT01014988)
Timeframe: Baseline (Day 1); Days 2, 3, 4, 5, 7, and 10; and post-treatment +2, +5, +9, +16, +23 days

,,,,,
InterventionLog10 copies per milliliter (Median)
Day 2, n=89, 0, 0, 2, 3, 2Day 3, n=82, 4, 7, 10, 15, 7Day 4, n=84, 0, 0, 2, 2, 1Day 5, n=75, 5, 4, 8, 12, 5Day 7, n=23, 1, 1, 1, 3, 1Day 10, n=19, 0, 2, 1, 4, 1PT +2 days, n=32, 0, 1, 2, 6, 3PT +5 days, n=26, 0, 2, 0, 5, 2PT +9 days, n=27, 0, 1, 0, 3, 2PT +16 days, n=21, 0, 1, 0, 4, 1PT +23 days, n=21, 2, 4, 0, 4, 0
Cohort 1: Infants (6 Months to <1 Year of Age)NA-1.655NA-2.720-1.820NANANANANA-4.455
Cohort 2: Children (1 to <2 Years of Age)NA-1.930NA-3.705-6.200-5.385-6.200-5.385-6.200-2.950-4.670
Cohort 3: Children (2 to <6 Years of Age)-3.750-2.215-4.895-3.285-3.030-6.430-2.495NANANANA
Cohort 4: Children (6 to <13 Years of Age)-1.160-1.330-2.060-2.930-3.040-4.760-3.825-4.190-4.190-3.825-3.825
Cohort 5: Adolescents (13 to <18 Years of Age)-2.280-2.550-2.550-2.550-1.610-1.670-3.060-3.275-3.865-4.610NA
Cohort 6: Adults (18 Years and Older)-0.92-1.42-1.59-1.57-1.58-1.75-1.38-1.84-2.58-2.48-2.89

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Median Time to Virologic Improvement

Time to virologic improvement is defined as a 2-log drop in viral load or undetectable viral ribonucleic acid (RNA) as measured by quantitative reverse transcriptase-polymerase chain reaction (RT-PCR) from nasopharyngeal samples (PCR positive at Baseline). Only those participants available at the specified time points were analyzed. (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

InterventionDays (Median)
Cohort 6: Adults (18 Years and Older)3.0
Cohort 1: Infants (6 Months to <1 Year of Age)4.0
Cohort 2: Children (1 to <2 Years of Age)4.0
Cohort 3: Children (2 to <6 Years of Age)3.0
Cohort 4: Children (6 to <13 Years of Age)5.0
Cohort 5: Adolescents (13 to <18 Years of Age)4.0

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Number of Participants Who Permanently Discontinued the Study Treatment Due to an AE

An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. (NCT01014988)
Timeframe: Up to 10 days

InterventionParticipants (Number)
Cohort 6: Adults (18 Years and Older)17
Cohorts 1-5: Pediatrics/Adolescents (6 Months to <18 Years)2

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Number of Participants Who Used Any Concomitant Antibiotic Medications for Complications of Influenza

Concomitant medications (prescription and non-prescription) were permitted during the course of the study at the Investigator's discretion (except for prohibited medications: during the treatment period with IV zanamivir, other influenza antiviral drugs were not permitted). The number of participants who were treated with antibiotics for influenza complications was summarized. (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

InterventionParticipants (Number)
Cohort 6: Adults (18 Years and Older)63
Cohort 1: Infants (6 Months to <1 Year of Age)5
Cohort 2: Children (1 to <2 Years of Age)7
Cohort 3: Children (2 to <6 Years of Age)7
Cohort 4: Children (6 to <13 Years of Age)12
Cohort 5: Adolescents (13 to <18 Years of Age)6

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Number of Participants Who Were Permanently Discontinued From the Study Due to an AE

An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

InterventionParticipants (Number)
Cohort 6: Adults (18 Years and Older)20
Cohorts 1-5: Pediatrics/Adolescents (6 Months to <18 Years)5

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Number of Participants With Treatment-emergent (TE) Mutations

Viral RNA isolated from participants at Baseline (Day 1) and post-Baseline visits were sequenced to determine the presence of TE neuraminidase (NA) and hemagglutinin (HA) mutations resulting from selective pressure. A mutation was considered to be TE if it was not present at Baseline and was present in the last post-Baseline sample analyzed.These mutations were classified as either known to confer zanamvir resistance or novel mutations with unknown clinical significance. Please note: pediatric data are pending and will be updated when available. (NCT01014988)
Timeframe: Baseline and up to post-treatment (PT) + 23 days

InterventionParticipants (Number)
Known Zanamivir-Resistant NA MutationsNovel NA MutationsResistant HA MutationsNovel HA Mutations
Cohort 6: Adults (18 Years and Older)0524

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Number of Participants With Any AE Categorized as an Influenza Complication

An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

InterventionParticipants (Number)
Cohort 6: Adults (18 Years and Older)45
Cohort 1: Infants (6 Months to <1 Year of Age)4
Cohort 2: Children (1 to <2 Years of Age)4
Cohort 3: Children (2 to <6 Years of Age)3
Cohort 4: Children (6 to <13 Years of Age)8
Cohort 5: Adolescents (13 to <18 Years of Age)3

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Number of Participants With Any Severe or Grade 3/4 AEs

An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. AEs that occured during the study were evaluated by the Investigator and graded according to the Division of Acquired Immunodeficiency Syndrome (DAIDS) table for grading the severity of adult and pediatric AEs. Grade 3=severe; Grade 4=potentially life threatening. (NCT01014988)
Timeframe: Up to post-treatment (PT) + 23 days

InterventionParticipants (Number)
Cohort 6: Adults (18 Years and Older)57
Cohorts 1-5: Pediatrics/Adolescents (6 Months to <18 Years)23

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Geometric Mean Area Under the Serum Drug Concentration-time Curve (AUC) Over a 12-hour Dosing Interval (AUC[0-tau]) and AUC Extrapolated to Infinity (AUC[0-inf]) of Zanamivir

"The AUC(0-tau) during the repeat dose interval and AUC(0-inf) for the initial dose were evaluated. Serial blood samples for PK analysis were collected if possible in conjunction with the initial dose on Day 1 (5-7 serial samples) and over a dosing interval during repeat dosing on Days 3, 4, or 5 (5 serial samples). PK data for all participants with available blood samples were analyzed. PK data for those participants with a CLcr >=80 mL/minutes (>=80 mL/minute/1.73m^2 for cohorts 1-4) and who received an ID and a MD of 14 mg/kg (6 months to <6 years of age), 12 mg/kg, not to exceed 600 mg (6 to <18 years of age) or 600 mg zanamivir (>=18 years of age) (represented by n=X in the category titles) were summarized. NA indicates that data are not available/analysis was not performed." (NCT01014988)
Timeframe: Day 1 and Days 3, 4, or 5

,,,,,
InterventionMicrograms*hour per milliliter (Geometric Mean)
AUC(0-inf), ID, 600 mg, CLcr>=80, n=63,0,0,0,0,5AUC(0-inf), ID, 12 mg/kg, CLcr>=80, n=0,0,0,0,8,1AUC(0-inf), ID, 14 mg/kg, CLcr>=80, n=0,3,4,9,0,0AUC(0-tau), MD, 600 mg, CLcr>=80, n=65,0,0, 0,0,2AUC(0-tau), MD, 12 mg/kg, CLcr>=80, n=0,0,0,0,4,0AUC(0-tau), MD, 14 mg/kg, CLcr>=80, n=0,0,1,4,0,0
Cohort 1: Infants (6 Months to <1 Year of Age)NANA75.31NANANA
Cohort 2: Children (1 to <2 Years of Age)NANA72.42NANA68.20
Cohort 3: Children (2 to <6 Years of Age)NANA80.28NANA81.02
Cohort 4: Children (6 to <13 Years of Age)NA107.21NANA90.33NA
Cohort 5: Adolescents (13 to <18 Years of Age)91.07135.22NA64.52NANA
Cohort 6: Adults (18 Years and Older)82.86NANA90.33NANA

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Geometric Mean Maximum Serum Concentration (Cmax) of Zanamivir at the End of Infusion

"The Cmax of zanamivir was evaluated at the end of infusion. Serial blood samples for pharmacokinetic (PK) analysis were collected if possible in conjunction with the initial dose on Day 1 (5-7 serial samples) and over a dosing interval during repeat dosing on Days 3, 4, or 5 (5 serial samples). PK data for all participants with available blood samples were analyzed. PK data for those participants who were neither on extracorporeal membrane oxygenation (ECMO) nor on continuous renal replacement therapy (CRRT), who were with CLcr >=80 mL/minutes (>=80mL/minute/1.73m^2 for cohorts 1-4) and who received an initial dose (ID) and a maintenance dose (MD) of 14 mg/kg (6 months to <6 years of age), 12 mg/kg, not to exceed 600 mg (6 to <18 years of age) or 600 mg zanamivir (>=18 years of age) (represented by n=X in the category titles) were summarized. NA indicates that data are not available/analysis was not performed." (NCT01014988)
Timeframe: Day 1 and Days 3, 4, or 5

,,,,,
InterventionMicrograms per mL (Geometric Mean)
ID, 600 mg, CLcr>=80, n=67, 0, 0, 0, 0, 6ID, 12 mg/kg, CLcr>=80, n=0, 0, 0, 0, 9, 3ID, 14 mg/kg, CLcr>=80, n=0, 4, 5, 9, 0, 0MD, 600 mg, CLcr>=80, n=72, 0, 0, 0, 0, 2MD, 12 mg/kg, CLcr>=80, n=0, 0, 0, 0, 4, 0MD, 14 mg/kg, CLcr>=80, n=0, 0, 1, 4, 0, 0
Cohort 1: Infants (6 Months to <1 Year of Age)NANA36.21NANANA
Cohort 2: Children (1 to <2 Years of Age)NANA37.78NANA38.01
Cohort 3: Children (2 to <6 Years of Age)NANA41.54NANA43.19
Cohort 4: Children (6 to <13 Years of Age)NA44.16NANA45.18NA
Cohort 5: Adolescents (13 to <18 Years of Age)34.474.99NA25.73NANA
Cohort 6: Adults (18 Years and Older)32.77NANA35.30NANA

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Geometric Mean Serum Clearance of Zanamivir

"The serum clearance of zanamivir was evaluated. Clearance is defined as the volume of zanamivir per unit time eliminated from serum. Serial blood samples for PK analysis were collected if possible in conjunction with the initial dose on Day 1 (5-7 serial samples) and over a dosing interval during repeat dosing on Days 3, 4, or 5 (5 serial samples). PK data for all participants with available blood samples were analyzed. PK data for those participants with a CLcr >=80 mL/minutes (>=80 mL/minute/1.73m^2 for cohorts 1-4) and who received an ID and a MD 14 mg/kg (6 months to <6 years of age), 12 mg/kg, not to exceed 600 mg (6 to <18 years of age) or 600 mg zanamivir (>=18 years of age) (represented by n=X in the category titles) were summarized. NA indicates that data are not available/analysis was not performed." (NCT01014988)
Timeframe: Day 1 and Days 3, 4, or 5

,,,,,
InterventionmL per minutes (Geometric Mean)
ID, 600 mg, CLcr>=80, n=63, 0, 0, 0, 0, 5ID, 12 mg/kg, CLcr>=80, n=0, 0, 0, 0, 8, 1ID, 14 mg/kg, CLcr>=80, n=0, 3, 4, 9, 0, 0MD, 600 mg, CLcr>=80, n=65, 0, 0, 0, 0, 0MD, 12 mg/kg, CLcr>=80, n=0, 0, 0, 0, 4, 0MD, 14 mg/kg, CLcr>=80, n=0, 0, 1, 4, 0, 0
Cohort 1: Infants (6 Months to <1 Year of Age)NANA27.31NANANA
Cohort 2: Children (1 to <2 Years of Age)NANA31.00NANA31.78
Cohort 3: Children (2 to <6 Years of Age)NANA41.95NANA40.35
Cohort 4: Children (6 to <13 Years of Age)NA46.70NANA68.61NA
Cohort 5: Adolescents (13 to <18 Years of Age)109.8353.70NA155.03NANA
Cohort 6: Adults (18 Years and Older)120.68NANA110.71NANA

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Number of Patients With Respiratory Outcomes

(NCT01156701)
Timeframe: Baseline

,,,
Interventionpatients (Number)
InfluenzaAsthmaChronic obstructive pulmonary disease (COPD)Exacerbation of COPDBronchospasmPneumoniaBronchitisSinusitisOtitis mediaAny of the above
Cohort 1: Prophylaxis With Untreated Index31000281216
Cohort 2: Prophylaxis With Treated Index10500011520450
Cohort 3: Untreated With Untreated Index253914881533411054125722708158210166
Cohort 4: Untreated With Treated Index9354305169614064420

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Number of Participants Experiencing Hospitalization or Death Due to Influenza

The frequency of hospitalization and death in the study population was analyzed. (NCT01156701)
Timeframe: Baseline

,,,
Interventionpatients (Number)
HospitalizationDeath
Cohort 1: Prophylaxis With Untreated Index00
Cohort 2: Prophylaxis With Treated Index60
Cohort 3: Untreated With Untreated Index10634
Cohort 4: Untreated With Treated Index410

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Number of Patients With Any Respiratory Diagnosis

The frequency of any respiratory diagnosis among the four cohorts was measured. (NCT01156701)
Timeframe: 2006-2009

,,,
Interventionpatients (Number)
Respiratory DiagnosisNo Respiratory Diagnosis
Cohort 1: Prophylaxis With Untreated Index16241
Cohort 2: Prophylaxis With Treated Index50957
Cohort 3: Untreated With Untreated Index10166153550
Cohort 4: Untreated With Treated Index4206305

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Number of Patients With Asthma

The frequency of asthma among the four cohorts was measured. (NCT01156701)
Timeframe: 2006-2009

,,,
Interventionpatients (Number)
AsthmaNo Asthma
Cohort 1: Prophylaxis With Untreated Index1256
Cohort 2: Prophylaxis With Treated Index51002
Cohort 3: Untreated With Untreated Index1488162228
Cohort 4: Untreated With Treated Index546671

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Number of Patients With Bronchitis

The frequency of bronchitis among the four cohorts was measured. (NCT01156701)
Timeframe: 2006-2009

,,,
Interventionpatients (Number)
BronchitisNo Bronchitis
Cohort 1: Prophylaxis With Untreated Index8249
Cohort 2: Prophylaxis With Treated Index15992
Cohort 3: Untreated With Untreated Index2572161144
Cohort 4: Untreated With Treated Index966629

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Number of Patients With Influenza

The frequency of influenza among the four cohorts was measured. (NCT01156701)
Timeframe: 2006-2009

,,,
Interventionpatients (Number)
InfluenzaNo Influenza
Cohort 1: Prophylaxis With Untreated Index3254
Cohort 2: Prophylaxis With Treated Index10997
Cohort 3: Untreated With Untreated Index2539161177
Cohort 4: Untreated With Treated Index936632

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Number of Patients With Pneumonia

The frequency of pneumonia among the four cohorts was measured.. (NCT01156701)
Timeframe: 2006-2009

,,,
Interventionpatients (Number)
PneumoniaNo Pneumonia
Cohort 1: Prophylaxis With Untreated Index2255
Cohort 2: Prophylaxis With Treated Index11006
Cohort 3: Untreated With Untreated Index541163175
Cohort 4: Untreated With Treated Index166709

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Number of Participants With Any Serious Adverse Drug Reaction (ADR)

"A serious ADR is defined as a serious adverse drug event (ADE) that a physician has determined to be related to the use of Relenza. Serious ADE: death caused by an ADR; an event that is life threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, results in severe symptoms requiring treatment so that symptoms do not lead to previously mentioned outcomes, and a congenital anomaly/birth defect. For a complete list of all serious ADRs recorded during the study, see Serious Adverse Events section." (NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
Relenza1

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Number of Male and Female Participants With Either a Serious or Non-serious Adverse Drug Reaction

(NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
MaleFemale
Relenza31

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Number of Participants in the Indicated Age Categories With Either a Serious or Non-serious Adverse Drug Reaction

(NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
>=3 to <7 years>=7 to <15 years>=15 to <65 years>=65 to <74 years
Relenza0310

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Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Categorized by Either Having Complications or Having no Complications

A complication is defined as asthma. (NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
ComplicationsNo complications
Relenza13

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Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Categorized by Either Having Risk Factors for Influenza or Having no Risk Factors

Risk factors are defined as pregnancy; infancy; being elderly; and having chronic respiratory disease, cardiocirculatory disease, and/or diabetes. (NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
Risk factorNo risk factor
Relenza13

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Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Categorized by Reason for the Use of Relenza

The dose given for treatment of influenza is 10 mg twice daily for 5days. Prophylaxis is defined as a measure taken for the prevention of a disease or condition. The prophylactic dose of Relenza is 10 mg once daily for 10 days. (NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
TreatmentProphylaxis
Relenza40

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Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Who Were Also in the Indicated High-risk Categories

Participants with only hypertension were excluded from the cardiocirculatory disease category. Participants in high-risk categories are at risk for the aggravation of both infection and symptoms. (NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
PregnantInfant (<7 years of age)Elderly (>=65 years of age)Chronic respiratory diseaseCardiocirculatory diseaseDiabetes
Relenza000100

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Number of Participants With Any Adverse Drug Reaction

"An adverse drug reaction is defined as a drug adverse event that a physician has determined to be related to the use of Relenza. A drug adverse event is defined as any unfavorable or unintended sign (including laboratory test abnormalities), symptom, or disease that occurs when a drug is administered, regardless of the relationship to the drug. For a complete list of all adverse drug reactions recorded during the study, see the section entitled Other (Non-serious) Adverse Events." (NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
Relenza4

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Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Who Were Vaccinated for Influenza

(NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
VaccinatedNot vaccinated
Relenza13

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Number of Participants With Either a Serious or Non-serious Adverse Drug Reaction Who Were Also Taking Concomitant Medications

Concomitant medications are defined as drugs used during the administration of Relenza. (NCT01199744)
Timeframe: 5 months (November 2009 to March 2010)

Interventionparticipants (Number)
Concomitant medicationNo concomitant medication
Relenza40

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Number of Participants With the Indicated Clinical Symptoms of Influenza

Influenza clinical symptoms included nasal symptoms (rhinorrhea, congestion), feverishness, cough, myalgias, fatigue, diarrhea, anorexia, dyspnea, headache, sore throat, nausea, and vomiting. Influenza symptoms were assessed once daily during inpatient hospitalization and once at each post-treatment assessment. (NCT01231620)
Timeframe: Up to 42 days

,,
InterventionParticipants (Count of Participants)
AnorexiaCoughDiarrheaDyspneaFatigueFeverishnessHeadacheMyalgiasNasal symptoms (rhinorrhea, congestion)NauseaSore throatVomiting
IV Zanamivir 300 mg10215164143144138104115118579427
IV Zanamivir 600 mg112150571451441451021171235111523
Oral Oseltamivir 75 mg12315766152148136103114122779745

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Number of Participants With the Indicated Hematology Values Shifts From Baseline (Day 1) and up to 42 Days

Blood samples for laboratory assessments were collected at Baseline (Day 1), Day 3, Day 5/6, Day 8, Day 10/11 (or last day of randomized treatment), S/R Day 1, S/R Day 3, and S/R Day 5/6 (last day of S/R treatment for those participants who utilized this option), Post-Treatment +2 (if hospitalized), and Post-Treatment +5, +16, and +28 Days. Hematology parameters included hemoglobin, lymphocytes, total neutrophils, platelet count, and white blood cell (WBC) count. Per the DAIDS table for grading the severity of adult and pediatric AEs, Grade (G) 1=mild, G2= moderate, G3=severe and G4=potentially life threatening. The number of participants with values that were G1, G2, G3 and G4 relative to the normal range for the indicated hematology parameters is summarized. Baseline is defined as the pre-dose value collected on Study Day 1. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionParticipants (Count of Participants)
Hemoglobin G1Hemoglobin G2Hemoglobin G3Hemoglobin G4Lymphocytes G1Lymphocytes G2Lymphocytes G3Lymphocytes G4Neutrophils G1Neutrophils G2Neutrophils G3Neutrophils G4Platelets G1Platelets G2Platelets G3Platelets G4Leukocytes G1Leukocytes G2Leukocytes G3Leukocytes G4
IV Zanamivir 300 mg281114081116182201818423301
IV Zanamivir 600 mg25191041815211920102212312510
Oral Oseltamivir 75 mg2813811011181430032116221302

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Number of Participants With the Indicated Treatment-emergent (TE) Grade (G) 3/4 Clinical Chemistry Toxicities

A toxicity was considered to be TE if it was greater than the Baseline grade, and if it had developed or increased post-Baseline in intensity (and prior to the last dose of investigational product). Clinical chemistry parameters included albumin, ALP, ALT, AST, total bilirubin, calcium, creatine kinase, chloride, CO2/bicarbonate, creatinine, potassium, magnesium and sodium. Per the DAIDS table for grading the severity of adult and pediatric AEs, Grade 3=severe and Grade 4=potentially life threatening. Baseline is defined as the pre-dose value collected on Study Day 1. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionParticipants (Count of Participants)
Albumin, G3Albumin, G4ALP, G3ALP, G4ALT, G3ALT, G4AST, G3AST, G4Total Bilirubin, G3Total Bilirubin, G4Creatine Kinase, G3Creatine Kinase, G4Carbon Dioxide, G3Carbon Dioxide, G4Creatinine, G3Creatinine, G4Magnesium, G3Magnesium, G4Hypercalcemia, G3Hypercalcemia, G4Hyperkalemia, G3Hyperkalemia, G4Hypernatremia, G3Hypernatremia, G4Hypocalcemia, G3Hypocalcemia, G4Hypokalemia, G3Hypokalemia, G4Hyponatremia, G3Hyponatremia G4
IV Zanamivir 300 mg6001202120230133100021001020010
IV Zanamivir 600 mg302022422031006200000510740000
Oral Oseltamivir 75 mg400141511021001001001350840000

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Number of Participants With the Indicated Treatment-emergent (TE) Grade 3/4 Hematology Toxicities

A toxicity was considered to be TE if it was greater than the Baseline grade, and if it had developed or increased post-Baseline in intensity (and prior to the last dose of investigational product). The hematology parameters included hemoglobin, lymphocytes, total neutrophils, platelet count, and WBC count. Per the DAIDS table for grading the severity of adult and pediatric AEs, Grade 3=severe and Grade 4=potentially life threatening. Baseline is defined as the pre-dose value collected on Study Day 1. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionParticipants (Count of Participants)
Hemoglobin, G3Hemoglobin, G4Lymphocytes, G3Lymphocytes, G4Total Neutrophils, G3Total Neutrophils, G4Platelet count, G3Platelet count, G4Leukocytes Count, G3Leukocytes Count, G4
IV Zanamivir 300 mg29263144312
IV Zanamivir 600 mg245514244311
Oral Oseltamivir 75 mg268117235203

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Number of Participants With the Indicated Ventilation Status: Modality of Invasive and Non-invasive Ventilator Support and Oxygen Supplementation

"Ventilation status was assessed three times daily during the treatment period/hospitalization. Ventilation status was assessed once daily during inpatient/hospitization and once at each post-treatment clinic visit. The number of participants reported for machine-assisted: extracorporeal membrane oxygenation (ECMO), endotracheal mechanical ventilation, and supplemental oxygen delivery (SOD), no supplemental oxygen (O2) or ventilation support, Respiratory support at any time (AT) on study and at Baseline (Day 1) are summarized. Data for the any time (AT) on study time point was reported." (NCT01231620)
Timeframe: Up to 42 days

,,
InterventionParticipants (Count of Participants)
Day 1, Machine-Assisted: ECMODay 1, Machine-Assisted: EndotrachealDay 1, SODDay 1, No supplemental O2 or ventilation supportDay 1, Respiratory SupportAT on Study, Machine-Assisted: ECMOAT on Study, Machine-Assisted: EndotrachealAT on Study, SODAT on Study, No supplemental O2 or ventilation supAT on Study, Respiratory Support
IV Zanamivir 300 mg02896323423613713846
IV Zanamivir 600 mg025103292903113713537
Oral Oseltamivir 75 mg02787373913712813150

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Serum Concentration of IV Zanamivir

Pharmacokinetic samples were collected at four time points to characterize peak concentration (end of infusion; C[EOI]) after the first dose on Day 1 and on Day 4 to characterize the pre-dose concentration (C[0]), the peak concentration C(EOI), and the trough concentration at 11-12 hours post-dose (C[12]) of zanamavir. Data was summarized by Creatinine clearance (CL) Category. The dose on Day 1 is the initial dose (unadjusted) and the dose on Day 4 is the maintenance dose. (NCT01231620)
Timeframe: Day 1 and Day 4

Interventionmicrogram/Liter (mcg/L) (Mean)
CL <15, Day 1, 30 minCL <15, Day 4, pre-doseCL <15, Day 4, 30 minCL <15, Day 4, 11-12 hrCL 15-<30, Day 13, 30 minCL 15-<30, Day 4, pre-doseCL 15-<30, Day 4, 30 minCL 15-<30, Day 4, 11-12 hrCL 30-<50, Day 1, 30 minCL 30-<50, Day 4, pre-doseCL 30-<50, Day 4, 30 minCL 30-<50, Day 4, 11-12 hrCL 50-<80, Day 1, 30 minCL 50-<80, Day 4, pre-doseCL 50-<80, Day 4, 30 minCL 50-<80, Day 4, 11-12 hrCL >=80, Day 1, 30 min,CL >=80, Day 4, pre-doseCL >=80, Day 4, 30 minCL >=80, Day 4, 11-12 hr
IV Zanamivir 300 mg14454.6293.21329.4605.120403.35906.413636.47600.318756.82094.812334.42932.519146.72793.331541.31345.918561.72342.621580.72036.2

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Serum Concentration of IV Zanamivir

Pharmacokinetic samples were collected at four time points to characterize peak concentration (end of infusion; C[EOI]) after the first dose on Day 1 and on Day 4 to characterize the pre-dose concentration (C[0]), the peak concentration C(EOI), and the trough concentration at 11-12 hours post-dose (C[12]) of zanamavir. Data was summarized by Creatinine clearance (CL) Category. The dose on Day 1 is the initial dose (unadjusted) and the dose on Day 4 is the maintenance dose. (NCT01231620)
Timeframe: Day 1 and Day 4

Interventionmicrogram/Liter (mcg/L) (Mean)
CL <15, Day 1, 30 minCL <15, Day 4, pre-doseCL <15, Day 4, 30 minCL <15, Day 4, 11-12 hrCL 15-<30, Day 13, 30 minCL 15-<30, Day 4, pre-doseCL 15-<30, Day 4, 30 minCL 15-<30, Day 4, 11-12 hrCL 30-<50, Day 1, 30 minCL 30-<50, Day 4, pre-doseCL 30-<50, Day 4, 30 minCL 30-<50, Day 4, 11-12 hrCL 50-<80, Day 1, 30 minCL 50-<80, Day 4, pre-doseCL 50-<80, Day 4, 30 minCL 50-<80, Day 4, 11-12 hrCL >=80, Day 1, 30 min,CL >=80, Day 4, pre-doseCL >=80, Day 4, 30 minCL >=80, Day 4, 11-12 hrMissing, Day 1, 30 min
IV Zanamivir 600 mg26410.89635.619828.915459.141102.84995.6133784953.442467.37637.4159292.119549.249666.113107.722220.422623.935139.219379.875255.119428.741109.7

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Median Time to Virologic Improvement

Virologic improvement is defined as a 2 log drop in viral load or sustained undetectable viral ribonucleic acid (RNA) (on two successive occasions) as measured by quantitative reverse transcriptase-polymerase chain reaction (RT-PCR) from nasopharyngeal samples. Nasopharyngeal swabs were collected daily from Baseline through Day 5. If randomized treatment was continued beyond Day 5, samples were taken on Treatment Days 6, 8, 10 and on the last day of randomized treatment. For participants who utilized the Switch (S)/Rescue (R) option, samples were taken on S/R Day 1, S/R Day 3, S/R Day 5, or S/R Day 6, whichever was the last day of S/R treatment. Nasopharyngeal swabs were taken if the participant was symptomatic and continued to be hospitalized on the Post-Treatment +2, +5, +9, +16, and +28 day assessment. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionDays (Median)
Influenza A and BInfluenza A/H1N1Influenza A/H3N2Influenza B
IV Zanamivir 300 mg3335
IV Zanamivir 600 mg3333
Oral Oseltamivir 75 mg3333

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Median Time to Return to the Pre-morbid Level of Activity as Measured by the 3-point Scale

Median time to return to pre-morbid level of activity was assessed once daily during treatment/hospitalization and once at each post-treatment assessment and was measured using the 3- point scale (bed rest, limited ambulation, or unrestricted). (NCT01231620)
Timeframe: Up to 42 days

InterventionDays (Median)
IV Zanamivir 300 mg5
IV Zanamivir 600 mg4
Oral Oseltamivir 75 mg4

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Number of Participants Who Permanently Discontinued the Study Treatment Due to an AE

An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. For marketed medicinal products, this also includes failure to produce expected benefits (i.e., lack of efficacy), abuse, or misuse. (NCT01231620)
Timeframe: Up to 42 days

InterventionParticipants (Count of Participants)
IV Zanamivir 300 mg8
IV Zanamivir 600 mg10
Oral Oseltamivir 75 mg11

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Number of Participants Who Were Permanently Discontinued From the Study Due to an AE

An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. For marketed medicinal products, this also includes failure to produce expected benefits (i.e., lack of efficacy), abuse, or misuse. (NCT01231620)
Timeframe: Up to 42 days

InterventionParticipants (Count of Participants)
IV Zanamivir 300 mg14
IV Zanamivir 600 mg16
Oral Oseltamivir 75 mg13

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Number of Participants With Any Severe or Grade 3/4 AE

An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. For marketed medicinal products, this also includes failure to produce expected benefits (i.e., lack of efficacy), abuse, or misuse. AEs that occurred during the study were evaluated by the Investigator and graded according to the Division of Acquired Immunodeficiency Syndrome (DAIDS) table for grading the severity of AEs. Grade 3=severe; Grade 4=potentially life threatening. (NCT01231620)
Timeframe: Up to 42 days

InterventionParticipants (Count of Participants)
IV Zanamivir 300 mg39
IV Zanamivir 600 mg45
Oral Oseltamivir 75 mg44

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Percentage of Participants With Respiratory Improvement

Respiratory Status (RS) is a component of TTCR. Response criteria included the return to the pre-morbid oxygen requirement (participants with chronic oxygen use), a need for supplemental oxygen (administered by any modality: ventilator, non-invasive ventilation, facemask, facetent, nasal canula, etc.) to no need for supplemental oxygen, or a respiratory rate of =<24 breaths/minute (without supplemental oxygen). Data are presented as the percentage of participants achieving respiratory improvement. (NCT01231620)
Timeframe: Up to 42 days

InterventionPercentage of participants (Number)
IV Zanamivir 300 mg77
IV Zanamivir 600 mg78
Oral Oseltamivir 75 mg74

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Time to Clinical Response (TTCR) in Participants With Confirmed Influenza

Clinical response is defined as the resolution of at least 4 of the 5 vital signs (temperature, oxygen saturation, respiratory status, heart rate, systolic blood pressure) within the respective resolution criteria, maintained for at least 24 hours, or hospital discharge, whichever occurred first. This analysis was performed for Influenza positive population, for those with symptom onset less than or equal to (<=) 4 days, and for those on mechanical (mech) ventilation or in intensive care unit (ICU). 99 days is censored time for the participants who did not achieve TTCR. (NCT01231620)
Timeframe: Up to 42 days

InterventionDays (Median)
IV Zanamivir 300 mg5.87
IV Zanamivir 600 mg5.14
Oral Oseltamivir 75 mg5.63

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Change From Baseline in Quantitative Virus Culture From Nasopharyngeal Swabs Positive at Baseline

Nasopharyngeal swabs were collected daily from Baseline through Day 5. If randomized treatment was continued beyond Day 5, samples were taken on Treatment Day 6, Day 8, Day 10, Day 11, and the last day of randomized treatment. For participants who utilized the S/R option, samples were taken on S/R Day1, S/R Day3, S/R Day5, or S/R Day6, whichever was the last day of S/R treatment. Samples were taken if the participant was symptomatic and continued to be hospitalized on the Post-Treatment +2, +5, +9, +16 and +28Day assessment. Viral load was measured by Quantitative Virus Culture, log10 50% Tissue Culture Infectious Dose (TCID50)/milliliter (mL). Baseline is defined as the pre-dose value collected on Study Day 1. Change from Baseline was calculated as the post-Baseline value minus Baseline value . (NCT01231620)
Timeframe: Baseline (Day 1), Day 3, Day 5, Day 8, Day 10, Day 11 and/or last day of randomized treatment, if randomized treatment was extended beyond 5 days, and S/R Day 5/6 (up to Day 14) if applicable

Interventionlog10 TCID50/mL (Median)
Day 3Day 5Day 8Day 10Day 11S/R Day 6
IV Zanamivir 300 mg-2.01-2.51-1.64-3.76-3.01-2.5

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Change From Baseline in Quantitative Virus Culture From Nasopharyngeal Swabs Positive at Baseline

Nasopharyngeal swabs were collected daily from Baseline through Day 5. If randomized treatment was continued beyond Day 5, samples were taken on Treatment Day 6, Day 8, Day 10, Day 11, and the last day of randomized treatment. For participants who utilized the S/R option, samples were taken on S/R Day1, S/R Day3, S/R Day5, or S/R Day6, whichever was the last day of S/R treatment. Samples were taken if the participant was symptomatic and continued to be hospitalized on the Post-Treatment +2, +5, +9, +16 and +28Day assessment. Viral load was measured by Quantitative Virus Culture, log10 50% Tissue Culture Infectious Dose (TCID50)/milliliter (mL). Baseline is defined as the pre-dose value collected on Study Day 1. Change from Baseline was calculated as the post-Baseline value minus Baseline value . (NCT01231620)
Timeframe: Baseline (Day 1), Day 3, Day 5, Day 8, Day 10, Day 11 and/or last day of randomized treatment, if randomized treatment was extended beyond 5 days, and S/R Day 5/6 (up to Day 14) if applicable

,
Interventionlog10 TCID50/mL (Median)
Day 3Day 5Day 8Day 10Day 11S/R Day 5S/R Day 6
IV Zanamivir 600 mg-2.01-2.26-2.01-0.3-0.3-4.3-4.3
Oral Oseltamivir 75 mg-2.01-2.26-2.26-2.26-2.26-3.00.0

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Change From Baseline in the Katz Activities of Daily Living (ADL) Score and Each ADL Activity Score

The Katz ADL scores were collected for bathing, dressing, toileting, transferring, continence, and feeding activities and were assessed once daily during the treatment period/hospitalization and once at each post-treatment Clinic Visit. For the six individual activities, a score of 1 indicates independence, and a score of 0 indicates dependence. The total score is generated by adding the scores of all six activities. A total score of 6 indicates that the participant was independent; a total score of 0 indicates that the participant was very dependent. Baseline is defined as the pre-dose value collected on Study Day 1. Change from Baseline is defined as the difference at each time point (Day 5/6, and Day 10/11, and last day S/R if treatment was extended beyond 5 days) and the end of the study (post-treatment [PT] +28 Days) compared to Baseline. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionScores on the scale (Mean)
Total Score Day 5/6Total Score Day 10/11Total Score Last Day of S/RTotal Score PT+28 DayBathing: DAY 5/6Bathing: DAY 10/11Bathing: Last Day of S/RBathing: PT + 28 DAYSDressing DAY 5/6Dressing: Day 10/11Dressing: Last Day of S/RDressing:PT+28 DayToileting: DAY 5/6Toileting: Day 10/11Toileting: Last Day of S/RToileting: PT+28 DayTransferring: DAY 5/6Transferring: Day 10/11Transferring: Last Day of S/RTransferring: PT+28 DayContinence: DAY 5/6Continence: Day 10/11Continence: Last Day of S/RContinence: PT+28 DayFeeding: Day 5/6Feeding: Day 10/11Feeding: Last Day of S/RFeeding: PT+28 Day
IV Zanamivir 300 mg1.070.880.22.130.240.190.20.430.230.130.20.420.190.130.20.40.280.190.00.450.070.13-0.20.220.070.13-0.20.21
IV Zanamivir 600 mg0.930.5-3.01.720.190.0-0.50.340.210.0-0.50.370.190.33-0.50.320.230.17-0.50.360.050.0-0.50.160.070.0-0.50.17
Oral Oseltamivir 75 mg0.78-0.080.751.980.180.00.00.390.14-0.080.130.410.140.080.00.370.170.080.250.40.07-0.080.130.230.08-0.080.250.19

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Change From Baseline Viral Load (Influenza A or B) by qPCR From Nasopharyngeal Swabs Positive at Baseline

Nasopharyngeal swabs were collected daily from Baseline through Day 5. If randomized treatment was continued beyond Day 5, samples were taken on Treatment Day 6, Day 8, Day 10, Day 11, and the last day of randomized treatment. For participants who utilized the S/R option, samples were taken on S/R Day 1, S/R Day 3, S/R Day 5, or S/R Day 6, whichever was the last day of S/R treatment. Samples were taken if the participant was symptomatic and continued to be hospitalized on the post-treatment +2, +5, +9, +16 and +28 day assessment. Viral load as measured by PCR. Baseline is defined as the pre-dose value collected on Study Day 1. Change from Baseline was calculated as the post-Baseline value minus the Baseline value. (NCT01231620)
Timeframe: Baseline (Day 1), Day 3, Day 5, Day 8, Day 10, Day 11 and/or last day of randomized treatment, if randomized treatment was extended beyond 5 days, and S/R Day 5/6 (up to Day 14) if applicable

Interventionlog10 vp/mL (Median)
Day 3Day 5Day 8Day 10Day 11S/R Day 6
IV Zanamivir 300 mg-1.5-2.51-2.38-2.75-3.58-5.2

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Change From Baseline Viral Load (Influenza A or B) by qPCR From Nasopharyngeal Swabs Positive at Baseline

Nasopharyngeal swabs were collected daily from Baseline through Day 5. If randomized treatment was continued beyond Day 5, samples were taken on Treatment Day 6, Day 8, Day 10, Day 11, and the last day of randomized treatment. For participants who utilized the S/R option, samples were taken on S/R Day 1, S/R Day 3, S/R Day 5, or S/R Day 6, whichever was the last day of S/R treatment. Samples were taken if the participant was symptomatic and continued to be hospitalized on the post-treatment +2, +5, +9, +16 and +28 day assessment. Viral load as measured by PCR. Baseline is defined as the pre-dose value collected on Study Day 1. Change from Baseline was calculated as the post-Baseline value minus the Baseline value. (NCT01231620)
Timeframe: Baseline (Day 1), Day 3, Day 5, Day 8, Day 10, Day 11 and/or last day of randomized treatment, if randomized treatment was extended beyond 5 days, and S/R Day 5/6 (up to Day 14) if applicable

,
Interventionlog10 vp/mL (Median)
Day 3Day 5Day 8Day 10Day 11S/R Day 5S/R Day 6
IV Zanamivir 600 mg-1.83-2.71-3.16-3.03-2.6-3.8-5.4
Oral Oseltamivir 75 mg-1.75-2.73-1.78-2.63-3.29-5.7-3.84

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Median Time of Duration of Clinical Symptoms of Influenza

Influenza clinical symptoms included nasal symptoms (rhinorrhea, congestion), feverishness, cough, myalgias, fatigue, diarrhea, anorexia, dyspnea, headache, sore throat, nausea, and vomiting. Influenza symptoms were assessed once daily during inpatient/hospitalization and once at each post-treatment assessment. (NCT01231620)
Timeframe: Up to 42 days

,,
InterventionDays (Median)
AnorexiaCoughDiarrheaDyspneaFatigueFeverishnessHeadacheMyalgiasNasal symptomsNauseaSore throatVomiting
IV Zanamivir 300 mg51437112346332
IV Zanamivir 600 mg31326112334221
Oral Oseltamivir 75 mg51538122.5445.5231

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Median Time of Duration of Hospitalization and Intensive Care Unit (ICU) Stay

Hospital duration and ICU duration was assessed from the first day of dosing. Hospital duration was calculated as the discharge date minus the admission date + 1. Hospital duration while on study was the earlier of discharge, completion, or withdrawal minus the later of the admission date or the study start date + 1. ICU duration-Modified was calculated as the original ICU duration minus ICU days prior to Study Day 1. (NCT01231620)
Timeframe: Day 1 to the end of the study (assessed up to 42 days)

,,
InterventionDays (Median)
HospitalizationHospitalization while on studyHospitalization-ICUICU Duration Modified
IV Zanamivir 300 mg10887
IV Zanamivir 600 mg867.56
Oral Oseltamivir 75 mg9787

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Median Time of Duration of Invasive and Non-invasive Ventilator Support and Oxygen Supplementation

Ventilation status was assessed three times daily during the treatment period/hospitalization. Ventilation status was assessed once daily during inpatient/hospitalization and once at each post-treatment clinic visit. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionDays (Median)
Ventilator SupportOxygen Supplementation
IV Zanamivir 300 mg94.4
IV Zanamivir 600 mg5.24.2
Oral Oseltamivir 75 mg8.23.7

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Median Time to no Detectable Viral RNA and the Absence of Cultivable Virus in Any Obtained Sample (Upper and Lower Respiratory Samples)

Upper (nasopharyngeal swabs) and lower (Endotracheal aspirates, bronchoalveolar lavage samples, where available) respiratory samples were collected daily from Baseline/Day 1 through Day 5 and Day 6 (if the last day of randomized treatment). Endotracheal aspirates were collected in participants who were intubated. If treatment was continued beyond Day 5, additional samples were taken on Treatment Day 6, Day 8, Day 10, and/or the day of the last dose of randomized treatment, if applicable, and S/R Day 1, S/R Day 3, S/R Day 5, or S/R Day 6 if the last day of S/R treatment. If the participant was symptomatic and hospitalized, samples were taken on the Post-treatment+2, +5, +9, +16 assessment days, and at the Post-Treatment +28 Day. Assessment of samples was done by quantitative RT-PCR. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionDays (Median)
Influenza A and BPositive at Baseline
IV Zanamivir 300 mg44
IV Zanamivir 600 mg34
Oral Oseltamivir 75 mg44

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Median Time to Return to Pre-morbid Functional Status as Measured by the Katz ADL Score and Each ADL Activity Score

Pre-morbid functional status is defined as the best functional status in the 4 weeks prior to enrolment. Median time to return to pre-morbid functional status was assessed via the Katz ADL score (bathing, dressing, toileting, transferring, continence, and feeding activities). For the six individual activities, a score of 1 indicates independence, and a score of 0 indicates dependence. The total score is generated by adding the scores of all six activities. A total score of 6 indicates that the participant was independent; a total score of 0 indicates that the participant was very dependent. (NCT01231620)
Timeframe: Up to 42 days

,,
InterventionDays (Median)
Total scoreBathingDressingToiletingTransferringContinenceFeeding
IV Zanamivir 300 mg2222222
IV Zanamivir 600 mg2222222
Oral Oseltamivir 75 mg2.5222222

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Median Time to the Absence of Fever and Improved Respiratory Status, Oxygen Saturation, Heart Rate, and Systolic Blood Pressure

The absence of fever is defined as a non-axillary temperature recording <=36.6 degrees Celsius axillary, <= 37.2 degrees Celsius oral or <= 37.7 degrees Celsius core. Respiratory Status (RS) response criteria included the return to the pre-morbid oxygen requirement (participants with chronic oxygen use), or the need for supplemental oxygen (administered by any modality: ventilator, non-invasive ventilation, facemask, facetent, nasal canula, etc.) to no need for supplemental oxygen, or a respiratory rate =<24 breaths/minute (without supplemental oxygen). Oxygen saturation response criteria: >=95% (without supplemental oxygen). Heart rate response criteria: =<100 beats/minute. Systolic blood pressure response criteria: >=90 millimeters of mercury. Vital signs were assessed three times daily during the treatment period/hospitalization. Vital signs were assessed once daily during inpatient/hospitization and once at each post-treatment clinic visit. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionDays (Median)
FeverOxygen SaturationRespiratory statusHeart rateSystolic blood pressure
IV Zanamivir 300 mg1.65.33.50.40.3
IV Zanamivir 600 mg0.85.63.60.40.3
Oral Oseltamivir 75 mg1.54.52.80.50.3

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Number of Participants Assessed as Normal/Abnormal (Clinically Significant [CS] and Not Clinically Significant [NCS]) for 12-lead Electrocardiogram (ECG) at Baseline (Day 1) and Day 4

On Baseline/Day 1, a 12-lead ECG was obtained within approximately 24 hours prior to dosing. The number of participants with an ECG status of normal and abnormal CS or NCS, as determined by the Investigator, is reported. Normal=all ECG parameters within the accepted normal ranges. Abnormal=ECG findings outside of normal ranges. CS=ECG with a CS abnormality that meets exclusion criteria. NCS=ECG with an abnormality that is not CS nor meets exclusion criteria, per Investigator, based on reasonable standards of clinical judgment. In the original protocol ECGs were also done on Day 4, however, amendment 2 removed this requirement and therefore not all participants had Day 4 ECGs. (NCT01231620)
Timeframe: Baseline (Day 1) and Day 4

,,
InterventionParticipants (Count of Participants)
NormalAbnormal - Not Clinically SignificantAbnormal - Clinically Significant
IV Zanamivir 300 mg100975
IV Zanamivir 600 mg121864
Oral Oseltamivir 75 mg991027

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Number of Participants Who Returned to Their Pre-morbid Functional Status as Assessed Per the Katz ADL Score and Each ADL Activity Score at the End of the Study

Pre-morbid functional status is defined as the best functional status in the 4 weeks prior to enrolment. The number of participants who returned to their pre-morbid functional status at the end of the study assessed per the Katz ADL score (bathing, dressing, toileting, transferring, continence and feeding activities) is summarized. (NCT01231620)
Timeframe: Up to 42 days

,,
InterventionParticipants (Count of Participants)
TotalBathingDressingToiletingTransferringContinenceFeeding
IV Zanamivir 300 mg139135138139140142145
IV Zanamivir 600 mg138133135136140143148
Oral Oseltamivir 75 mg130126126130133139144

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Number of Participants With All Cause and Attributable Mortality at Day 14, at Day 28, and at the End of Study Visit

The number of participants who died on or before Day 14, Day 28, and the End of Study Visit were summarized. (NCT01231620)
Timeframe: On or before Day 14, Day 28, End of Study Visit (assessed up to 42 days)

,,
InterventionParticipants (Count of Participants)
Died on or before Study Day 14: all causeDied on or before Study Day 28: all causeDied while on-study: all causeDied on or before Study Day 14: attributableDied on or before Study Day 28: attributableDied while on-study: attributable
IV Zanamivir 300 mg5810355
IV Zanamivir 600 mg8912456
Oral Oseltamivir 75 mg5910456

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Number of Participants With Complications of Influenza and Associated Antibiotic Use

The number of participants with complications of influenza and associated antibiotic use were summarized (NCT01231620)
Timeframe: Up to 42 days

,,
InterventionParticipants (Count of Participants)
Associated use of any antibioticAny complication of influenza
IV Zanamivir 300 mg2234
IV Zanamivir 600 mg1633
Oral Oseltamivir 75 mg2941

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Number of Participants With no Detectable Viral RNA and the Absence of Cultivable Virus in Lower Respiratory Samples (Bronchoalveolar Lavage Sample [BAL], Endotracheal Aspirate)

Lower respiratory samples included BAL and endotracheal aspirates. Endotracheal aspirates were requested in participants (par.) who were intubated. Upper (nasopharyngeal swabs) and lower (Endotracheal aspirates, bronchoalveolar lavage samples) respiratory samples were collected daily from Baseline/Day 1 through Day 5 and Day 6 (if the last day of randomized treatment [trt]). Endotracheal aspirates were collected in participants who were intubated. If trt was continued beyond Day 5, additional samples were taken on Trt Day 6, Day 8, Day 10, and/or the day of the last dose of randomized trt, if applicable, and S/R Day 1, S/R Day 3, S/R Day 5, or S/R Day 6 if the last day of S/R trt. If the par. was symptomatic and hospitalized, samples were taken on the Post-Trt +2, +5, +9, +16 assessment days, and at the Post-Trt [PT]+28 Day assessment. Assessment of samples was done by quantitative RT-PCR and viral culture. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

InterventionParticipants (Count of Participants)
Influenza A and B Day 1Influenza A and B Day 2Influenza A and B Day 3Influenza A and B Day 4Influenza A and B Day 5Influenza A and B Day 6Influenza A and B Day 8Influenza A and B Day 10Influenza A and B PT + 2 DaysInfluenza A and B PT + 5 DaysInfluenza A and B PT + 9 DaysInfluenza A and B PT + 16 Days
IV Zanamivir 600 mg042241001111

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Number of Participants With no Detectable Viral RNA and the Absence of Cultivable Virus in Lower Respiratory Samples (Bronchoalveolar Lavage Sample [BAL], Endotracheal Aspirate)

Lower respiratory samples included BAL and endotracheal aspirates. Endotracheal aspirates were requested in participants (par.) who were intubated. Upper (nasopharyngeal swabs) and lower (Endotracheal aspirates, bronchoalveolar lavage samples) respiratory samples were collected daily from Baseline/Day 1 through Day 5 and Day 6 (if the last day of randomized treatment [trt]). Endotracheal aspirates were collected in participants who were intubated. If trt was continued beyond Day 5, additional samples were taken on Trt Day 6, Day 8, Day 10, and/or the day of the last dose of randomized trt, if applicable, and S/R Day 1, S/R Day 3, S/R Day 5, or S/R Day 6 if the last day of S/R trt. If the par. was symptomatic and hospitalized, samples were taken on the Post-Trt +2, +5, +9, +16 assessment days, and at the Post-Trt [PT]+28 Day assessment. Assessment of samples was done by quantitative RT-PCR and viral culture. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

InterventionParticipants (Count of Participants)
Influenza A and B Day 1Influenza A and B Day 2Influenza A and B Day 3Influenza A and B Day 4Influenza A and B Day 5Influenza A and B Day 6Influenza A and B Day 8Influenza A and B Day 10Influenza A and B S/R Day 1Influenza A and B S/R Day 3Influenza A and B PT + 2 DaysInfluenza A and B PT + 5 DaysInfluenza A and B PT + 9 DaysInfluenza A and B PT + 16 DaysInfluenza A and B PT + 28 Days
Oral Oseltamivir 75 mg010223200130321

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Number of Participants With no Detectable Viral RNA and the Absence of Cultivable Virus in Lower Respiratory Samples (Bronchoalveolar Lavage Sample [BAL], Endotracheal Aspirate)

Lower respiratory samples included BAL and endotracheal aspirates. Endotracheal aspirates were requested in participants (par.) who were intubated. Upper (nasopharyngeal swabs) and lower (Endotracheal aspirates, bronchoalveolar lavage samples) respiratory samples were collected daily from Baseline/Day 1 through Day 5 and Day 6 (if the last day of randomized treatment [trt]). Endotracheal aspirates were collected in participants who were intubated. If trt was continued beyond Day 5, additional samples were taken on Trt Day 6, Day 8, Day 10, and/or the day of the last dose of randomized trt, if applicable, and S/R Day 1, S/R Day 3, S/R Day 5, or S/R Day 6 if the last day of S/R trt. If the par. was symptomatic and hospitalized, samples were taken on the Post-Trt +2, +5, +9, +16 assessment days, and at the Post-Trt [PT]+28 Day assessment. Assessment of samples was done by quantitative RT-PCR and viral culture. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

InterventionParticipants (Count of Participants)
Influenza A and B Day 1Influenza A and B Day 2Influenza A and B Day 3Influenza A and B Day 4Influenza A and B Day 5Influenza A and B Day 6Influenza A and B Day 8Influenza A and B Day 10Influenza A and B S/R Day 3Influenza A and B S/R Day 5Influenza A and B PT + 2 DaysInfluenza A and B PT + 5 DaysInfluenza A and B PT + 9 DaysInfluenza A and B PT + 16 DaysInfluenza A and B PT + 28 Days
IV Zanamivir 300 mg001233200044431

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Number of Participants With Resistance-associated Mutations Detected in the Neuraminidase (NA) and Hemagglutinin (HA) Gene of Influenza A and B Viruses in Nasopharyngeal Swabs and Endotracheal/BAL Samples

Nasopharyngeal swabs and endotracheal /BAL samples were collected for viral susceptibility analysis. Susceptibility analyses consisted of phenotyping and genotyping. Resistance mutations were detected by genotyping. Viral susceptibility to zanamivir and oral oseltamivir at Baseline and throughout treatment determined by NA and HA (gene of influenza A and B viruses) sequence analysis and NA enzyme inhibition. Number of participants with viral mutation events are summarized, this includes all resistance mutations (substitutions) i.e. those present at Baseline and those that emerged during treatment. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionParticipants (Count of Participants)
NA Gene,H3N2: Y155FNA Gene,H3N2:S245NNA Gene,H3N2:I222VNA Gene,H3N2:N294S/NNA Gene,H3N2:V149ANA Gene,H3N2:D198D/GNA Gene,H3N2:G248G/ENA Gene,H3N2:N294D/NNA Gene,H3N2:R292R/KNA Gene,H3N2:T325INA Gene,H3N2:Y155HNA Gene,H1N1: H275H/YNA Gene,H1N1:H275YNA Gene,H1N1:Q313RNA Gene,H1N1:D199NNA Gene,H1N1:E278G/ENA Gene,H1N1:I223I/KNA Gene,H1N1:Q136Q/RNA Gene,H1N1:S247NNA Gene,H1N1:S247S/INA Gene,H1N1:S247S/NNA Gene,B: E148GNA Gene,B: G141ENA Gene,B: M403IHA Gene, H3N2:R142GHA Gene, H3N2:S198AHA Gene, H3N2:A138SHA Gene, H3N2:R142KHA Gene, H3N2:A304A/PHA Gene, H3N2:A304DHA Gene, H3N2:L194P/LHA Gene, H3N2:Q75HHA Gene, H3N2:S124GHA Gene, H3N2:S262NHA Gene, H3N2:H1N1: S183PHA Gene, H1N1 :D222D/GHA Gene, H1N1 :D222D/NHA Gene, H1N1 :D222NHA Gene, H1N1 :S162NHA Gene, H1N1 :D187EHA Gene, H1N1 :D222GHA Gene, H1N1 :D222S/D/N/GHA Gene, H1N1 :L151P/LHA Gene, H1N1 :V152I
IV Zanamivir 300 mg5402001001000110001101011813300010001000001100
IV Zanamivir 600 mg741010010001100000001000218100101010020010010
Oral Oseltamivir 75 mg5020110010143201110000102111221000102202200001

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Number of Participants With the Indicated Chemistry Laboratory Values Shifts From Baseline (Day 1) and up to 42 Days

Samples for laboratory assessments were collected at Baseline (Day 1), Day 3, Day 5/6, Day 8, Day 10/11 (or last day of randomized treatment), switch/rescue (S/R) Day 1, S/R Day 3, and S/R Day 5/6 (last day of S/R treatment for those participants who utilized this option), Post-Treatment +2 (if hospitalized), and Post-Treatment +5, +16, and +28 Days. Clinical chemistry parameters included albumin, alkaline phosphatase (ALP), alanine amino transferase (ALT), aspartate amino tranferase (AST), total bilirubin, calcium, creatine kinase, chloride, carbon dioxide content (CO2), creatinine, potassium, magnesium, sodium. Per the DAIDS table for grading the severity of adult and pediatric AEs, Grade (G) 1=mild, G2= moderate, G3=severe and G4=potentially life threatening. The number of participants with values that were G1, G2, G3 and G4 relative to the normal range are summarized. (NCT01231620)
Timeframe: Baseline (Day 1) and up to 42 days

,,
InterventionParticipants (Count of Participants)
Albumin G1Albumin G2Albumin G3Albumin G4ALP G1ALP G2ALP G3ALP G4ALT G1ALT G2ALT G3ALT G4AST G1AST G2AST G3AST G4Total Bilirubin G1Total Bilirubin G2Total Bilirubin G3Total Bilirubin G4Creatine Kinase G1Creatine Kinase G2Creatine Kinase G3Creatine Kinase G4CO2 G1CO2 G2,CO2 G3CO2 G4Creatinine G1Creatinine G2Creatinine G3Creatinine G4Magnesium G1Magnesium G2,Magnesium G3Magnesium G4Hypercalcemia G1Hypercalcemia G2Hypercalcemia G3Hypercalcemia G4Hyperkalemia G1Hyperkalemia G2Hyperkalemia G3Hyperkalemia G4Hypernatremia G1Hypernatremia G2Hypernatremia G3Hypernatremia G4Hypocalcemia G1Hypocalcemia G2Hypocalcemia G3Hypocalcemia G4Hypokalemia G1Hypokalemia G2Hypokalemia G3Hypokalemia G4Hyponatremia G1Hyponatremia G2Hyponatremia G3Hyponatremia G4
IV Zanamivir 300 mg1232101000013200238205310103113440061180147000000000141004326701611042200
IV Zanamivir 600 mg1843501542010100278002220113214390157701490000001000101104839811210034220
Oral Oseltamivir 75 mg1540009100121011962123016642476004441154000000100140104042802110026401

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Mean Oxygen Saturation (OS) of Participants Over Period

Vital signs of OS was assessed three times daily during the treatment period/hospitalization at Day 1, Day 2, Day 3, Day 4, Day 5 and Day 6. The baseline assessments were referred to assessments at Day 1. Minimum value in a day is reported, where a 'day' is defined as a 24 h period (Treatment Day). (NCT01527110)
Timeframe: Baseline (Day 1) to Day 6

InterventionPercent oxygen saturation (Mean)
Baseline (Day 1)Day 2Day 3Day 4Day 5Day 6
Zanamivir 600 mg BID95.694.195.094.294.894.6

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Mean Respiratory Rate (RR) of Participants Over Period

Vital signs of RR was assessed three times daily during the treatment period/hospitalization at Day 1, Day 2, Day 3, Day 4, Day 5 and Day 6. The baseline assessments were referred to assessments at Day 1. Maximum value in a day is reported, where a 'day' was defined as a 24 h period (Treatment Day). (NCT01527110)
Timeframe: Baseline (Day 1) to Day 6

InterventionBreaths/min (Mean)
Baseline (Day 1)Day 2Day 3Day 4Day 5Day 6
Zanamivir 600 mg BID22.922.321.721.421.221.1

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Mean Systolic and Diastolic Blood Pressure (SBP and DBP) of Participants Over Period

Vital signs of SBP and DBP were assessed three times daily during the treatment period/hospitalization at Day 1, Day 2, Day 3, Day 4, Day 5 and Day 6. The baseline assessments were referred to assessments at Day 1. Minimum value in a day for SBP is reported where a 'day' is defined as a 24 h period (Treatment Day). DBP is measured at the same time as minimum SBP. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 6

InterventionMillimeter of mercury (mmHg) (Mean)
SBP, Baseline (Day 1)SBP, Day 2SBP, Day 3SBP, Day 4SBP, Day 5SBP, Day 6DBP, Baseline (Day 1)DBP, Day 2DBP, Day 3DBP, Day 4DBP, Day 5DBP, Day 6
Zanamivir 600 mg BID122.5106.3110.7114.2116.1117.871.059.063.965.266.270.5

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Mean Temperature of Participants Over Period

Vital signs of temperature was assessed three times daily during the treatment period/hospitalization at Day 1, Day 2, Day 3, Day 4, Day 5 and Day 6. The baseline assessments were referred to assessments at Day 1. Maximum value in a day is reported, where a'day' was defined as a 24 h period (Treatment Day). (NCT01527110)
Timeframe: Baseline (Day 1) to Day 6

InterventionDegrees celcius (C) (Mean)
Baseline (Day 1)Day 2Day 3Day 4Day 5Day 6
Zanamivir 600 mg BID37.7537.5437.0136.7736.6736.81

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Median Duration of Clinical Symptoms of Influenza Over Period

Influenza symptoms were assessed at Baseline (pre-dose) and throughout the study period as presence of the following symptoms were recorded: nasal symptoms (rhinorrhea, congestion), feverishness, cough, myalgias, fatigue, diarrhea, anorexia, dyspnea, headache, sore throat, nausea and vomiting. The investigator assessed and recorded influenza symptoms based on interview with the participants. In cases where participants were not able to communicate their symptoms, in participants ventilated and/or sedated, the investigator recorded those signs/symptoms as 'unable to assess'. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionDays (Median)
CoughDyspneaNausea and vomitingDiarrheaFeverishnessFatigueSore throatHeadacheNasal symptomsMyalgiasAnorexia
Zanamivir 600 mg BID7.01.01.02.03.03.02.01.52.02.02.0

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Median Duration of Use of Invasive and Non-invasive Ventilatory Support and Oxygen Supplementation Over Period

The non-invasive ventilator support includes modalities of machine-assisted: CPAP and BiPAP. The invasive ventilator support included modalities of machine-assisted: ECMO and endotracheal mechanical ventilation. Participants with use of modality of invasive, non-invasive ventilatory support and oxygen supplementation was assessed from Baseline (Day 1) to Day 33 (follow-up). (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

Interventionhour (Median)
Invasive and non-invasive ventilatory supportOxygen supplementation
Zanamivir 600 mg BID62.33046.250

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Median Time to Absence of Fever, Improved Respiratory Status, Improved OS, Improved HR and Improved SBP Over Period

Absence of fever, improved respiratory status, OS, HR and SBP was defined according to clinical response criteria as: temperature, <= 36.6 degree C-axilla or <= 37.2 degree C-oral or <= 37.7 degree C-rectal and tympanic, without the use of antipyretics within 8 hour; OS of >= 95%; respiratory status of return to pre-morbid oxygen requirement (participants with chronic oxygen use) or need for supplemental oxygen (administered by any modality) to no need for supplemental oxygen or RR <=24 breaths/min without supplemental oxygen; HR <=100 beats/min; SBP of >=90 mmHg without inotropic support within 8 hour. For OS, participants with a history of chronic hypoxia (without supplemental oxygen) satisfied normalization criteria for OS if the value without supplemental oxygen was <=2% from participants historical OS and waiver for participants with a history of chronic supplemental oxygen requirement with baseline OS <95% with supplemental oxygen, recorded within 12 months prior to enrolment. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

Interventionhour (Median)
Absence of feverImproved respiratory statusImproved OSImproved HRImproved SBP
Zanamivir 600 mg BID24.90035.14011.1706.63011.865

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Median Time to no Detectable Viral RNA by Quantitative RT-PCR and Viral Culture From Nasopharyngeal Samples Over Period

Quantitative RT-PCR and quantitative viral culture was carried out on nasopharyngeal swabs collected on Baseline (Day 1) up to Day 33 (follow-up) depending on the extend of continuation of treatment and duration of hospitalization. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionDays (Median)
Viral RNA by quantitative RT-PCRQuantitative viral culture
Zanamivir 600 mg BID5.53.0

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Median Duration of Hospital Stay for the Participants Over Period

The duration of hospital stay was assessed from the first day of dosing (Day 1) up to Day 33 (follow-up). The duration was calculated as duration in hospital = date/time of discharge - date/time of 1st day of dosing. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

Interventionhour (Median)
Zanamivir 600 mg BID138.215

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Number of Participants of Treatment Emergent Toxicities in Clinical Chemistry and Hematology Over Period

The normal reference ranges for clinical chemistry and hematology parameters were ALT 5 to 45 IU/L, ALP 100 to 325 IU/L, creatine kinase 60 to 270 IU/L, AST 10 to 40 IU/L, creatinine 41.548 to 69.836 µmol/L, direct bilirubin 0 to 5.13 µmol/L, total bilirubin 3.42 to 20.52 µmol/L, calcium 2.0958 to 2.5948 mmol/L, CO2/ bicarbonate 19.2 to 27.1 mmol/L, chloride 98 to 108 mmol/L, magnesium 0.7809 to 1.0275 mmol/L, potassium 3.5 to 5 mmol/L, sodium 137 to 147 mmol/L, urea/ BUN 2.856 to 8.211 mmol/L, basophils 0 to 2%, eosinophils 0 to 8%, lymphocytes 18 to 49%, monocytes 2 to 10%, total neutrophils 40 to 75%, platelet count 140 to 340 GI/L, WBC count 3.3 to 9 GI/L, hemoglobin 135 to 175 g/L and haematocrit 0.397 to 0.524 ratio. Participants with treatment emergent toxicities for grade 3 (severe) and grade 4 (potentially life threatening) were assessed at Day 1, Day 3 and Day 5. Classification of the toxicities as potentially drug-related was done based on the investigator's judgment. (NCT01527110)
Timeframe: Day 1, Day 3 and Day 5

InterventionParticipants (Count of Participants)
Hemoglobin decreaseHypokalaemia
Zanamivir 600 mg BID11

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Number of Participants With Abnormal Clinically Significant Electrocardiograph (ECG) Findings Over Period

12-lead ECG assessments were obtained at Baseline (Day 1) and Day 4 of the treatment period. On Baseline (Day 1), 2 baseline ECGs were obtained prior to study drug infusion. On Day 4, 2 ECGs were obtained, 1 ECG just prior to study drug infusion and 1 ECG at the end of infusion. Overall ECG findings were summarized with regard to visits at Day 1 (pre-dose [ECG 1 and ECG 2]) and Day 4 (pre-dose and 30-min post dose). (NCT01527110)
Timeframe: Baseline (Day 1, pre-dose) and Day 4

InterventionParticipants (Count of Participants)
Baseline (Day 1), pre-dose, ECG 1Baseline (Day 1), pre-dose, ECG 2Day 4, pre-doseDay 4, 30 min post-dose
Zanamivir 600 mg BID1111

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Number of Participants With and Without Use of Modality of Invasive, Non-invasive Ventilatory Support and Oxygen Supplementation Over Period

The non-invasive ventilator support includes modalities of machine-assisted: continuous positive airway pressure (CPAP) and bi-level positive airway pressure (BiPAP). The invasive ventilator support included modalities of machine-assisted: extra corporeal membrane oxygenation (ECMO) and endotracheal mechanical ventilation. Participants with and without use of modality of invasive, non-invasive ventilatory support and oxygen supplementation was assessed from Baseline (Day 1) to Day 33 (follow-up). (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionParticipants (Count of Participants)
Invasive and non-invasive ventilatory support, noInvasive and non-invasive ventilatory support, yesCPAPBiPAPECMOEndotracheal mechanical ventilationOxygen supplementation, noOxygen supplementation, yes
Zanamivir 600 mg BID18311021011

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Number of Participants With Clinical Chemistry Parameters of Alanine Amino Transferase (ALT), Alkaline Phosphatase (ALP), Creatine Kinase and Aspartate Amino Transferase (AST) Outside the Normal Reference Range at Any Time During Treatment

The reference ranges for clinical chemistry parameters were ALT 5 to 45 international units per litre [IU/L]), ALP 100 to 325 IU/L, creatine kinase 60 to 270 IU/L and AST 10 to 40 IU/L. The baseline assessments were referred to assessments at Day 1. Assessments were done at Day 1, 3 and 5. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 5

InterventionParticipants (Count of Participants)
ALT, Baseline, highALT, Day 3, highALT, Day 5, highALP, Baseline, highALP, Day 3, highALP, Day 5, highAST, Baseline, highAST, Day 3, highAST, Day 5, highCreatine kinase, Baseline, highCreatine kinase, Baseline, lowCreatine kinase, Day 3, highCreatine kinase, Day 3, lowCreatine kinase, Day 5, highCreatine kinase, Day 5, low
Zanamivir 600 mg BID2242226651225114

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Number of Participants With Clinical Chemistry Parameters of Albumin and Total Protein Outside the Normal Reference Range at Any Time During Treatment

The reference ranges for clinical chemistry parameters were albumin 38 to 53 grams per liter (g/L) and total protein 67 to 83 g/L. The baseline assessments were referred to assessments at Day 1. Assessments were done at Day 1, 3 and 5. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 5

InterventionParticipants (Count of Participants)
Albumin, Baseline, lowAlbumin, Day 3, lowAlbumin, Day 5, lowTotal protein, Baseline, lowTotal protein, Day 3, lowTotal protein, Day 5, low
Zanamivir 600 mg BID101212151717

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Number of Participants With Clinical Chemistry Parameters of Calcium, Carbon Dioxide Content/ Bicarbonate, Chloride, Magnesium, Potassium, Sodium and Urea/ Blood Urea Nitrogen (BUN) Outside the Normal Reference Range at Any Time During Treatment

The reference ranges for clinical chemistry parameters were calcium 2.0958 to 2.5948 millimole per litre (mmol/L), carbon dioxide content/ bicarbonate 19.2 to 27.1 mmol/L, chloride 98 to 108 mmol/L, magnesium 0.7809 to 1.0275 mmol/L, potassium 3.5 to 5 mmol/L, sodium 137 to 147 mmol/L and urea/BUN 2.856 to 8.211 mmol/L. The baseline assessments were referred to assessments at Day 1. Assessments were done at Day 1, 3 and 5. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 5

InterventionParticipants (Count of Participants)
Calcium, Baseline, lowCalcium, Day 3, lowCalcium, Day 5, lowCarbon dioxide content/bicarbonate, Baseline, highCarbon dioxide content/bicarbonate, Baseline, lowCarbon dioxide content/bicarbonate, Day 3, lowCarbon dioxide content/bicarbonate, Day 5, highCarbon dioxide content/bicarbonate, Day 5, lowChloride, Baseline, highChloride, Baseline, lowChloride, Day 3, highChloride, Day 3, lowUrea/ BUN, Baseline, highUrea/ BUN, Baseline, lowUrea/ BUN, Day 3, highUrea/ BUN, Day 3, lowUrea/ BUN, Day 5, highUrea/ BUN, Day 5, lowMagnesium, Baseline, lowMagnesium, Day 3, lowMagnesium, Day 5, lowSodium, Baseline, lowSodium, Day 3, lowSodium, Day 5, lowPotassium, Baseline, lowPotassium, Day 3, lowPotassium, Day 5, low
Zanamivir 600 mg BID91010161111521523222623821222

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Number of Participants With Clinical Chemistry Parameters of Creatinine, Direct Bilirubin and Total Bilirubin Outside the Normal Reference Range at Any Time During Treatment

The reference ranges for clinical chemistry parameters were creatinine 41.548 - 69.836 micromole per litre (µmol/L), direct bilirubin 0 to 5.13 µmol/L and total bilirubin 3.42 to 20.52 µmol/L. The baseline assessments were referred to assessments at Day 1. Assessments were done at Day 1, 3 and 5. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 5

InterventionParticipants (Count of Participants)
Creatinine, Baseline, highCreatinine, Baseline, lowCreatinine, Day 3, highCreatinine, Day 3, lowCreatinine, Day 5, highCreatinine, Day 5, lowDirect bilirubin, Baseline, highDirect bilirubin, Baseline, lowDirect bilirubin, Day 3, highDirect bilirubin, Day 3, lowDirect bilirubin, Day 5, highDirect bilirubin, Day 5, lowTotal bilirubin, Baseline, highTotal bilirubin, Baseline, lowTotal bilirubin, Day 3, highTotal bilirubin, Day 3, lowTotal bilirubin, Day 5, highTotal bilirubin, Day 5, low
Zanamivir 600 mg BID822425200000100000

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Number of Participants With Complications of Influenza and Associated Use of Antibiotics Over Period

"The details of complications of influenza like bacterial pneumonia, pneumothorax, pleural effusion, acute respiratory distress syndrome (ARDS), myositis, encephalitis, myocarditis and associated antibiotic use were assessed from Baseline (Day 1) to Day 33 (follow-up). Participants with complications of influenza, with associated use of antibiotics as associated antibiotic use yes and without associated use of antibiotics as associated antibiotic use no were categorized." (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionParticipants (Count of Participants)
Complications of influenzaAssociated antibiotic use, noAssociated antibiotic use, yes
Zanamivir 600 mg BID11011

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Number of Participants With Hematology Parameters of Basophiles, Eosinophils, Lymphocytes, Monocytes, Total Neutrophils, Platelet Count, White Blood Cell(WBC) Count, Hemoglobin and Hematocrit Outside the Normal Reference Range at Any Time During Treatment

The reference ranges for hematology parameters were basophils 0 to 2 percentage (%), eosinophils 0 to 8%, lymphocytes 18 to 49%, monocytes 2 to 10%, total neutrophils 40 to 75%, platelet count 140 to 340 giga cells per liter (GI/L), WBC count 3.3 to 9 GI/L, hemoglobin 135 to 175 g/L and haematocrit 0.397 to 0.524 ratio. The baseline assessments were referred to assessments at Day 1. Assessments were done at Day 1, 3, and 5. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 5

InterventionParticipants (Count of Participants)
Hemoglobin, Baseline, lowHemoglobin, Day 3, lowHemoglobin, Day 5, lowHematocrit, Baseline, lowHematocrit, Day 3, lowHematocrit, Day 5, lowLymphocytes, Baseline, lowLymphocytes, Day 3, highLymphocytes, Day 3, lowLymphocytes, Day 5, highLymphocytes, Day 5, lowMonocytes, Baseline, highMonocytes, Baseline, lowMonocytes, Day 3, highMonocytes, Day 5, highTotal neutrophils, Baseline, highTotal neutrophils, Day 3, highTotal neutrophils, Day 3, lowTotal neutrophils, Day 5, highTotal neutrophils, Day 5, lowPlatelet Count, Baseline, lowPlatelet Count, Day 3, lowPlatelet Count, Day 5, lowWBC count, Baseline, highWBC count, Baseline, lowWBC count, Day 3, highWBC count, Day 3, lowWBC count, Day 5, highWBC count, Day 5, low
Zanamivir 600 mg BID1111101110101827247185147242654523212

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Number of Participants With or Without Treatment Emergent Resistance or Suspected Treatment Emergent Resistance to Zanamivir Over Period

A total of 30 neuraminidase gene sequences (23 influenza A/H3N2, 5 influenza B and 2 negative) from 21 participants were obtained from 76 samples. There were no resistance associated neuraminidase mutations or mutations in the neuraminidase active site identified in viruses isolated during this study. Therefore the frequency of resistance emergence to zanamivir could not be determined. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionParticipants (Count of Participants)
Influenza A/H3N2, resistence or suspectedInfluenza A/H3N2, without resistenceInfluenzavirus B, resistence or suspectedInfluenzavirus B, without resistence
Zanamivir 600 mg BID01703

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Number of Participants With Toxicity Shifts From Baseline in Clinical Chemistry Over Period

The reference ranges for clinical chemistry parameters were ALT 5 to 45 IU/L, ALP 100 to 325 IU/L, creatine kinase 60 to 270 IU/L, AST 10 to 40 IU/L, creatinine 41.548 to 69.836 µmol/L, direct bilirubin 0 to 5.13 µmol/L, total bilirubin 3.42 to 20.52 µmol/L, calcium 2.0958 to 2.5948 mmol/L, CO2/ bicarbonate 19.2 to 27.1 mmol/L, chloride 98 to 108 mmol/L, magnesium 0.7809 to 1.0275 mmol/L, potassium 3.5 to 5 mmol/L, sodium 137 to 147 mmol/L and urea/ BUN 2.856 to 8.211 mmol/L. The baseline assessments were referred to assessments at Day 1. Number of participants with shifts between normal range (NR) high, within NR and NR low values in hematology parameters from baseline (Day 1) at Day 3 and Day 5 is reported. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

InterventionParticipants (Count of Participants)
Albumin, Day 3, within NR to NR lowAlbumin, Day 5, within NR to NR lowAST, Day 3, within NR to NR highAST, Day 5, within NR to NR highCalcium, Day 3, within NR to NR lowCalcium, Day 5, within NR to NR lowCreatine Kinase, Day 3, within NR to NR lowCreatine Kinase, Day 5, NR high to NR lowCreatine Kinase, Day 5, within NR to NR lowChloride, Day 3, within NR to NR lowCO2 content/Bicarbonate,Day 5,within NR to NR highCreatinine, Day 3, within NR to NR lowCreatinine, Day 5, NR high to NR lowCreatinine, Day 5, within NR to NR lowPotassium, Day 3, within NR to NR lowPotassium, Day 5, within NR to NR lowMagnesium, Day 3, within NR to NR lowTotal Protein, Day 3, within NR to NR lowTotal Protein, Day 5, within NR to NR lowUrea/BUN, Day 3, within NR to NR lowUrea/BUN, Day 5, within NR to NR low
Zanamivir 600 mg BID552344112113221115411

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Number of Participants With Toxicity Shifts From Baseline in Hematology Parameters Over Period

The reference ranges for hematology parameters were basophils 0 to 2%, eosinophils 0 to 8%, lymphocytes 18 to 49%, monocytes 2 to 10%, total neutrophils 40 to 75%, platelet count 140 to 340 GI/L, WBC count 3.3 to 9 GI/L, hemoglobin 135 to 175 g/L and haematocrit 0.397 to 0.524 ratio. The baseline assessments were referred to assessments at Day 1. Number of participants with shifts between NR high, within NR and NR low values in hematology parameters from baseline (Day 1) at Day 3 and Day 5 is reported. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

InterventionParticipants (Count of Participants)
Hemoglobin, Day 3, within NR to NR lowHemoglobin, Day 5, within NR to NR lowHematocrit, Day 3, within NR to NR lowHematocrit, Day 5, within NR to NR lowLymphocytes, Day 3, NR low to NR highLymphocytes, Day 5, NR low to NR highMonocytes, Day 3, within NR to NR highMonocytes, Day 3, within NR to NR lowMonocytes, Day 5, within NR to NR highMonocytes, Day 5, within NR to NR lowTotal Neutrophils, Day 3, NR high to NR lowTotal Neutrophils, Day 3, within NR to NR lowTotal Neutrophils, Day 5, NR high to NR lowWBC count, Day 3, within NR to NR highWBC count, Day 3, within NR to NR lowWBC count, Day 5, within NR to NR low
Zanamivir 600 mg BID3323223121112122

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Percentage of Participants With Abnormal Clinically Significant ECG Findings Over Period

12-lead ECG assessments were obtained at Baseline (Day 1) and Day 4 of the treatment period. On Baseline (Day 1), 2 baseline ECGs were obtained. On Day 4, 2 ECGs were obtained, 1 ECG just prior to study drug infusion and 1 ECG at the end of infusion. Overall ECG findings were summarized at Day 1 (ECG 1 and ECG 2) and Day 4 (pre-dose and 30-min post dose). (NCT01527110)
Timeframe: Baseline ( pre-dose Day 1) and Day 4

Intervention% of participants (Number)
Baseline (Day 1), pre-dose, ECG 1Baseline (Day 1), pre-dose, ECG 2Day 4, pre-doseDay 4, 30 min post-dose
Zanamivir 600 mg BID5566

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Percentage of Participants With Undetectable Viral RNA and Absence Cultivable Virus From Samples Obtained From Nasopharyngeal Samples Over Period

Quantitative RT-PCR and quantitative viral culture was carried out on nasopharyngeal swabs collected from Baseline (Day 1) up to Day 33 (follow-up) depending on the extend of continuation of treatment and duration of hospitalization of the participants. Undetectable RNA concentrations were below the level of quantification. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

Intervention% of participants (Number)
BASELINE (DAY 1)DAY 2DAY 3DAY 4DAY 5DAY 6LAST DAY
Zanamivir 600 mg BID55519192938

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Percentage of Participants With Undetectable Viral RNA and Absence of Cultivable Virus in Lower Respiratory Samples Over Period

Quantitative RT-PCR and quantitative viral culture was carried out on lower respiratory samples (endotracheal aspirates) collected on Baseline (Day 1) up to Day 33 (follow-up) depending on the extend of continuation of treatment and duration of hospitalization. Endotracheal aspirates were used in participants who were intubated. Undetectable RNA concentrations were below the level of quantification. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

Intervention% of participants (Number)
BASELINE (DAY 1)DAY 2DAY 3DAY 4DAY 5
Zanamivir 600 mg BID00000

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Number of Participants of Clinical Symptoms of Influenza Over Period

Influenza symptoms were assessed at Baseline (pre-dose): the presence of the following symptoms were recorded: nasal symptoms (rhinorrhea, congestion), feverishness, cough, myalgias, fatigue, diarrhea, anorexia, dyspnea, headache, sore throat, nausea and vomiting. The investigator assessed and recorded influenza symptoms based on interview with the participants. In cases where participants were not able to communicate their symptoms, in participants ventilated and/or sedated, the investigator recorded those signs/symptoms as 'unable to assess'. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionParticipants (Count of Participants)
CoughDyspneaNauseaDiarrheaFeverishnessFatigueSore throatHeadacheNasal symptomsMyalgiasAnorexia
Zanamivir 600 mg BID201526191671013815

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Median Duration of Intensive Care Unit (ICU) Stay for the Participants Over Period

The duration of ICU stay was assessed from the first day of dosing (Day 1) up to Day 33 (follow-up). Duration in ICU was captured from the eCRF. If the duration in ICU was missing, then the data was set to 0. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionDays (Median)
Zanamivir 600 mg BID0.0

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Median Time to Clinical Response Over Period

Clinical response was defined as resolution of at least 4 of the 5 vital signs within the respective resolution criteria of temperature <= 36.6 degree C-axilla or <= 37.2 degree C-oral or <= 37.7 degree C-rectal/ tympanic, without the use of antipyretics within 8 hour; OS of >= 95%; respiratory status of return to pre-morbid oxygen requirement (participants with chronic oxygen use) or need for supplemental oxygen (administered by any modality) to no need for supplemental oxygen or RR <= 24 breaths/min without supplemental oxygen; HR <=100 beats/min; SBP of >= 90 mmHg without inotropic support within 8 h, maintained for at least 24 hour, or hospital discharge, which ever occurred first. Participants discharged from hospital due to clinical improvement/resolution were considered to have met the clinical response endpoint at the time of hospital discharge and were not required to have documented resolution of at least 4 response criteria i.e. achieved success at the time of discharge. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

Interventionhour (Median)
Zanamivir 600 mg BID85.050

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Median Time to Return to Pre-morbid Level of Activity Over Period

Pre-morbid functional status was defined as the best functional status in the 4 weeks prior to enrolment and status at Baseline (Day 1). The participants were assessed on a 3-point scale by activity level (bed rest, limited ambulation or unrestricted) recorded in thee electronic case report form (eCRF). For participants who were unable to communicate their pre-morbid functional status, the information was requested from another close member of the household or close family member. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

Interventionhour (Median)
Zanamivir 600 mg BID87.645

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Median Time to Virologic Improvement Over Period

Virologic improvement was defined as a 2 log drop in viral load or sustained undetectable viral ribonucleic acid (RNA), on 2 successive occasions as measured by quantitative reverse transcriptase - polymerase chain reaction (RT-PCR) from nasopharyngeal samples. Assessment was done from Baseline (Day 1) up to Day 33 (follow-up). (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionDays (Median)
Zanamivir 600 mg BID3.0

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Mean 50% Inhibitory Concentration (IC50) for Phenotypes of Influenza for the Measure of Viral Susceptibility to Zanamivir at All Visits

IC50 value is defined as the concentration of zanamivir required to achieve half maximal inhibition of the influenza viral enzyme neuraminidase of influenza A and B to prevent the release and spread of influenza virus in the respiratory tract. Susceptibility analyses were performed on nasopharyngeal swabs collected on Baseline (Day 1) up to Day 33 (follow-up) depending on the extend of continuation of treatment and duration of hospitalization. Endotracheal aspirates were used in participants who were intubated. Data is categorized for participants with influenza A/H3N2 and influenza B. (NCT01527110)
Timeframe: Baseline (Day 1) to Day 33 (follow-up)

InterventionNanomole per liter (nmol/L) (Mean)
Influenzavirus A/H3N2, at all visitsInfluenzavirus B, at all visits
Zanamivir 600 mg BID2.048.85

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Mean Change Baseline in Hematocrit at the Indicated Time Points

Hematocrit was measured at Baseline, Day 3 and Day 5 during the treatment period. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

InterventionRatio (Mean)
Day 3Day 5
Zanamivir 600 mg BID-0.0127-0.0088

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Mean Change From Baseline in Albumin and Total Protein at the Indicated Time Points

Albumin and total protein were measured at Baseline , Day 3 and Day 5 during the treatment period. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

Interventiong/L (Mean)
Albumin, Day 3Albumin, Day 5Total protein, Day 3Total protein, Day 5
Zanamivir 600 mg BID-3.2-2.6-4.1-3.1

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Mean Change From Baseline in ALT, ALP, Creatine Kinase and AST at the Indicated Time Points

ALT, ALP, creatine kinase and AST were measured at Baseline, Day 3 and Day 5 during the treatment period. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

InterventionIU/L (Mean)
ALT, Day 3ALT, Day 5ALP, Day 3ALP, Day 5Creatine kinase, Day 3Creatine kinase, Day 5AST, Day 3AST, Day 5
Zanamivir 600 mg BID0.23.1-37.1-27.9-44.8-192.7-0.5-0.2

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Mean Change From Baseline in Counts of WBC and Platelets at the Indicated Time Points

WBC and platelet counts were measured at Baseline, Day 3 and Day 5 during the treatment period. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

InterventionGI/L (Mean)
Platelet count, Day 3Platelet count, Day 5WBC count, Day 3WBC count, Day 5
Zanamivir 600 mg BID-1.614.3-1.76-1.82

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Mean Change From Baseline in Creatinine, Direct Bilirubin and Total Bilirubin at the Indicated Time Points

Creatinine, direct bilirubin and total bilirubin were measured at Baseline, Day 3 and Day 5 during the treatment period. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

Interventionµmol/L (Mean)
Creatinine, Day 3Creatinine, Day 5Direct bilirubin, Day 3Direct bilirubin, Day 5Total bilirubin, Day 3Total bilirubin, Day 5
Zanamivir 600 mg BID-14.6351-19.2024-0.950-0.475-3.040-1.520

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Mean Change From Baseline in Hemoglobin at the Indicated Time Points

Hemoglobin was measured at Baseline, Day 3 and Day 5 during the treatment period. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

Interventiong/L (Mean)
Day 3Day 5
Zanamivir 600 mg BID-4.9-3.6

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Mean Change From Baseline in Percentage of Basophils, Eosinophils, Lymphocytes, Monocytes and Total Neutrophils at the Indicated Time Points

Percentages of basophils, eosinophils, lymphocytes, monocytes and total neutrophils were measured at Baseline, Day 3 and Day 5 during the treatment period. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. (NCT01527110)
Timeframe: Baseline, Day 3 and Day 5

InterventionPercent of blood cells (Mean)
Basophils, Day 3Basophils, Day 5Eosinophils, Day 3Eosinophils, Day 5Lymphocytes, Day 3Lymphocytes, Day 5Monocytes, Day 3Monocytes, Day 5Total neutrophils, Day 3Total neutrophils, Day 5
Zanamivir 600 mg BID-0.04-0.081.572.2615.2618.600.16-0.19-16.95-20.59

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Mean Change From Baseline in Quantitative Viral Load Measured by RT-PCR From Nasopharyngeal Swabs Positive at Baseline Over Period

Quantitative RT-PCR was carried out on nasopharyngeal swabs collected on Day 1 up to Day 33 (last day) depending on the extend of continuation of treatment and duration of hospitalization. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. Analysis was done for participants with positive Influenza A RNA and Influenza B RNA. Data is presented for Day 3, Day 5 and last day. (NCT01527110)
Timeframe: Baseline (Day 1) up to Day 33 (follow-up)

InterventionLogarithmic base 10 (log 10) copies/mL (Mean)
Influenza A RNA, Day 3Influenza A RNA, Day 5Influenza A RNA, Last Day (Day 33)Influenza B RNA, Day 3Influenza B RNA, Day 5Influenza B RNA, Last Day (Day 33)
Zanamivir 600 mg BID-2.53-3.77-4.13-2.01-3.73-4.43

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Mean Change From Baseline in Quantitative Viral Load Measured by Viral Culture From Nasopharyngeal Swabs Over Period

Quantitative viral culture as 50 % tissue culture infectious dose (TCID50) defined as median tissue culture infective dose is that amount of a pathogenic agent that produces pathological change in 50% of cell cultures inoculated. It was carried out on nasopharyngeal swabs collected on Day 1 up to Day 33 (last day) depending on the extend of continuation of treatment and duration of hospitalization. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. Any undetectable viral load values were calculated as x.x Log10 TCID50: x.x Log10 (1.5 or 7.5 was the lower or upper limit of quantification in TCID50). Data is presented for Day 3, Day 5 and last day. (NCT01527110)
Timeframe: Baseline (Day 1) up to Day 33 (follow-up)

InterventionLOG TCID50/mL (Mean)
Day 3Day 5Last Day (Day 33)
Zanamivir 600 mg BID-2.10-2.23-2.14

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Mean Change From Baseline in Sodium, Calcium, Potassium, Chloride, Magnesium, Carbon Dioxide Content/Bicarbonate and Urea/BUN at the Indicated Time Points

Calcium, potassium, chloride, magnesium, carbon dioxide content/bicarbonate, sodium and urea/BUN were measured at Baseline, Day 3 and Day 5 during the treatment period. The baseline assessments were referred to assessments at Day 1. Change from Baseline was calculated as the value at the indicated time point minus the Baseline value. (NCT01527110)
Timeframe: Baseline (Day 1), Day 3 and Day 5

Interventionmmol/L (Mean)
Calcium, Day 3Calcium, Day 5Potassium, Day 3Potassium, Day 5Chloride, Day 3Chloride, Day 5Magnesium, Day 3Magnesium, Day 5Carbon dioxide content/bicarbonate, Day 3Carbon dioxide content/bicarbonate, Day 5Sodium, Day 3Sodium, Day 5Urea/BUN, Day 3Urea/BUN, Day 5
Zanamivir 600 mg BID-0.0370.019-0.010.023.63.30.0730.0390.541.372.42.80.1388-1.4280

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Mean Heart Rate (HR) of Participants Over Period

Vital sign of HR was assessed three times daily during the treatment period/hospitalization at Day 1, Day 2, Day 3, Day 4, Day 5 and Day 6. The baseline assessments were referred to assessments at Day 1. Maximum value in a day is reported where a 'day' is defined as a 24 h period (Treatment Day). (NCT01527110)
Timeframe: Baeline (Day 1) to Day 6

InterventionBeats/min (Mean)
Baseline (Day 1)Day 2Day 3Day 4Day 5Day 6
Zanamivir 600 mg BID84.486.380.377.373.280.3

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Time to Alleviation of Influenza Symptoms

Time to alleviation of influenza will be assessed through Flu-iiQ (Influenza intensity and impact Questionnaire) and diary cards from Day 1 to 14. (NCT01793883)
Timeframe: Efficacy will be assessed over 14 days post-randomization.

Interventionhours (Median)
40 mg Laninamivir Octanoate DPI102.30
80 mg Laninamivir Octanoate DPI103.20
Placebo104.10

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