Page last updated: 2024-11-06

oseltamivir

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Description

Oseltamivir is a neuraminidase inhibitor used to treat and prevent influenza A and B infections. Its synthesis involves a multi-step process starting from shikimic acid, a natural compound extracted from the Chinese star anise. Oseltamivir inhibits the neuraminidase enzyme, which is crucial for the release of new virus particles from infected cells, thereby reducing the spread of the virus. Its importance lies in its ability to shorten the duration of influenza symptoms and reduce the risk of complications. Oseltamivir is studied extensively to understand its mechanism of action, develop resistance-resistant variants, and explore its potential in combination therapies. Studies also focus on evaluating its efficacy and safety in different patient populations and for various influenza strains.'

Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza. [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]

Cross-References

ID SourceID
PubMed CID65028
CHEMBL ID1229
CHEBI ID7798
SCHEMBL ID32035
MeSH IDM0282076

Synonyms (85)

Synonym
BIDD:GT0426
ethyl (3r,4r,5s)-5-amino-4-acetamido-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate
bdbm5025
gop-a-flu
HY-13317
AB00173476-02
BRD-K76011241-045-01-5
AKOS015843442
gs-4104 ,
tamvir
1-cyclohexene-1-carboxylic acid, 4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-, ethyl ester, (3r,4r,5s)-
hsdb 7433
oseltamivir [inn:ban]
NCGC00178698-01
oseltamivir
C08092
196618-13-0
gs 4104
ro-64-0796
gs4104
ethyl (3r,4r,5s)-4-acetamido-5-amino-3-(1-ethylpropoxy)cyclohexene-1-carboxylate
ethyl (5s,3r,4r)-4-(acetylamino)-5-amino-3-(ethylpropoxy)cyclohex-1-enecarboxylate
tamiflu (*phosphate salt 1:1*)
1-cyclohexene-1-carboxylic acid, 4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-, ethyl ester, (3r-(3alpha,4beta,5alpha))-
ethyl (3r,4r,5s)-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate
(-)-oseltamivir
DB00198
ethyl (3r,4r,5s)-4-acetamido-5-amino-3-pentan-3-yloxy-cyclohexene-1-carboxylate
oseltamivirum
ethyl (3r,4r,5s)-4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate
CHEBI:7798 ,
agucort
HMS2090C11
ro64-0796
CHEMBL1229
gs-4071 ethyl ester
ro-640796
ro 640796
ethyl (3r,4r,5s)-4-acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylate
oseltamivir (inn)
D08306
agucort (tn)
NCGC00178698-02
tamiflu-free
unii-20o93l6f9h
20o93l6f9h ,
ebilfumin
AKOS015960501
NCGC00178698-04
oseltamivir [inn]
oseltamivir [vandf]
oseltamivir [mi]
oseltamivir [who-dd]
oseltamivir [hsdb]
oseltamivir [ema epar]
CS-0552
SCHEMBL32035
(3r,4r,5s)-4-acetylamino-5-amino-3-(1-ethyl-propoxy)-cyclohex-1-enecarboxylic acid ethyl ester
ethyl (3r, 4r, 5s)-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate
(3r,4r,5s)-ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate
(3r,4r,5s)-4-acetylamino-5-amino-3-(1-ethyl-propoxy)cyclohex-1-enecarboxylic acid ethyl ester
VSZGPKBBMSAYNT-RRFJBIMHSA-N
DTXSID9044291 ,
AB00173476_04
sr-05000001499
(3r,4r,5s)-4-acetylamino-5-amino-3(1-ethylpropoxy) -1-cyclohexene-1-carboxylic acid ethyl ester
SR-05000001499-1
DT-0013
oseltamivir 100 microg/ml in acetonitrile
Q211509
EX-A3415
oseltamivir-phosphate
gs 4104;gop-a-flu;gs-4104;tamiflu-free;tamvir
NCGC00095191-12
NCGC00095191-16
NCGC00095191-06
gtpl11427
ro640796
O0591
E84533
rel-ethyl (3r,4r,5s)-4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate
182367-47-1
dtxcid7024291
j05ah02
ethyl (3r,4r,5s)-4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate

Research Excerpts

Overview

Oseltamivir is an orally administered antiviral medication. It selectively inhibits the influenza neuraminidase enzymes that are essential for viral replication and it is active against both influenza A and B viruses.

ExcerptReferenceRelevance
"Oseltamivir is a potent neuraminidase inhibitor for influenza treatment. "( Tamiphosphor monoesters as effective anti-influenza agents.
Chen, CL; Cheng, YS; Fang, JM; Jan, JT; Lin, CJ; Lin, TC; Shie, JJ; Tsai, KC; Wang, SY; Wong, CH, 2014
)
1.85
"Oseltamivir is an orally administered antiviral medication that selectively inhibits the influenza neuraminidase enzymes that are essential for viral replication and it is active against both influenza A and B viruses. "( Oseltamivir and acute hepatitis, reality association or coincidence?
Chidichimo, L; Greco, F; Greco, S; Mastroianni, A; Mauro, MV; Urso, F; Vangeli, V, 2021
)
3.51
"Oseltamivir is a widely used influenza virus neuraminidase (NA) inhibitor that prevents the release of new virus particles from host cells. "( Binding mechanism of oseltamivir and influenza neuraminidase suggests perspectives for the design of new anti-influenza drugs.
Chen, M; Feng, S; Guo, W; He, Z; Li, G; Li, X; Liang, X; Liu, J; Liu, X; Mi, N; Ouyang, J; Tao, J; Wang, H; Wang, W; Wang, X; Wen, Q; Zhang, W; Zhao, H; Zhao, Z, 2022
)
2.48
"Oseltamivir (OT) is an effective antiviral agent, but continuous use of oseltamivir leads to a diminished therapeutic effect in the clinic."( Functionalized selenium nanoparticles enhance the anti-EV71 activity of oseltamivir in human astrocytoma cell model.
Cao, H; Hua, L; Liu, X; Xia, Y; Xiao, M; Xu, T; Zhong, J; Zhu, B, 2019
)
1.47
"Oseltamivir is an antiviral drug approved to treat influenza in humans. "( Pharmacokinetics of oseltamivir phosphate and oseltamivir carboxylate in non-pregnant and pregnant rhesus monkeys.
Basavarajappa, M; Beland, FA; Fisher, J; Gamboa da Costa, G; Loukotková, L; Lumen, A; Mattison, D; Morris, SM; Roberts, R, 2020
)
2.32
"Oseltamivir is a neuraminidase inhibitor widely used to treat and prevent influenza A and B infections, although its safety and pharmacokinetics have not been evaluated in patients with severe hepatic impairment. "( Simulation of the Pharmacokinetics of Oseltamivir and Its Active Metabolite in Normal Populations and Patients with Hepatic Cirrhosis Using Physiologically Based Pharmacokinetic Modeling.
Chen, Y; Ke, M; Lin, C; Xu, J, 2020
)
2.27
"Oseltamivir is a common therapy against influenza A virus (IAV) infections. "( Differential Viral-Host Immune Interactions Associated with Oseltamivir-Resistant H275Y and Wild-Type H1N1 A(pdm09) Influenza Virus Pathogenicity.
Baratelli, M; Casas, I; Córdoba, L; Fraile, L; Majó, N; Martínez, J; Martínez-Orellana, P; Martorell, JM; Migura-Garcia, L; Montoya, M; Pérez, M; Pozo, F; Vidaña, B, 2020
)
2.24
"Oseltamivir is a first-line antiviral drug, especially in primary hospitals. "( Is oseltamivir suitable for fighting against COVID-19: In silico assessment, in vitro and retrospective study.
Duan, L; Geng, W; Huang, Q; Jin, Y; Li, Y; Li, Z; Ma, P; Ma, Y; Mao, K; Song, S; Sun, Y; Tan, Q; Wu, F; Xia, H; Xiao, W; Yin, Z; Zhang, S; Zhao, Z; Zhou, E, 2020
)
2.62
"Oseltamivir is an effective treatment, but benefits beyond immediate hospitalization are unknown."( Effectiveness of Oseltamivir in reducing 30-day readmissions and mortality among patients with severe seasonal influenza in Australian hospitalized patients.
Hakendorf, P; Horwood, C; Sharma, Y; Thompson, C, 2021
)
1.68
"Oseltamivir caryboxylase is a potent inhibitor of the enzyme neuramidase of the influenza virus particle and it is active against both influenza A and B viruses. "( First case of acute cholestatic hepatitis attributed to oseltamivir in a young girl with ah1n1 influenza.
Greco, S; Guadagnino, G; Mastroianni, A; Mauro, MV; Ritacca, R; Vangeli, V,
)
1.82
"Oseltamivir is an antiviral drug often preferred in treating viral infections. "( Oseltamivir-Induced Mania in a Patient With Influenza A.
Ferahkaya, E,
)
3.02
"Oseltamivir is a very commonly prescribed anti-viral medication by the Emergency Medicine (EM) physicians for the prophylactic and therapeutic treatment of Influenza infection. "( Review of potential drug interaction between Oseltamivir and Warfarin and why it is important for emergency medicine physicians.
Gambhir, HS; Patel, KM; Shah, SP; Subedi, R, 2017
)
2.16
"Oseltamivir is a substrate of P-glycoprotein, an efflux drug transporter encoded by ABCB1. "( Role of the ABCB1 Drug Transporter Polymorphisms in the Pharmacokinetics of Oseltamivir in Humans: a Preliminary Report.
Cha, YJ; Ghim, JL, 2017
)
2.13
"Oseltamivir is a neuraminidase inhibitor efficiently supporting recovery from influenza infections."( PK/PD-based adaptive tailoring of oseltamivir doses to treat within-host influenza viral infections.
Boianelli, A; Hernandez-Vargas, EA; Meyer-Hermann, M; Montaseri, G, 2018
)
1.48
"Oseltamivir is a potent inhibitor of influenza virus neuraminidase enzymes essential for viral replication. "( Population pharmacokinetics of oseltamivir: pediatrics through geriatrics.
Ambrose, PG; Bhavnani, SM; Bulik, CC; Forrest, A; Kamal, MA; Rayner, CR; Reynolds, DK; Smith, PF; Subramoney, V; Van Wart, SA, 2013
)
2.12
"Oseltamivir (Tamiflu) is a potent and selective antiviral drug employed to fight the flu virus in infected individuals by inhibiting neuraminidase (NA), a flu protein responsible for the release and spread of the progeny virions."( Insight into the oseltamivir resistance R292K mutation in H5N1 influenza virus: a molecular docking and molecular dynamics approach.
Karthick, V; Ramanathan, K, 2014
)
1.46
"Oseltamivir is an antiviral drug that was developed for the treatment of influenza infections."( Managing seasonal influenza: oseltamivir treatment policy in indonesia?
Bratasena, A; Kosasih, H; Laras, K; Pangesti, K; Samaan, G, 2014
)
1.41
"Oseltamivir phosphate is a sialidase inhibitor agent used to treat influenza in the conventional sense."( Successful treatment with oseltamivir phosphate in a patient with chronic immune thrombocytopenia positive for anti-GPIb/IX autoantibody.
Hou, M; Ni, H; Peng, J; Qin, P; Shao, L; Wu, Y; Zhou, H, 2015
)
1.44
"Oseltamivir is a neuraminidase inhibitor indicated for the treatment of uncomplicated influenza in patients two weeks of age or older who have been symptomatic for no more than two days; the recommended dosage is 75 mg twice daily by mouth for five days. "( Influenza treatment with oseltamivir outside of labeled recommendations.
Blair, M; McQuade, B, 2015
)
2.16
"Oseltamivir phosphate is a widely used anti-influenza sialidase inhibitor. "( Anti-influenza neuraminidase inhibitor oseltamivir phosphate induces canine mammary cancer cell aggressiveness.
Barros, R; de Matos, AJ; de Oliveira, JT; Gärtner, F; Gomes, C; Mendes, N; Oliveira, MJ; Reis, CA; Ribeiro, C; Santos, AL; Vasconcelos, MH, 2015
)
2.13
"Oseltamivir is a neuraminidase inhibitor-a new class of antiviral therapy for influenza."( Oseltamivir Treatment for Children with Influenza-Like Illness in China: A Cost-Effectiveness Analysis.
Shen, K; Tan, SC; Wu, J; Xiong, T, 2016
)
2.6
"Oseltamivir is a neuraminidase inhibitor approved for the prevention and treatment of influenza. "( Unexpected platelets elevation in a patient with idiopathic thrombocytopenia treated with oseltamivir for influenza infection.
Auffret, M; Bigot, P; Coupé, P; Ettahar, NK; Gautier, S; Weinborn, M, 2016
)
2.1
"Oseltamivir is an antiviral that inhibits the sialidase activity of the viral neuraminidase (NA) protein and was shown to be effective against pH1N1 viruses in ferrets."( Reduction of Neuraminidase Activity Exacerbates Disease in 2009 Pandemic Influenza Virus-Infected Mice.
Collignon, B; Cutts, T; Embury-Hyatt, C; Hagan, MW; Kobasa, D; Leung, A; Ranadheera, C; Theriault, S, 2016
)
1.16
"Oseltamivir (Tamiflu®) is a prodrug of Ro 64-0802, a selective inhibitor of influenza virus neuraminidase. "( Pharmacokinetic Modeling and Monte Carlo Simulation to Predict Interindividual Variability in Human Exposure to Oseltamivir and Its Active Metabolite, Ro 64-0802.
Fujita, T; Horita, S; Ito, M; Kondo, T; Kusuhara, H; Nakayama, H; Ose, A; Sugiyama, Y; Tanabe, K, 2017
)
2.11
"Oseltamivir is an important antiviral drug, which possess three chirality centers in its structure. "( Stereoisomers of oseltamivir - synthesis, in silico prediction and biological evaluation.
Durmis, J; Fišera, R; Frecer, V; Hajzer, V; Kollár, J; Kostolanský, F; Latika, A; Miertuš, S; Šebesta, R; Tučeková, Z; Varečková, E, 2017
)
2.24
"Oseltamivir is an influenza neuraminidase inhibitor that along with supportive therapy has shown to help critically ill patients infected with H7N9 and H1N1pdm influenza virus strains to recover from disease. "( Aerosol administration increases the efficacy of oseltamivir for the treatment of mice infected with influenza viruses.
Leyva-Grado, VH; Palese, P, 2017
)
2.15
"Oseltamivir is a potent, selective, oral neuraminidase inhibitor for the treatment and prophylaxis of influenza. "( Population pharmacokinetics of oseltamivir when coadministered with probenecid.
Boak, LM; Chanu, P; Gieschke, R; Jonsson, EN; Rayner, CR, 2008
)
2.07
"Oseltamivir is an inhibitor of influenza virus neuraminidase, which is approved for use for the treatment and prophylaxis of influenza A and B virus infections. "( Pharmacokinetics and tolerability of oseltamivir combined with probenecid.
Cunningham, F; Davey, RT; Deyton, LR; Goetz, MB; Holodniy, M; Lee, KK; Lin, ET; Olivo, N; Penzak, SR; Raisch, DW; Straight, TM, 2008
)
2.06
"Oseltamivir is a potent, well-tolerated antiviral for the treatment and prophylaxis of influenza. "( Low penetration of oseltamivir and its carboxylate into cerebrospinal fluid in healthy Japanese and Caucasian volunteers.
Boak, L; Ereshefsky, L; Hoffmann, G; Jhee, SS; Kaeser, B; Leibowitz, M; Patel, A; Prinssen, EP; Rayner, CR; Schulte, M; Yen, M, 2008
)
2.12
"Oseltamivir phosphate is an ethyl ester prodrug widely used in the treatment and prevention of both Influenzavirus A and B infections. "( Activation of the antiviral prodrug oseltamivir is impaired by two newly identified carboxylesterase 1 variants.
Markowitz, JS; Zhu, HJ, 2009
)
2.07
"Oseltamivir is a neuraminidase inhibitor preventing the release of the infectious influenza virus particles from the infected respiratory tract cells of the patients. "( [The smaller number of influenza patients with neuropsychiatric events had taken oseltamivir beforehand].
Shiro, H; Tomono, N, 2008
)
2.01
"Oseltamivir is a neuraminidase inhibitor that inhibits influenza virus proliferation, and is used as an antiviral drug against influenza A and B viruses. "( Oseltamivir and abnormal behaviors: true or not?
Suzuki, E; Tsuda, T; Yorifuji, T, 2009
)
3.24
"Oseltamivir is an effective treatment for childhood influenza, but few data are available in infants <1 year."( Oseltamivir for treatment of influenza in infants less than one year: a retrospective analysis.
Siedler, K; Skopnik, H, 2010
)
2.52
"As oseltamivir is a keystone of preparedness and treatment for pandemic H1N1, the potential for resistance to oseltamivir is an ongoing concern. "( Selection for resistance to oseltamivir in seasonal and pandemic H1N1 influenza and widespread co-circulation of the lineages.
Alexandrov, BB; Hardman, J; Janies, DA; Studer, J; Treseder, TW; Valson, C; Voronkin, IO, 2010
)
1.28
"Oseltamivir is an orally administered antiviral medication that selectively inhibits the influenza neuraminidase enzymes that are essential for viral replication."( Pharmacokinetics of oseltamivir: an oral antiviral for the treatment and prophylaxis of influenza in diverse populations.
Davies, BE, 2010
)
1.41
"Oseltamivir is a prodrug that requires metabolic activation but there is little information on whether natural health products interact to prevent the biotransformation by the carboxylesterase."( The effect of natural health products and traditional medicines on the activity of human hepatic microsomal-mediated metabolism of oseltamivir.
Arnason, JT; Foster, BC; Krantis, A; Liu, R; Mao, J; Saleem, A; Tam, TW, 2010
)
2.01
"Oseltamivir is an antiviral drug which works by blocking the function of the viral neuraminidase protein."( Oseltamivir: a first line defense against swine flu.
Agrawal, R; Kalra, A; Kokil, GR; Rewatkar, PV; Verma, A, 2010
)
2.52
"Oseltamivir is a widely used antiviral drug for influenza."( Absence of adverse effects of oseltamivir on sleep: a double-blind, randomized study in healthy volunteers in Japan.
Abe, M; Davies, BE; Hosaka, Y; Inoue, Y; Kumagai, Y; Kuwahara, H; Mishima, K; Prinssen, EP; Rayner, CR; Toovey, S; Uchimura, N, 2011
)
1.38
"Oseltamivir is a prodrug of oseltamivir carboxylate (OC), a neuraminidase inhibitor used for treatment and prevention of influenza. "( Pharmacokinetics and diffusion into sputum of oseltamivir and oseltamivir carboxylate in adults with cystic fibrosis.
Babany, G; Hubert, D; Jullien, V; Launay, O; Lortholary, O; Sermet, I, 2011
)
2.07
"Oseltamivir resistance is an increasing problem."( 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
)
1.31
"Oseltamivir is an effective treatment for the management of seasonal influenza and H1N1, and should be initiated immediately without waiting for laboratory confirmation of diagnosis."( Effectiveness of a new bioequivalent formulation of oseltamivir (Enfluvir®) on 2010-2011 seasonal influenza viruses: an open phase IV study.
Alhan, E; Badur, S; Celik, M; Celik, US; Ceyhan, M; Ciblak, MA; Karadag Oncel, E; Kurugol, Z; Ozsurekci, Y; Parlakay, AO; Saz, EU, 2012
)
2.07
"Oseltamivir is a new class of anti-viral agent approved for the treatment and prevention of influenza infections."( In silico analysis of drug-resistant mutant of neuraminidase (N294S) against oseltamivir.
Karthick, V; Rajasekaran, R; Ramanathan, K; Shanthi, V, 2013
)
1.34
"Oseltamivir is an oral ester prodrug of its active metabolite Ro 64-0802, a potent and selective neuraminidase inhibitor of the influenza virus. "( Lack of pharmacokinetic interaction between the oral anti-influenza neuraminidase inhibitor prodrug oseltamivir and antacids.
Barrett, J; Dorr, A; Oo, C; Snell, P, 2002
)
1.97
"Oseltamivir carboxylate is a potent and specific inhibitor of influenza neuraminidase (NA). "( Mechanism by which mutations at his274 alter sensitivity of influenza a virus n1 neuraminidase to oseltamivir carboxylate and zanamivir.
Mendel, DB; Tai, CY; Wang, MZ, 2002
)
1.97
"Oseltamivir (Tamiflu) is a neuraminidase inhibitor-a new class of antiviral treatment for influenza where efficacy and safety has been established but cost-effectiveness is unknown."( Oseltamivir for treatment of influenza in healthy adults: pooled trial evidence and cost-effectiveness model for Canada.
Blackhouse, G; Goeree, R; Loeb, M; O'Brien, BJ; Smieja, M,
)
2.3
"Oseltamivir is a novel agent approved for the treatment and prevention of influenza infection and illnesses in adults and children. "( Safety and pharmacology of oseltamivir in clinical use.
Dutkowski, R; Froehlich, E; Oo, C; Suter, P; Thakrar, B; Ward, P, 2003
)
2.06
"Oseltamivir phosphate is an FDA-approved treatment for influenza that has been available for prescription use in the USA since 1999. "( Skin reactions in patients with influenza treated with oseltamivir: a retrospective cohort study.
L'Italien, GJ; Nordstrom, BL; Oh, K; Sacks, ST, 2004
)
2.01
"Oseltamivir is an effective inhibitor of influenza virus neuraminidase. "( Resistant influenza A viruses in children treated with oseltamivir: descriptive study.
Hayden, FG; Kawakami, C; Kawaoka, Y; Kimura, K; Kiso, M; Mitamura, K; Sakai-Tagawa, Y; Shiraishi, K; Sugaya, N,
)
1.82
"(1) Oseltamivir is an antiviral drug used for influenza. "( Oseltamivir: cutaneous and neurological adverse effects in children.
, 2006
)
2.33
"Oseltamivir phosphate is a prodrug of oseltamivir carboxylate, a highly specific inhibitor of influenza virus neuraminidases. "( Influenza virus susceptibility and resistance to oseltamivir.
Aoki, FY; Boivin, G; Roberts, N, 2007
)
2.04
"Oseltamivir is an ethyl ester prodrug of [3R,4R,5S]-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate phosphate (Ro 64-0802), the anti-influenza drug. "( P-glycoprotein restricts the penetration of oseltamivir across the blood-brain barrier.
Fujita, T; Kanai, M; Kusuhara, H; Ose, A; Shibasaki, M; Sugiyama, Y; Yamamoto, A; Yamatsugu, K, 2008
)
2.05
"Oseltamivir is an ethyl ester prodrug of Ro 64-0802, a selective inhibitor of influenza virus neuraminidase. "( Clinical pharmacokinetics of the prodrug oseltamivir and its active metabolite Ro 64-0802.
He, G; Massarella, J; Ward, P, 1999
)
2.01
"Oseltamivir is a prodrug of oseltamivir carboxylate (Ro 64-0802, GS4071), a potent and selective inhibitor of the neuraminidase glycoprotein essential for replication of influenza A and B viruses. "( Oseltamivir: a review of its use in influenza.
McClellan, K; Perry, CM, 2001
)
3.2
"Oseltamivir is a well tolerated orally active neuraminidase inhibitor which significantly reduces the duration of symptomatic illness and hastens the return to normal levels of activity when initiated promptly in patients with naturally acquired influenza. "( Oseltamivir: a review of its use in influenza.
McClellan, K; Perry, CM, 2001
)
3.2
"Oseltamivir (Ro 64-0796) is an ester prodrug of the active metabolite Ro 64-0802 (oseltamivir carboxylate), a potent and selective inhibitor of the neuraminidase enzyme of influenza virus. "( Pharmacokinetics and dosage recommendations for an oseltamivir oral suspension for the treatment of influenza in children.
Barrett, J; Dorr, A; Dutkowski, R; Hill, G; Mann, J; Oo, C; Ward, P, 2001
)
2.01
"Oseltamivir is an ester prodrug of the active metabolite [3R,4R,5S]-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate phosphate (Ro 64-0802), a potent and selective inhibitor of neuraminidase enzyme of influenza virus. "( The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies.
Barrett, J; Cihlar, T; Hill, G; Ho, ES; Liu, B; Oo, C; Prior, K; Ward, P; Wiltshire, H, 2002
)
2.06
"Oseltamivir carboxylate is a potent and specific inhibitor of influenza A and B neuraminidase (NA). "( The H274Y mutation in the influenza A/H1N1 neuraminidase active site following oseltamivir phosphate treatment leave virus severely compromised both in vitro and in vivo.
Carr, JA; Hayden, FG; Ives, JA; Kelly, L; Lambkin, R; Mendel, DB; Oxford, JS; Roberts, NA; Tai, CY, 2002
)
1.98

Effects

Oseltamivir for PEP has an efficacy of 58.5% (15.6% to 79.6) for households and of 68% (34.9 to 84.2%) to 89% in contacts of index cases. The drug has a good tolerability profile in infants and children aged ≤24 months.

Oseltamivir has been used for treatment of influenza A and B infections, but recent reports documented that it was less active against the latter. By April 30, 2010, a total of 285 resistant cases were reported worldwide, including 45 in the United Kingdom.

ExcerptReferenceRelevance
"Oseltamivir has a good tolerability profile in infants and children aged ≤24 months. "( A prospective observational study of oseltamivir safety and tolerability in infants and young children ≤24 months.
Blumentals, WA; Miller, MK; Rath, BA; Starzyk, K; Tetiurka, B; Wollenhaupt, M, 2015
)
2.13
"Oseltamivir for PEP has an efficacy of 58.5% (15.6% to 79.6) for households and of 68% (34.9 to 84.2%) to 89% in contacts of index cases."( Neuraminidase inhibitors for preventing and treating influenza in healthy adults.
Demicheli, V; Di Pietrantonj, C; Jefferson, TO; Jones, M; Rivetti, D, 2006
)
1.06
"Oseltamivir has the most abundant evidence, including in the hospital and long-term care (LTC) facilities, and the strongest evidence for reducing mortality and complications."( Treatment and prevention of influenza in geriatric patients.
Bulloch, MN,
)
0.85
"Oseltamivir has the most versatility in preventing and treating influenza in geriatric patients. "( Treatment and prevention of influenza in geriatric patients.
Bulloch, MN,
)
1.57
"Oseltamivir has not been shown to have efficacy, and corticosteroids are currently not recommended."( Pharmacologic Treatments for Coronavirus Disease 2019 (COVID-19): A Review.
Cutrell, JB; Jodlowski, TZ; Monogue, ML; Sanders, JM, 2020
)
1.28
"Oseltamivir has been used to treat children with influenza for nearly 2 decades, with treatment currently approved for infants aged ≥2 weeks. "( Efficacy and Safety of Oseltamivir in Children: Systematic Review and Individual Patient Data Meta-analysis of Randomized Controlled Trials.
Brooks, WA; Heikkinen, T; Malosh, RE; Martin, ET; Monto, AS; Whitley, RJ, 2018
)
2.23
"Oseltamivir has been found less binding affinity with MT."( The inhibitory performance of flavonoid cyanidin-3-sambubiocide against H274Y mutation in H1N1 influenza virus.
Kannan, S; Kolandaivel, P, 2018
)
1.2
"Oseltamivir has complex PK which requires modelling to properly understand the relationship between dose and concentration with time, and there is a lack of clarity on appropriate pharmacodynamic endpoints."( Pharmacokinetics and pharmacodynamics of oseltamivir in neonates, infants and children.
Lutsar, I; Standing, JF; Tsolia, M, 2013
)
1.38
"Oseltamivir has been demonstrated to prevent disease among exposed individuals, as well as to shorten the duration of illness and lessen the likelihood of complications among those infected."( Oseltamivir for influenza in pregnancy.
Beigi, RH; Caritis, SN; Venkataramanan, R, 2014
)
2.57
"Oseltamivir has a good tolerability profile in infants and children aged ≤24 months. "( A prospective observational study of oseltamivir safety and tolerability in infants and young children ≤24 months.
Blumentals, WA; Miller, MK; Rath, BA; Starzyk, K; Tetiurka, B; Wollenhaupt, M, 2015
)
2.13
"Oseltamivir has been demonstrated to prevent disease after exposure, treat infected individuals, as well as lessen the likelihood of complications."( Oseltamivir for the treatment of H1N1 influenza during pregnancy.
Beigi, RH; Caritis, SN; Pillai, VC; Venkataramanan, R, 2015
)
2.58
"Oseltamivir has been widely used to treat patients with influenza; however, its effects have been debated. "( Effectiveness and safety of oseltamivir for treating influenza: an updated meta-analysis of clinical trials.
Pan, H; Qiu, S; Shen, Y; Wang, J; Zhang, Q, 2015
)
2.15
"Oseltamivir has no protective effect on mortality among patients with 2009A/H1N1 influenza."( Neuraminidase inhibitors for influenza: a systematic review and meta-analysis of regulatory and mortality data.
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, 2016
)
1.16
"Oseltamivir has been predicted to reach high concentrations in surface waters and sewage works."( An environmental risk assessment for oseltamivir (Tamiflu) for sewage works and surface waters under seasonal-influenza- and pandemic-use conditions.
Straub, JO, 2009
)
1.35
"Oseltamivir carboxylate has high bioavailability and penetrates sites of infection at concentrations that are sufficient to inhibit viral replication."( Pharmacokinetics of oseltamivir: an oral antiviral for the treatment and prophylaxis of influenza in diverse populations.
Davies, BE, 2010
)
1.41
"Oseltamivir (has known by its brand name 'Tamiflu') is a prodrug, requiring ester hydrolysis for conversion to the active form, Oseltamivir carboxylate. "( Oseltamivir: a first line defense against swine flu.
Agrawal, R; Kalra, A; Kokil, GR; Rewatkar, PV; Verma, A, 2010
)
3.25
"Oseltamivir has been used widely for prophylaxis or treatment during outbreaks of the pandemic influenza virus (H1N1) in several countries. "( Detection of oseltamivir sensitive/resistant strains of pandemic influenza A virus (H1N1) from patients admitted to hospitals in Thailand.
Makkoch, J; Payungporn, S; Poomipak, W; Poovorawan, Y; Rianthavorn, P; Theamboonlers, A, 2011
)
2.18
"Oseltamivir has been widely used for pandemic (H1N1) 2009 virus infection, and by April 30, 2010, a total of 285 resistant cases were reported worldwide, including 45 in the United Kingdom. "( Oseltamivir-resistant pandemic (H1N1) 2009 virus infection in England and Scotland, 2009-2010.
Calatayud, L; Lackenby, A; McMenamin, J; Pebody, R; Phin, NF; Reynolds, A; Zambon, M, 2011
)
3.25
"Oseltamivir has dominated the U.S. "( U.S. utilization patterns of influenza antiviral medications during the 2009 H1N1 influenza pandemic.
Borders-Hemphill, V; Mosholder, A, 2012
)
1.82
"Oseltamivir (Tamiflu) has been shown to be effective as a treatment and chemoprophylaxis for influenza virus infections. "( Oseltamivir inhibits both viral entry and release but enhances apoptosis of cells infected with influenza A H1N1.
Du, N; Gao, R; Li, Z; Liu, D; Shu, Y; Zhu, Y, 2013
)
3.28
"Oseltamivir has been shown to prevent influenza when given for long-term prophylaxis or for post-exposure prophylaxis."( Early therapy with the neuraminidase inhibitor oseltamivir maximizes its efficacy in influenza treatment.
Gillissen, A; Höffken, G, 2002
)
1.29
"Oseltamivir has been studied over the course of a 5-year development programme in >11000 subjects from North America, Europe and the Southern Hemisphere, including otherwise healthy adults, approximately 500 elderly/high-risk subjects, and children (>1000) aged 1-12 years."( Safety and pharmacology of oseltamivir in clinical use.
Dutkowski, R; Froehlich, E; Oo, C; Suter, P; Thakrar, B; Ward, P, 2003
)
1.34
"Oseltamivir (Tamiflu) has been shown to be effective in the treatment and prevention of epidemic influenza infection in adults, adolescents and children (> or = 1 year)."( Oseltamivir (Tamiflu) and its potential for use in the event of an influenza pandemic.
Dutkowski, R; Small, I; Smith, J; Suter, P; Ward, P, 2005
)
2.49
"Oseltamivir has proven to be safe and effective for the prevention or treatment of all known influenza subtypes, reducing the severity and duration of symptoms, the complications arising from influenza infection (pneumonia, hospitalisation, antibiotic use) and mortality."( Oseltamivir in the management of influenza.
Oxford, J, 2005
)
2.49
"Oseltamivir for PEP has an efficacy of 58.5% (15.6% to 79.6) for households and of 68% (34.9 to 84.2%) to 89% in contacts of index cases."( Neuraminidase inhibitors for preventing and treating influenza in healthy adults.
Demicheli, V; Di Pietrantonj, C; Jefferson, TO; Jones, M; Rivetti, D, 2006
)
1.06
"Oseltamivir has been shown to decrease antibiotic use, the number of hospitalizations, and, probably, the risk of death after influenza."( Antiviral management of seasonal and pandemic influenza.
Hayden, FG; Pavia, AT, 2006
)
1.06
"Oseltamivir resistance has been reported in up to 2% of patients in clinical trials of oseltamivir and in up to 18% of treated children."( Neuraminidase inhibitor resistance in influenza viruses.
Reece, PA, 2007
)
1.06
"Oseltamivir has shown excellent tolerability and a low potential for viral resistance in pediatric studies."( The role of oseltamivir in the treatment and prevention of influenza in children.
Whitley, RJ, 2007
)
1.44
"Oseltamivir has been used for treatment of influenza A and B infections, but recent reports documented that it was less active against the latter. "( Effectiveness of oseltamivir treatment among children with influenza A or B virus infections during four successive winters in Niigata City, Japan.
Gejyo, F; Li, D; Oguma, T; Saito, R; Sakai, T; Sasaki, A; Sato, I; Sato, M; Shobugawa, Y; Suzuki, H; Suzuki, Y; Tanabe, N; Tsukada, H, 2008
)
2.13

Actions

Oseltamivir may increase survival when used within five days of symptom onset in influenza H1N1-infected patients who require ICU admission. A lower virological response was associated with female gender (OR, 0.45; 0.21-0.96) and baseline viral load ≥5 log cgeq/μL. OseltAmivir did not produce clinically relevant changes on nocturnal polysomnographic variables in young men.

ExcerptReferenceRelevance
"Oseltamivir may increase survival when used within five days of symptom onset in influenza H1N1-infected patients who require ICU admission. "( Influenza treatment with oseltamivir outside of labeled recommendations.
Blair, M; McQuade, B, 2015
)
2.16
"Oseltamivir and zanamivir cause small reductions in the time to first alleviation of influenza symptoms in adults. "( Neuraminidase inhibitors for influenza: a systematic review and meta-analysis of regulatory and mortality data.
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, 2016
)
1.88
"Oseltamivir did not produce clinically relevant changes on nocturnal polysomnographic variables in young Japanese men."( Absence of adverse effects of oseltamivir on sleep: a double-blind, randomized study in healthy volunteers in Japan.
Abe, M; Davies, BE; Hosaka, Y; Inoue, Y; Kumagai, Y; Kuwahara, H; Mishima, K; Prinssen, EP; Rayner, CR; Toovey, S; Uchimura, N, 2011
)
1.38
"For oseltamivir, a lower clinical response was associated with female gender (HR, 0.53; 95% CI, 0.36-0.79), baseline symptoms score >14 (HR, 0.47; 0.32-0.70), viral load ≥5 log cgeq/μL (HR, 0.63; 0.43-0.93), and initiation of antibiotics (HR, 0.30; 0.12-0.76); a lower virological response was associated with female gender (OR, 0.45; 0.21-0.96), baseline viral load ≥5 log cgeq/μL (OR, 0.40; 0.20-0.84) and days 0-2 incomplete compliance (OR, 0.31; 0.10-0.98)."( Factors associated with clinical and virological response in patients treated with oseltamivir or zanamivir for influenza A during the 2008-2009 winter.
Blanchon, T; Bouscambert, M; Carrat, F; Charlois-Ou, C; Dornic, Q; Duval, X; Enouf, V; Leport, C; Mentré, F; Mosnier, A, 2013
)
1.1

Treatment

Oseltamivir treatment of intranasally infected mice with the mouse hepatitis coronavirus 3 (MHV-3) decreased lung neutrophil infiltration, viral load, and tissue damage. Odds of death were reduced by two thirds (odds ratio (OR): 0.32; 95% confidence interval (CI):”0.11-0.93), in inpatients treated with a standard course of oseltimivir 75 mg two times daily for 5 days.

ExcerptReferenceRelevance
"Oseltamivir treatment may be a promising regenerative strategy to manage IVDD and osteoarthritic cartilage tissues."( Does oseltamivir protect human chondrocyte and nucleus pulposus cells from degeneration by inhibiting senescence and proinflammation mediated by the NLRP3 inflammasome and NF-κB?
Akalan, H; Karaarslan, N; Ozbek, H; Oznam, K; Yasar Sirin, D; Yilmaz, I, 2022
)
2.68
"Oseltamivir treatment of intranasally infected mice with the mouse hepatitis coronavirus 3 (MHV-3) decreased lung neutrophil infiltration, viral load, and tissue damage."( Neuraminidase is a host-directed approach to regulate neutrophil responses in sepsis and COVID-19.
Aires, L; Alisson-Silva, F; Amaral, FC; Antônia, J; Báfica, A; Barroso, SPC; Burgel, PR; Chollet-Martin, S; Costa, VV; Cunha, FQ; de Oliveira Formiga, R; de Souza, FRO; Faria, LF; Fonseca, FR; Heck, N; Hurtado-Nedelec, MM; Lorenzini, CB; Macauley, MS; Mansur, DS; Martin, C; Maurici, R; Mendes, DAGB; Morrot, A; Natale, CC; Paula, NM; Queiroz-Junior, CM; Rocha, EL; Santos, AA; Santos, FRS; Silva, PCS; Sordi, R; Souza, CF; Spiller, F; Starick, MR; Van Weyenbergh, J; Wanderley, CWS; Witko-Sarsat, V, 2023
)
1.63
"Oseltamivir treatment effect on odds of inpatient death was assessed by backward stepwise multivariable logistic regression analysis.ResultsThe odds of death were reduced by two thirds (odds ratio (OR): 0.32; 95% confidence interval (CI): 0.11-0.93), in inpatients treated with a standard course of oseltamivir 75 mg two times daily for 5 days - compared with those untreated with oseltamivir, after adjustment for age, sex, current excess alcohol intake, receipt of 2016/17 seasonal influenza vaccine, serum haemoglobin and hospital vs community attribution of acquisition of influenza.ConclusionsOseltamivir treatment given according to National Institutes of Clinical Excellence (NICE); United States Centres for Disease Control and Prevention (CDC); Infectious Diseases Society of America (IDSA) and World Health Organization (WHO) guidelines was shown to be effective in reducing the odds of mortality in inpatients with PCR-confirmed seasonal influenza A(H3N2) after adjustment in a busy routine English hospital setting."( Influenza-associated mortality in hospital care: a retrospective cohort study of risk factors and impact of oseltamivir in an English teaching hospital, 2016 to 2017.
Choudhry, S; Christou, S; Jalal, H; Jones, NK; Ranellou, K; Reacher, M; Reeve, L; Sander, C; Verlander, NQ; Warne, B; Wright, C; Zambon, M; Zhang, H, 2019
)
1.45
"Oseltamivir-treated patients were less likely to require antibacterials than baloxavir-treated patients (RR, 0.87 [.82-.91])."( Comparison of Hospitalization Incidence in Influenza Outpatients Treated With Baloxavir Marboxil or Neuraminidase Inhibitors: A Health Insurance Claims Database Study.
Ajisawa, Y; Fujiwara, M; Hara, K; Honda, K; Hosogaya, N; Iwata, S; Kitanishi, Y; Komeda, T; Miyauchi, H; Miyazaki, T; Mukae, H; Ogura, E; Takazono, T; Watanabe, H, 2021
)
1.34
"Oseltamivir treatment is currently the only way of managing influenza in young infants for whom influenza vaccines are not licensed, but little data exist on the effectiveness of the treatment in this age group."( Oseltamivir treatment of influenza A and B infections in infants.
Antikainen, P; Heikkinen, T; Mattila, JM; Vuorinen, T; Waris, M, 2021
)
3.51
"Oseltamivir treatment of infants with influenza rapidly decreased the viral load in nasopharyngeal secretions and shortened the duration and severity of symptoms. "( Oseltamivir treatment of influenza A and B infections in infants.
Antikainen, P; Heikkinen, T; Mattila, JM; Vuorinen, T; Waris, M, 2021
)
3.51
"Oseltamivir treatment at 2 different doses reduced A(H7N9) viral titers in infected animals, but even high-dose oseltamivir did not block viral replication sufficiently to suppress the emergence of resistant variants."( Emergence of Oseltamivir-Resistant H7N9 Influenza Viruses in Immunosuppressed Cynomolgus Macaques.
Friedrich, TC; Fukuyama, S; Hasegawa, H; Imai, M; Ito, M; Itoh, Y; Iwatsuki-Horimoto, K; Kawakami, E; Kawaoka, Y; Kiso, M; Lopes, TJS; Moncla, LH; Nakajima, N; Neumann, G; Ogasawara, K; Tomita, Y; Uraki, R; Watanabe, T; Yamada, S; Yamayoshi, S, 2017
)
1.55
"Oseltamivir versus no treatment was associated with a decrease in hospitalization and pneumonia risk/odds in 2/4 SR/MAs."( 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
)
1.18
"Oseltamivir treatment is recommended in any patients with influenza and pneumonia or severe illness, and critically ill patients, especially during the first 48hours of illness."( [Oseltamivir for the treatment of influenza in children and adolescents].
Alfayate, S; Couceiro, JA; Cruz-Cañete, M; Launes, C; Otheo, E; Pérez, C; Tagarro, A, 2019
)
2.15
"Oseltamivir treatment of patients with seasonal influenza already receiving OTC medications produced a faster reduction in severity of most symptoms and a quicker return to ability to perform normal activities compared with patients who took OTC medications and placebo."( Oseltamivir effectiveness in seasonal influenza patients taking symptomatic therapy: retrospective analysis of RCT data.
Dutkowski, R; Smith, JR; Smith, P; Toovey, S, 2013
)
3.28
"Oseltamivir treatment resulted in a modest reduction in the duration of symptoms and virus shedding in people with uncomplicated influenza infections, even when treatment was started 48 h or longer after illness onset."( Efficacy of oseltamivir treatment started within 5 days of symptom onset to reduce influenza illness duration and virus shedding in an urban setting in Bangladesh: a randomised placebo-controlled trial.
Azim, T; Bresee, J; Brooks, WA; Fry, AM; Goswami, D; Gubareva, L; Luby, SP; Nahar, K; Rahman, M; Sharmin, AT, 2014
)
2.22
"Oseltamivir-treated and untreated ferrets were challenged with high (106 pfu) and low (102 pfu) doses of influenza H1N1pdm09 virus."( Low dose influenza virus challenge in the ferret leads to increased virus shedding and greater sensitivity to oseltamivir.
Barclay, WS; Bean, TJ; Bruce, C; Carroll, MW; Dimmock, NJ; Dove, BK; Dowall, S; Easton, AJ; Hallis, B; Marriott, AC; Newman, E; Pearson, G; Plank, J; Rayner, E; Ryan, KA; Silman, NJ; Taylor, I; Whittaker, CJ, 2014
)
1.34
"Oseltamivir in the treatment of adults increased the risk of nausea (risk difference 3.66%, 0.90% to 7.39%; number needed to treat to harm (NNTH) 28, 95% confidence interval 14 to 112) and vomiting (4.56%, 2.39% to 7.58%; 22, 14 to 42)."( Oseltamivir for influenza in adults and children: systematic review of clinical study reports and summary of regulatory comments.
Doshi, P; Heneghan, CJ; Jefferson, T; Jones, M; Onakpoya, I; Spencer, EA, 2014
)
2.57
"NTZ-oseltamivir combination treatment was synergistic also against the avian A/chicken/Italy/9097/1997 (H5N9) IAV (CI=0.18 to 0.31)."( Synergistic effect of nitazoxanide with neuraminidase inhibitors against influenza A viruses in vitro.
Belardo, G; Cenciarelli, O; La Frazia, S; Rossignol, JF; Santoro, MG, 2015
)
0.9
"Oseltamivir treatment of animals was associated with an improvement in clinical symptoms, including reduced inflammatory responses in the upper respiratory tract, lower body weight loss and a smaller rise in body temperature, despite there being no significant reduction in viral shedding."( A novel video tracking method to evaluate the effect of influenza infection and antiviral treatment on ferret activity.
Barr, IG; Hurt, AC; Oh, DY, 2015
)
1.14
"Oseltamivir treatment (5 or 25 mg/kg of body weight/dose) was given 4 h postinfection, followed by twice-daily treatment for 5 days."( Neuraminidase Mutations Conferring Resistance to Oseltamivir in Influenza A(H7N9) Viruses.
Chesnokov, AP; Davis, CT; De La Cruz, JA; Fry, AM; Gubareva, LV; Marjuki, H; Mishin, VP; Villanueva, JM, 2015
)
1.39
"Oseltamivir treatment was applied to 28 patients, where 24 had severe symptoms, nine had comorbid factors and two did not have any of these."( Experience of influenza A H1N1 in a paediatric emergency unit.
Biçer, S; Ercan Sariçoban, H; Ergenekon Ulutaş, P; Gürol, Y; Özelgün, B; Özen, AO; Saf, C; Vitrinel, A; Yilmaz, G, 2015
)
1.14
"Oseltamivir treatment of adults increased the risk of nausea (RD 3.66%, 95% CI 0.90% to 7.39%) and vomiting (RD 4.56%, 95% CI 2.39% to 7.58%)."( Neuraminidase inhibitors for influenza: a systematic review and meta-analysis of regulatory and mortality data.
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, 2016
)
1.16
"Oseltamivir treatment was well tolerated among hospitalized children, including among infants aged <1 year."( A randomized, double-blind, placebo-controlled trial evaluating the safety of early oseltamivir treatment among children 0-9 years of age hospitalized with influenza in El Salvador and Panama.
Azziz-Baumgartner, E; Barahona, A; Castillo, JM; Castillo, M; Cazares, RA; Clara, W; Dawood, FS; De León, T; de Viana, D; Estripeaut, D; Franco, D; Fry, AM; Gargiullo, P; Gonzalez, R; Gubareva, L; Hughes, M; Jara, J; Lawson, AM; Luciani, K; Rodriguez, M; Sujey Brizuela, Y; Tamura, D; Widdowson, MA, 2016
)
2.1
"Oseltamivir treatment shows benefit, but treatment with corticosteroids is associated with an increased risk of death."( Clinical features of human influenza A (H5N1) infection in Vietnam: 2004-2006.
Chau, NQ; Farrar, J; Hien, ND; Hien, NT; Hien, TT; Horby, P; Khang, DD; Liem, NT; Long, HT; Mai, le Q; Taylor, WR; Tung, CV; Wertheim, H, 2009
)
1.07
"Oseltamivir, a treatment for influenza, has been shown to decrease the severity of an influenza episode, but few data exist regarding its potentially protective effect against recurrent vascular outcomes among influenza patients with a history of vascular disease."( Use of oseltamivir after influenza infection is associated with reduced incidence of recurrent adverse cardiovascular outcomes among military health system beneficiaries with prior cardiovascular diseases.
Casscells, SW; Cottrell, L; Granger, E; Kress, AM; Linton, A; Madjid, M, 2009
)
1.53
"Oseltamivir treatment was not associated with statistically significant reduction in the duration of viral shedding."( Effects of oseltamivir treatment on duration of clinical illness and viral shedding and household transmission of influenza virus.
Chan, KH; Cheng, CK; Cowling, BJ; Fang, VJ; Houck, PM; Ip, DK; Leung, GM; Malik Peiris, JS; Ng, S; Uyeki, TM, 2010
)
1.47
"Oseltamivir treatment is effective in reducing the duration of symptoms, but evidence of household reduction in transmission of influenza virus was inconclusive."( Effects of oseltamivir treatment on duration of clinical illness and viral shedding and household transmission of influenza virus.
Chan, KH; Cheng, CK; Cowling, BJ; Fang, VJ; Houck, PM; Ip, DK; Leung, GM; Malik Peiris, JS; Ng, S; Uyeki, TM, 2010
)
2.19
"Oseltamivir treatment significantly reduces the emergence of new AOM infections in children with LCI; effects are most pronounced in those <5 years."( Impact of oseltamivir treatment on the incidence and course of acute otitis media in children with influenza.
Block, SL; Dutkowski, R; Reisinger, K; Winther, B, 2010
)
2.21
"Oseltamivir treatment was initiated on day seven (median) after onset of symptoms."( Patients with influenza A/H1N1v- associated pneumonia: the perspective of a tertiary care hospital in Switzerland.
Bertisch, B; Boggian, K; Vernazza, P, 2010
)
1.08
"Oseltamivir index treatment on onset day or the following day (early treatment) was associated with a 42% reduction (OR: 0.58, 95% CI: 0.19, 1.73) in the odds of one or more secondary infections in a household and a 50% reduction (OR: 0.5, 95% CI: 0.17, 1.46) in the odds of a secondary infection in individual contacts. "( Oseltamivir for treatment and prevention of pandemic influenza A/H1N1 virus infection in households, Milwaukee, 2009.
Biedrzycki, P; Cowling, BJ; Danon, L; Fang, VJ; Goldstein, E; Hagy, A; Lipsitch, M; Miller, JC; O'Hagan, JJ; Reshef, D; Robins, J, 2010
)
3.25
"Oseltamivir treatment started within 24 hours of symptom onset provides substantial benefits to children with influenza A infection. "( Early oseltamivir treatment of influenza in children 1-3 years of age: a randomized controlled trial.
Heikkinen, T; Heinonen, S; Ikonen, N; Lehtinen, P; Puhakka, T; Silvennoinen, H; Vahlberg, T; Vainionpää, R; Ziegler, T, 2010
)
2.28
"Oseltamivir treatment did not shorten the duration of fever."( Epidemiological and clinical features of 308 hospitalized patients with novel 2009 influenza A (H1N1) virus infection in China during the first pandemic wave.
Li, X; Liang, L; Liu, Y; Nie, G; Tan, X; Tian, Y; Xia, Z; Zhang, G; Zhou, B, 2011
)
1.09
"In oseltamivir- or zanamivir-treated influenza patients who were statistically comparable in their age distribution, vaccination history, and type or subtype of virus isolates, the virus-shedding period in zanamivir-treated patients was significantly shorter than that in oseltamivir-treated patients. "( Frequency of drug-resistant viruses and virus shedding in pediatric influenza patients treated with neuraminidase inhibitors.
Ichikawa, M; Kawakami, C; Kawakami, E; Kawaoka, Y; Kiso, M; Mitamura, K; Ozawa, M; Shimizu, H; Sugaya, N; Takano, R; Tamura, D; Uehara, R; Yamazaki, M, 2011
)
0.99
"Mass oseltamivir prophylactic treatment was used to contain the outbreak."( Pandemic influenza A(H1N1) 2009 virus outbreak among boarding school pupils in Madagascar: compliance and adverse effects of prophylactic oseltamivir treatment.
Heraud, JM; Rajatonirina, S; Ramandimbisoa, T; Randrianasolo, L; Ratsitorahina, M; Razanajatovo, N; Richard, V, 2011
)
1.03
"Oseltamivir treatment was initiated in 72 children and discontinued in 42 (63%) when RT-PCR results turned negative."( Characterization of 2009 H1N1 pandemic influenza in a population of Dutch children with influenza-like signs and symptoms.
Bongers, KM; Brandjes, DP; Kuiper, RJ; Smit, PM; Smits, PH; von Rosenstiel, IA, 2012
)
1.1
"Oseltamivir treatment in 3/6 infants was without side effects."( Pandemic A/H1N1(2009) influenza infections in very-low-birth-weight infants--a case series from the German Neonatal Network.
Felderhoff-Müser, U; Göpel, W; Härtel, C; Heitmann, F; Hoehn, T; Keller, M; Roggendorf, M; Ross, S; Stein, A, 2011
)
1.09
"Oseltamivir treatment was well-tolerated even among premature infants and appeared to be effective, because neonates with influenza had complete recovery and only one of those who received prophylaxis developed the infection."( Influenza A/H1N1/2009 outbreak in a neonatal intensive care unit.
Harahousou, E; Kapetanakis, I; Kyriakou, D; Maltezou, H; Nika, A; Stripeli, F; Tsagris, V; Tsolia, M, 2012
)
1.1
"Oral oseltamivir treatment does not significantly reduce the duration of illness or influenza-related complications in mild pandemic influenza A H1N1 2009 virus infection in previously healthy adults."( The clinical effectiveness of oseltamivir in mild cases of pandemic influenza A H1N1 2009 infection.
Eom, JS; Ju, YS; Kim, JS; Lee, JS; Park, SY; You, JY, 2012
)
1.18
"In oseltamivir treated patients, oseltamivir-resistant influenza A(H1N1)pdm09 virus continue to emerge with three of 23 (13%) post-treatment samples containing the H275Y mutation."( Frequency of oseltamivir resistance in Sydney, during the Newcastle outbreak of community transmitted oseltamivir-resistant influenza A(H1N1)pdm09 virus, Australia, June to August 2011.
Booy, R; Dixit, R; Dwyer, DE; Hurt, A; Kesson, A; McPhie, K; Ratnamohan, M; Saksena, N; Taylor, J; Wang, B, 2012
)
1.26
"Oseltamivir treatment may have played a role for improving in our patients' condition."( Documented 2009 H1N1 Influenza A infection in pediatric liver transplant patients--description and follow-up of 7 patients.
Cantez, MS; Durmaz, Ö; Gerenlı, N; Hançerlı Törün, S; Salman, N; Somer, A, 2012
)
1.1
"Oseltamivir-treated and untreated patients were matched according to calendar week, age, sex, site, and propensity for treatment."( Risk of adverse events following oseltamivir treatment in influenza outpatients, Vaccine Safety Datalink Project, 2007-2010.
Baxter, R; Fry, AM; Greene, SK; Irving, SA; Jackson, ML; Jacobsen, SJ; Lee, GM; Li, L; Lieu, TA; Naleway, AL; Narwaney, KJ; Nordin, JD; Shay, DK, 2013
)
1.39
"Oseltamivir for treatment of patients with ILI is potentially cost-effective if clinical diagnostic specificity for influenza observed in clinical trials is applicable to routine practice. "( Oseltamivir for treatment of influenza in healthy adults: pooled trial evidence and cost-effectiveness model for Canada.
Blackhouse, G; Goeree, R; Loeb, M; O'Brien, BJ; Smieja, M,
)
3.02
"Oseltamivir treatment of influenza illness reduces LRTCs, antibiotic use, and hospitalization in both healthy and "at-risk" adults."( Impact of oseltamivir treatment on influenza-related lower respiratory tract complications and hospitalizations.
Hayden, F; Kaiser, L; Mahoney, P; Mills, T; Ward, P; Wat, C, 2003
)
2.16
"(1) Oseltamivir treatment significantly reduced the duration of fever about 25 hours post treatment."( [A multicenter study of efficacy and safety of oseltamivir in the treatment of suspected influenza patients].
Deng, WW; Li, QY; Zhong, NS, 2004
)
1.06
"Oseltamivir-treated patients also experienced fewer asthma exacerbations up to day 7 (68% versus 51%; P = 0.031)."( Oral oseltamivir improves pulmonary function and reduces exacerbation frequency for influenza-infected children with asthma.
Dutkowski, R; Ferrero, F; Garcia, ML; Johnston, SL, 2005
)
1.56
"Oseltamivir treatment decreased RSV-induced weight loss and inhibited RSV clearance."( Cutting Edge: Oseltamivir decreases T cell GM1 expression and inhibits clearance of respiratory syncytial virus: potential role of endogenous sialidase in antiviral immunity.
Chi, MH; Goleniewska, K; Higginbotham, JN; Moore, ML; O'Neal, JF; Peebles, RS; Zhou, W, 2007
)
1.42
"The oseltamivir and untreated control groups each included 36 751 eligible patients. "( Impact of oseltamivir on the incidence of secondary complications of influenza in adolescent and adult patients: results from a retrospective population-based study.
Blumentals, WA; Schulman, KL, 2007
)
1.3
"Oseltamivir treatment also reduced symptom scores (median [IQR] score-hours, 225 [97-349] vs 400 [189-645]; P = .05), and nasal proinflammatory cytokine levels."( Use of the oral neuraminidase inhibitor oseltamivir in experimental human influenza: randomized controlled trials for prevention and treatment.
Betts, RF; Fritz, RS; Hayden, FG; Kinnersley, N; Lobo, M; Miller, M; Mills, RG; Straus, SE; Treanor, JJ; Ward, P, 1999
)
1.29
"Oseltamivir treatment reduced the duration of fever and oseltamivir recipients returned to usual activities 2 to 3 days earlier than placebo recipients (P < or = .05)."( Efficacy and safety of the oral neuraminidase inhibitor oseltamivir in treating acute influenza: a randomized controlled trial. US Oral Neuraminidase Study Group.
Barbarash, R; Bettis, R; Hayden, FG; Kinnersley, N; Mills, RG; Riff, D; Singh, S; Treanor, JJ; Vrooman, PS; Ward, P, 2000
)
1.27
"Oseltamivir treatment also reduced cough, coryza and duration of fever."( Oral oseltamivir treatment of influenza in children.
Dutkowski, R; Hayden, FG; Ipe, D; Mills, RG; Reisinger, KS; Ward, P; Whitley, RJ; Young, N, 2001
)
1.55
"Oseltamivir for treatment or prophylaxis during 11 influenza outbreaks in 1999/2000."( Use of oseltamivir during influenza outbreaks in Ontario nursing homes, 1999-2000.
Bowles, SK; Fearon, M; Lee, W; Li, Y; Loeb, M; McGeer, A; Simor, AE; Tamblyn, S; Vearncombe, M, 2002
)
2.21
"Treatment with oseltamivir was prescribed to 90% of patients; adults had higher rates of treatment (96% vs."( Characteristics of hospitalised patients with influenza in 2015-2016 in northern Israel: three circulating strains and continued fear of 2009 A/H1N1.
Azrad, M; Ben-Amram, H; Glikman, D; Kalish, T; Miron, D; Peretz, A; Rechnitzer, H, 2019
)
0.85
"Treatment with oseltamivir was initiated as recommended in 96% of hospitalized patients presenting with influenza. "( Analysis of delays in the prescription of oseltamivir in hospitals and potential for improvement.
De Briel, D; Gerber, V; Greigert, V; Gronnwald, A; Martinot, M; Mohseni Zadeh, M; Rosolen, B; Thibaud, E, 2019
)
1.13
"Treatment with oseltamivir and anticonvulsants led to complete neurologic recovery by day 14."( Simply influenza A (H3N2)-associated encephalitis with seizure.
Chen, PC; Ho, TH; Lee, JT; Wang, CW; Yang, FC; Yuan, HT, 2019
)
0.85
"Mice treated with oseltamivir plus fenofibrate exhibited the longest mean survival time, the largest reduction of viral titre in lung tissue, the highest levels of CD4(+) and CD8(+) T-lymphocytes, and the greatest decrease in pulmonary inflammation."( Combinations of oseltamivir and fibrates prolong the mean survival time of mice infected with the lethal H7N9 influenza virus.
Bao, L; Deng, W; Gao, Z; Gu, S; Li, F; Li, Y; Lv, Q; Qin, C; Xu, L; Xu, Y; Yao, Y; Yu, P; Yuan, J; Zhu, H, 2015
)
1.09
"Treatment with oseltamivir (75mg twice daily) did not improve the patient's condition."( Successful treatment of avian-origin influenza A (H7N9) infection using convalescent plasma.
Gao, HN; Li, LJ; Ou, HL; Peng, XM; Wu, HB; Wu, XX, 2015
)
0.76
"Treatment with oseltamivir 75 mg twice daily and serial nasal swabs were performed at the discretion of the treating physician."( Outcome of influenza infections in outpatients after allogeneic hematopoietic stem cell transplantation.
Flückiger, U; Gratwohl, A; Halter, J; Hirsch, HH; Khanna, N; Lehmann, T; Schreiber, A; Steffen, I; Studt, JD; Weisser, M, 2009
)
0.69
"Treatment with Oseltamivir was statistically associated with survival with a crude OR of .11 (95% CI: 0.04-0.30) and .13 (95% CI: 0.04-0.40) after controlling for age."( Severe human influenza infections in Thailand: oseltamivir treatment and risk factors for fatal outcome.
Areechokechai, D; Hanshaoworakul, W; Kaewchana, S; Levy, J; Narueponjirakul, U; Sanasuttipun, W; Shinde, V; Simmerman, JM; Ungchusak, K, 2009
)
0.95
"Treatment with Oseltamivir is associated with survival in hospitalized human influenza pneumonia patients."( Severe human influenza infections in Thailand: oseltamivir treatment and risk factors for fatal outcome.
Areechokechai, D; Hanshaoworakul, W; Kaewchana, S; Levy, J; Narueponjirakul, U; Sanasuttipun, W; Shinde, V; Simmerman, JM; Ungchusak, K, 2009
)
0.95
"Treatment with oseltamivir significantly protected against subsequent development of radiographically confirmed pneumonia (odds ratio 0.12, 95% confidence interval 0.08 to 0.18), and treatment started within two days of symptom onset reduced the duration of fever and viral RNA shedding."( Effectiveness of oseltamivir on disease progression and viral RNA shedding in patients with mild pandemic 2009 influenza A H1N1: opportunistic retrospective study of medical charts in China.
Farrar, J; Feng, Z; Gao, Z; Guo, X; Huai, Y; Liao, Q; van Doorn, HR; Wang, Y; Xiang, N; Yang, W; Yu, H; Yuan, Y; Zheng, Y; Zhou, L, 2010
)
1.04
"Treatment with oseltamivir was associated with a significantly reduced development of radiographically confirmed pneumonia and a shorter duration of fever and viral RNA shedding."( Effectiveness of oseltamivir on disease progression and viral RNA shedding in patients with mild pandemic 2009 influenza A H1N1: opportunistic retrospective study of medical charts in China.
Farrar, J; Feng, Z; Gao, Z; Guo, X; Huai, Y; Liao, Q; van Doorn, HR; Wang, Y; Xiang, N; Yang, W; Yu, H; Yuan, Y; Zheng, Y; Zhou, L, 2010
)
1.04
"Treatment with oseltamivir was well tolerated."( Clinical and epidemiological characteristics of patients with influenza A (H1N1) 2009 attended to at the emergency room of a children's hospital.
Borrego, A; Campins, M; Casquero, A; Cebrián, R; Fàbregas, A; Figueras, C; Lera, E; Melendo, S; Miserachs, M; Moraga, F; Sancosmed, M; Tórtola, T; Wörner, NT, 2011
)
0.71
"Treatment with oseltamivir of all patients with suspected cases of influenza and prompt modifications to infection control practices, including playroom closures and enhanced education of visitors and staff, terminated nosocomial transmission."( Pandemic (H1N1) 2009 influenza in hospitalized children in Manitoba: nosocomial transmission and lessons learned from the first wave.
Bridger, NA; Bullard, JM; Coombs, JM; Crockett, ME; Embree, JE; Fanella, ST; Olekson, KL; Pinto, MA; Poliquin, PG; Van Caeseele, PG, 2011
)
0.71
"A treatment with oseltamivir or zanamivir was prescribed in 13%, and 3% of the patients was admitted to a hospital."( Online monitoring of flu in Belgium.
Devroey, D; Semaille, P; Van De Vijver, E; Vandevoorde, J; Vansintejan, J, 2011
)
0.7
"Treatment with oseltamivir, plasma exchange and hemodiafiltration for the hemolytic uremic syndrome and meticulous supportive care with steroid pulse therapy for the pulmonary alveolar hemorrhage was successful in this case."( Pandemic H1N1 influenza A viral infection complicated by atypical hemolytic uremic syndrome and diffuse alveolar hemorrhage.
Ahn, JH; Choi, HJ; Kwak, IS; Lee, SB; Lee, YJ; Rhee, H; Seong, EY; Song, SH, 2011
)
0.71
"Treatment with oseltamivir improved survival in mice from 0% to 75%, even when therapy was delayed for up to 5 days after infection with influenza virus."( Effect of antiviral treatment on the outcome of secondary bacterial pneumonia after influenza.
McCullers, JA, 2004
)
0.66
"Treatment with oseltamivir is a cost-effective strategy for otherwise healthy adults in the UK from both the healthcare payer and societal perspective."( Influenza treatment with neuraminidase inhibitors: cost-effectiveness and cost-utility in healthy adults in the United Kingdom.
Bergemann, R; Gyldmark, M; Hayden, FG; Morris, J; Mueller, E; Sander, B, 2005
)
0.67
"Treatment with oseltamivir was associated with an incremental cost-effectiveness of approximately 27,619 dollars per quality-adjusted life-year gained relative to providing supportive care."( Cost-effectiveness of vaccination versus treatment of influenza in healthy adolescents and adults.
Khan, K; Muennig, PA, 2001
)
0.65

Toxicity

There were no statistically significant differences in the occurrence of adverse neurologic events during therapy among subjects treated with oseltamivir versus those treated with the adamantanes (P = 0.02). Importantly, osel tamsivir phosphate administration had adverse effects on the liver of mice and significantly increased messenger R.

ExcerptReferenceRelevance
" Our results demonstrate that oseltamivir is safe and effective for the prevention of influenza."( [Efficacy and safety of the selective oral neuraminidase inhibitor oseltamivir for prophylaxis against influenza--placebo-controlled double-blind multicenter phase III trial].
Kashiwagi, S; Kudoh, S; Watanabe, A; Yoshimura, I, 2000
)
0.83
" Safety evaluations included treatment-emergent adverse events, hospitalisations and deaths, as well as haematological and biochemical laboratory safety tests."( Safety and pharmacology of oseltamivir in clinical use.
Dutkowski, R; Froehlich, E; Oo, C; Suter, P; Thakrar, B; Ward, P, 2003
)
0.62
" We studied the severity of illness due to influenza among adults residing in a center for the developmentally disabled and assessed adverse reactions to amantadine and oseltamivir prophylaxis."( Adverse effects of amantadine and oseltamivir used during respiratory outbreaks in a center for developmentally disabled adults.
Benjamin, JH; Gardner, C; Green, K; Lee, W; Loeb, M; McArthur, M; McGeer, AJ; Simor, AE, 2004
)
0.8
" Potential adverse events were documented during amantadine and oseltamivir therapy, and during a baseline period with neither medication."( Adverse effects of amantadine and oseltamivir used during respiratory outbreaks in a center for developmentally disabled adults.
Benjamin, JH; Gardner, C; Green, K; Lee, W; Loeb, M; McArthur, M; McGeer, AJ; Simor, AE, 2004
)
0.84
" Twenty-eight (25%) of 112 residents had an adverse neurologic event while receiving amantadine prophylaxis, compared with 3 (2."( Adverse effects of amantadine and oseltamivir used during respiratory outbreaks in a center for developmentally disabled adults.
Benjamin, JH; Gardner, C; Green, K; Lee, W; Loeb, M; McArthur, M; McGeer, AJ; Simor, AE, 2004
)
0.6
" The rate of adverse neurologic events associated with amantadine was significantly higher than that associated with oseltamivir."( Adverse effects of amantadine and oseltamivir used during respiratory outbreaks in a center for developmentally disabled adults.
Benjamin, JH; Gardner, C; Green, K; Lee, W; Loeb, M; McArthur, M; McGeer, AJ; Simor, AE, 2004
)
0.81
" Adverse events reported were similar in oseltamivir and placebo group."( [A multicenter study of efficacy and safety of oseltamivir in treatment of naturally acquired influenza].
Cai, B; Li, L; Wang, M; Zhu, Y, 2001
)
0.83
" 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
" (5) Severe cutaneous adverse effects, including cases of Lyell syndrome, were reported in children taking oseltamivir."( Oseltamivir: cutaneous and neurological adverse effects in children.
, 2006
)
1.99
"Oseltamivir is safe and effective in immunocompetent persons, and prophylactic use is recommended during influenza outbreaks."( Safety and tolerability of oseltamivir prophylaxis in hematopoietic stem cell transplant recipients: a retrospective case-control study.
Boeckh, M; Corey, L; Englund, JA; Nichols, WG; Peck, AJ; Varley, C; Vu, D, 2007
)
2.08
" Retrospectively, 45 patients (25 of whom had undergone HSCT, and 20 of whom were pre-HSCT candidates) who received oseltamivir prophylaxis were evaluated for adverse events."( Safety and tolerability of oseltamivir prophylaxis in hematopoietic stem cell transplant recipients: a retrospective case-control study.
Boeckh, M; Corey, L; Englund, JA; Nichols, WG; Peck, AJ; Varley, C; Vu, D, 2007
)
0.85
" The proportions of clinical and laboratory adverse events meeting common terminology criteria grades 2-4 or 3-4 were not significantly different between the case patients who received oseltamivir prophylaxis and control subjects."( Safety and tolerability of oseltamivir prophylaxis in hematopoietic stem cell transplant recipients: a retrospective case-control study.
Boeckh, M; Corey, L; Englund, JA; Nichols, WG; Peck, AJ; Varley, C; Vu, D, 2007
)
0.83
"Oseltamivir prophylaxis appeared to be safe and well tolerated in managing an influenza outbreak in an HSCT outpatient residence."( Safety and tolerability of oseltamivir prophylaxis in hematopoietic stem cell transplant recipients: a retrospective case-control study.
Boeckh, M; Corey, L; Englund, JA; Nichols, WG; Peck, AJ; Varley, C; Vu, D, 2007
)
2.08
"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
" In contrast, OE was an order of magnitude more toxic than OA towards algae, with a more pronounced effect when the direct inhibition of photosystem II was used as toxicity endpoint opposed to the 24h growth rate endpoint."( Mixture toxicity of the antiviral drug Tamiflu((R)) (oseltamivir ethylester) and its active metabolite oseltamivir acid.
Bramaz, N; Escher, BI; Lienert, J; Neuwoehner, J; Straub, JO, 2010
)
0.61
" To assess potential neurologic adverse effects of oseltamivir use in infants, a retrospective chart review was performed in infants less than 12 months of age who received oseltamivir, amantadine, or rimantadine."( Safety of oseltamivir compared with the adamantanes in children less than 12 months of age.
Abughali, N; Abzug, MJ; Bradley, JS; Cloud, GA; Englund, J; Griffin, J; Guzman-Cottrill, J; Jacobs, RF; Jester, P; Kimberlin, DW; Lang, D; Leach, C; Ramilo, O; Robinson, J; Romero, JR; Shalabi, M; Shelton, M; Storch, G; Wade, KC; Whitley, RJ, 2010
)
1.01
"The primary objective was to describe the frequency of neurologic adverse events among children less than 12 months of age who received oseltamivir compared with those receiving adamantanes."( Safety of oseltamivir compared with the adamantanes in children less than 12 months of age.
Abughali, N; Abzug, MJ; Bradley, JS; Cloud, GA; Englund, J; Griffin, J; Guzman-Cottrill, J; Jacobs, RF; Jester, P; Kimberlin, DW; Lang, D; Leach, C; Ramilo, O; Robinson, J; Romero, JR; Shalabi, M; Shelton, M; Storch, G; Wade, KC; Whitley, RJ, 2010
)
0.97
" Volunteers were followed up to Day 7 for pharmacokinetic parameters, vital signs, adverse events and cardiac safety."( Safety and pharmacokinetics of oseltamivir at standard and high dosages.
Davies, BE; Dutkowski, R; Smith, JR, 2010
)
0.65
" This article reviews pre-clinical and clinical data to assess the safety of oseltamivir administered during pregnancy, in the context of the effects of influenza on adverse pregnancy outcomes and fetal malformations."( Safety of oseltamivir in pregnancy: a review of preclinical and clinical data.
Donner, B; Hoffmann, G; Niranjan, V, 2010
)
0.99
" No marked side effect was reported."( High levels and safety of oseltamivir carboxylate plasma concentrations after nasogastric administration in critically ill children in a pediatric intensive care unit.
Chappuy, H; Duchêne, P; Ducrocq, S; Giraud, C; Hubert, P; Manceau, S; Mogenet, A; Oualha, M; Treluyer, JM, 2011
)
0.67
"7% of sample participants reported at least one side effect (experienced during the regime)."( Side effects of oseltamivir in end-stage renal failure patients.
Choo, D; Chowdhury, S; Hossain, M; Liew, P; Tan, J, 2011
)
0.72
" This study aimed to determine the transmission of infection among boarding school pupils and to evaluate the adverse effects of oseltamivir chemoprophylactic treatment and their impact on compliance."( Pandemic influenza A(H1N1) 2009 virus outbreak among boarding school pupils in Madagascar: compliance and adverse effects of prophylactic oseltamivir treatment.
Heraud, JM; Rajatonirina, S; Ramandimbisoa, T; Randrianasolo, L; Ratsitorahina, M; Razanajatovo, N; Richard, V, 2011
)
0.78
" Questions addressed symptoms of influenza-like illness, compliance with chemoprophylaxis, and adverse effects."( Pandemic influenza A(H1N1) 2009 virus outbreak among boarding school pupils in Madagascar: compliance and adverse effects of prophylactic oseltamivir treatment.
Heraud, JM; Rajatonirina, S; Ramandimbisoa, T; Randrianasolo, L; Ratsitorahina, M; Razanajatovo, N; Richard, V, 2011
)
0.57
" Bad compliance was not associated with adverse effects."( Pandemic influenza A(H1N1) 2009 virus outbreak among boarding school pupils in Madagascar: compliance and adverse effects of prophylactic oseltamivir treatment.
Heraud, JM; Rajatonirina, S; Ramandimbisoa, T; Randrianasolo, L; Ratsitorahina, M; Razanajatovo, N; Richard, V, 2011
)
0.57
"Since the symptoms of pandemic influenza A(H1N1) 2009 virus were generally mild, the burden of adverse effects must be considered when deciding on mass oseltamivir chemoprophylaxis among teenagers."( Pandemic influenza A(H1N1) 2009 virus outbreak among boarding school pupils in Madagascar: compliance and adverse effects of prophylactic oseltamivir treatment.
Heraud, JM; Rajatonirina, S; Ramandimbisoa, T; Randrianasolo, L; Ratsitorahina, M; Razanajatovo, N; Richard, V, 2011
)
0.77
" The incidence of adverse events (AEs) during the pandemic (1 May 2009 to 31 December 2009) was compared with that beforehand (during previous influenza seasons) for USA and Japan only, as exposure data in other countries were collected inconsistently."( Safety profile of oseltamivir during the 2009 influenza pandemic.
Bader-Weder, S; Donner, B; Niranjan, V; Peng, MM; Schwarz, R; Smith, JR, 2011
)
0.7
" However, not much is known about its adverse effects."( Potential adverse effects of oseltamivir in rats: males are more vulnerable than females.
Al-Kahtani, MA; El-Sayed, WM, 2011
)
0.66
"To examine the safety profile of oseltamivir in children and evaluate the impact of P-glycoprotein polymorphisms on the incidence of neuropsychiatric adverse events (NPAE) in oseltamivir-treated children."( ABCB1 polymorphisms and neuropsychiatric adverse events in oseltamivir-treated children during influenza H1N1/09 pandemia.
Barbe, RP; Crisinel, PA; Dayer, P; Desmeules, JA; Fluss, J; Ing Lorenzini, K; Korff, CM; L'Huillier, AG; Posfay-Barbe, KM; Rebsamen, MC; Siegrist, CA, 2011
)
0.89
" Adverse events were systematically recorded by pediatricians and/or by parents at home using a diary card, with a 30-day follow-up period."( ABCB1 polymorphisms and neuropsychiatric adverse events in oseltamivir-treated children during influenza H1N1/09 pandemia.
Barbe, RP; Crisinel, PA; Dayer, P; Desmeules, JA; Fluss, J; Ing Lorenzini, K; Korff, CM; L'Huillier, AG; Posfay-Barbe, KM; Rebsamen, MC; Siegrist, CA, 2011
)
0.61
" There were no serious adverse events and no deaths."( Pharmacokinetics and safety of coadministered oseltamivir and rimantadine in healthy volunteers: an open-label, multiple-dose, randomized, crossover study.
Ballester-Sanchis, RM; Brennan, BJ; Cirrincione-Dall, G; Davies, BE; Navarro, MT, 2012
)
0.64
" No influenza, neurologic, or laboratory adverse effects occurred."( Safety and pharmacokinetics of oseltamivir for prophylaxis of neonates exposed to influenza H1N1.
Dotsikas, Y; Drakoulis, N; Karalis, V; Loukas, YL; Maltezou, HC; Siahanidou, T; Theodoridou, M; Zervaki, E, 2012
)
0.66
" No serious adverse events were identified during treatment."( Survey of Japanese infants younger than 3 months who were treated with oseltamivir for influenza: safety of oseltamivir treatment.
Hosoya, M; Ihara, T; Kumagai, T; Morioka, I; Morishima, T; Nonoyama, S; Okabe, N; Okada, K; Sugaya, N; Tanaka-Taya, K; Ueta, I, 2012
)
0.61
"5-2 mg/kg twice daily may be safe in infants aged < 3 months."( Survey of Japanese infants younger than 3 months who were treated with oseltamivir for influenza: safety of oseltamivir treatment.
Hosoya, M; Ihara, T; Kumagai, T; Morioka, I; Morishima, T; Nonoyama, S; Okabe, N; Okada, K; Sugaya, N; Tanaka-Taya, K; Ueta, I, 2012
)
0.61
" Seventeen participants reported 22 adverse events (AEs); in three participants, AEs were considered probably drug related (nausea or vomiting)."( Safety and tolerability of a 6-week course of oseltamivir prophylaxis for seasonal influenza in children.
Cupelli, L; Dutkowski, R; Marcadis, I; Reisinger, K; Shu, D, 2013
)
0.65
" Serious adverse events (oseltamivir 8% and placebo 10%) and adverse events (oseltamivir 55% and placebo 58%) were reported in both arms with a similar frequency."( Efficacy and safety of oral oseltamivir for influenza prophylaxis in transplant recipients.
Dutkowski, R; Ison, MG; Kriván, G; Nist, A; Shapira, MY; Szakaly, P, 2012
)
0.98
"A 2008 review by our group concluded that the risk of neuropsychiatric adverse events (NPAEs) in influenza patients was not increased by oseltamivir exposure, and did not identify any mechanism by which oseltamivir or its metabolites could cause or worsen such events."( Post-marketing assessment of neuropsychiatric adverse events in influenza patients treated with oseltamivir: an updated review.
Bansod, S; Britschgi, M; Chu, T; Donner, B; Dutkowski, R; Koerner, A; Prinssen, EP; Rayner, CR; Sirzen-Zelenskaya, A; Thakrar, BT; Toovey, S, 2012
)
0.8
" Within this matched cohort, conditional logistic regression models were used to estimate the risk of four neuropsychiatric and five other adverse events (AEs) during pre-specified risk intervals."( Risk of adverse events following oseltamivir treatment in influenza outpatients, Vaccine Safety Datalink Project, 2007-2010.
Baxter, R; Fry, AM; Greene, SK; Irving, SA; Jackson, ML; Jacobsen, SJ; Lee, GM; Li, L; Lieu, TA; Naleway, AL; Narwaney, KJ; Nordin, JD; Shay, DK, 2013
)
0.67
" 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,
)
0.63
"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,
)
0.61
"To compare the rates of adverse effects and compliance with oseltamivir treatment among hospitalized children aged < 1-year-old with suspected influenza and older children."( [Compliance and safety of oseltamivir treatment in children and infants less than one year of age].
Bishop, B; Somekh, E; Stein, M; Tasher, D, 2012
)
0.92
" Adverse effects were reported in 53."( [Compliance and safety of oseltamivir treatment in children and infants less than one year of age].
Bishop, B; Somekh, E; Stein, M; Tasher, D, 2012
)
0.68
" Difficulties in oseltamivir administrating and/or possible adverse effects have rarely influenced compliance."( [Compliance and safety of oseltamivir treatment in children and infants less than one year of age].
Bishop, B; Somekh, E; Stein, M; Tasher, D, 2012
)
1.02
" The risk factors of adverse events were: lack of typical symptoms, lack of detailed medical history, clinical masking of a "trivial" illness, doctors' ignorance and insufficient knowledge, several physicians treating the same patient during hospitalization."( Adverse event analysis in fatal cases of influenza A (H1N1) - a lesson from Poland.
Jurek, T; Rorat, M, 2013
)
0.39
"The data reviewed in this article reinforce the findings of a previous review, suggesting that oseltamivir is unlikely to cause adverse pregnancy or fetal outcomes."( The safety of oseltamivir in pregnancy: an updated review of post-marketing data.
Chandrasekaran, A; Tomianovic, D; Wollenhaupt, M, 2014
)
0.98
" TCN-032 was safe and well tolerated with no additional safety signals after administration of oseltamivir."( Efficacy and safety of treatment with an anti-m2e monoclonal antibody in experimental human influenza.
Balaratnam, G; Bonavia, A; Fredlund, P; Koller, TD; Mitcham, JL; Ramos, EL; Swiderek, KM; Usner, DW, 2015
)
0.64
" TCN-032 was safe with no evidence of immune exacerbation based on serum cytokine expression."( Efficacy and safety of treatment with an anti-m2e monoclonal antibody in experimental human influenza.
Balaratnam, G; Bonavia, A; Fredlund, P; Koller, TD; Mitcham, JL; Ramos, EL; Swiderek, KM; Usner, DW, 2015
)
0.42
" Assessments included pharmacokinetics, on-treatment adverse events, resistance testing and viral shedding."( Safety, virology and pharmacokinetics of oseltamivir in infants with laboratory-confirmed influenza: a Phase I/II, prospective, open-label, multicentre clinical trial.
Brzostek, J; Chappey, C; Clinch, B; Guillén, S; Niranjan, V; Rath, BA; Rayner, CR, 2015
)
0.68
" On-treatment adverse events (n=48) were reported by 32 patients (49%)."( Safety, virology and pharmacokinetics of oseltamivir in infants with laboratory-confirmed influenza: a Phase I/II, prospective, open-label, multicentre clinical trial.
Brzostek, J; Chappey, C; Clinch, B; Guillén, S; Niranjan, V; Rath, BA; Rayner, CR, 2015
)
0.68
" Adverse events (AEs) were monitored for 30 days from treatment initiation."( Pharmacokinetics and safety of intravenous oseltamivir in infants and children in open-label studies.
Anderson, EJ; Clinch, B; Deville, JG; Kamal, MA; Muñoz, FM, 2015
)
0.68
"There have been concerns that oseltamivir causes neuropsychiatric adverse events (NPAEs)."( Analysis of Neuropsychiatric Adverse Events in Patients Treated with Oseltamivir in Spontaneous Adverse Event Reports.
Abe, J; Kato, Y; Kato, Z; Kinosada, Y; Nakamura, M; Nakayama, Y; Ueda, N; Umetsu, R, 2015
)
0.94
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43
" Children were randomized 1:1 to receive oseltamivir or placebo; had swabs collected at enrollment for influenza RT-PCR testing; were assessed at enrollment and every 12 h for work of breathing; and were followed for adverse events through 7 days after discharge."( A randomized, double-blind, placebo-controlled trial evaluating the safety of early oseltamivir treatment among children 0-9 years of age hospitalized with influenza in El Salvador and Panama.
Azziz-Baumgartner, E; Barahona, A; Castillo, JM; Castillo, M; Cazares, RA; Clara, W; Dawood, FS; De León, T; de Viana, D; Estripeaut, D; Franco, D; Fry, AM; Gargiullo, P; Gonzalez, R; Gubareva, L; Hughes, M; Jara, J; Lawson, AM; Luciani, K; Rodriguez, M; Sujey Brizuela, Y; Tamura, D; Widdowson, MA, 2016
)
0.92
" There was no difference in adverse events between groups."( A randomized, double-blind, placebo-controlled trial evaluating the safety of early oseltamivir treatment among children 0-9 years of age hospitalized with influenza in El Salvador and Panama.
Azziz-Baumgartner, E; Barahona, A; Castillo, JM; Castillo, M; Cazares, RA; Clara, W; Dawood, FS; De León, T; de Viana, D; Estripeaut, D; Franco, D; Fry, AM; Gargiullo, P; Gonzalez, R; Gubareva, L; Hughes, M; Jara, J; Lawson, AM; Luciani, K; Rodriguez, M; Sujey Brizuela, Y; Tamura, D; Widdowson, MA, 2016
)
0.66
" The incidence of adverse events did not differ significantly between the groups, nor were there any serious adverse events."( Efficacy and safety of Ergoferon versus oseltamivir in adult outpatients with seasonal influenza virus infection: a multicenter, open-label, randomized trial.
Andrianova, E; Averyanov, A; Bart, B; Epstein, O; Minina, E; Putilovskiy, M; Rafalsky, V, 2016
)
0.7
"Ergoferon and oseltamivir were equally effective and safe in adult outpatients with seasonal influenza A or B virus infection."( Efficacy and safety of Ergoferon versus oseltamivir in adult outpatients with seasonal influenza virus infection: a multicenter, open-label, randomized trial.
Andrianova, E; Averyanov, A; Bart, B; Epstein, O; Minina, E; Putilovskiy, M; Rafalsky, V, 2016
)
1.06
" 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
)
0.69
" 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
)
0.74
"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
)
0.71
" 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
" Vomiting was the only adverse event with a significantly higher risk in the treatment group."( Efficacy and Safety of Oseltamivir in Children: Systematic Review and Individual Patient Data Meta-analysis of Randomized Controlled Trials.
Brooks, WA; Heikkinen, T; Malosh, RE; Martin, ET; Monto, AS; Whitley, RJ, 2018
)
0.79
"Estimating the rate of adverse events (AEs) caused by a treatment in clinical trials typically involves comparing the proportions of patients experiencing AEs in intervention and control groups."( Psychiatric adverse events in oseltamivir prophylaxis trials: Novel comparative analysis using data obtained from clinical study reports.
Del Mar, C; Jones, M; Tett, SE, 2018
)
0.77
"Although the potential risk of neuropsychiatric adverse events (NPAEs) upon administration of oseltamivir has been raised in case reports, the association between the use of oseltamivir and the risk of NPAEs is unclear."( Risk of neuropsychiatric adverse events associated with the use of oseltamivir: a nationwide population-based case-crossover study.
Kang, HR; Kim, WJ; Lee, EK; Shin, JY, 2019
)
0.97
"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
" Analyses were based on data from electronic medical records and our standardized LTR database with prospective documentation of clinical information including medication, laboratory and radiological results, outcomes and adverse events."( Use of oseltamivir in lung transplant recipients with suspected or proven influenza infection: a 1-year observational study of outcomes and safety.
Benden, C; Jungo, C; Russmann, S; Schuurmans, MM, 2019
)
0.97
" We discovered a wide range of adverse events but none occurred in >5%, and most were mild and of questionable causal relationship to oseltamivir administration."( Use of oseltamivir in lung transplant recipients with suspected or proven influenza infection: a 1-year observational study of outcomes and safety.
Benden, C; Jungo, C; Russmann, S; Schuurmans, MM, 2019
)
1.17
"This non-controlled retrospective analysis suggests that the pre-emptive use of oseltamivir for respiratory tract infections pending microbiological results is safe in LTRs."( Use of oseltamivir in lung transplant recipients with suspected or proven influenza infection: a 1-year observational study of outcomes and safety.
Benden, C; Jungo, C; Russmann, S; Schuurmans, MM, 2019
)
1.2
" 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
" Importantly, oseltamivir phosphate administration had adverse effects on the liver of mice and significantly increased messenger RNA expression levels of F4/80, interleukin-1β, transforming growth factor-β1, matrix metalloproteinase-12, and collagen."( Adverse Effects of Oseltamivir Phosphate Therapy on the Liver of LDLR-/- Mice Without Any Benefit on Atherosclerosis and Thrombosis.
Bennasroune, A; Blaise, S; Bocquet, O; Boulagnon, C; Duca, L; Fougerat, A; Gayral, S; Gillery, P; Henry, A; Jaisson, S; Laffargue, M; Martiny, L; Maurice, P; Romier-Crouzet, B; Sarazin, T; Sartelet, H; Schneider, C; Vincent, E; Wahart, A, 2021
)
1.31
" Favipiravir is a safe effective alternative for hydroxychloroquine in mild or moderate COVID-19 infected patients."( Safety and efficacy of favipiravir versus hydroxychloroquine in management of COVID-19: A randomised controlled trial.
Dabbous, HM; Ebeid, FFS; El Assal, G; El-Sayed, MH; Elgaafary, M; Elghazaly, H; Fawzy, E; Hassany, SM; Riad, AR; Sherief, AF; TagelDin, MA, 2021
)
0.62
" Compared with oseltamivir and placebo, baloxavir appears to be a relatively safe anti-influenza agent."( Clinical efficacy and safety of baloxavir marboxil in the treatment of influenza: A systematic review and meta-analysis of randomized controlled trials.
Chen, CH; Kuo, YC; Lai, CC; Wang, CY; Wang, YH, 2021
)
0.97
" The primary endpoint was the time to normal body temperature, and the secondary endpoints included the time to remission of influenza symptoms, incidence of influenza-like complications, and incidence of adverse reactions."( Multicenter, randomized controlled, open label evaluation of the efficacy and safety of arbidol hydrochloride tablets in the treatment of influenza-like cases.
Bai, X; Chen, G; Fan, X; Li, Y; Tian, Y; Wang, K; Wang, W; Xi, S; Zhao, Y, 2023
)
0.91
" Regarding the incidence of complications and adverse events, there was only one case of tracheitis, one case of nausea, one case of vomiting, and one case of dizziness in the control group."( Multicenter, randomized controlled, open label evaluation of the efficacy and safety of arbidol hydrochloride tablets in the treatment of influenza-like cases.
Bai, X; Chen, G; Fan, X; Li, Y; Tian, Y; Wang, K; Wang, W; Xi, S; Zhao, Y, 2023
)
0.91
" Further, the patients treated with arbidol hydrochloride tablets had fewer adverse reactions, and thus, the tablets were safe to use."( Multicenter, randomized controlled, open label evaluation of the efficacy and safety of arbidol hydrochloride tablets in the treatment of influenza-like cases.
Bai, X; Chen, G; Fan, X; Li, Y; Tian, Y; Wang, K; Wang, W; Xi, S; Zhao, Y, 2023
)
0.91

Pharmacokinetics

The prodrug oseltamivir has been shown to be efficacious and safe for the treatment of influenza. However, pharmacokinetic information was lacking for children below 5 years of age. Two studies were conducted to assess the potential for pharmacokinetics of peramvir when coadministered with oselmivir or rimantadine. Pregnancy had only a modest effect upon the pharmacokinetically parameters of osel tamivirs.

ExcerptReferenceRelevance
" The pharmacokinetic profile of oseltamivir is simple and predictable, and twice daily treatment results in effective antiviral plasma concentrations over the entire administration interval."( Clinical pharmacokinetics of the prodrug oseltamivir and its active metabolite Ro 64-0802.
He, G; Massarella, J; Ward, P, 1999
)
0.85
" In study 2, a randomised, placebo controlled phase III study in paediatric children (1 to 12 years) presenting with influenza symptoms, 199 pharmacokinetic sparse samples were obtained from 87 patients, and serial samples were obtained from 5 patients."( Pharmacokinetics and dosage recommendations for an oseltamivir oral suspension for the treatment of influenza in children.
Barrett, J; Dorr, A; Dutkowski, R; Hill, G; Mann, J; Oo, C; Ward, P, 2001
)
0.56
" The plasma and urine results demonstrated no pharmacokinetic interaction between oseltamivir and aspirin."( Lack of pharmacokinetic interaction between the oral anti-influenza prodrug oseltamivir and aspirin.
Barrett, J; Dorr, A; Liu, B; Oo, C; Ward, P, 2002
)
0.77
" Pharmacokinetic parameters were calculated for oseltamivir and Ro 64-0802."( Lack of pharmacokinetic interaction between the oral anti-influenza neuraminidase inhibitor prodrug oseltamivir and antacids.
Barrett, J; Dorr, A; Oo, C; Snell, P, 2002
)
0.79
"Bioequivalence was achieved for the primary pharmacokinetic parameters Cmax and AUC(0, infinity ) of Ro 64-0802 following administration of oseltamivir with either Maalox suspension or Titralac(R) tablets vs administration of oseltamivir alone."( Lack of pharmacokinetic interaction between the oral anti-influenza neuraminidase inhibitor prodrug oseltamivir and antacids.
Barrett, J; Dorr, A; Oo, C; Snell, P, 2002
)
0.73
" There was no pharmacokinetic interaction between oseltamivir with either antacid, demonstrating that the oral absorption of oseltamivir was not impaired in the presence of antacids containing magnesium, aluminium or calcium."( Lack of pharmacokinetic interaction between the oral anti-influenza neuraminidase inhibitor prodrug oseltamivir and antacids.
Barrett, J; Dorr, A; Oo, C; Snell, P, 2002
)
0.78
" Pharmacokinetic parameters of oseltamivir and its carboxylate metabolite show that absorption was similar in the proximal and distal small bowel compared to stomach delivery, but reduced from the ascending colon, demonstrating that absorption-rate limited disposition occurred only for the ascending colon."( Pharmacokinetics and delivery of the anti-influenza prodrug oseltamivir to the small intestine and colon using site-specific delivery capsules.
Barrett, J; Dorr, A; Liu, B; Oo, C; Snell, P; Wilding, I, 2003
)
0.85
"The prodrug oseltamivir has been shown to be efficacious and safe for the treatment of influenza for patients 1 year of age or older; however, pharmacokinetic information was lacking for children below 5 years of age."( Pharmacokinetics of anti-influenza prodrug oseltamivir in children aged 1-5 years.
Boellner, S; Dorr, A; Hill, G; Liu, B; Oo, C; Ward, P, 2003
)
0.96
" Plasma and urine samples were collected (24 h) for pharmacokinetic analysis, and safety was assessed."( Pharmacokinetics of oseltamivir in young and very elderly subjects.
Abe, M; Barrett, J; Kinoshita, H; Rayner, CR; Smith, J; Urae, A, 2006
)
0.66
" For the active metabolite, oseltamivir carboxylate, Cmax and AUC(inf) values were, respectively, 22% and 91% higher in the very elderly subjects than in the young subjects, while oral clearance was 50% lower in the elderly population."( Pharmacokinetics of oseltamivir in young and very elderly subjects.
Abe, M; Barrett, J; Kinoshita, H; Rayner, CR; Smith, J; Urae, A, 2006
)
0.95
" Although many more subjects would need to be studied to rule out a synergistic increase in adverse events, the combination in this small human drug-drug interaction trial appears safe and without pharmacokinetic consequences."( A randomized, crossover study to evaluate the pharmacokinetics of amantadine and oseltamivir administered alone and in combination.
Amer, A; Evans, TG; Howard, D; Morrison, D; Rayner, C; Roy, S; Smith, JR, 2007
)
0.57
" To investigate this proposal, we developed a population pharmacokinetic model and simulated the pharmacokinetics of candidate combination regimens of oral oseltamivir (45 mg and 30 mg twice a day) plus oral probenecid (500 mg/6 hourly)."( Population pharmacokinetics of oseltamivir when coadministered with probenecid.
Boak, LM; Chanu, P; Gieschke, R; Jonsson, EN; Rayner, CR, 2008
)
0.83
" Pharmacokinetic data, obtained by noncompartmental methods, and safety data are reported."( Pharmacokinetics and tolerability of oseltamivir combined with probenecid.
Cunningham, F; Davey, RT; Deyton, LR; Goetz, MB; Holodniy, M; Lee, KK; Lin, ET; Olivo, N; Penzak, SR; Raisch, DW; Straight, TM, 2008
)
0.62
" A significant difference in the pharmacokinetic parameters of O (except for T(max) and t(1/2,lambdaz)) was found when the plasma samples were treated with dichlorvos."( Studies on the influence of esterase inhibitor to the pharmacokinetic profiles of oseltamivir and oseltamivir carboxylate in rats using an improved LC/MS/MS method.
Chang, Q; Chow, MS; Zuo, Z, 2009
)
0.58
" Each infusion dose was followed by a no-drug washout, producing the appropriate half-life for this drug."( Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
Brown, A; Drusano, GL; Kulawy, R; McSharry, JJ; Weng, Q, 2009
)
0.6
" We documented the pharmacokinetic profile of oseltamivir in patients admitted to intensive care units (ICUs) with suspected or confirmed pandemic (H1N1) influenza."( Enteric absorption and pharmacokinetics of oseltamivir in critically ill patients with pandemic (H1N1) influenza.
Ahern, S; Ariano, RE; Kanji, S; Kumar, A; Pisipati, A; Rello, J; Sitar, DS; Zarychanski, R; Zelenitsky, SA, 2010
)
0.88
" Volunteers were followed up to Day 7 for pharmacokinetic parameters, vital signs, adverse events and cardiac safety."( Safety and pharmacokinetics of oseltamivir at standard and high dosages.
Davies, BE; Dutkowski, R; Smith, JR, 2010
)
0.65
" This review aims to describe the current knowledge of the pharmacokinetic and pharmacodynamic characteristics of this agent, and to address the issue of possible therapeutic drug monitoring."( Oseltamivir in seasonal, avian H5N1 and pandemic 2009 A/H1N1 influenza: pharmacokinetic and pharmacodynamic characteristics.
Aouri, M; Buclin, T; Decosterd, LA; Ivanyuk, A; Meylan, P; Widmer, N, 2010
)
1.8
" Pharmacokinetic data of oseltamivir phosphate in postpartum women, however, are lacking."( Pharmacokinetics of oseltamivir in breast milk and maternal plasma.
Greer, LG; Leff, RD; McCracken, GH; Roberts, SW; Rogers, VL; Sheffield, JS; Wendel, GD, 2011
)
1
" Using a noncompartmental model, area under the curve (AUC), maximum concentration (C(max)), time to maximum concentration, and half-life were estimated."( Pharmacokinetics of oseltamivir in breast milk and maternal plasma.
Greer, LG; Leff, RD; McCracken, GH; Roberts, SW; Rogers, VL; Sheffield, JS; Wendel, GD, 2011
)
0.69
"The purpose of this study was to determine pharmacokinetic parameters for oseltamivir in all trimesters of pregnancy."( Pharmacokinetics of oseltamivir according to trimester of pregnancy.
Greer, LG; Leff, RD; McCracken, GH; Roberts, SW; Rogers, VL; Sheffield, JS; Wendel, GD, 2011
)
0.92
" This should nevertheless be confirmed by a controlled pharmacokinetic study performed on a larger number of patients."( Pharmacokinetics and diffusion into sputum of oseltamivir and oseltamivir carboxylate in adults with cystic fibrosis.
Babany, G; Hubert, D; Jullien, V; Launay, O; Lortholary, O; Sermet, I, 2011
)
0.63
" 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
)
0.59
"The OPTIMO trial was a single-centre, non-randomized, open-label pharmacokinetic study of single-dose and steady-state oral oseltamivir phosphate and its carboxylate metabolite in healthy, morbidly obese [body mass index (BMI) >  40)] and healthy, non-obese (BMI  <  30) subjects."( Oseltamivir pharmacokinetics in morbid obesity (OPTIMO trial).
Goralski, KB; Hatchette, TF; Johnston, BL; McNeil, SA; Slayter, KL; Thorne-Humphrey, LM, 2011
)
2.02
" Based on these pharmacokinetic data, an oseltamivir dose adjustment for body weight would not be needed in morbidly obese individuals."( Oseltamivir pharmacokinetics in morbid obesity (OPTIMO trial).
Goralski, KB; Hatchette, TF; Johnston, BL; McNeil, SA; Slayter, KL; Thorne-Humphrey, LM, 2011
)
2.08
"The pharmacokinetic parameters in this patient were unexpected because the clearances occurred more quickly than in phase I trials."( Postpartum pharmacokinetics of peramivir in the treatment of 2009 H1N1 influenza.
Adiga, RB; Alsup, R; Clay, PG; Gerk, PM; McRae, M; Taylor, TAH, 2011
)
0.37
"Physiologically based pharmacokinetic (PBPK) modelling can assist in the development of drug therapies and regimens suitable for challenging patient populations such as very young children."( Development of a physiologically based model for oseltamivir and simulation of pharmacokinetics in neonates and infants.
Davies, B; Hoffmann, G; Koerner, A; Lave, T; Parrott, N; Prinssen, E; Singer, T; Theogaraj, E, 2011
)
0.62
" These models incorporated physicochemical properties and in vitro metabolism data into mechanistic representations of pharmacokinetic processes."( Development of a physiologically based model for oseltamivir and simulation of pharmacokinetics in neonates and infants.
Davies, B; Hoffmann, G; Koerner, A; Lave, T; Parrott, N; Prinssen, E; Singer, T; Theogaraj, E, 2011
)
0.62
" The population pharmacokinetic exposure profiles of oseltamivir carboxylate (the active metabolite) were comparable between class III obese subjects and nonobese adults (healthy and infected)."( Oseltamivir and oseltamivir carboxylate pharmacokinetics in obese adults: dose modification for weight is not necessary.
Lodise, TP; Pai, MP, 2011
)
2.06
" Two studies were conducted to assess the potential for pharmacokinetic interactions of peramivir when coadministered with oseltamivir or rimantadine."( Absence of pharmacokinetic interaction between intravenous peramivir and oral oseltamivir or rimantadine in humans.
Atiee, G; Baughman, S; Collis, P; Hernandez, J; Hollister, A; Lasseter, K; McCullough, A, 2012
)
0.81
" Elimination half-life was unaffected by coadministration."( Pharmacokinetics and safety of coadministered oseltamivir and rimantadine in healthy volunteers: an open-label, multiple-dose, randomized, crossover study.
Ballester-Sanchis, RM; Brennan, BJ; Cirrincione-Dall, G; Davies, BE; Navarro, MT, 2012
)
0.64
" A pharmacokinetic (PK) interaction between Os and immunosuppressive drugs might adversely affect the efficacy and/or toxicity of the latter agents."( Oseltamivir, an influenza neuraminidase inhibitor drug, does not affect the steady-state pharmacokinetic characteristics of cyclosporine, mycophenolate, or tacrolimus in adult renal transplant patients.
Aoki, FY; Jeffery, J; Lam, H; Sitar, DS, 2011
)
1.81
" The mean Cmax values for oseltamivir and oseltamivir carboxylate were found to be lower than those reported for children 1 to 5 years old, whereas Tmax values were similar to children 1 to 5 years old."( Safety and pharmacokinetics of oseltamivir for prophylaxis of neonates exposed to influenza H1N1.
Dotsikas, Y; Drakoulis, N; Karalis, V; Loukas, YL; Maltezou, HC; Siahanidou, T; Theodoridou, M; Zervaki, E, 2012
)
0.97
" OC, the active form of oseltamivir, was quantified in plasma, and main pharmacokinetic parameters were determined."( Impact of extracorporeal membrane oxygenation and continuous venovenous hemodiafiltration on the pharmacokinetics of oseltamivir carboxylate in critically ill patients with pandemic (H1N1) influenza.
Antignac, M; Combes, A; Corvol, E; Farinotti, R; Fernandez, C; Lemaitre, F; Luyt, CE; Nieszkowska, A; Roullet-Renoleau, F; Zahr, N, 2012
)
0.9
"OC Cmax (1029 ± 478 ng/mL) and area under the curve (9."( Impact of extracorporeal membrane oxygenation and continuous venovenous hemodiafiltration on the pharmacokinetics of oseltamivir carboxylate in critically ill patients with pandemic (H1N1) influenza.
Antignac, M; Combes, A; Corvol, E; Farinotti, R; Fernandez, C; Lemaitre, F; Luyt, CE; Nieszkowska, A; Roullet-Renoleau, F; Zahr, N, 2012
)
0.59
" A pharmacokinetic study has been conducted during an influenza A(H1N1) outbreak in a neonatal intensive care unit."( Oseltamivir pharmacokinetics and clinical experience in neonates and infants during an outbreak of H1N1 influenza A virus infection in a neonatal intensive care unit.
Kafetzis, DA; Kapetanakis, I; Maltezou, HC; Nika, A; Standing, JF; Tsagris, V; Tsolia, MN, 2012
)
1.82
" No significant differences in the pharmacokinetic parameters of oseltamivir and oseltamivir carboxylate were observed according to CES1A genotype."( The effect of carboxylesterase 1 (CES1) polymorphisms on the pharmacokinetics of oseltamivir in humans.
Hamasaki, H; Hosokawa, M; Imai, H; Inano, A; Itohda, A; Morimoto, T; Ohashi, K; Ohyama, T; Suzaki, Y; Takada, M; Tateishi, M; Uemura, N, 2013
)
0.85
"Prospective, open-label, pharmacokinetic study."( Pharmacokinetics of oseltamivir and oseltamivir carboxylate in critically ill patients receiving continuous venovenous hemodialysis and/or extracorporeal membrane oxygenation.
Eyler, RF; Heung, M; Mueller, BA; Napolitano, LM; Park, PK; Pleva, M; Sowinski, KM, 2012
)
0.7
" Pharmacokinetic parameters for the patient who received only ECMO were not reported."( Pharmacokinetics of oseltamivir and oseltamivir carboxylate in critically ill patients receiving continuous venovenous hemodialysis and/or extracorporeal membrane oxygenation.
Eyler, RF; Heung, M; Mueller, BA; Napolitano, LM; Park, PK; Pleva, M; Sowinski, KM, 2012
)
0.7
" This study aimed to investigate the impact of covariates on pharmacokinetic (PK) variability of oseltamivir and its active metabolite form, oseltamivir carboxylate (OC)."( Population pharmacokinetics of oseltamivir: pediatrics through geriatrics.
Ambrose, PG; Bhavnani, SM; Bulik, CC; Forrest, A; Kamal, MA; Rayner, CR; Reynolds, DK; Smith, PF; Subramoney, V; Van Wart, SA, 2013
)
0.89
" Oseltamivir has complex PK which requires modelling to properly understand the relationship between dose and concentration with time, and there is a lack of clarity on appropriate pharmacodynamic endpoints."( Pharmacokinetics and pharmacodynamics of oseltamivir in neonates, infants and children.
Lutsar, I; Standing, JF; Tsolia, M, 2013
)
1.57
" The aim of this study was to investigate the pharmacokinetic properties of oseltamivir and its active metabolite, oseltamivir carboxylate, in obese and nonobese healthy subjects."( Pharmacokinetics of orally administered oseltamivir in healthy obese and nonobese Thai subjects.
Charunwattana, P; Day, NP; Hanpithakpong, W; Jittamala, P; Lawpoolsri, S; Lindegardh, N; Panapipat, S; Pukrittayakamee, S; Tarning, J; Taylor, WR; White, NJ, 2014
)
0.9
"Dose selection is an important step in pharmacokinetic (PK) studies of hemodialysis patients."( Dose selection method for pharmacokinetic study in hemodialysis patients using a subpharmacological dose: oseltamivir as a model drug.
Joo, KW; Kim, DK; Kim, M; Kim, S; Kim, YS; Lee, JP; Lee, JW; Lim, CS; Oh, KH; Shin, KH; Yu, KS, 2014
)
0.62
" Physiology-based pharmacokinetic (PBPK) model could be used to evaluate different dosing regimens for pregnant women and to correctly predict drug exposure and response on the personal level."( [Peculiarities and clinical significance of drug pharmacokinetics and pharmacodynamics during pregnancy].
Lutsevich, KA; Reshet'ko, OV; Sanina, II, 2014
)
0.4
" Here, data for 133 infants were pooled from two prospective pharmacokinetic/pharmacodynamic safety studies to develop a population pharmacokinetic model."( The posology of oseltamivir in infants with influenza infection using a population pharmacokinetic approach.
Acosta, EP; Ampofo, K; Clinch, B; Gibiansky, L; Jester, P; Kamal, MA; Kimberlin, DW; Niranjan, V; Rath, B; Rayner, CR; Sánchez, PJ; Whitley, R, 2014
)
0.75
" The aim of this study is to develop a physiologically based pharmacokinetic (PBPK) model to predict changes in CES1 substrate drug exposure in humans with CES1 activity impaired by ethanol or loss-of-function CES1 genetic polymorphisms."( Physiologically based pharmacokinetic modeling of impaired carboxylesterase-1 activity: effects on oseltamivir disposition.
Edginton, AN; Hu, ZY; Laizure, SC; Parker, RB, 2014
)
0.62
" This study aimed to characterize the pharmacokinetics and tolerability of oseltamivir in automated peritoneal dialysis (APD) and construct a pharmacokinetic model to assist with optimized dosing."( Pharmacokinetics and safety of oseltamivir in patients with end-stage renal disease treated with automated peritoneal dialysis.
Giraudon, M; Kamal, MA; Kirkpatrick, CM; Morcos, PN; Patel, K; Rayner, CR; Robson, R, 2015
)
0.93
"A multicentre steady-state pharmacokinetic study of OS was performed in 35 non-pregnant and 29 pregnant women."( Population pharmacokinetics of oseltamivir in non-pregnant and pregnant women.
Beigi, RH; Caritis, SN; Clark, S; Easterling, TR; Han, K; Hankins, GD; Hebert, MF; Pillai, VC; Ren, Z; Venkataramanan, R; Zajicek, A, 2015
)
0.7
" Both non-compartmental and population pharmacokinetic approaches documented approximately 45 (23-62)% increase in clearance (CL/F) of OC during pregnancy."( Population pharmacokinetics of oseltamivir in non-pregnant and pregnant women.
Beigi, RH; Caritis, SN; Clark, S; Easterling, TR; Han, K; Hankins, GD; Hebert, MF; Pillai, VC; Ren, Z; Venkataramanan, R; Zajicek, A, 2015
)
0.7
" Pharmacokinetic data for 24 adults with ESRD were pooled from a single-dose and a multiple-dose study to develop a population pharmacokinetic model using nonlinear mixed-effects modeling."( Investigating clinically adequate concentrations of oseltamivir carboxylate in end-stage renal disease patients undergoing hemodialysis using a population pharmacokinetic approach.
Clinch, B; Gibiansky, L; Kamal, MA; Lien, KY; Rayner, CR; Robson, R; Subramoney, V, 2015
)
0.67
"The aims of the present study were to compare the pharmacokinetics of oseltamivir and its active antiviral metabolite oseltamivir carboxylate in obese and non-obese individuals and to determine the effect of obesity on the pharmacokinetic properties of oseltamivir and oseltamivir carboxylate."( Population pharmacokinetics of oseltamivir and oseltamivir carboxylate in obese and non-obese volunteers.
Chairat, K; Day, NP; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2016
)
0.95
"The population pharmacokinetic properties of oseltamivir and oseltamivir carboxylate were evaluated in 12 obese [body mass index (BMI) ≥30 kg m(-2) ) and 12 non-obese (BMI <30 kg m(-2) ) Thai adult volunteers receiving a standard dose of 75 mg and a double dose of 150 mg in a randomized sequence."( Population pharmacokinetics of oseltamivir and oseltamivir carboxylate in obese and non-obese volunteers.
Chairat, K; Day, NP; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2016
)
0.98
" However, these altered pharmacokinetic properties were small and did not change the overall exposure to oseltamivir carboxylate."( Population pharmacokinetics of oseltamivir and oseltamivir carboxylate in obese and non-obese volunteers.
Chairat, K; Day, NP; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2016
)
0.93
"Organic anion transporters (OATs) are important in the renal secretion, and thus, the clearance, of many drugs; and their functional change can result in pharmacokinetic variability."( Quantitative Prediction of Human Renal Clearance and Drug-Drug Interactions of Organic Anion Transporter Substrates Using In Vitro Transport Data: A Relative Activity Factor Approach.
Feng, B; Litchfield, J; Mathialagan, S; Piotrowski, MA; Tess, DA; Varma, MV, 2017
)
0.46
" In this investigation, PBPK modeling was used to assess the impact of pregnancy on the pharmacokinetic profiles of three medications (metformin, tacrolimus, oseltamivir) using the Simcyp® simulator."( Application of physiologically based pharmacokinetic modeling to predict drug disposition in pregnant populations.
Avvari, S; Gollen, R; Jogiraju, VK; Taft, DR, 2017
)
0.65
" Pharmacokinetic analysis was carried out."( Role of the ABCB1 Drug Transporter Polymorphisms in the Pharmacokinetics of Oseltamivir in Humans: a Preliminary Report.
Cha, YJ; Ghim, JL, 2017
)
0.68
" Pharmacokinetic analyses showed increased clearance and decreased plasma levels compared to healthy volunteers."( Pharmacokinetics of favipiravir during continuous venovenous haemofiltration in a critically ill patient with influenza.
Favié, LM; Meijer, A; Murk, JL; Nijstad, AL; Sikma, MA; van Maarseveen, EM, 2018
)
0.48
" Pharmacokinetic analysis also exhibited similar plasma concentrations of the active drug, oseltamivir carboxylate, metabolised from both OSV-B and OSV-P."( Comparison of anti-influenza virus activity and pharmacokinetics of oseltamivir free base and oseltamivir phosphate.
Bae, MA; Go, YY; Jang, Y; Kim, M; Kim, SS; Ku, KB; Kwon, OS; Shin, D; Shin, JS; Yoon, YS, 2017
)
0.91
" With our continuous interest in developing AM2-S31N inhibitors as oral influenza antivirals, we report here the progress of optimizing the in vitro pharmacokinetic (PK) properties of AM2-S31N inhibitors."( In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
Hau, RK; Hu, Y; Ma, C; Musharrafieh, R; Wang, J; Wang, Y; Xu, S; Zhang, Y, 2018
)
0.48
" Population pharmacokinetic analysis of the baloxavir acid was performed using 8310 plasma concentration data points from 1109 subjects."( Population Pharmacokinetic and Exposure-Response Analyses of Baloxavir Marboxil in Adults and Adolescents Including Patients With Influenza.
Ishibashi, T; Koshimichi, H; Tsuda, Y; Wajima, T, 2019
)
0.51
" Pregnancy had only a modest effect upon the pharmacokinetic parameters of oseltamivir and oseltamivir carboxylate."( Pharmacokinetics of oseltamivir phosphate and oseltamivir carboxylate in non-pregnant and pregnant rhesus monkeys.
Basavarajappa, M; Beland, FA; Fisher, J; Gamboa da Costa, G; Loukotková, L; Lumen, A; Mattison, D; Morris, SM; Roberts, R, 2020
)
1.11
" A physiologically based pharmacokinetic (PBPK) model of the prodrug oseltamivir and its active metabolite, oseltamivir carboxylate (OC), was established and validated to simulate their disposition in adults and predict the exposure in patients with Child-Pugh C cirrhosis (CP-C)."( Simulation of the Pharmacokinetics of Oseltamivir and Its Active Metabolite in Normal Populations and Patients with Hepatic Cirrhosis Using Physiologically Based Pharmacokinetic Modeling.
Chen, Y; Ke, M; Lin, C; Xu, J, 2020
)
1.06
" Serum, nasopharyngeal, and tracheal aspirate pharmacokinetic samples were collected on days 1-60 from MHAA4549A-treated groups."( Pharmacokinetics of the Monoclonal Antibody MHAA4549A Administered in Combination With Oseltamivir in Patients Hospitalized With Severe Influenza A Infection.
Castro, A; Deng, R; Hanley, WD; Horn, P; Kulkarni, P; Lim, JJ; Maia, M; McBride, JM; Newton, E; Peck, MC; She, G; Tavel, JA, 2020
)
0.78
" Virtual BE studies have been conducted using physiologically based pharmacokinetic absorption models (PBPK AMs) to aid the evaluations of generic drug products."( Using a Physiologically Based Pharmacokinetic Absorption Model to Establish Dissolution Bioequivalence Safe Space for Oseltamivir in Adult and Pediatric Populations.
Miao, L; Mousa, YM; Raines, K; Seo, P; Wu, F; Zhao, L, 2020
)
0.77

Compound-Compound Interactions

This study aims to explore the efficacy and safety of Lianhua Qingwen preparations combined with Oseltamivir in the treatment of influenza patients.

ExcerptReferenceRelevance
" In vivo and in vitro studies were conducted to evaluate the renal drug-drug interaction potential of oseltamivir."( The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies.
Barrett, J; Cihlar, T; Hill, G; Ho, ES; Liu, B; Oo, C; Prior, K; Ward, P; Wiltshire, H, 2002
)
0.84
" Probenecid plus oseltamivir 45 mg achieved all the pharmacokinetic parameters expected of oseltamivir alone, but combination with oseltamivir 30 mg and dose interval extension approaches did not."( Population pharmacokinetics of oseltamivir when coadministered with probenecid.
Boak, LM; Chanu, P; Gieschke, R; Jonsson, EN; Rayner, CR, 2008
)
0.97
" Healthy volunteers were randomized to a three-arm, open-label study and given 75 mg oral oseltamivir every 24 h (group 1), 75 mg oseltamivir every 48 h (q48h) combined with 500 mg probenecid four times a day (group 2), or 75 mg oseltamivir q48h combined with 500 mg probenecid twice a day (group 3) for 15 days."( Pharmacokinetics and tolerability of oseltamivir combined with probenecid.
Cunningham, F; Davey, RT; Deyton, LR; Goetz, MB; Holodniy, M; Lee, KK; Lin, ET; Olivo, N; Penzak, SR; Raisch, DW; Straight, TM, 2008
)
0.84
" 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
" Along with the case studies, several hurdles for drug development such as dose selection, frequency of dosing, and duration of the clinical studies, picking the right surrogate(s) for efficacy, evaluation of drug-drug interaction potential with other co-substrates have been discussed in line with the current day requirements for a sound clinical and regulatory strategy."( Is there a place for drug combination strategies using clinical pharmacology attributes?--review of current trends in research.
Srinivas, NR, 2009
)
0.35
" The adverse events related to ribavirin and drug-drug interactions during therapy for hepatitis C are discussed."( Severe anaemia related to oseltamivir during treatment of chronic hepatitis C: a new drug interaction?
Buti, M; Esteban, R; Simón-Talero, M, 2012
)
0.68
" Three dimensional analysis of drug-drug interactions revealed that IFN-λ1 interacted with IFN-β and oseltamivir carboxylate in an additive or synergistic manner, respectively, to inhibit influenza A virus replication in human airway epithelial cells."( In vitro anti-influenza A activity of interferon (IFN)-λ1 combined with IFN-β or oseltamivir carboxylate.
Donnelly, RP; Ilyushina, NA, 2014
)
0.84
" Here, we investigated the antiviral efficacy of the peptidomimetic furin inhibitor MI-701 in combination with oseltamivir carboxylate and ribavirin against the infection of highly pathogenic avian influenza viruses (HPAIV) that are activated by the host protease furin."( Peptidomimetic furin inhibitor MI-701 in combination with oseltamivir and ribavirin efficiently blocks propagation of highly pathogenic avian influenza viruses and delays high level oseltamivir resistance in MDCK cells.
Böttcher-Friebertshäuser, E; Dahms, SO; Garten, W; Hardes, K; Klenk, HD; Lu, Y; Steinmetzer, T; Than, ME, 2015
)
0.87
" This mechanistic static approach was further applied to quantitatively predict renal drug-drug interactions (AFE ∼1."( Quantitative Prediction of Human Renal Clearance and Drug-Drug Interactions of Organic Anion Transporter Substrates Using In Vitro Transport Data: A Relative Activity Factor Approach.
Feng, B; Litchfield, J; Mathialagan, S; Piotrowski, MA; Tess, DA; Varma, MV, 2017
)
0.46
" This study evaluated the therapeutic antiviral effects of PUL-042 against established influenza A pneumonia, when given alone or in combination with oseltamivir."( Combined aerosolized Toll-like receptor ligands are an effective therapeutic agent against influenza pneumonia when co-administered with oseltamivir.
Dickey, BF; Evans, SE; Gilbert, BE; Kirkpatrick, CT; Leiva-Juarez, MM; Markesich, D; Scott, B; Tuvim, MJ, 2018
)
0.88
"To assess correlation of cytokines levels and therapy regimes a relationship of the time course of changes in the cytokines IFN-γ, IFN-α, IL-18, and TNF-α to the treatment option for influenza A (H1N1) pdm09 with umifenovir (Arbidol) 800 mg/day for 5 days (n=50); oseltamivir (Tamiflu) 150 mg/day for 5 days (n=50); umifenovir (Arbidol) 800 mg/day for 5 days in combination with Kagocel 72 mg/day for 2 days."( [Time course of changes in cytokines (IFN-γ, IFN-α, IL-18, TNF-α) in the treatment of moderate influenza A (H1N1) pdm09 (2013-2016) with oseltamivir (Tamiflu) and umifenovir (Arbidol) alone and in combination with Kagocel].
Dmitrenko, KA; Popov, AF; Shchelkanov, MY; Simakova, AI,
)
0.51
" The aim of this study was to assess the drug-drug interaction between baloxavir marboxil and oseltamivir."( Evaluation of Drug-Drug Interaction Potential between Baloxavir Marboxil and Oseltamivir in Healthy Subjects.
Ishibashi, T; Kawaguchi, N; Koshimichi, H; Wajima, T, 2018
)
0.93
"Eighteen healthy adult subjects received three treatments in a crossover fashion: single administration of baloxavir marboxil 40 mg alone, repeated twice-daily administration of oseltamivir at 75 mg for 5 days, or single administration of baloxavir marboxil at 40 mg in combination with repeated twice-daily administration of oseltamivir at 75 mg for 5 days."( Evaluation of Drug-Drug Interaction Potential between Baloxavir Marboxil and Oseltamivir in Healthy Subjects.
Ishibashi, T; Kawaguchi, N; Koshimichi, H; Wajima, T, 2018
)
0.9
"The lack of a clinically meaningful drug-drug interaction between baloxavir marboxil and oseltamivir has been established."( Evaluation of Drug-Drug Interaction Potential between Baloxavir Marboxil and Oseltamivir in Healthy Subjects.
Ishibashi, T; Kawaguchi, N; Koshimichi, H; Wajima, T, 2018
)
0.93
" Here we examined the use of TIZ in combination with oseltamivir, both in vitro and using the ferret model for influenza infection and found that the combination of the two drugs did not provide significant benefit in reducing the emergence or selection of oseltamivir-resistant virus."( Host-targeted nitazoxanide has a high barrier to resistance but does not reduce the emergence or proliferation of oseltamivir-resistant influenza viruses in vitro or in vivo when used in combination with oseltamivir.
Barr, IG; Hurt, AC; Koszalka, P; Mifsud, E; Rossignol, JF; Tilmanis, D, 2020
)
1.02
" The aim of this study was to interpret the clinical efficacy and safety of CPM combined with oseltamivir in the treatment of adult influenza by reviewing all relevant randomized controlled trials, and to provide new ideas and methods for the treatment of influenza."( Clinical Efficacy and Safety of Chinese Patent Medicine Combined with Oseltamivir for the Treatment of Adult Influenza: A Systematic Review and Meta-Analysis.
Duan, N; Li, L; Li, X; Liu, B; Lu, C; Xiong, Y; Zhang, C; Zhang, Y, 2022
)
1.17
"This study aims to explore the efficacy and safety of Lianhua Qingwen preparations combined with Oseltamivir in the treatment of influenza patients."( [Systematic review and Meta-analysis of Lianhua Qingwen preparations combined with Oseltamivir in treatment of influenza].
Guo, YH; Li, B; Li, ZY; Liu, QQ; Yan, YM; Yang, XJ; Zhao, CX; Zhao, GZ, 2022
)
1.16
" Combined with LFD, the limit of detection of RPA-CRISPR/Cas12a-LFD is about 20 copies of target sequence per reaction."( An ultrasensitive, rapid and portable method for screening oseltamivir-resistant virus based on CRISPR/Cas12a combined with immunochromatographic strips.
Fei, C; Gu, F; Liu, J; Liu, Y; Wang, M; Xue, F; Yang, F; Yang, M; Zhang, H; Zhang, L; Zhu, C, 2022
)
0.96

Bioavailability

The goal of this study was to improve the intestinal mucosal cell membrane permeability of the poorly absorbed guanidino analogue of a neuraminidase inhibitor, oseltamivir carboxylate. The results support the feasibility of modified-release formulation development.

ExcerptReferenceRelevance
"GS4071 is a novel potent inhibitor of influenza neuraminidase (Ki < 1 nM) with low (< 5%) oral bioavailability in animals."( Penetration of GS4071, a novel influenza neuraminidase inhibitor, into rat bronchoalveolar lining fluid following oral administration of the prodrug GS4104.
Bidgood, A; Cundy, KC; Eisenberg, EJ, 1997
)
0.3
" Both parent compounds and the prodrug of the guanidino analog exhibited poor oral bioavailability (2 to 4%) and low peak concentrations in plasma (Cmaxs; Cmax <0."( Identification of GS 4104 as an orally bioavailable prodrug of the influenza virus neuraminidase inhibitor GS 4071.
Bischofberger, N; Chen, MS; Cundy, KC; Eisenberg, EJ; Escarpe, PA; Jakeman, KJ; Kim, CU; Lew, W; Li, W; Mendel, DB; Merson, J; Sweet, C; Williams, M; Zhang, L, 1998
)
0.3
" The absolute bioavailability of the active metabolite from orally administered oseltamivir is 80%."( Clinical pharmacokinetics of the prodrug oseltamivir and its active metabolite Ro 64-0802.
He, G; Massarella, J; Ward, P, 1999
)
0.8
" 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
)
0.53
"We have investigated the long-term prophylactic efficacy and safety of oseltamivir phosphate (Ro64-0796), an orally bioavailable prodrug of novel, potent and selective type A and type B influenzavirus neuraminidase inhibitor, when Ro64-0796 was administered orally to the healthy volunteers."( [Efficacy and safety of the selective oral neuraminidase inhibitor oseltamivir for prophylaxis against influenza--placebo-controlled double-blind multicenter phase III trial].
Kashiwagi, S; Kudoh, S; Watanabe, A; Yoshimura, I, 2000
)
0.78
" It is highly bioavailable in capsule and suspension formulations and, after conversion to the active metabolite in the liver, distributes throughout the body, including the upper and lower respiratory tract."( Oseltamivir: a clinical and pharmacological perspective.
Aoki, FY; Doucette, KE, 2001
)
1.75
" The bioavailability (90% confidence intervals) of Ro 64-0802 following administration of oseltamivir together with Maalox suspension vs administration of oseltamivir alone, was 90% (83."( Lack of pharmacokinetic interaction between the oral anti-influenza neuraminidase inhibitor prodrug oseltamivir and antacids.
Barrett, J; Dorr, A; Oo, C; Snell, P, 2002
)
0.75
" The results support the feasibility of modified-release formulation development whilst confirming the high and consistent oral bioavailability of oseltamivir."( Pharmacokinetics and delivery of the anti-influenza prodrug oseltamivir to the small intestine and colon using site-specific delivery capsules.
Barrett, J; Dorr, A; Liu, B; Oo, C; Snell, P; Wilding, I, 2003
)
0.76
" The C-1 ethyl ester prodrugs of the substituted C-4 vinyl analogues gave compounds with excellent oral bioavailability (F > 60%) when dosed in rat."( Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
Carrick, RJ; Gu, YG; Kati, WM; Kempf, DJ; Kempf-Grote, A; Kohlbrenner, WE; Krueger, AC; Laver, WG; Madigan, DL; Maring, CJ; Marsh, KC; Molla, A; Montgomery, DA; Sham, HL; Steffy, KR; Stewart, KD; Stoll, VS; Sun, M; Xu, Y; Zhao, C, 2005
)
0.33
" This review describes the surprising breakthrough findings leading to the development of Tamiflu, a clinically efficacious orally bioavailable drug targeting the active site of influenza neuraminidase (NA)."( Optimization of small molecule drugs binding to highly polar target sites: lessons from the discovery and development of neuraminidase inhibitors.
Graves, BJ; Klumpp, K, 2006
)
0.33
"The bioavailability of oseltamivir phosphate and oseltamivir carboxylate were assessed in healthy volunteers when delivered as a solution of the active pharmaceutical ingredient (API) compared with the commercial capsule formulation."( Active metabolite from Tamiflu solution is bioequivalent to that from capsule delivery in healthy volunteers: a cross-over, randomised, open-label study.
Brewster, M; Dutkowski, R; Robson, R; Smith, JR, 2006
)
0.64
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" 150 mg bid of oseltamivir was well absorbed and converted extensively to OC."( Oseltamivir is adequately absorbed following nasogastric administration to adult patients with severe H5N1 influenza.
Anh, GT; Bien, NM; Binh, NG; Chau, NQ; Crusat, M; Day, N; de Jong, MD; Farrar, JJ; Fox, A; Ha, NH; Hanh, TT; Hien, ND; Horby, P; Lien, TT; Lindegardh, N; Ngoc, NM; Stepniewska, K; Taylor, WR; Thinh, BN; Trung, NV; Wertheim, H; White, NJ, 2008
)
2.14
" The purpose of this study was to compare the bioavailability of two 75 mg oral formulations of oseltamivir: a generic drug, GOP-A-Flu (test, Government Pharmaceutical Organization, Thailand) and Tamiflu (reference, Hoffmann-La Roche Ltd."( A randomized, open-label, 2-period, crossover bioequivalence study of two oral formulations of 75 mg oseltamivir in healthy Thai volunteers.
Chatsiricharoenkul, S; Kongpatanakul, S; Panich, U; Pongnarin, P; Sangvanich, P; Sathirakul, K, 2008
)
0.78
" The low affinity of OC to sediments suggests that presence of sediments would not reduce its bioavailability to microbial degradation."( Environmental fate of the antiviral drug Tamiflu in two aquatic ecosystems.
Accinelli, C; Fick, J; Lindberg, R; Olsen, B; Saccà, ML, 2009
)
0.35
" Case studies discussed in this review include: a) the use of probenecid to block the organic anion renal transport of oseltamivir carboxylate (a key active metabolite of oseltamivir phosphate) to reduce the oral dose of oseltamivir phosphate; b) the use of rifampicin to induce the CYP2C19 enzyme and thereby, promote the formation of a potent active metabolite M8 (nelfinavir hydroxyl-t-butylamide) and achieve sustained blood levels to combat HIV infection along with ritonavir; c) the use of CYP3A4 inhibitors such as ketoconazole, cyclosporin A, ritonavir etc to overcome the extensive presystemic metabolism of docetaxel and enhance the oral bioavailability of docetaxel."( Is there a place for drug combination strategies using clinical pharmacology attributes?--review of current trends in research.
Srinivas, NR, 2009
)
0.56
"The objective of this study was to assess the relative bioavailability of oseltamivir carboxylate (active metabolite) following oral administration of the market suspension, the clinical trial suspension and the market capsule formulations of oseltamivir (prodrug) in healthy subjects."( Oseltamivir oral suspension and capsules are bioequivalent for the active metabolite in healthy adult volunteers.
Barrett, J; Kirkpatrick, C; Lennon, S; Rayner, C, 2009
)
2.03
"Oseltamivir was well absorbed enterically in critically ill patients admitted to the ICU with suspected or confirmed pandemic (H1N1) influenza."( Enteric absorption and pharmacokinetics of oseltamivir in critically ill patients with pandemic (H1N1) influenza.
Ahern, S; Ariano, RE; Kanji, S; Kumar, A; Pisipati, A; Rello, J; Sitar, DS; Zarychanski, R; Zelenitsky, SA, 2010
)
2.07
" Oseltamivir carboxylate has high bioavailability and penetrates sites of infection at concentrations that are sufficient to inhibit viral replication."( Pharmacokinetics of oseltamivir: an oral antiviral for the treatment and prophylaxis of influenza in diverse populations.
Davies, BE, 2010
)
1.59
" According to the currently available literature, the pharmacokinetics of oseltamivir carboxylate after oral administration of oseltamivir are characterized by mean ± SD bioavailability of 79 ± 12%, apparent clearance of 25."( Oseltamivir in seasonal, avian H5N1 and pandemic 2009 A/H1N1 influenza: pharmacokinetic and pharmacodynamic characteristics.
Aouri, M; Buclin, T; Decosterd, LA; Ivanyuk, A; Meylan, P; Widmer, N, 2010
)
2.03
" This drug is available in oral solid and liquid formulations, has excellent peroral bioavailability in adults, and generally has a very favorable safety profile."( Pharmacologic considerations for oseltamivir disposition: focus on the neonate and young infant.
Abdel-Rahman, SM; Kearns, GL; Newland, JG, 2011
)
0.65
" 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
)
0.73
" Guanidine oseltamivir carboxylate (GOCarb) is a highly active polar antiviral agent with insufficient oral bioavailability (4%) to be an effective therapeutic agent."( Increasing oral absorption of polar neuraminidase inhibitors: a prodrug transporter approach applied to oseltamivir analogue.
Amidon, GL; Dahan, A; Gupta, D; Hilfinger, J; Lee, KD; Tsume, Y; Varghese Gupta, S, 2013
)
0.99
" 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
)
0.85
" 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
)
0.63
" 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 goal of this study was to improve the intestinal mucosal cell membrane permeability of the poorly absorbed guanidino analogue of a neuraminidase inhibitor, oseltamivir carboxylate (GOC) using a carrier-mediated strategy."( Carrier-Mediated Prodrug Uptake to Improve the Oral Bioavailability of Polar Drugs: An Application to an Oseltamivir Analogue.
Amidon, GL; Gose, T; Hilfinger, J; Incecayir, T; Lipka, E; Nakanishi, T; Sun, J; Tamai, I; Tsume, Y; Xu, H, 2016
)
0.84
" Transport experiments using Caco-2 cell monolayers often lead to misestimation of the intestinal absorption of prodrugs because of this difference, as prodrugs designed to increase the bioavailability of parent drugs are made to be resistant to hCE2 in the intestine, so that they can be hydrolyzed by hCE1 in the liver."( Establishment and Characterization of a Novel Caco-2 Subclone with a Similar Low Expression Level of Human Carboxylesterase 1 to Human Small Intestine.
Imai, T; Kurokawa, K; Nishiyama, H; Ohura, K; Saco, S, 2016
)
0.43
" 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
)
0.74
"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
" This comprehensive review covers a range of OS analogs shown to be effective against influenza virus, comparing different types of substituent group that contribute to the activity and bioavailability of these compounds."( Oseltamivir analogs with potent anti-influenza virus activity.
Durvasula, R; Goicoechea, S; Kempaiah, P; Kumar, S; Pearce, CM; Rathi, B, 2020
)
2

Dosage Studied

Oseltamivir had no physiologically relevant effect on body temperature, but induced a short-lived and small dose-independent decrease in temperature in all active treatment groups at 1 hr after dosing only. The pharmacokinetic profile of the active metabolite is linear and dose-proportional, with less th th.

ExcerptRelevanceReference
"The degradation profile indicates that development of solution or solid dosage from of GS-4104 with adequate shelf-life stability at room temperature is feasible."( Biexponential decomposition of a neuraminidase inhibitor prodrug (GS-4104) in aqueous solution.
Dahl, TC; Lee, WA; Oliyai, R; Swaminathan, S; Wang, KY; Yuan, LC, 1998
)
0.3
" Transient mild to moderate nausea after dosing was observed in 15 (17%) of 88 oseltamivir and 2 (7%) of 29 placebo recipients (95% confidence interval for difference, -11% to 68%), which was largely prevented by ingestion with food."( Use of the oral neuraminidase inhibitor oseltamivir in experimental human influenza: randomized controlled trials for prevention and treatment.
Betts, RF; Fritz, RS; Hayden, FG; Kinnersley, N; Lobo, M; Miller, M; Mills, RG; Straus, SE; Treanor, JJ; Ward, P, 1999
)
0.8
" The pharmacokinetic profile of the active metabolite is linear and dose-proportional, with less than 2-fold accumulation over a dosage range of oseltamivir 50 to 500 mg twice daily."( Clinical pharmacokinetics of the prodrug oseltamivir and its active metabolite Ro 64-0802.
He, G; Massarella, J; Ward, P, 1999
)
0.77
" This metabolite was purified from urine of rats dosed orally with oseltamivir and was identified by liquid chromatography-mass spectrometry and NMR as the (R)-omega-carboxylic acid metabolite of oseltamivir."( Metabolism of the influenza neuraminidase inhibitor prodrug oseltamivir in the rat.
Bidgood, AM; Cundy, KC; Lew, W; Lynch, G; Sweeny, DJ; Wang, KY, 2000
)
0.79
" 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
)
0.54
" A 75 mg capsule may be a viable dosage formulation in children (e."( Pharmacokinetics and dosage recommendations for an oseltamivir oral suspension for the treatment of influenza in children.
Barrett, J; Dorr, A; Dutkowski, R; Hill, G; Mann, J; Oo, C; Ward, P, 2001
)
0.56
"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
" Although amantadine has a lower acquisition cost than oseltamivir, it is associated with more adverse events, lower efficacy, and individualized dosing requirements, leading to higher overall costs and more influenza-like illness cases than oseltamivir."( Economic evaluation of oseltamivir phosphate for postexposure prophylaxis of influenza in long-term care facilities.
Bowles, SK; McGeer, A; Oh, PI; Risebrough, NA; Simor, AE, 2005
)
0.89
" Secondary endpoints included the area under the symptom score-hour curve, the proportion of patients with asthma exacerbations and changes in forced expiratory volume at 1 second during the dosing period."( Oral oseltamivir improves pulmonary function and reduces exacerbation frequency for influenza-infected children with asthma.
Dutkowski, R; Ferrero, F; Garcia, ML; Johnston, SL, 2005
)
0.84
" The C-1 ethyl ester prodrugs of the substituted C-4 vinyl analogues gave compounds with excellent oral bioavailability (F > 60%) when dosed in rat."( Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
Carrick, RJ; Gu, YG; Kati, WM; Kempf, DJ; Kempf-Grote, A; Kohlbrenner, WE; Krueger, AC; Laver, WG; Madigan, DL; Maring, CJ; Marsh, KC; Molla, A; Montgomery, DA; Sham, HL; Steffy, KR; Stewart, KD; Stoll, VS; Sun, M; Xu, Y; Zhao, C, 2005
)
0.33
" However, dosing recommendations are not available for treatment or prophylaxis of influenza in these patients."( The pharmacokinetics and tolerability of oseltamivir suspension in patients on haemodialysis and continuous ambulatory peritoneal dialysis.
Brewster, M; Buttimore, A; Lynn, K; Robson, R; Ward, P, 2006
)
0.6
"In HD patients, the C(max) for oseltamivir carboxylate after single and repeated dosing were 943 and 1120 ng/ml, respectively."( The pharmacokinetics and tolerability of oseltamivir suspension in patients on haemodialysis and continuous ambulatory peritoneal dialysis.
Brewster, M; Buttimore, A; Lynn, K; Robson, R; Ward, P, 2006
)
0.89
"5 and 5 mg/kg/day; ribavirin at 5, 10 and 20 mg/kg/day) certain dosage combinations were superior to either compound used alone as assessed by decreased mortality, lung virus titre, lung score and lung weight parameters."( Activities of oseltamivir and ribavirin used alone and in combination against infections in mice with recent isolates of influenza A (H1N1) and B viruses.
Bailey, KW; Sidwell, RW; Smee, DF; Wong, MH, 2006
)
0.69
" 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
" Higher incidences of resistance were observed in two small Japanese studies, in which children received a different dosing schedule from their Western counterparts."( Influenza virus susceptibility and resistance to oseltamivir.
Aoki, FY; Boivin, G; Roberts, N, 2007
)
0.59
" In addition, increased dosing requirements may affect compliance and attainment of optimal oseltamivir exposure, potentially facilitating the emergence of viral strains with reduced susceptibility to oseltamivir."( Population pharmacokinetics of oseltamivir when coadministered with probenecid.
Boak, LM; Chanu, P; Gieschke, R; Jonsson, EN; Rayner, CR, 2008
)
0.85
" In the event of an influenza pandemic, oseltamivir supplies may be limited; thus, alternative dosing strategies for oseltamivir prophylaxis should be explored."( Pharmacokinetics and tolerability of oseltamivir combined with probenecid.
Cunningham, F; Davey, RT; Deyton, LR; Goetz, MB; Holodniy, M; Lee, KK; Lin, ET; Olivo, N; Penzak, SR; Raisch, DW; Straight, TM, 2008
)
0.89
" Explanations for this include late institution of treatment, suboptimal dosing and drug delivery, and development of drug resistance, the latter of which may not be a rare event."( H5N1 transmission and disease: observations from the frontlines.
de Jong, MD, 2008
)
0.35
" 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
)
0.58
" Blood samples were collected before dosing and at various time points up to 48 hours after dosing and analyzed for plasma oseltamivir and oseltamivir carboxylate concentrations."( A randomized, open-label, 2-period, crossover bioequivalence study of two oral formulations of 75 mg oseltamivir in healthy Thai volunteers.
Chatsiricharoenkul, S; Kongpatanakul, S; Panich, U; Pongnarin, P; Sangvanich, P; Sathirakul, K, 2008
)
0.77
" Emergence of drug-resistant influenza viruses after treatment has been reported, particularly in children in Japan, where the dosing schedule is different from that used throughout the rest of the world."( Neuraminidase inhibitor resistance after oseltamivir treatment of acute influenza A and B in children.
Bermingham, A; Democratis, J; Ellis, J; Lackenby, A; McNally, T; Nicholson, K; Pareek, M; Smith, J; Stephenson, I; Zambon, M, 2009
)
0.62
" In this Debate, Nicholas White argues that such dosing is inadequate, Robert Webster and Elena Govorkova say that combination antiviral therapy should be used, and Tim Uyeki reminds us that clinical care of patients with H5N1 entails much more than antiviral treatment."( What is the optimal therapy for patients with H5N1 influenza?
Govorkova, EA; Uyeki, TM; Webster, RG; White, NJ, 2009
)
0.35
" Dose-response curves were generated for all drug combinations, and the degree of drug interaction was quantified using a model that calculates the synergy (or antagonism) between the drugs in double and triple combinations."( Triple combination of oseltamivir, amantadine, and ribavirin displays synergistic activity against multiple influenza virus strains in vitro.
Driebe, EM; Engelthaler, DM; Hoopes, JD; Keim, PS; Le, MH; Nguyen, JT; Prichard, MN; Smee, DF; Spence, RP; Went, GT, 2009
)
0.67
" Dosing of oseltamivir was variable, illustrating the need for pharmacokinetic data in this younger population."( Safety of oseltamivir compared with the adamantanes in children less than 12 months of age.
Abughali, N; Abzug, MJ; Bradley, JS; Cloud, GA; Englund, J; Griffin, J; Guzman-Cottrill, J; Jacobs, RF; Jester, P; Kimberlin, DW; Lang, D; Leach, C; Ramilo, O; Robinson, J; Romero, JR; Shalabi, M; Shelton, M; Storch, G; Wade, KC; Whitley, RJ, 2010
)
1.15
" A standard-free electrospray ionization mass spectrometry method is used to directly determine the dosage in the prescription and over-the-counter drugs Tamiflu, Sudafed, and Dramamine."( Direct standard-free quantitation of Tamiflu and other pharmaceutical tablets using clustering agents with electrospray ionization mass spectrometry.
Flick, TG; Leib, RD; Williams, ER, 2010
)
0.36
" The dosage of 75 mg twice daily achieved plasma levels that were comparable to those in ambulatory patients and were far in excess of concentrations required to maximally inhibit neuraminidase activity of the virus."( Enteric absorption and pharmacokinetics of oseltamivir in critically ill patients with pandemic (H1N1) influenza.
Ahern, S; Ariano, RE; Kanji, S; Kumar, A; Pisipati, A; Rello, J; Sitar, DS; Zarychanski, R; Zelenitsky, SA, 2010
)
0.62
" Outcomes are influenced by the virulence of the viral strain, dosage regimen and treatment delay; it is also critical for the compound to act systemically."( Oseltamivir in human avian influenza infection.
Smith, JR, 2010
)
1.8
" Treatment of infected children > or =1 year and adults of all ages may decrease the severity and duration of the symptoms of infection, while prophylactic dosing can prevent their onset."( Pharmacokinetics of oseltamivir: an oral antiviral for the treatment and prophylaxis of influenza in diverse populations.
Davies, BE, 2010
)
0.68
" The age-specific oseltamivir dosage was doubled to counter expected decreased plasma drug concentrations due to increased volume of distribution on ECMO support."( Plasma concentrations of oseltamivir and oseltamivir carboxylate in critically ill children on extracorporeal membrane oxygenation support.
Ahsman, MJ; de Hoog, M; Fraaij, PL; Osterhaus, AD; Tibboel, D; Wildschut, ED, 2010
)
1
" These increased plasma concentrations related to the increased oseltamivir dosage and decreased kidney function."( Plasma concentrations of oseltamivir and oseltamivir carboxylate in critically ill children on extracorporeal membrane oxygenation support.
Ahsman, MJ; de Hoog, M; Fraaij, PL; Osterhaus, AD; Tibboel, D; Wildschut, ED, 2010
)
0.9
" No data exist on the dosing of oseltamivir in premature babies."( Oseltamivir dosing for influenza infection in premature neonates.
Acosta, EP; Gal, P; Jester, P; Kimberlin, DW; Wade, J; Whitley, RJ; Wimmer, J, 2010
)
2.09
" 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
)
0.65
" The apparent clearance is highly correlated with renal function, hence the dosage needs to be adjusted in proportion to the glomerular filtration rate."( Oseltamivir in seasonal, avian H5N1 and pandemic 2009 A/H1N1 influenza: pharmacokinetic and pharmacodynamic characteristics.
Aouri, M; Buclin, T; Decosterd, LA; Ivanyuk, A; Meylan, P; Widmer, N, 2010
)
1.8
" In this study, we exposed an aerobic granular sludge sequencing batch reactor, operated for enhanced biological phosphorus removal (EBPR), to a simulated influenza-pandemic dosing of antibiotics and antivirals for 8 weeks."( Pandemic pharmaceutical dosing effects on wastewater treatment: no adaptation of activated sludge bacteria to degrade the antiviral drug oseltamivir (Tamiflu®) and loss of nutrient removal performance.
Barr, JJ; Bond, PL; Singer, AC; Slater, FR; Turner, S, 2011
)
0.57
" Given that recent in vitro data support the importance of a target exposure-response profile for the active metabolite of oseltamivir and that many processes known to modulate drug disposition have a developmental basis, understanding the potential impact of age on oseltamivir disposition becomes crucial in the development of age-appropriate dosing regimens for the drug."( Pharmacologic considerations for oseltamivir disposition: focus on the neonate and young infant.
Abdel-Rahman, SM; Kearns, GL; Newland, JG, 2011
)
0.86
" In light of the high incidence of H1N1 infections in renal replacement therapy patients in Brunei Darussalam, an Oseltamivir (Tamiflu) prophylactic dosing regimen of 75 mg every 5 days for renal replacement therapy patients was initiated by the Ministry of Health in August 2009."( Side effects of oseltamivir in end-stage renal failure patients.
Choo, D; Chowdhury, S; Hossain, M; Liew, P; Tan, J, 2011
)
0.93
" These results, together with no incidence of H1N1 cases in the sample participants, showed that the dosing regimen of 75 mg every 5 days in both haemodialysis and continuous ambulatory peritoneal dialysis patients is both tolerable and effective and should be considered for future prophylactic regimes."( Side effects of oseltamivir in end-stage renal failure patients.
Choo, D; Chowdhury, S; Hossain, M; Liew, P; Tan, J, 2011
)
0.72
"A total of 11 neonates received twice daily dosing and 21 neonates received once daily dosing (12 to 25 mg per dose) for treatment and prophylaxis of influenza, respectively."( Oseltamivir treatment and prophylaxis in a neonatal intensive care unit during a 2009 H1N1 influenza outbreak.
Akan, D; Pannaraj, PS; Tam, B, 2011
)
1.81
" More studies are needed to determine optimal dosing for treatment and prophylaxis in this vulnerable age group."( Oseltamivir treatment and prophylaxis in a neonatal intensive care unit during a 2009 H1N1 influenza outbreak.
Akan, D; Pannaraj, PS; Tam, B, 2011
)
1.81
" 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
)
0.82
"The post-neonatal surge in CES1 expression ensures the hydrolytic capacity to be gained rapidly after birth in infants, but the larger variability during this period suggests that caution should be exercised on the extrapolated dosing regimens of ester drugs from other age groups."( Surge in expression of carboxylesterase 1 during the post-neonatal stage enables a rapid gain of the capacity to activate the anti-influenza prodrug oseltamivir.
Davies, BE; Prinssen, EP; Shi, D; Yan, B; Yang, D, 2011
)
0.57
" Increasing the dose and/or dosing frequency of oseltamivir during pregnancy may be necessary to achieve comparable exposure in pregnant and nonpregnant women."( Pharmacokinetics of oseltamivir among pregnant and nonpregnant women.
Beigi, RH; Caritis, SN; Clark, S; Easterling, T; Han, K; Hankins, GD; Hebert, MF; Mattison, DR; Ren, Z; Venkataramanan, R; Zajicek, A, 2011
)
0.95
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
"To study the effects of pre- and post-infection dosing with OS on viral replication and inflammation in a mouse model of non-lethal influenza infection."( Oseltamivir treatment of mice before or after mild influenza infection reduced cellular and cytokine inflammation in the lung.
Anderson, GP; Gualano, RC; Jones, JE; Wong, ZX, 2011
)
1.81
"Pre-infection dosing of OS reduced total cells, neutrophils and macrophages in BALF."( Oseltamivir treatment of mice before or after mild influenza infection reduced cellular and cytokine inflammation in the lung.
Anderson, GP; Gualano, RC; Jones, JE; Wong, ZX, 2011
)
1.81
"Detailed pharmacokinetics to guide oseltamivir (Tamiflu®) dosing in morbidly obese patients is lacking."( Oseltamivir pharmacokinetics in morbid obesity (OPTIMO trial).
Goralski, KB; Hatchette, TF; Johnston, BL; McNeil, SA; Slayter, KL; Thorne-Humphrey, LM, 2011
)
2.09
" Finally, exposures after intravenous dosing in neonates were predicted."( Development of a physiologically based model for oseltamivir and simulation of pharmacokinetics in neonates and infants.
Davies, B; Hoffmann, G; Koerner, A; Lave, T; Parrott, N; Prinssen, E; Singer, T; Theogaraj, E, 2011
)
0.62
" For adult humans, simulated and observed data after both intravenous and oral dosing showed good agreement and although the data are currently limited, simulations in 1-year-olds and neonates are in reasonable agreement with published results for oral doses."( Development of a physiologically based model for oseltamivir and simulation of pharmacokinetics in neonates and infants.
Davies, B; Hoffmann, G; Koerner, A; Lave, T; Parrott, N; Prinssen, E; Singer, T; Theogaraj, E, 2011
)
0.62
" Given the poor outcomes observed among adult obese patients with H1N1, the dosing of antiviral agents in this population has been questioned, and use of twice the standard oseltamivir dose has been suggested."( Oseltamivir and oseltamivir carboxylate pharmacokinetics in obese adults: dose modification for weight is not necessary.
Lodise, TP; Pai, MP, 2011
)
2.01
"Peramivir, an intravenous investigational neuraminidase inhibitor with activity against influenza viruses, has limited data for dosing in the setting of CVVH."( Pharmacokinetic assessment of peramivir in a hospitalized adult undergoing continuous venovenous hemofiltration.
Ghossein, C; Griffith, MM; Hollister, AS; Ison, MG; Scheetz, MH, 2011
)
0.37
" The dosage and duration of oseltamivir treatment were similar whether the INR values increased or not."( Effect of oseltamivir on bleeding risk associated with warfarin therapy: a retrospective review.
Cho, SH; Hong, KS; Jung, JW; Kang, HR; Kwon, JW; Lee, SH; Yu, KS, 2012
)
1.08
" Oseltamivir had no physiologically relevant effect on body temperature, but induced a short-lived and small dose-independent decrease in temperature in all active treatment groups at 1 hr after dosing only."( Absence of central nervous system and hypothermic effects after single oral administration of high doses of oseltamivir in the rat.
Bansod, S; Bellot, M; Breidenbach, A; Donner, B; Freichel, C; Gand, L; Gatti, S; Hoffmann, G; Körner, A; Prinssen, EP; Singer, T; Weiser, T, 2012
)
1.5
" 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
" Based on these results, we recommend that oseltamivir dosage should be decreased and plasma levels of OC be monitored in patients receiving CVVHDF because of acute kidney injury."( Impact of extracorporeal membrane oxygenation and continuous venovenous hemodiafiltration on the pharmacokinetics of oseltamivir carboxylate in critically ill patients with pandemic (H1N1) influenza.
Antignac, M; Combes, A; Corvol, E; Farinotti, R; Fernandez, C; Lemaitre, F; Luyt, CE; Nieszkowska, A; Roullet-Renoleau, F; Zahr, N, 2012
)
0.85
" This method is now applied for the determination of both compounds in specific patient populations to evaluate current dosing guidelines."( Quantitative determination of oseltamivir and oseltamivir carboxylate in human fluoride EDTA plasma including the ex vivo stability using high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry.
Beijnen, JH; Huitema, AD; Kromdijk, W; Rosing, H; van den Broek, MP, 2012
)
0.67
" pastoris expressing human, mouse, and rat peptide transporter 1 (PEPT1), in which uptake was examined as a function of time, concentration, potential inhibitors, and the dose-response inhibition of GlySar by oseltamivir."( Species-dependent uptake of glycylsarcosine but not oseltamivir in Pichia pastoris expressing the rat, mouse, and human intestinal peptide transporter PEPT1.
Chen, X; Hu, Y; Smith, DE, 2012
)
0.82
" In humans, oral dosing after a high-fat meal resulted in a statistically significant but moderate lower exposure than after an overnight fasting."( Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
Belli, S; Funk, C; Heinig, K; Hoffmann, G; Lazic, SE; Otteneder, MB; Poirier, A; Portmann, R; Prinssen, E; Rayner, CR; Schuler, F; Singer, T; Smith, DE, 2012
)
0.63
" At higher dosage (0."( Prophylactic and therapeutic combination effects of rimantadine and oseltamivir against influenza virus A (H3N2) infection in mice.
Galabov, AS; Gegova, G; Simeonova, L, 2012
)
0.61
" To examine the clinical effect of peramivir, the time from dosing to defervescence (body temperature <37."( [Clinical efficiency in children treated with intravenous drip infusion of peramivir].
Sakata, H, 2011
)
0.37
"Liver, kidney, or liver-kidney transplant or allogeneic HSCT recipients aged ≥1 year were randomized to oseltamivir (75 mg once daily for those ≥13 years or weight-based dosing for children 1-12 years) or placebo for 12 weeks during periods of local influenza circulation."( Efficacy and safety of oral oseltamivir for influenza prophylaxis in transplant recipients.
Dutkowski, R; Ison, MG; Kriván, G; Nist, A; Shapira, MY; Szakaly, P, 2012
)
0.89
" Urine was collected throughout the 12-hour dosing interval."( Pharmacokinetics of oseltamivir and oseltamivir carboxylate in critically ill patients receiving continuous venovenous hemodialysis and/or extracorporeal membrane oxygenation.
Eyler, RF; Heung, M; Mueller, BA; Napolitano, LM; Park, PK; Pleva, M; Sowinski, KM, 2012
)
0.7
" The median maximum plasma concentration and area under the plasma concentration-time curve for the 12-hour dosing interval (AUC(0-12) ) for the remaining 12 patients were 83."( Pharmacokinetics of oseltamivir and oseltamivir carboxylate in critically ill patients receiving continuous venovenous hemodialysis and/or extracorporeal membrane oxygenation.
Eyler, RF; Heung, M; Mueller, BA; Napolitano, LM; Park, PK; Pleva, M; Sowinski, KM, 2012
)
0.7
"Although the optimal pharmacokinetic-pharmacodynamic targets for oseltamivir carboxylate remain unclear, in the patients receiving CVVHD with or without ECMO, a regimen of oseltamivir 150 mg every 12 hours yielded a median oseltamivir carboxylate AUC(0-12) considerably higher than would be expected in non-critically ill patients receiving the same dosage regimen."( Pharmacokinetics of oseltamivir and oseltamivir carboxylate in critically ill patients receiving continuous venovenous hemodialysis and/or extracorporeal membrane oxygenation.
Eyler, RF; Heung, M; Mueller, BA; Napolitano, LM; Park, PK; Pleva, M; Sowinski, KM, 2012
)
0.94
" Dosage adjustment for ECMO, per se, appears not to be necessary; however, doses should be reduced in patients with renal dysfunction."( Oseltamivir pharmacokinetics in critically ill adults receiving extracorporeal membrane oxygenation support.
Harvey, C; Kidy, Z; Mulla, H; Peek, GJ; Ramaiah, R; Westrope, C, 2013
)
1.83
" Dosing history, plasma drug concentrations, and demographic information were pooled from 13 clinical trials providing data for 390 healthy and infected subjects ranging in age from 1 to 78 years and given oseltamivir doses of 20 to 1,000 mg."( Population pharmacokinetics of oseltamivir: pediatrics through geriatrics.
Ambrose, PG; Bhavnani, SM; Bulik, CC; Forrest, A; Kamal, MA; Rayner, CR; Reynolds, DK; Smith, PF; Subramoney, V; Van Wart, SA, 2013
)
0.86
" These results provide the first demonstration of exposure-response relationships for efficacy for oseltamivir against influenza and suggest that OC exposures beyond those achieved with the approved oseltamivir dosing regimen will provide enhanced efficacy."( Pharmacokinetic-pharmacodynamic determinants of oseltamivir efficacy using data from phase 2 inoculation studies.
Ambrose, PG; Bhavnani, SM; Bulik, CC; Forrest, A; Hammel, JP; Kamal, MA; Rayner, CR; Reynolds, DK; Smith, PF; Toovey, S; Van Wart, SA, 2013
)
0.86
" Since influenza mortality is highest in neonates and infants, optimal dosing of oseltamivir in this high risk population is of utmost public health concern."( Oseltamivir pharmacology in young children: a commentary.
Kamal, MA, 2013
)
2.06
" This approach is often best suited to situations where dose-response relationships need to be elucidated and where randomisation is not feasible."( Pharmacokinetics and pharmacodynamics of oseltamivir in neonates, infants and children.
Lutsar, I; Standing, JF; Tsolia, M, 2013
)
0.66
" To sum up, dry powders formulation of liposome-encapsulated OP for inhalation was suitable for pulmonary administration, which offering the opportunity to reduce dosing frequency."( Development and evaluation of a dry powder formulation of liposome-encapsulated oseltamivir phosphate for inhalation.
Jiang, L; Liu, J; Lu, X; Tang, Y; Xi, X; Zhang, H; Zhu, J, 2015
)
0.64
" Drug dose-response curves confirmed complete drug resistance to oseltamivir, partial sensitivity to peramivir, and retained susceptibility to zanamivir and favipiravir against the A/Hong Kong/2369/2009 virus."( In vitro activity of favipiravir and neuraminidase inhibitor combinations against oseltamivir-sensitive and oseltamivir-resistant pandemic influenza A (H1N1) virus.
Barnard, DL; Furuta, Y; Hurst, BL; Smee, DF; Tarbet, EB; Vollmer, AH, 2014
)
0.87
" Standard dosing is appropriate for obese subjects."( Pharmacokinetics of orally administered oseltamivir in healthy obese and nonobese Thai subjects.
Charunwattana, P; Day, NP; Hanpithakpong, W; Jittamala, P; Lawpoolsri, S; Lindegardh, N; Panapipat, S; Pukrittayakamee, S; Tarning, J; Taylor, WR; White, NJ, 2014
)
0.67
" The production of inflammatory cytokines/chemokines was also significantly suppressed by multiple dosing of peramivir compared with oseltamivir."( The effect of intravenous peramivir, compared with oral oseltamivir, on the outcome of post-influenza pneumococcal pneumonia in mice.
Homma, T; Imamura, Y; Iwanaga, N; Izumikawa, K; Kajihara, T; Kakeya, H; Kitano, M; Kohno, S; Kurihara, S; Miyazaki, T; Nakamura, S; Seki, M; Tanaka, A; Yanagihara, K, 2015
)
0.87
" Changes in maternal physiology and metabolic processes during pregnancy effect on PK and show that standard adult dosing is likely to be incorrect during pregnancy."( [Peculiarities and clinical significance of drug pharmacokinetics and pharmacodynamics during pregnancy].
Lutsevich, KA; Reshet'ko, OV; Sanina, II, 2014
)
0.4
" Until recently, few data were available with which to optimize oseltamivir dosing in this high-risk population."( The posology of oseltamivir in infants with influenza infection using a population pharmacokinetic approach.
Acosta, EP; Ampofo, K; Clinch, B; Gibiansky, L; Jester, P; Kamal, MA; Kimberlin, DW; Niranjan, V; Rath, B; Rayner, CR; Sánchez, PJ; Whitley, R, 2014
)
0.99
" Clinical resolution did not differ by dosing regimen (P=0."( A randomized study of standard versus double dose oseltamivir for treating influenza in the community.
Booy, R; Dixit, R; Dwyer, D; Hay, P; Heron, L; Khandaker, G; McPhie, K; Rashid, H; Taylor, J, 2015
)
0.67
"Published evidence regarding the use of the antiinfluenza agent oseltamivir outside of the standard dosing recommendations is reviewed."( Influenza treatment with oseltamivir outside of labeled recommendations.
Blair, M; McQuade, B, 2015
)
0.96
"Oseltamivir is a neuraminidase inhibitor indicated for the treatment of uncomplicated influenza in patients two weeks of age or older who have been symptomatic for no more than two days; the recommended dosage is 75 mg twice daily by mouth for five days."( Influenza treatment with oseltamivir outside of labeled recommendations.
Blair, M; McQuade, B, 2015
)
2.16
" 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
" dosing regimens for treatment of influenza in patients with normal renal function and with various degrees of renal impairment."( Population pharmacokinetic analysis of oseltamivir and oseltamivir carboxylate following intravenous and oral administration to patients with and without renal impairment.
Brennan, BJ; Gibiansky, L; Giraudon, M; Kamal, MA; Rayner, CR; Robson, R; Subramoney, V, 2015
)
0.69
" More information is needed on oseltamivir safety at different dosing levels in this vulnerable age group."( Safety, virology and pharmacokinetics of oseltamivir in infants with laboratory-confirmed influenza: a Phase I/II, prospective, open-label, multicentre clinical trial.
Brzostek, J; Chappey, C; Clinch, B; Guillén, S; Niranjan, V; Rath, BA; Rayner, CR, 2015
)
0.97
" The current study supports the adoption of a universal dosing recommendation for infants."( Safety, virology and pharmacokinetics of oseltamivir in infants with laboratory-confirmed influenza: a Phase I/II, prospective, open-label, multicentre clinical trial.
Brzostek, J; Chappey, C; Clinch, B; Guillén, S; Niranjan, V; Rath, BA; Rayner, CR, 2015
)
0.68
" Seven patients switched from IV to oral dosing before the 10th dose."( Pharmacokinetics and safety of intravenous oseltamivir in infants and children in open-label studies.
Anderson, EJ; Clinch, B; Deville, JG; Kamal, MA; Muñoz, FM, 2015
)
0.68
" The serum level determination of active metabolite Ro 64-0802 determined at 154 h after final dosing of oseltamivir was higher than the expected value, suggesting delayed elimination of Ro 64-0802."( Analysis of a child who developed abnormal neuropsychiatric symptoms after administration of oseltamivir: a case report.
Hosokawa, M; Kashii, H; Kubota, M; Morimoto, K; Nagai, A; Nagaoka, K; Ogihara, T; Takahashi, Y, 2015
)
0.85
"End-stage renal disease (ESRD) patients receiving hemodialysis (HD) are at heightened risk for influenza, but the optimal oseltamivir dosage regimen for treating or preventing influenza in this high-risk population is still uncertain."( Investigating clinically adequate concentrations of oseltamivir carboxylate in end-stage renal disease patients undergoing hemodialysis using a population pharmacokinetic approach.
Clinch, B; Gibiansky, L; Kamal, MA; Lien, KY; Rayner, CR; Robson, R; Subramoney, V, 2015
)
0.88
" Orally administered SA-2 effectively protected mice infected with lethal doses of H1N1 or oseltamivir-resistant strain H1N1-H275Y, conferring 70% or 50% survival at a dosage of 100 mg/kg/d, reducing body weight loss, alleviating the influenza-induced acute lung injury, and reducing lung virus titer."( Antiviral activity of SA-2 against influenza A virus in vitro/vivo and its inhibition of RNA polymerase.
Dou, J; Jin, J; Li, M; Wang, D; Wang, H; Xu, J; Yu, J; Zhou, C, 2016
)
0.65
" Inadequate dosing increases the risk of treatment failure and drug resistance, especially in severely ill patients with elevated virus loads."( Pharmacokinetics of Oral and Intravenous Oseltamivir Treatment of Severe Influenza B Virus Infection Requiring Organ Replacement Therapy.
Amann, V; Berger, F; Chen, X; de Zwart, M; Duwe, S; Fraaij, P; Francis, RC; Heider, A; Karsch, K; Miera, O; Obermeier, P; Osterhaus, A; Peters, B; Rath, B; Schweiger, B, 2017
)
0.72
"Patient #1, a 9-year-old female with severe influenza B virus infection, biventricular assist device, and continuous veno-venous hemodiafiltration, received 75 mg oral oseltamivir twice-daily for 2 days, then intravenous oseltamivir with one-time renoprotective dosing (40 mg), followed by regular intravenous administration of 100 mg twice-daily."( Pharmacokinetics of Oral and Intravenous Oseltamivir Treatment of Severe Influenza B Virus Infection Requiring Organ Replacement Therapy.
Amann, V; Berger, F; Chen, X; de Zwart, M; Duwe, S; Fraaij, P; Francis, RC; Heider, A; Karsch, K; Miera, O; Obermeier, P; Osterhaus, A; Peters, B; Rath, B; Schweiger, B, 2017
)
0.92
" Evidence-based pediatric dosing recommendations and effective intravenous antiviral treatment modalities are needed for intensive care patients with life-threatening influenza disease."( Pharmacokinetics of Oral and Intravenous Oseltamivir Treatment of Severe Influenza B Virus Infection Requiring Organ Replacement Therapy.
Amann, V; Berger, F; Chen, X; de Zwart, M; Duwe, S; Fraaij, P; Francis, RC; Heider, A; Karsch, K; Miera, O; Obermeier, P; Osterhaus, A; Peters, B; Rath, B; Schweiger, B, 2017
)
0.72
"Availability of lower-dose oseltamivir capsules, an increased pharmacokinetic database, and a desire to align drug exposure across the spectrum of renal function prompted reassessment of oral dosing in patients with renal impairment."( Identification of new oral dosing regimens for the neuraminidase inhibitor oseltamivir in patients with moderate and severe renal impairment.
Brennan, BJ; Frey, N; Kamal, MA; Lien, YT; Morcos, PN; Rayner, CR; Subramoney, V, 2015
)
0.94
"Use of adjunct oxygenation therapies and nontraditional antiviral dosing has changed significantly since the 2009 pandemic, although this has not resulted in a measurable impact on clinical outcomes."( Clinical characteristics of critically ill patients with suspected influenza during the 2009-10 and 2013-14 outbreaks.
Franquiz, MJ; Gonzales, JP; Saleeb, PG; Shanholtz, CB, 2017
)
0.46
"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
)
0.97
"A modular interdisciplinary platform was developed to investigate the economic impact of oseltamivir treatment by dosage regimen under simulated influenza pandemic scenarios."( Interdisciplinary pharmacometrics linking oseltamivir pharmacology, influenza epidemiology and health economics to inform antiviral use in pandemics.
Chaiyakunapruk, N; Chong, HY; Dall, G; Kamal, MA; Kamauu, A; Kirkpatrick, CM; Kong, DCM; Lee, KKC; Nelson, RE; Nieforth, K; Pratoomsoot, C; Rayner, CR; Smith, PF; Toovey, S; Wu, DBC, 2017
)
0.94
"Baloxavir marboxil monotherapy with 96 h-delayed oral dosing achieved drastic reductions in virus titre, inflammatory response and mortality in a mouse model."( Combination treatment with the cap-dependent endonuclease inhibitor baloxavir marboxil and a neuraminidase inhibitor in a mouse model of influenza A virus infection.
Ando, Y; Baba, K; Fukao, K; Higuchi, N; Ikeda, M; Kitano, M; Matsumoto, K; Naito, A; Noda, T; Noshi, T; Shishido, T; Yamamoto, A, 2019
)
0.51
" Although the dosing regimen of this drug is well established for non-pregnant patients, it is not clear if the significant physiological alterations associated with pregnancy affect the pharmacokinetics of oseltamivir and, thus, warrant different dosing regimens to assure efficacy."( Pharmacokinetics of oseltamivir phosphate and oseltamivir carboxylate in non-pregnant and pregnant rhesus monkeys.
Basavarajappa, M; Beland, FA; Fisher, J; Gamboa da Costa, G; Loukotková, L; Lumen, A; Mattison, D; Morris, SM; Roberts, R, 2020
)
1.07
"The preliminary findings of this study suggest that the higher CQ dosage should not be recommended for critically ill patients with COVID-19 because of its potential safety hazards, especially when taken concurrently with azithromycin and oseltamivir."( Effect of High vs Low Doses of Chloroquine Diphosphate as Adjunctive Therapy for Patients Hospitalized With Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Infection: A Randomized Clinical Trial.
Albuquerque, BC; Alexandre, MAA; Baía-da-Silva, D; Balieiro, AAS; Bassat, Q; Borba, MGS; Brito, M; Brito-Sousa, JD; Croda, J; Daniel-Ribeiro, CT; Fontes, CJ; Guerra, MVF; Hajjar, LA; Lacerda, MVG; Melo, GC; Monteiro, WM; Mourão, MPG; Naveca, FG; Nogueira, ML; Pacheco, AGF; Pinto, RC; Romero, GAS; Sampaio, VS; Santos, JDO; Schwarzbold, A; Siqueira, AM; Val, FFA; Xavier, MS, 2020
)
0.74
"Prepared novel and scalable OP-DPI may have the potential to overcome the problems associated with existing marketed dosage forms of OP."( Development of Sustained Release Oseltamivir Phosphate Dry Powder Inhaler:
Kenjale, P; Pokharkar, V; Sahastrabudhe, H, 2020
)
0.84
"Ferrets were dosed orally with BXM (10 and 30 mg/kg twice daily for 1 day), oseltamivir phosphate (OSP) (5 mg/kg twice daily for 2 days) or vehicle to measure the antiviral effects of BXM and OSP."( The antiviral effects of baloxavir marboxil against influenza A virus infection in ferrets.
Baba, K; Kamimori, H; Kitano, M; Kiyota, K; Matsuzaki, T; Mizutare, T; Naito, A; Noda, T; Oka, R; Sato, A; Sato, K; Shishido, T; Yoshida, R; Yoshida, Y, 2020
)
0.79
"The results highlight the rapid antiviral action of BXM with post-exposure prophylaxis or therapeutic dosing in ferrets and offer support for further research on prevention of influenza virus infection and transmission."( The antiviral effects of baloxavir marboxil against influenza A virus infection in ferrets.
Baba, K; Kamimori, H; Kitano, M; Kiyota, K; Matsuzaki, T; Mizutare, T; Naito, A; Noda, T; Oka, R; Sato, A; Sato, K; Shishido, T; Yoshida, R; Yoshida, Y, 2020
)
0.56
" The dosage and course of treatment were more standardised, but there were too many types of combined drugs, and the indications of preventive use were insufficient in some cases."( Risks in clinical applications of oseltamivir phosphate in the real world.
Guan, Y; Han, Y; Song, C; Yang, J; Zhang, X; Zheng, L, 2020
)
0.84
"Studies that informed dosage regimens for patients with mild to moderately impaired renal function focused on attaining steady-state concentrations similar to those observed in patients with normal renal function."( Oseltamivir-Current Dosing Recommendations Reduce the Therapeutic Benefit in Patients With Mild to Moderate Renal Function and/or Large Body Mass: A Review of the Literature With Recommendations to Optimize Dosing, Including the Use of Therapeutic Drug Mo
Jones, TE, 2021
)
2.06
"Current dosing advice for oseltamivir in patients with mild to moderate renal impairment and those with a larger body mass are likely to reduce (or even negate) its efficacy."( Oseltamivir-Current Dosing Recommendations Reduce the Therapeutic Benefit in Patients With Mild to Moderate Renal Function and/or Large Body Mass: A Review of the Literature With Recommendations to Optimize Dosing, Including the Use of Therapeutic Drug Mo
Jones, TE, 2021
)
2.36
"Peramivir offers a single-dose intravenous (IV) treatment option for influenza (vs 5-day oral dosing for oseltamivir)."( Intravenous peramivir vs oral oseltamivir in high-risk emergency department patients with influenza: Results from a pilot randomized controlled study.
Dugas, AF; Hsieh, YH; LoVecchio, F; McBryde, B; Ricketts, EP; Rothman, RE; Saliba-Shaw, K, 2021
)
1.12
" However, the capsule form of oseltamivir is not of the recommended dosage for children."( Reconstitution of Oseltamivir Capsules for Pediatric Use on a Long-Term Cruise: A Treatment Option.
Amaya Dimas, LDC; Aoki, Y; Kitazawa, K; Mizushiro, N, 2021
)
1.24
"To optimise the dosing regimen of oseltamivir for immunocompromised (IC) paediatric patients (<18 years) with influenza, we used an extrapolation approach alongside clinical data."( Dosing regimen optimisation for oseltamivir in immunocompromised paediatric patients with influenza: Extrapolation of efficacy.
Bhardwaj, R; Gibiansky, L; Hernández-Sánchez, J; Jolivet, S; Jordie, EB; Knab, T; Lemenuel-Diot, A; Nasmyth-Miller, C; Ravva, P; Sturm, S; Zwanziger, E, 2022
)
1.28
" Simulations were performed to identify the optimal dosing regimen."( Dosing regimen optimisation for oseltamivir in immunocompromised paediatric patients with influenza: Extrapolation of efficacy.
Bhardwaj, R; Gibiansky, L; Hernández-Sánchez, J; Jolivet, S; Jordie, EB; Knab, T; Lemenuel-Diot, A; Nasmyth-Miller, C; Ravva, P; Sturm, S; Zwanziger, E, 2022
)
1
"An oseltamivir dosage recommendation (conventional dose, twice daily for 10 days) was established in IC paediatric patients with influenza, based on extrapolation of efficacy from IC adults, leveraging population PK, PK/PD, and disease modelling, whilst taking resistance and safety data into account."( Dosing regimen optimisation for oseltamivir in immunocompromised paediatric patients with influenza: Extrapolation of efficacy.
Bhardwaj, R; Gibiansky, L; Hernández-Sánchez, J; Jolivet, S; Jordie, EB; Knab, T; Lemenuel-Diot, A; Nasmyth-Miller, C; Ravva, P; Sturm, S; Zwanziger, E, 2022
)
1.63
" The studies of pharmacokinetics of camphecene have demonstrated that it does not accumulate in blood plasma and that its m ultiple applications with dosage interval of 65 min are safe."( Optimization of application schedule of camphecene, a novel anti-influenza compound, based on its pharmacokinetic characteristics.
Bykov, VV; Garshinina, AV; Khazanov, VA; Leonov, KA; Motov, VS; Salakhutdinov, NF; Slita, AV; Volobueva, AS; Yarovaya, OI; Zarubaev, VV, 2022
)
0.72
" As dosage errors may occur when prescribing medication to children, professionals' need for reliable medical information has increased in public health care centers and hospitals."( Online searches of children's oseltamivir in public primary and specialized care: Detecting influenza outbreaks in Finland using dedicated databases for health care professionals.
Helve, O; Juutinen, A; Kaila, M; Mukka, M; Mustonen, P; Pesälä, S; Virtanen, MJ, 2022
)
1.01
" The model was run under three candidate profiles whereby infectiousness was assumed to be proportional to viral titer on a natural-scale, log-scale, or dose-response model."( Novel modelling approaches to predict the role of antivirals in reducing influenza transmission.
Arguello, CJ; Asher, J; Charoin, JE; Clay, M; Clinch, B; Durham, DP; Jolivet, S; Kuhlbusch, K; Lemenuel-Diot, A; Mier-Y-Teran-Romero, L; Wong, DY, 2023
)
0.91
" The present study tested whether a clinically relevant antiviral dosing regimen of oseltamivir would disrupt behavior in the 5XFAD mouse model of Alzheimer's disease amyloid pathology or wild-type littermates."( Increased α-2,6 sialic acid on microglia in amyloid pathology is resistant to oseltamivir.
Bieniek, KF; Fastenau, C; Hopp, SC; Odfalk, KF; Smith, S; Solano, L; Wickline, JL, 2023
)
1.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
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 drugA substance used in the prophylaxis or therapy of virus diseases.
environmental contaminantAny minor or unwanted substance introduced into the environment that can have undesired effects.
xenobioticA xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
[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 (4)

ClassDescription
cyclohexenecarboxylate ester
amino acid esterAny carboxylic ester derivative of an amino acid.
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
acetamidesCompounds with the general formula RNHC(=O)CH3.
[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 (20)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency0.00740.001310.157742.8575AID1259253
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.70790.009610.525035.4813AID1479145
[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)
Neuraminidase Influenza A virus (A/Turkey/651242/2006(H5N1))IC50 (µMol)0.11040.00030.31032.8247AID1401152; AID560872
Neuraminidase Influenza A virus (A/Turkey/651242/2006(H5N1))Ki0.00790.00100.00440.0079AID560877
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))IC50 (µMol)13.00760.00000.503510.0000AID1059386; AID1059387; AID1064127; AID1064128; AID1064131; AID1064132; AID1073042; AID1073043; AID1073044; AID1073045; AID1156845; AID1266207; AID1266208; AID1266209; AID1266210; AID1401148; AID1401151; AID1588930; AID294072; AID384920; AID443293; AID443294; AID443295; AID443296; AID455703; AID527157; AID527158; AID527159; AID527160; 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; AID591600; AID636870; AID648767; AID648768; AID753435; AID753436
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))Ki0.00050.00011.78687.7000AID314411; AID560879
Neuraminidase Influenza A virus (A/duck/Laos/25/2006(H5N1))IC50 (µMol)2.03170.00011.10476.0950AID1401149; AID560875; AID561145
Neuraminidase Influenza A virus (A/duck/Laos/25/2006(H5N1))Ki0.00110.00050.00080.0011AID560880
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))IC50 (µMol)1.13440.00050.976710.0000AID1401150; AID147493; AID1502944; AID1588927; AID1588929; AID532114
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))Ki12.10000.01000.43500.8600AID1365369
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC50 (µMol)27.17600.00140.00550.0130AID1167295; AID1167296; AID1186763; AID1186764
NeuraminidaseInfluenza B virus (B/Lee/1940)IC50 (µMol)0.00500.00100.402810.0000AID147494
NeuraminidaseInfluenza B virus (B/Lee/1940)Ki0.00110.00010.00100.0025AID314410
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)1,300.00000.00022.318510.0000AID582049
SialidaseClostridium perfringensIC50 (µMol)61.10000.00102.45729.8000AID1372135
Acyl-CoA desaturase 1Mus musculus (house mouse)IC50 (µMol)0.00800.00100.68303.4000AID1064128
Neuraminidase Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1))IC50 (µMol)0.00430.00070.00250.0049AID560873; AID561143
Neuraminidase Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1))Ki0.00490.00040.00270.0049AID560878
Neuraminidase Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))IC50 (µMol)0.00030.00020.00130.0048AID560871; AID561141
Neuraminidase Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))Ki0.00010.00010.00030.0005AID560876
NeuraminidaseInfluenza A virus (A/Singapore/1/1957(H2N2))IC50 (µMol)0.00300.00100.00500.0170AID1795726
NeuraminidaseInfluenza A virus (A/Aichi/2/1968(H3N2))IC50 (µMol)0.00160.00160.00210.0027AID532115
Sialidase-4Homo sapiens (human)IC50 (µMol)3,666.66678.30008.30008.3000AID1405015; AID1889679; AID532109
Sialidase-3Homo sapiens (human)IC50 (µMol)5,250.00002.40005.99808.1700AID1405014; AID1889678; AID532108; AID539786
Sialidase-2Homo sapiens (human)IC50 (µMol)2,333.33333.90006.73337.8000AID1405013; AID1889677; AID532107
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-dependent translocase ABCB1Homo sapiens (human)Km4,200.00000.01403.717210.0000AID581725
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
viral release from host cellNeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
cholesterol biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
response to toxic substanceLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol effluxLiver carboxylesterase 1Homo sapiens (human)
negative regulation of cholesterol storageLiver carboxylesterase 1Homo sapiens (human)
epithelial cell differentiationLiver carboxylesterase 1Homo sapiens (human)
cholesterol homeostasisLiver carboxylesterase 1Homo sapiens (human)
reverse cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
medium-chain fatty acid metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cellular response to cholesterolLiver carboxylesterase 1Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusLiver carboxylesterase 1Homo sapiens (human)
cholesterol ester hydrolysis involved in cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid secretionLiver carboxylesterase 1Homo sapiens (human)
lipid catabolic processLiver carboxylesterase 1Homo sapiens (human)
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 (24)

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))
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
sterol esterase activityLiver carboxylesterase 1Homo sapiens (human)
methylumbelliferyl-acetate deacetylase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylesterase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylic ester hydrolase activityLiver carboxylesterase 1Homo sapiens (human)
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 (29)

Processvia Protein(s)Taxonomy
extracellular regionNeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))
plasma membraneNeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulum lumenLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
cytosolLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
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 (1185)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
AID443832Antiviral activity against Influenza B virus (B/Hong Kong/5/72) assessed as cell viability by cell-based MTS assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Diazo transfer-click reaction route to new, lipophilic teicoplanin and ristocetin aglycon derivatives with high antibacterial and anti-influenza virus activity: an aggregation and receptor binding study.
AID1553317Antiviral activity against Influenza A virus A/JiangXi-DongHu/312/2006(H3N2) infected in human A549 cells assessed as inhibition of virus plaque formation by CPE reduction assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of privileged structures into 3-O-β-chacotriosyl ursolic acid can enhance inhibiting the entry of the H5N1 virus.
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]
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.
AID510177Cytotoxicity against african green monkey Vero cells after 48 hrs2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
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.
AID561129Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID387575Cytotoxicity against MDCK cells assessed as alteration in cell morphology by MTS assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and antiviral evaluation of acyclic azanucleosides developed from sulfanilamide as a lead structure.
AID455703Noncompetitive inhibition of recombinant influenza A virus rvH1N1 A/Bervig_Mission/1/18 neuraminidase2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral 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.
AID286172Antiviral activity against 10 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as day of death at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID581718AUC (0 to infinity) ratio in brain to plasma in perfused Sprague-Dawley rat at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222258AUC(0 to 24 hrs) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
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.
AID658749Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by colorimetric formazan-based MTS assay2012European journal of medicinal chemistry, Jun, Volume: 522-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
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.
AID1418310Inhibition of wild type Influenza A virus (A/chicken/Hubei/327/2004(H5N1)) M2 proton channel V27A/S31N mutant expressed in yeast after 46 to 48 hrs by yeast growth restoration assay2018European journal of medicinal chemistry, Nov-05, Volume: 159Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors.
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.
AID634759Antiviral activity against Punta Toro virus infected in african green monkey Vero cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID611763Antiviral activity against Sindbis virus infected in Vero cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID768189Antiviral activity against influenza A virus H1N1 subtype infected in dog MDCK cells assessed as reduction of virus-induced cytopathogenicity by MTS assay2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies.
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.
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.
AID733267Antiviral activity against Influenza B virus (B/Panama/45/1990) infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity at 1 hr post-infection measured after 3 days by fluorescein-diacetate based fluorimetric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Efficient synthesis of 3H,3'H-spiro[benzofuran-2,1'-isobenzofuran]-3,3'-dione as novel skeletons specifically for influenza virus type B inhibition.
AID1222302AUC(0 to infinity) in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID582070Prodrug conversion in commercial liver S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID766686Antiviral activity against Influenza A virus H3N3 infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity2013European journal of medicinal chemistry, Sep, Volume: 67Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity.
AID561123Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in lung at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
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.
AID1183510Antiviral activity against Influenza A virus A/New York/18/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
AID542557Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as reduction in body weight at 10 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 5 (Rvb = 22.2 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID674367Antiviral activity against influenza A virus A/Hanfang/359/95 (H3N2) assessed as inhibition of virus-induced cytopathic effect in cell-based assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Alkaloids from the root of Isatis indigotica.
AID1502944Inhibition of neuraminidase activity in Influenza A virus (A/PR/8/34 (H1N1)) infected in MDCK cells using 4-MU-NANA as substrate pretreated for 30 mins followed by substrate addition measured after 2 hrs by fluorescence assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
C-Methylated Flavonoid Glycosides from Pentarhizidium orientale Rhizomes and Their Inhibitory Effects on the H1N1 Influenza Virus.
AID648767Inhibition of Influenza A virus H7N1 N1 neuraminidase expressed in baculovirus using 2'-(4-Methylumbelliferyl)-alpha-D-acetyl neuraminic acid as substrate incubated for 2 hrs prior to substrate addition measured after 5 hrs by fluorimetry2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Synthesis and in vitro study of novel neuraminidase inhibitors against avian influenza virus.
AID286181Survival of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets at 25 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID581707Cmax in perfused Sprague-Dawley rat cerebrospinal fluid at 1000 mg/kg, po2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID581523Prodrug conversion in 42 days old female rat brain S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1771093Cytotoxicity against dog MDCK cells assessed as decrease in cell viability by CCK8 assay
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.
AID582045Permeability from basolateral to apical side of pig LLC-PK1 cells over expressing human MDR12009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID634833Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
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.
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.
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.
AID560892Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 6 postinfection2009Antimicrobial 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.
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.
AID582037Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 7000 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1077000Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus A/hanfang/359/95(H3N2)2014European journal of medicinal chemistry, Apr-09, Volume: 761,2,3-Triazole-containing derivatives of rupestonic acid: click-chemical synthesis and antiviral activities against influenza viruses.
AID1073033Inhibition of Clostridium perfringens neuraminidase by chemiluminescence based assay2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
AID582073Prodrug conversion in 42 days old male rat brain S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1409726Cytotoxicity against MDCK cells after 72 hrs by crystal violet staining based spectrophotometric method2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Unraveling the Binding, Proton Blockage, and Inhibition of Influenza M2 WT and S31N by Rimantadine Variants.
AID582048Efflux ratio of permeability from apical to basolateral side over basolateral to apical side in pig LLC-PK1 cells over expressing human MDR1 in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1222298Inhibition of human PEPT1 expressed in CHOK1 cells assessed as Gly-Sar uptake at 0.3 to 10 mM after 10 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1365376Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated immediately after virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID1204726Half life in CD1 mouse at 30 mg/kg, po2015Bioorganic & 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.
AID581682Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in non-perfused Sprague-Dawley rat cerebrospinal fluid at 30 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
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.
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.
AID1432501Cytotoxicity against MDCK cells after 48 hrs by by Reed and Muench analysis2017Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
Structure-activity relationship studies of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses.
AID286191Inhibition of influenza A/Vietnam/1203/04 virus replication in ferrets upper respiratory tract at 10 mg/kg twice daily after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
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.
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.
AID634755Antiviral activity against Parainfluenza-3 virus infected in african green monkey Vero cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1222310AUC(0 to infinity) in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID634831Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID294072Inhibition of Influenza A virus type A H3N2 neuraminidase2007Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7
Design, synthesis, inhibitory activity, and SAR studies of pyrrolidine derivatives as neuraminidase inhibitors.
AID416779Cytotoxicity against MDCK cells by MTS assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID561137Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL1alpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1222273Tmax in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fasting conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID542579Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as reduction in body weight at 1 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 5 (Rvb = 17.4 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID611770Cytotoxicity against dog MDCK cells assessed as alteration of cell morphology after 3 days by microscopy2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
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.
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.
AID658606Cytotoxicity against MDCK cells assessed as cell viability by colorimetric formazan-based MTS assay2012European journal of medicinal chemistry, Jun, Volume: 522-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
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.
AID237325Half-life determined after administration of compound dosed at 5 mg equiv/kg (iv) and 10 mg/equiv/kg (oral) in rat2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
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.
AID1222305AUC(0 to 6 hrs) in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1498124Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus-induced cytopathicity by MTS assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
AID1156846Inhibition of Influenza A H1N1 virus neuraminidase at 100 nM after 1 hr by spectrofluorimetry using 2-(4-meythylumbelliferyl)-alpha-D-acetylneuramic acid as substrate2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
AID1073040Antiviral activity against Influenza A virus (A/Hong Kong/1/1968(H3N2)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
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.
AID1401151Inhibition of Influenza A virus A/Anhui/1/2013(H7N9) neuraminidase 150 cavity at 10 uM using MUNANA as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 30 mins by fluorescence assay relative to control2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis and biological evaluation of NH
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.
AID561130Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID561345Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IFNalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1365384Inhibition of neuraminidase in influenza A virus (A/Puerto Rico/8/1934(H1N1)) assessed as remaining enzyme activity at 0.1 ug/ml pre-incubated for 30 mins before NA-Star substrate addition for 30 mins by luminescence based assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID539955Antiviral activity against influenza B virus infected in MDCK cells assessed as protection against virus-induced cytopathogenicity after 2 days2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
AID581685Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in perfused Sprague-Dawley rat cerebrospinal fluid at 30 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID542578Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as reduction in body weight at 1 mg/kg, po administered 4 hrs before infection for 5 days measured on day 5 (Rvb = 17.4 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
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.
AID1222291Drug uptake in CHOK1 cells at 100 uM after 10 mins by HPLC coupled with radiodetection analysis in presence of PEPT1 inhibitor cefadroxil2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID527160Inhibition of oseltamivir-resistant Influenza A virus (A/California/08/2009(H1N1)) neuraminidase H274Y mutant expressed in human 293T cells after 30 mins by spectrofluorimetric analysis2010Journal of natural products, Oct-22, Volume: 73, Issue:10
C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase.
AID1204731AUC in CD1 mouse at 30 mg/kg, po2015Bioorganic & 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.
AID1386762Inhibition of Influenza A virus (A/Puerto Rico/8/1934(H1N1)) neuraminidase at 0.1 to 1000 uM by chemiluminescence based assay2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
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.
AID283463Lowering of Arterial oxygen saturation decline in BALB/c mouse infected with influenza A virus (A/duck/Minnesota/1525/1981 (H5N1)) at 20 mg/kg/day, po twice daily for 5 days administered 1 hr after infection measured on day 11 relative to carboxymethyl ce2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID558688Half life in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system at 1 ng/ml administered as 1 hr infusion every 12 hrs by LC-MS-MS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1473441Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 1:10 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
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.
AID1056522Antiviral activity against Influenza virus A/Hanfang/359/95 (H3N2)2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Homosecoiridoid alkaloids with amino acid units from the flower buds of Lonicera japonica.
AID236746Maximum plasma concentration determined after administration of compound dosed at 5 mg equiv/kg (iv) and 10 mg/equiv/kg (oral) in rat2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
AID582053Prodrug conversion in 86 years old male human brain S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID661916Inhibition of oseltamivir-resistant H1N1 swine influenza virus neuraminidase H274Y mutant using 4-MU-NANA as substrate by fluorescence assay2012Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11
Xanthones from Polygala karensium inhibit neuraminidases from influenza A viruses.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1767878Cytotoxicity against dog MDCK cells assessed as reduction in cell viability2021European journal of medicinal chemistry, Oct-15, Volume: 222Optimization and SAR research at the piperazine and phenyl rings of JNJ4796 as new anti-influenza A virus agents, part 1.
AID581521Prodrug conversion in 7 days old female rat liver S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID539953Antiviral activity against influenza A virus H1N1 infected in MDCK cells assessed as protection against virus-induced cytopathogenicity after 2 days2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
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.
AID1415635Cytotoxicity against MDCK cells after 48 hrs by MTT assay2017MedChemComm, May-01, Volume: 8, Issue:5
Synthesis and
AID558678Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in viral replication at 1 ng/ml administered as 1 hr infusion every 24 hrs for 62009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1266210Inhibition of Influenza A virus H1N1 neuraminidase H275Y mutant2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
AID561131Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 6 postinfection2009Antimicrobial 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.
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.
AID527159Inhibition of Influenza A virus (A/California/08/2009(H1N1)) wild type neuraminidase expressed in human 293T cells after 30 mins by spectrofluorimetric analysis2010Journal of natural products, Oct-22, Volume: 73, Issue:10
C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase.
AID581717AUC (0 to infinity) ratio in brain to plasma in non-perfused Sprague-Dawley rat at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222246Renal clearance in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fed conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID455706Antiviral activity against influenza A virus H9N2 A/Chicken/Korea/MS96/96 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities.
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).
AID581730Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 1665 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1502946Antiviral 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 MTT assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
C-Methylated Flavonoid Glycosides from Pentarhizidium orientale Rhizomes and Their Inhibitory Effects on the H1N1 Influenza Virus.
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.
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]
AID1365379Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 4 hrs after virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID1222288Drug uptake in CHOK1 cells expressing human PEPT1 by HPLC coupled with radiodetection analysis in presence of KH and Hanks' balanced salt solution2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1553315Antiviral activity against Influenza A virus A/Duck/Guangdong/99(H5N1) infected in human A549 cells assessed as inhibition of virus plaque formation by CPE reduction assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of privileged structures into 3-O-β-chacotriosyl ursolic acid can enhance inhibiting the entry of the H5N1 virus.
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.
AID1553316Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in human A549 cells assessed as inhibition of virus plaque formation by CPE reduction assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of privileged structures into 3-O-β-chacotriosyl ursolic acid can enhance inhibiting the entry of the H5N1 virus.
AID561153Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL6 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
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.
AID558677Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in viral replication at 1 ng/ml administered as continuous infusion for 6 days m2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID581708Cmax in perfused Sprague-Dawley rat brain at 1000 mg/kg, po2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID768212Cytotoxicity against MDCK cells assessed as cell viability after 4 days by MTS assay2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies.
AID1713960Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza A virus (A/Puerto Rico/8/34 (H1N1)) infected in MDCK cells2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Biological evaluation of tetracationic compounds based on two 1,4-diazabicyclo[2.2.2]octane moieties connected by different linkers.
AID558676Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in viral replication at 1000 ng/ml administered as continuous infusion for 6 day2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
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).
AID581522Prodrug conversion in 7 days old male rat liver S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID582042Permeability from apical to basolateral side of Spodoptera frugiperda Sf9 cells over expressing human MRP32009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID1156845Inhibition of Influenza A H1N1 virus neuraminidase after 1 hr by spectrofluorimetry using 2-(4-meythylumbelliferyl)-alpha-D-acetylneuramic acid as substrate2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
AID561133Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1553314Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of privileged structures into 3-O-β-chacotriosyl ursolic acid can enhance inhibiting the entry of the H5N1 virus.
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.
AID1222254AUC(0 to infinity) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1222297Drug uptake in CHOK1 cells expressing human PEPT1 at 100 uM at 4 degC after 10 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1438094Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) expressing M2 proton channel S31N mutant infected in MDCK cells assessed as reduction in cytopathic effect after 48 hrs by crystal violet staining-based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Binding and Proton Blockage by Amantadine Variants of the Influenza M2
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1201117Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as reduction of virus-induced cytopathic effect after 72 hrs by microscopic analysis2015European journal of medicinal chemistry, Apr-13, Volume: 94A few atoms make the difference: synthetic, CD, NMR and computational studies on antiviral and antibacterial activities of glycopeptide antibiotic aglycon derivatives.
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.
AID542566Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as lung viral titer at 10 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 4 (Rvb = 1 x 10'6 +/- 0.3 x 10'6 PF2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1409722Antiviral activity against Influenza A virus (A/Hong Kong/68(H3N2)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect by crystal violet staining based light-microscopic analysis2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Unraveling the Binding, Proton Blockage, and Inhibition of Influenza M2 WT and S31N by Rimantadine Variants.
AID542554Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as lung viral titer at 10 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 4 (Rvb = 1.9 x 10'6 +/- 0.1 x 10'6 PFU)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID581684Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in perfused Sprague-Dawley rat plasma at 30 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID548443Antiviral activity against Influenza B virus infected in MDCK cells assessed as inhibition of virus induced cytopathicity by visual scoring of CPE2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
AID1460756Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Kunming mouse assessed as intact columnar epithelium in bronchiole without inflammatory cell infiltration at 20 mg/kg/day, po qd for 4 days by hematoxylin and eosin staini2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Boronic Acid Modifications Enhance the Anti-Influenza A Virus Activities of Novel Quindoline Derivatives.
AID1365380Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 7 hrs after virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID527169Cytotoxicity against MDCK cells at 97.56 uM after 48 hrs by neutral red dye assay2010Journal of natural products, Oct-22, Volume: 73, Issue:10
C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase.
AID1365371Antiviral activity against Influenza B virus (B/Lee/40) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
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.
AID581738Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 1000 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1505282Antiviral activity against Influenza A virus (A/PR/8/34 (H1N1)(NA-H274Y)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by microscopic analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
AID527158Inhibition of Influenza A virus (A/Sw/Kor/CAH1/04 (H1N1) KCTC 11165BP neuraminidase after 30 mins by spectrofluorimetric analysis2010Journal of natural products, Oct-22, Volume: 73, Issue:10
C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase.
AID1858129Antiviral activity against group 2 influenza A virus H3N2 (A/Hong Kong-11/1968) infected in human A549 cells assessed as inhibition of viral entry preincubated with compound for 30 mins followed by viral infection for 1 hour further incubated for 48 hrs w2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-
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.
AID1113454Antiviral activity against Unidentified Influenza A virus (H1N1) infected MDCK cells assessed as reduction of virus-induced cytopathic effect after 3 days by colorimetric formazan-based MTS assay2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
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.
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.
AID658750Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by colorimetric formazan-based MTS assay2012European journal of medicinal chemistry, Jun, Volume: 522-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
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.
AID443297Inhibition of oseltamivir-resistant Influenza Virus A/342/0 (H1N1) neuraminidase at 100 nM2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
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.
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).
AID542563Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as time to death at 1 mg/kg, po administered 4 hrs before infection on day 5 (Rvb = 5.1 days)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID766706Cytotoxicity against MDCK cells assessed as morphological changes2013European journal of medicinal chemistry, Sep, Volume: 67Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity.
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.
AID1222306AUC(0 to infinity) in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID763864Antiviral activity against Influenza A virus (A/Perth/16/2009(H3N2)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect by cell-based neutral red uptake assay2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
AID286178Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as inhibition of virus spread in spleen at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID561148Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in TNFalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
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.
AID1767879Selectivity index, ratio of CC50 for cytotoxicity against dog MDCK cells to IC50 for antiviral activity against Influenza A virus HINI infected in dog MDCK cells2021European journal of medicinal chemistry, Oct-15, Volume: 222Optimization and SAR research at the piperazine and phenyl rings of JNJ4796 as new anti-influenza A virus agents, part 1.
AID1266208Inhibition of oseltamivir-resistant Influenza A virus H3N2 neuraminidase E119V mutant2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
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.
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.
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.
AID1160748Antiviral activity against Influenza A virus H3N2 VR1679 infected in MDCK cells assessed as inhibition of viral nucleoprotein production at 10 uM after 6 hrs by immunostaining-based confocal microscopy2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
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.
AID581686Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in perfused Sprague-Dawley rat brain at 30 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID416781Antiviral activity against influenza H1N1 virus in MDCK cells assessed as reduction of virus-induced cytopathicity by MTS method2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 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.
AID560881Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as survival rate at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
AID539948Cytotoxicity against MDCK cells by MTS assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
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.
AID1771096Antiviral activity against Influenza A virus H5N1 infected in human A549 cells assessed as inhibition of viral replication by TCID50 assay
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.
AID582040Permeability from apical to basolateral side of Spodoptera frugiperda Sf9 cells over expressing human MRP12009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1280362Antiviral activity against amantadine-resistant influenza A virus JX/312 (H3N2) infected in dog MDCK cells assessed as inhibition of virus induced cytopathic effect after 40 hrs by Cell-Titer-Glo assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Spiromastilactones: A new class of influenza virus inhibitors from deep-sea fungus.
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.
AID581525Prodrug conversion in 42 days old male rat brain S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1858133Selectivity index, ratio of CC50 for human A549 cells to EC50 for group 2 influenza A virus H3N2 (A/Victoria361/2011) infected in human A549 cells2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-
AID350634Antiviral activity against Influenza A virus (A/Viet Nam/1203/2004(H5N1)) in MDCK cells assessed as inhibition of viral replication at 100 uM after 18 hrs by transmission electron microscopy2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
A novel small-molecule inhibitor of the avian influenza H5N1 virus determined through computational screening against the neuraminidase.
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.
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).
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.
AID560893Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 6 postinfection2009Antimicrobial 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.
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.
AID581518Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 335 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
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.
AID1385613Cytotoxicity against MDCK cells measured after 48 hrs2018Journal of natural products, 08-24, Volume: 81, Issue:8
Minor Nortriterpenoids from the Twigs and Leaves of Rhododendron latoucheae.
AID561152Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL6 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID733268Antiviral activity against Influenza A virus (A/Hong kong/8/1968(H2N3)) infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity at 1 hr post-infection measured after 3 days by fluorescein-diacetate based fluorimetric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Efficient synthesis of 3H,3'H-spiro[benzofuran-2,1'-isobenzofuran]-3,3'-dione as novel skeletons specifically for influenza virus type B inhibition.
AID1427857Antiviral activity against Influenza A virus A/95-359 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect
AID542559Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as mortality rate at 1 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 5 (Rvb = 100 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1767880Antiviral activity against Oseltamivir resistant Influenza A virus (A/Tianjin-Jinnan/15/2009(H1N1) infected in dog MDCK cells assessed as inhibition of surface glycoprotein hemagglutinin2021European journal of medicinal chemistry, Oct-15, Volume: 222Optimization and SAR research at the piperazine and phenyl rings of JNJ4796 as new anti-influenza A virus agents, part 1.
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.
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.
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.
AID1222285Drug uptake in CHOK1 cells incubated for 30s to 15 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID561116Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
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.
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).
AID1365372Antiviral activity against Influenza B virus (B/Maryland/1/59) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID582072Prodrug conversion in 7 days old female rat brain S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID634747Antiviral activity against Herpes simplex virus 2 G infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1077002Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus (A/Tianjinjinnan/15/2009/H1N1)2014European journal of medicinal chemistry, Apr-09, Volume: 761,2,3-Triazole-containing derivatives of rupestonic acid: click-chemical synthesis and antiviral activities against influenza viruses.
AID1222265AUC(0 to 5 hrs) in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID455704Cytotoxicity against MDCK cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities.
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.
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.
AID1502947Cytotoxicity against MDCK cells after 2 days by MTT assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
C-Methylated Flavonoid Glycosides from Pentarhizidium orientale Rhizomes and Their Inhibitory Effects on the H1N1 Influenza Virus.
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.
AID1266207Inhibition of oseltamivir-resistant Influenza A virus H3N2 neuraminidase2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
AID286198Inhibition of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus replication in ferrets brain at 25 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID634837Antiviral activity against Human immunodeficiency virus 2 infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 days by microscopic analysis2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1773429Antiviral activity against Influenza A virus H1N1 (A/PR/8/34) infected in MDCK cells assessed as reduction in virus titer treated 1 hr post viral infection followed by replacement with fresh medium with compounds and measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Novel betulin dicarboxylic acid ester derivatives as potent antiviral agents: Design, synthesis, biological evaluation, structure-activity relationship and in-silico study.
AID1222251Tmax in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1767881Selectivity index, ratio of CC50 for cytotoxicity against dog MDCK cells to IC50 for antiviral activity against Oseltamivir resistant Influenza A virus (A/Tianjin-Jinnan/15/2009(H1N1)) infected in dog MDCK cells2021European journal of medicinal chemistry, Oct-15, Volume: 222Optimization and SAR research at the piperazine and phenyl rings of JNJ4796 as new anti-influenza A virus agents, part 1.
AID1771092Antiviral activity against Influenza A virus H5N1 (A/chicken/Hubei/327/2004(H5N1)) infected in dog MDCK cells assessed as inhibition of virus replication by plaque reduction assay
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.
AID581531Cmax in perfused Sprague-Dawley rat plasma at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID582047Efflux ratio of permeability from apical to basolateral side over basolateral to apical side in pig LLC-PK1 cells over expressing human MDR12009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1849916Inhibition of Influenza virus neuraminidase2021European journal of medicinal chemistry, Jan-15, Volume: 210Chemistry, biosynthesis and biological activity of terpenoids and meroterpenoids in bacteria and fungi isolated from different marine habitats.
AID581674Cmax in perfused Sprague-Dawley rat brain at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID733269Antiviral activity against Influenza A virus (A/Taiwan/1/1986(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity at 1 hr post-infection measured after 3 days by fluorescein-diacetate based fluorimetric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Efficient synthesis of 3H,3'H-spiro[benzofuran-2,1'-isobenzofuran]-3,3'-dione as novel skeletons specifically for influenza virus type B inhibition.
AID1404181Antiviral activity against Influenza A virus H3N2 A/Hong Kong/68 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs
AID1401152Inhibition of Influenza A virus A/Anhui/1/2005(H5N1) neuraminidase using MUNANA as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis and biological evaluation of NH
AID558683Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in hemagglutinination units at 1 ng/ml administered as 1 hr infusion every 12 hr2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
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.
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.
AID561151Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL6 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID561124Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in lung at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID611772Cytotoxicity against human CEM cells assessed as growth inhibition after 3 days by coulter counting analysis2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID1222275AUC(0 to 24 hrs) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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
AID1473449Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 1:1 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]a2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
AID1183522Antiviral activity against Influenza A virus A/Puerto Rico/8/34 infected in BALB/c mouse assessed as body weight loss at 30 mg/kg bid treated after 48 hrs of infection for 10 days2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
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.
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.
AID582062Prodrug conversion in 7 days old male rat liver S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222290Drug uptake in CHOK1 cells at 100 uM after 10 mins by HPLC coupled with radiodetection analysis in presence of PEPT1 inhibitor valacyclovir2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1660683Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in Kunming mouse assessed as decrease in lung TNFalpha level at 10 mg/kg/day, po starting 4 hrs after viral challenge and continued for 4 days by ELISA2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.
AID634760Antiviral activity against Vesicular stomatitis virus infected in human Hela cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1773419Cytotoxicity against MDCK cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Novel betulin dicarboxylic acid ester derivatives as potent antiviral agents: Design, synthesis, biological evaluation, structure-activity relationship and in-silico study.
AID558681Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in hemagglutinination units at 1 ng/ml administered as continuous infusion for 62009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID443295Inhibition of Influenza Virus A/Horneburg/IDT7489/08 (H1N1) neuraminidase2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
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.
AID582052Prodrug conversion assessed as oseltamivir carboxylate level in presence of Sf9 cell culture supernatant expressing human recombinant HCE2 after 30 mins2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID581705Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 162 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1200483Antiviral activity against influenza A virus A/WSN/33 (H1N1) infected in MDCK cells assessed as reduction in cytopathic effect after 48 hrs by plaque assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin.
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.
AID1858135Antiviral activity against group 2 influenza A virus H3N2 (A/Hong Kong-11/1968) infected in MDCK cells infected with supernatant of compound treated virus-producing human A549 cells assessed as reduction in viral titer at 1 to 10 uM treated for 48 hrs wit2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-
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.
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.
AID286176Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as inhibition of virus spread in brain at 5 mg/kg after 4 hrs of inoculum for 5days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID1386750Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in HEK293T cells assessed as inhibition of viral replicon activity incubated for 30 hrs by dual-Glo luciferase assay2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
AID542551Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as time to death at 1 mg/kg, po administered 48 hrs postinfection for 5 days (Rvb = 5.8 days)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID286195Inhibition of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus replication in ferrets lungs at 25 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID548437Cytotoxicity against MDCK cells assessed as cell viability by MTS assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
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.
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.
AID1160745Cytotoxicity against MDCK cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
AID1473422Antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in plaque formation after 2 days by crystal violet staining based assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
AID1365369Inhibition of neuraminidase in influenza A virus (A/Puerto Rico/8/1934(H1N1)) pre-incubated for 30 mins before NA-Star substrate addition for 30 mins by luminescence based assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
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.
AID549516Inhibition of wild type H1N1 swine influenza virus neuraminidase activity expressed in HEK293T cells after 2 hrs by spectrofluorometry2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Chalcones as novel influenza A (H1N1) neuraminidase inhibitors from Glycyrrhiza inflata.
AID1143482Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as increase in survival rate at 2.6 umol/kg/day, po bid administered on day 0 prior to viral infection continued for day 1 to day 4 measured on day 142014European journal of medicinal chemistry, Jun-23, Volume: 81Tamiphosphor monoesters as effective anti-influenza agents.
AID1266206Inhibition of oseltamivir-resistant Influenza A virus H3N2 neuraminidase at 50 uM2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
AID582069Prodrug conversion in commercial brain S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222260Cmax in juvenile breast-fed Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1222292Drug uptake in CHOK1 cells expressing human PEPT1 at 100 uM after 10 mins by HPLC coupled with radiodetection analysis in presence of PEPT1 inhibitor Trp-Gly2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
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.
AID582079Prodrug conversion in 86 years old male human brain S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID581725Activity of human MDR1-mediated drug permeability expressed in pig LLC-PK1 cells2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID286185Antiviral activity against 10 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as increase in temperature at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID286192Inhibition of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus replication in ferrets lungs at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID528272Non-competitive inhibition of influenza A virus H1N1 Neuraminidase using 4-methylumbelliferyl-alpha-D-N-acetylneuraminic acid sodium salt hydrate substrate by Lineweaver burk plot2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
New stilbenoid with inhibitory activity on viral neuraminidases from Erythrina addisoniae.
AID582057Prodrug conversion in commercial liver S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1418311Cytotoxicity in yeast assessed as reduction in cell proliferation2018European journal of medicinal chemistry, Nov-05, Volume: 159Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors.
AID1222294Drug uptake in CHOK1 cells expressing human PEPT1 at 100 uM after 10 mins by HPLC coupled with radiodetection analysis in presence of PEPT1 inhibitor cefadroxil2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1183509Antiviral activity against Influenza A virus A/Mexico/4108/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
AID1073041Antiviral activity against Influenza A virus J/8178/09 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
AID1293611Cytotoxicity against MDCK cells assessed as decrease in cell viability after 48 hrs by MTT assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA-PB1 Protein-Protein Interaction: Structure-Activity Relationships Exploration with the Aid of Molecular Modeling.
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.
AID1201121Antiviral activity against Influenza B virus (B/Hong Kong/05/1972) infected in MDCK cells assessed as reduction of virus-induced cytopathic effect after 72 hrs by microscopic analysis2015European journal of medicinal chemistry, Apr-13, Volume: 94A few atoms make the difference: synthetic, CD, NMR and computational studies on antiviral and antibacterial activities of glycopeptide antibiotic aglycon derivatives.
AID561115Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID581735Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 175 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1365382Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 24 hrs after virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID455708Selectivity index, ratio of CC50 for MDCK cells to EC50 for influenza virus H9N2 A/Chicken/Korea/MS96/962009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities.
AID1432502Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 40 hrs2017Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
Structure-activity relationship studies of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses.
AID561118Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 15 postinfection2009Antimicrobial 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.
AID1156847Inhibition of Influenza A H1N1 virus neuraminidase at 20 nM after 1 hr by spectrofluorimetry using 2-(4-meythylumbelliferyl)-alpha-D-acetylneuramic acid as substrate2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
AID661913Inhibition of Influenza A virus H1N1 neuraminidase using 4-MU-NANA as substrate by fluorescence assay2012Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11
Xanthones from Polygala karensium inhibit neuraminidases from influenza A viruses.
AID1222319Drug uptake in CHOK1 cells at 100 uM after 10 mins by HPLC coupled with radiodetection analysis in presence of PEPT1 inhibitor Trp-Gly2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1222299Cmax in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1578003Antiviral activity against Influenza A virus H1N1 infected in dog MDCK cells assessed as inhibition in virus-induced cytopathic effect incubated for 40 hrs2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.
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.
AID1293608Inhibition of Influenza A virus PR/8/34 6His-tagged PA (239 to 716 residues) interaction with GST-tagged PB1 (1 to 25 residues) expressed in Escherichia coli compound treated in PBS buffer measured after overnight incubation by ELISA2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA-PB1 Protein-Protein Interaction: Structure-Activity Relationships Exploration with the Aid of Molecular Modeling.
AID561344Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL6 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1222267Tmax in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID542553Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as lung viral titer at 1 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 4 (Rvb = 1.9 x 10'6 +/- 0.1 x 10'6 PFU)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1222293Drug uptake in CHOK1 cells expressing human PEPT1 at 100 uM after 10 mins by HPLC coupled with radiodetection analysis in presence of PEPT1 inhibitor valacyclovir2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1113453Antiviral activity against Influenza A virus H3N2 infected MDCK cells assessed as reduction of virus-induced cytopathic effect after 3 days by colorimetric formazan-based MTS assay2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
AID236505Area under concentration time curve determined after administration of compound dosed at 5 mg equiv/kg (iv) and 10 mg/equiv/kg (oral) in rat2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
AID763861Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza A virus (A/California/07/2009(H1N1))2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
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.
AID611764Antiviral activity against Punta Toro virus infected in Vero cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
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.
AID582043Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR12009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID648768Inhibition of Influenza A virus H7N3 N3 neuraminidase expressed in baculovirus using 2'-(4-Methylumbelliferyl)-alpha-D-acetyl neuraminic acid as substrate incubated for 2 hrs prior to substrate addition measured after 5 hrs by fluorimetry2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Synthesis and in vitro study of novel neuraminidase inhibitors against avian influenza virus.
AID549517Inhibition of oseltamivir-resistant H1N1 swine influenza virus neuraminidase H274Y mutant activity expressed in HEK293T cells after 2 hrs by spectrofluorometry2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Chalcones as novel influenza A (H1N1) neuraminidase inhibitors from Glycyrrhiza inflata.
AID455705Antiviral activity against influenza A virus H1N1 A/PR/8/34 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities.
AID286203Antiviral activity against 10^6 EID50 influenza A/turkey/15/06 H5N1 virus inoculated ferrets assessed as viral titer in brain at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID1606652Antiviral activity against Influenza A virus (A/PA/10/2010 (H3N2)) infected in BALB/c mouse assessed as increase in animal survival rate at 10 mg/kg, po administered via gavage starting at 8 hrs post infection and continuing BID for 6 days2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Targeting Endoplasmic Reticulum α-Glucosidase I with a Single-Dose Iminosugar Treatment Protects against Lethal Influenza and Dengue Virus Infections.
AID1222250Cmax in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
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.
AID1409725Antiviral activity against Influenza A virus A/WSN/33 H1N1 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect by crystal violet staining based light-microscopic analysis2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Unraveling the Binding, Proton Blockage, and Inhibition of Influenza M2 WT and S31N by Rimantadine Variants.
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.
AID1160747Antiviral activity against Influenza A virus H3N2 VR1679 infected in MDCK cells assessed as inhibition of virus-induced cytocidal activity after 48 hrs by CellTiter-Glo assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a 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.
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.
AID286171Survival of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1186763Inhibition of influenza A virus (A/California/07/2009(H1N1)) pdm09 neuraminidase using MUNANA substrate pre-incubated for 30 mins before substrate addition by fluorometric assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Inhibitory potency of flavonoid derivatives on influenza virus neuraminidase.
AID510176Antiviral activity against parainfluenza-3 virus infected in Vero cells assessed as reduction of virus-induced cytopathic effect2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID561139Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL1alpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID561353Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in MCP1 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID581675Terminal half life in non-perfused Sprague-Dawley rat plasma at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID1222244AUC(0 to infinity) in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fed conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1385614Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus A/95-359 infected in MDCK cells2018Journal of natural products, 08-24, Volume: 81, Issue:8
Minor Nortriterpenoids from the Twigs and Leaves of Rhododendron latoucheae.
AID1222284Drug uptake in CHOK1 cells expressing human PEPT1 at pH 6 by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID658607Cytotoxicity against MDCK cells assessed as minimum compound concentration required to causes microscopically detectable alteration of normal cell morphology2012European journal of medicinal chemistry, Jun, Volume: 522-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
AID1160746Selectivity ratio of EC50 for Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells to EC50 for Influenza A virus H3N2 VR1679 infected in MDCK cells2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
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.
AID1250470Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 hrs by crystal violet staining2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Dicarabrol, a new dimeric sesquiterpene from Carpesium abrotanoides L.
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.
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.
AID1222253AUC(0 to 24 hrs) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1889676Inhibition of human NEU12022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID1235020Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus (A/FM/1/47(H1N1))-induced cytopathic effect in MDCK cells2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bioactive Sesquiterpenes and Lignans from the Fruits of Xanthium sibiricum.
AID581711Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in perfused Sprague-Dawley rat plasma at 1000 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID581731Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 3415 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID582059Prodrug conversion in 7 days old female rat brain S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID542580Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as reduction in body weight at 10 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 5 (Rvb = 17.4 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1222240Tmax in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fed conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1372135Inhibition of Clostridium perfringenes neuraminidase activity using 4-methylumbelliferyl-1-alpha-D-N-acetylneuramic acid sodium salt hydrate as substrate by fluorescence based assay2017Bioorganic & medicinal chemistry letters, 12-15, Volume: 27, Issue:24
Design, synthesis and biological evaluation of novel oseltamivir derivatives as potent neuraminidase inhibitors.
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.
AID581715Volume of distribution at steady state in Sprague-Dawley rat at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID581859Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 1665 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID286175Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as inhibition of viral replication in lungs at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID236132Bioavailability in rat (dose 5 mg equiv/kg i.v. and 10 mg/equiv/kg p.o.)2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
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.
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.
AID582076Prodrug conversion in 7 days old female rat liver S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID1578006Selectivity index, ratio of TC50 for cytotoxicity against dog MDCK cells to IC50 for antiviral activity against Influenza A virus H3N2 infected in dog MDCK cells2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID581712Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in perfused Sprague-Dawley rat cerebrospinal fluid at 1000 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1403783Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) harboring neuraminidase H275Y mutant infected in BALB/c mouse assessed as mouse survival at 0.96 umol/day, po for 5 consecutive days measured on day 10 post dose2018European journal of medicinal chemistry, Feb-10, Volume: 145Peramivir conjugates as orally available agents against influenza H275Y mutant.
AID558680Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in viral replication at 1 ng/ml administered as 1 hr infusion every 8 hrs for 6 2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1201119Antiviral activity against Influenza A virus (A/Hong Kong/7/1987(H3N2)) infected in MDCK cells assessed as reduction of virus-induced cytopathic effect after 72 hrs by microscopic analysis2015European journal of medicinal chemistry, Apr-13, Volume: 94A few atoms make the difference: synthetic, CD, NMR and computational studies on antiviral and antibacterial activities of glycopeptide antibiotic aglycon derivatives.
AID1293609Antiviral activity against Influenza A virus PR/8/34 infected in MDCK cells assessed as inhibition of plaque formation treated for 1 hr measured after 2 days by toluidine blue staining-based assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA-PB1 Protein-Protein Interaction: Structure-Activity Relationships Exploration with the Aid of Molecular Modeling.
AID1365370Antiviral activity against Influenza A virus (A/Victoria/3/1975(H3N2)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID558686Half life in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system at 1 ng/ml administered as continuous infusion by LC-MS-MS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1386752Cytotoxicity in MDCK cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer-Glo cell viability assay2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
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.
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.
AID1226071Antiviral activity against oseltamivir/amantadine-resistant Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as protection against virus-induced cytocidal effect after 48 hrs by CellTiter-Glo assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Phenolic diterpenoid derivatives as anti-influenza a virus agents.
AID1156848Inhibition of Influenza A H1N1 virus neuraminidase at 4 nM after 1 hr by spectrofluorimetry using 2-(4-meythylumbelliferyl)-alpha-D-acetylneuramic acid as substrate2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
AID658746Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as reduction visual scoring of virus-induced cytopathogenicity after 4 days2012European journal of medicinal chemistry, Jun, Volume: 522-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
AID674871Antiviral activity against Influenza A virus (A/Guangdong-Luohu/219/2006(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors.
AID1201116Cytotoxicity against MDCK cells after 72 hrs by MTS assay2015European journal of medicinal chemistry, Apr-13, Volume: 94A few atoms make the difference: synthetic, CD, NMR and computational studies on antiviral and antibacterial activities of glycopeptide antibiotic aglycon derivatives.
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.
AID1767877Antiviral activity against Influenza A virus (H1N1) infected in dog MDCK cells assessed as inhibition of surface glycoprotein hemagglutinin2021European journal of medicinal chemistry, Oct-15, Volume: 222Optimization and SAR research at the piperazine and phenyl rings of JNJ4796 as new anti-influenza A virus agents, part 1.
AID1505286Antiviral activity against Influenza A virus (A/duck/HK/Y280/97 (H9N2)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by microscopic analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
AID286187Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as weight loss at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID1365377Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 1 hr after virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID542560Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as mortality rate at 10 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 5 (Rvb = 100 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1200496Antiviral activity against amantadine and ribavirin-resistant influenza A virus A/HuNan-huHui/1222/2010 (H3N2) strain2015European journal of medicinal chemistry, Mar-26, Volume: 93Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin.
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.
AID1183507Antiviral activity against Influenza A virus A/Puerto Rico/8/34 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
AID1200482Antiviral activity against influenza A virus A/WSN/33 (H1N1) infected in MDCK cells assessed as reduction in cytopathic effect at 100 uM after 48 hrs by plaque assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin.
AID1470965Antiviral activity against Influenza A virus (A/Hong Kong/498/97(H3N2)) harboring wild type neuraminidase infected in MDCK cells assessed as inhibition of viral replication preincubated for 36 hrs followed by reinfection in new monolayer of MDCK cells eve2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors.
AID763923Cytotoxicity against MDCK cells2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
AID753432Antiviral activity against Influenza A virus (A/chicken/Sandong/Li/2008(H9N2)) infected in chicken embryo fibroblast assessed as protection against virus-induced cytopathic effect after 2 days by MTS assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Caffeic acid derivatives: a new type of influenza neuraminidase inhibitors.
AID1222315Drug uptake in CHOK1 cells expressing human PEPT1 at 100 uM at pH 4 to 8 after 10 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1617144Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in human A549 cells assessed as reduction in virus neuraminidase level incubated for 24 hrs by fluorescence based assay2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region.
AID1889677Inhibition of human NEU22022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID1222234Apparent oral clearance in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fasting conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID561114Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in lung at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID1771091Inhibition of Influenza A virus H5N1 neuraminidase
AID478323Antiviral activity against Influenza A virus H3N2 assessed as cell viability by cell based MTS assay2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Click reaction synthesis of carbohydrate derivatives from ristocetin aglycon with antibacterial and antiviral activity.
AID1073042Inhibition of Influenza A virus (A/Hong Kong/1/1968(H3N2)) neuraminidase by chemiluminescence based assay2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
AID416783Antiviral activity against influenza H3N2 virus in MDCK cells assessed as reduction of virus-induced cytopathicity by MTS method2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID542552Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as lung viral titer at 1 mg/kg, po administered 4 hrs before infection for 5 days measured on day 4 (Rvb = 1.9 x 10'6 +/- 0.1 x 10'6 PFU)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1250471Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 hrs by crystal violet staining2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Dicarabrol, a new dimeric sesquiterpene from Carpesium abrotanoides L.
AID1222236AUC(0 to infinity) in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fasting conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID611760Antiviral activity against Coxsackievirus B4 infected in Vero cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
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.
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.
AID611766Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID1222301AUC(0 to 6 hrs) in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID661914Inhibition of Influenza A virus H9N2 neuraminidase using 4-MU-NANA as substrate by fluorescence assay2012Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11
Xanthones from Polygala karensium inhibit neuraminidases from influenza A viruses.
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.
AID1222256Tmax in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1222237Drug excretion in healthy human urine assessed as unchanged drug level at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fasting conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID625277FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
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.
AID542582Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as mortality rate at 1 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 5 (Rvb = 100 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID528271Inhibition of influenza A virus H1N1 Neuraminidase using 4-methylumbelliferyl-alpha-D-N-acetylneuraminic acid sodium salt hydrate substrate2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
New stilbenoid with inhibitory activity on viral neuraminidases from Erythrina addisoniae.
AID611758Antiviral activity against RSV infected in HeLa cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID581714Clearance in Sprague-Dawley rat at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID455707Selectivity index, ratio of CC50 for MDCK cells to EC50 for influenza virus H1N1 A/PR/8/342009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities.
AID1401146Inhibition of Influenza A virus A/Anhui/1/2005(H5N1) neuraminidase at 10 uM using MUNANA as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 30 mins by fluorescence assay relative to control2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis and biological evaluation of NH
AID1071442Half life in Sprague-Dawley rat plasma2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
AID1077001Antiviral activity against Influenza A virus A/hanfang/359/95(H3N2) infected in MDCK cells assessed as inhibition of virus-induced cytopathicity after 40 hrs2014European journal of medicinal chemistry, Apr-09, Volume: 761,2,3-Triazole-containing derivatives of rupestonic acid: click-chemical synthesis and antiviral activities against influenza viruses.
AID443830Antiviral activity against Influenza A virus (A/Hong Kong/7/87(H3N2)) assessed as cell viability by cell-based MTS assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Diazo transfer-click reaction route to new, lipophilic teicoplanin and ristocetin aglycon derivatives with high antibacterial and anti-influenza virus activity: an aggregation and receptor binding study.
AID1365385Inhibition of neuraminidase in influenza A virus (A/Puerto Rico/8/1934(H1N1)) assessed as remaining enzyme activity at 1 ug/ml pre-incubated for 30 mins before NA-Star substrate addition for 30 mins by luminescence based assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID1386751Antiviral activity against influenza A virus Hong Kong/8/1968(H3N2) infected in HEK293T cells assessed as inhibition of viral replicon activity incubated for 30 hrs by dual-Glo luciferase assay2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
AID1588928Inhibition of Influenza A virus (A/Babol/36/2005 (H3N2) neuraminidase expressed by HEK293 cells incubated for 1 hr using 4-MU-NANA substrate by spectrofluorometric assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases.
AID1113452Antiviral activity against Influenza B virus infected in MDCK cells assessed as reduction of virus-induced cytopathic effect after 3 days by colorimetric formazan-based MTS assay2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
AID1473440Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 1:5 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]a2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
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.
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.
AID1059383Antiviral activity against Influenza A virus (A/Chicken/Shandong/LY/08(H9N2)) infected in chicken embryo fibroblasts assessed as protection against virus-induced cytopathic effect preincubated for 1 hr followed by viral-infection measured after 2 days by 2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Further discovery of caffeic acid derivatives as novel influenza neuraminidase inhibitors.
AID1222311Cmax in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID561128Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID392531Antiviral activity against influenza 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.
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.
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.
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.
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.
AID581729AUC (0 to 8 hrs) ratio in cerebrospinal fluid to plasma in perfused Sprague-Dawley rat at 1000 mg/kg, po2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
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.
AID456232Activity at human recombinant CES1 expressed in baculovirus-infected Spodoptera frugiperda Sf21 cells assessed as substrate hydrolysis by fluorescence assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations.
AID1183518Antiviral activity against Influenza A virus A/Puerto Rico/8/34 infected in BALB/c mouse assessed as mouse survival at 1 to 10 mg/kg bid treated after 48 hrs of infection for 10 days2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
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.
AID1578007Antiviral activity against Influenza B virus infected in MDCK cells assessed as inhibition in virus-induced cytopathic effect incubated for 40 hrs2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.
AID658751Antiviral activity against Influenza B virus infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by colorimetric formazan-based MTS assay2012European journal of medicinal chemistry, Jun, Volume: 522-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
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.
AID581745Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 618 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID286199Survival of 10^6 EID50 influenza A/turkey/15/06 H5N1 virus inoculated ferrets at 10 mg/kg twice daily after 24 hrs inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
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.
AID1578005Antiviral activity against Influenza A virus H3N2 infected in dog MDCK cells assessed as inhibition in virus-induced cytopathic effect incubated for 40 hrs2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.
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.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1222282Drug uptake in CHOK1 cells expressing human PEPT1 at pH 5 by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID581726Activity of human MDR1-mediated permeability from apical to basolateral side in pig LLC-PK1 cells in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID560886Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as mean day to death at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
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.
AID1222304Tmax in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID582031Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 6918 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1470964Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) harboring wild type neuraminidase assessed as inhibition of viral replication preincubated for 36 hrs followed by reinfection in new monolayer of MDCK cells every 1 hr for 12 hrs2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors.
AID561117Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID581520Prodrug conversion in 42 days old male rat liver S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID561127Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
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.
AID560884Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as survival rate at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
AID1234207Selectivity index, ratio of TC50 for African green monkey MDCK cells to IC50 for influenza A virus (A/Hanfang/359/95(H3N2))2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Antiviral Matrine-Type Alkaloids from the Rhizomes of Sophora tonkinensis.
AID549515Inhibition of Influenza A H1N1 virus neuraminidase activity after 2 hrs by spectrofluorometry2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Chalcones as novel influenza A (H1N1) neuraminidase inhibitors from Glycyrrhiza inflata.
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.
AID286173Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as day of death at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1446880Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 40 hrs by CellTiter-Glo assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and biological evaluation of gentiopicroside derivatives as potential antiviral inhibitors.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
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.
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.
AID1160752Antiviral activity against Influenza A virus H3N2 VR1679 infected in MDCK cells assessed as inhibition of virus-induced cytocidal activity pretreated with compound before infection by time of addition assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
AID542555Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as reduction in body weight at 1 mg/kg, po administered 4 hrs before infection for 5 days measured on day 5 (Rvb = 22.2 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1222241Terminal half life in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fed conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID582030Cmax in perfused Sprague-Dawley rat cerebrospinal fluid at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1266212Inhibition of Influenza B virus neuraminidase R152K mutant2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
AID582071Prodrug conversion in 7 days old male rat brain S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID611765Antiviral activity against Feline coronavirus infected in CRFK cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
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.
AID1654868Antiviral activity against influenza A virus H3N2/95-359 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect incubated for 48 hrs by Reed-Muench method2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action.
AID1654873Selectivity index, ratio of CC50 for cytotoxicity in MDCK cells to EC50 for Antiviral activity against influenza A virus H3N2/95-359 infected in MDCK cells2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action.
AID1160751Antiviral activity against Influenza A virus H3N2 VR1679 infected in MDCK cells assessed as inhibition of virus-induced cytocidal activity compound treated 2 hrs post infection by time of addition assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
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.
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.
AID1505280Antiviral activity against Influenza A virus (A/WSN/33 (H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by microscopic analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
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.
AID581743Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 83 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222264Tmax in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1222283Drug uptake in CHOK1 cells at pH 6 by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1440171Oral bioavailability in human2017European journal of medicinal chemistry, Feb-15, Volume: 127Prodrug approach: An overview of recent cases.
AID286183Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as day of death at 25 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1113455Cytotoxicity against MDCK cells assessed as change in cellular morphology2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
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.
AID1386757Antiviral activity against oseltamivir-resistant Influenza A virus (H1N1) TJ/15 up to 100 uM2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
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]
AID532124Inhibition of human NEU3 expressed in HEK293 cells assessed as hydrolysis of ganglioside GM3 by TLC method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
AID286193Inhibition of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus replication in ferrets liver at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID443828Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) assessed as cell viability by cell-based MTS assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Diazo transfer-click reaction route to new, lipophilic teicoplanin and ristocetin aglycon derivatives with high antibacterial and anti-influenza virus activity: an aggregation and receptor binding study.
AID1222259AUC(0 to infinity) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1708993Inhibition of Influenza virus H5N1 neuraminidase2021Bioorganic & medicinal chemistry letters, 04-01, Volume: 37Design, synthesis and biological evaluation of dihydrofurocoumarin derivatives as potent neuraminidase inhibitors.
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.
AID558679Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in viral replication at 1 ng/ml administered as 1 hr infusion every 12 hrs for 62009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1222289Drug uptake in CHOK1 cells expressing human PEPT2 by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1578004Selectivity index, ratio of TC50 for cytotoxicity against dog MDCK cells to IC50 for antiviral activity against Influenza A virus H1N1 infected in dog MDCK cells2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.
AID1365381Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 12 hrs after virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID416784Antiviral activity against influenza B virus in MDCK cells assessed as reduction of virus-induced cytopathicity by visual cytopathic effect scoring method2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID1073044Inhibition of Influenza A virus (A/Puerto Rico/8/1934(H1N1)) neuraminidase by chemiluminescence based assay2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
AID1289285Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs by crystal violet staining-based microplate reader analysis2016Journal of natural products, Jan-22, Volume: 79, Issue:1
Antiviral Merosesquiterpenoids Produced by the Antarctic Fungus Aspergillus ochraceopetaliformis SCSIO 05702.
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.
AID582060Prodrug conversion in 42 days old male rat brain S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
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.
AID763860Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza A virus (A/duck/Minnesota/1525/1981(H5N1))2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
AID1470962Inhibition of Influenza A virus (A/Hong Kong/498/97(H3N2)) neuraminidase using 4-MU-NANA as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors.
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.
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.
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.
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.
AID286179Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as inhibition of viral replication in small intestine at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
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.
AID1222270Tmax in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID561352Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in MCP1 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1858136Antiviral activity against group 2 influenza A virus H3N2 (A/Victoria/361/2011) infected in MDCK cells infected with supernatant of compound treated virus-producing human A549 cells assessed as reduction in viral titer at 1 to 10 uM treated for 48 hrs wit2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-
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.
AID1059386Inhibition of influenza A virus A/duck/China/QJ/01(H5N1) neuraminidase using 4-MU-NANA as substrate incubated for 5 mins prior to substrate addition measured after 30 to 60 mins by fluorescence assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Further discovery of caffeic acid derivatives as novel influenza neuraminidase inhibitors.
AID768187Antiviral activity against influenza B virus infected in dog MDCK cells assessed as reduction of virus-induced cytopathogenicity by MTS assay2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies.
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.
AID350631Antiviral activity against influenza A virus H1N1 A/HK/54/98 in MDCK cells assessed as inhibition of viral replication after 48 hrs by hemagglutinination assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
A novel small-molecule inhibitor of the avian influenza H5N1 virus determined through computational screening against the neuraminidase.
AID1889679Inhibition of human NEU42022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID561149Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in TNFalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1204729Cmax in CD1 mouse at 30 mg/kg, po2015Bioorganic & 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.
AID1293615Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza A virus PR/8/34 infected in MDCK cells2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA-PB1 Protein-Protein Interaction: Structure-Activity Relationships Exploration with the Aid of Molecular Modeling.
AID582077Prodrug conversion in 42 days old male rat liver S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1235018Cytotoxicity against MDCK cells assessed as growth inhibition by CPE assay2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bioactive Sesquiterpenes and Lignans from the Fruits of Xanthium sibiricum.
AID674873Antiviral activity against Influenza B virus (strain B/Jifang/13/97) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors.
AID581524Prodrug conversion in 7 days old female rat brain S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1280364Antiviral activity against influenza B virus B/SZ/155 infected in dog MDCK cells assessed as inhibition of virus induced cytopathic effect after 40 hrs by Cell-Titer-Glo assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Spiromastilactones: A new class of influenza virus inhibitors from deep-sea fungus.
AID581744Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 335 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1858130Antiviral activity against group 2 influenza A virus H3N2 (A/Victoria/361/2011) infected in human A549 cells assessed as inhibition of viral entry preincubated with compound for 30 mins followed by viral infection for 1 hour further incubated for 48 hrs w2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-
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.
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).
AID1156850Inhibition of Influenza A H1N1 virus neuraminidase at 0.16 nM after 1 hr by spectrofluorimetry using 2-(4-meythylumbelliferyl)-alpha-D-acetylneuramic acid as substrate2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
AID1222242Apparent oral clearance in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fed conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1857995Inhibition of influenza virus neuraminidase2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Sialidase Inhibitors with Different Mechanisms.
AID286189Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as increase in temperature at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID581679Terminal half life in perfused Sprague-Dawley rat cerebrospinal fluid at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID1204734Oral bioavailability in CD1 mouse at 30 mg/kg2015Bioorganic & 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.
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.
AID582039Permeability from apical to basolateral side of Spodoptera frugiperda Sf9 cells over expressing human BCRP12009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222255Cmax in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
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.
AID1612770Cytotoxicity against MDCK cells after 40 hrs by CellTiter-Glo assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis, structure activity relationship and in vitro anti-influenza virus activity of novel polyphenol-pentacyclic triterpene conjugates.
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.
AID542564Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as lung viral titer at 1 mg/kg, po administered 4 hrs before infection for 5 days measured on day 4 (Rvb = 1 x 10'6 +/- 0.3 x 10'6 P2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1234206Antiviral activity against influenza A virus (A/Hanfang/359/95(H3N2)) infected in MDCK cells assessed as inhibition of virus-induced cytopathogenic effect dosed 1 hr after viral adsorption2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Antiviral Matrine-Type Alkaloids from the Rhizomes of Sophora tonkinensis.
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.
AID1266218Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza A virus2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B 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.
AID1384747Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in C57BL/6J mouse assessed as decrease in viral load in bronchoalveolar lavage at 8 mg/mouse/day, ip qd treated up to day 2 starting at 5 to 10 mins post infection relative2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
From Naproxen Repurposing to Naproxen Analogues and Their Antiviral Activity against Influenza A Virus.
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.
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.
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.
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.
AID1222266Cmax in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1073037Cytotoxicity against MDCK cells after 72 hrs2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
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.
AID561134Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 6 postinfection2009Antimicrobial 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.
AID558689Half life in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system at 1 ng/ml administered as 1 hr infusion every 8 hrs by LC-MS-MS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID582063Prodrug conversion in 7 days old female rat liver S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID582055Prodrug conversion in human liver S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1401149Inhibition of Influenza A virus A/Anhui/1/2005(H5N1) neuraminidase H274Y mutant using MUNANA as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis and biological evaluation of NH
AID478322Antiviral activity against Influenza A virus H3N2 assessed as inhibition of viral induced cytopathic effect2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Click reaction synthesis of carbohydrate derivatives from ristocetin aglycon with antibacterial and antiviral activity.
AID1293610Cytotoxicity against HEK293T cells assessed as decrease in cell viability after 24 hrs by MTT assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA-PB1 Protein-Protein Interaction: Structure-Activity Relationships Exploration with the Aid of Molecular Modeling.
AID527157Inhibition of Influenza A virus (A/chicken/Korea/01310/2001 (H9N2)) neuraminidase after 30 mins by spectrofluorimetric analysis2010Journal of natural products, Oct-22, Volume: 73, Issue:10
C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase.
AID582064Prodrug conversion in 42 days old male rat liver S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID561120Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 15 postinfection2009Antimicrobial 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.
AID539949Cytotoxicity against MDCK cells assessed as minimum concentration required to cause microscopically detectable alteration after 2 days2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
AID582035Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 700 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222261Tmax in juvenile breast-fed Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1473447Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 10:1 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
AID611627Antiviral activity against HIV 1 3B infected in CEM cells assessed as inhibition of virus-induced giant cell formation after 4 days by microscopy2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
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.
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.
AID478320Antiviral activity against influenza A virus H1N1 assessed as inhibition of viral induced cytopathic effect2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Click reaction synthesis of carbohydrate derivatives from ristocetin aglycon with antibacterial and antiviral activity.
AID646596Inhibition of viral neuraminidase after 20 mins by fluorescence assay2012Journal of natural products, Jan-27, Volume: 75, Issue:1
p-Terphenyl and diterpenoid metabolites from endophytic Aspergillus sp. YXf3.
AID1365387Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity at 1 ug/ml pre-incubated for 1 hr with virus before virus infection of cells and measured after 48 hr2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
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.
AID1222238Renal clearance in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fasting conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID560885Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as survival rate at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
AID286196Inhibition of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus replication in ferrets liver at 25 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1384743Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in C57BL/6J mouse assessed as increase in mouse survival at 8 mg/mouse/day, ip qd treated up to day 2 starting at 5 to 10 mins post infection measured at day 122018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
From Naproxen Repurposing to Naproxen Analogues and Their Antiviral Activity against Influenza A Virus.
AID611768Antiviral activity against Influenza B virus infected in MDCK cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
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.
AID1077003Antiviral activity against oseltamivir-resistant Influenza A virus (A/Tianjinjinnan/15/2009/H1N1) infected in MDCK cells assessed as inhibition of virus-induced cytopathicity after 40 hrs2014European journal of medicinal chemistry, Apr-09, Volume: 761,2,3-Triazole-containing derivatives of rupestonic acid: click-chemical synthesis and antiviral activities against influenza viruses.
AID283455Reduction of lung viral titre in BALB/c mouse infected with influenza A virus (A/duck/Minnesota/1525/1981 (H5N1)) at 20 mg/kg/day, po twice daily for 5 days administered 1 hr after infection measured on day 1 relative to carboxymethyl cellulose2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID1588929Inhibition of Influenza A virus (A/Anhui/1/2005(H5N1)) neuraminidase expressed by HEK293 cells incubated for 1 hr using 4-MU-NANA substrate by spectrofluorometric assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases.
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.
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.
AID443831Antiviral activity against Influenza B virus (B/Hong Kong/5/72) assessed as inhibition of virus-induced cytopathic effect by cell-based assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Diazo transfer-click reaction route to new, lipophilic teicoplanin and ristocetin aglycon derivatives with high antibacterial and anti-influenza virus activity: an aggregation and receptor binding study.
AID1201120Antiviral activity against Influenza A virus (A/Hong Kong/7/1987(H3N2)) infected in MDCK cells assessed as cell viability after 72 hrs by MTS assay2015European journal of medicinal chemistry, Apr-13, Volume: 94A few atoms make the difference: synthetic, CD, NMR and computational studies on antiviral and antibacterial activities of glycopeptide antibiotic aglycon derivatives.
AID1222300Tmax in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID611761Antiviral activity against Parainfluenza virus 3 infected in Vero cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID561350Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in MCP1 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1578002Cytotoxicity against MDCK cells assessed as reduction in cell viability incubated for 48 hrs2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.
AID1858137Antiviral activity against group 2 influenza A virus LPAI H7N7 (A/Netherlands/219/2003) infected in MDCK cells infected with supernatant of compound treated virus-producing human A549 cells assessed as reduction in viral titer at 1 to 10 uM treated for 482022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-
AID582050Prodrug conversion in 42 days old female rat liver S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1502945Inhibition of neuraminidase activity in H9N2 A/chicken/Korea/01210/2001 infected in MDCK cells using 4-MU-NANA as substrate pretreated for 30 mins followed by substrate addition measured after 2 hrs by fluorescence assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
C-Methylated Flavonoid Glycosides from Pentarhizidium orientale Rhizomes and Their Inhibitory Effects on the H1N1 Influenza Virus.
AID1470968Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza A virus (A/Puerto Rico/8/1934(H1N1)) harboring neuraminidase H259Y mutant2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors.
AID443827Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) assessed as inhibition of virus-induced cytopathic effect by cell-based assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Diazo transfer-click reaction route to new, lipophilic teicoplanin and ristocetin aglycon derivatives with high antibacterial and anti-influenza virus activity: an aggregation and receptor binding study.
AID1222287Drug uptake in CHOK1 cells by HPLC coupled with radiodetection analysis in presence of KH and Hanks' balanced salt solution2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo 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.
AID634757Antiviral activity against Sindbis virus infected in african green monkey Vero cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1222243AUC(0 to 24 hrs) in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fed conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1266213Ratio of IC50 for oseltamivir-resistant Influenza A virus H3N2 wild type neuraminidase to IC50 for oseltamivir-resistant Influenza A virus H3N2 neuraminidase E119V mutant2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
AID1183505Antiviral activity against Influenza A virus A/Georgia/20/2006 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
AID1222272Cmax in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fasting conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID733264Antiviral activity against Influenza B virus (B/Brisbane/60/2008) infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity at 1 hr post-infection measured after 3 days by fluorescein-diacetate based fluorimetric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Efficient synthesis of 3H,3'H-spiro[benzofuran-2,1'-isobenzofuran]-3,3'-dione as novel skeletons specifically for influenza virus type B inhibition.
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.
AID560882Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as survival rate at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
AID733265Antiviral activity against Influenza B virus (B/Lee/40) infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity at 1 hr post-infection measured after 3 days by fluorescein-diacetate based fluorimetric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Efficient synthesis of 3H,3'H-spiro[benzofuran-2,1'-isobenzofuran]-3,3'-dione as novel skeletons specifically for influenza virus type B inhibition.
AID674875Antiviral activity against Influenza A virus (A/Tianjin-Jinnan/15/2009(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors.
AID1077006Cytotoxicity against MDCK cells after 48 hrs2014European journal of medicinal chemistry, Apr-09, Volume: 761,2,3-Triazole-containing derivatives of rupestonic acid: click-chemical synthesis and antiviral activities against influenza viruses.
AID674874Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza B virus (strain B/Jifang/13/97)2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors.
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.
AID634758Antiviral activity against Coxsackievirus B4 infected in african green monkey Vero cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
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.
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.
AID661915Inhibition of wild type H1N1 swine influenza virus neuraminidase using 4-MU-NANA as substrate by fluorescence assay2012Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11
Xanthones from Polygala karensium inhibit neuraminidases from influenza A viruses.
AID1404182Antiviral activity against Influenza A virus H1N1 A/Jena/8178/09 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs
AID1386763Inhibition of influenza A virus Hong Kong/8/1968(H3N2) neuraminidase at 0.1 to 1000 uM by chemiluminescence based assay2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
AID542562Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as time to death at 10 mg/kg, po administered 48 hrs postinfection for 5 days (Rvb = 5.1 days)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID582075Prodrug conversion in 7 days old male rat liver S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1427859Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus (A/95-359) infected in MDCK cells
AID591600Inhibition of influenza A virus neuraminidase assessed as cleavage of MUNANA substrate by fluorescence assay2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Design, synthesis and biological activity of thiazolidine-4-carboxylic acid derivatives as novel influenza neuraminidase inhibitors.
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.
AID1222308Tmax in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1317960Inhibition of Influenza A virus (A/California/07/2009(H1N1)) recombinant wild type N-terminal FLAG-tagged neuraminidase ectodomain (82 to 469 residues) transfected in Drosophila Schneider S2 cells using 4-MUNANA as substrate after 20 mins by fluorometric 2016European journal of medicinal chemistry, Oct-04, Volume: 121Kinetic, thermodynamic and structural analysis of tamiphosphor binding to neuraminidase of H1N1 (2009) pandemic influenza.
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.
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.
AID1266215Ratio of IC50 for Influenza B virus wild type neuraminidase to IC50 for Influenza B virus neuraminidase R152K mutant2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
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.
AID561354Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in MCP1 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID561119Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in lung at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID582061Prodrug conversion in 42 days old female rat brain S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID1889678Inhibition of human NEU32022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Human Neuraminidases: Structures and Stereoselective Inhibitors.
AID582074Prodrug conversion in 42 days old female rat brain S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1438096Cytotoxicity against MDCK cells measured after 72 hrs et staining-based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Binding and Proton Blockage by Amantadine Variants of the Influenza M2
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.
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.
AID1222309AUC(0 to 6 hrs) in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1073043Inhibition of oseltamivir-resistant Influenza A virus H1N1 B/55/08 neuraminidase by chemiluminescence based assay2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
AID1660674Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in Kunming mouse assessed as mouse survival at 10 mg/kg/day, po starting 4 hrs after viral challenge and continued for 7 days by plaque assay2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.
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.
AID753431Cytotoxicity against chicken embryo fibroblast after 2 days by MTS assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Caffeic acid derivatives: a new type of influenza neuraminidase inhibitors.
AID387576Cytotoxicity against MDCK cells assessed as decrease in cell viability by MTS assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and antiviral evaluation of acyclic azanucleosides developed from sulfanilamide as a lead structure.
AID286182Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as day of death at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID561346Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IFNalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID286184Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as maximal change in weight loss at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1505281Antiviral activity against Influenza A virus (A/PR/8/34 (H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by microscopic analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
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.
AID581680Terminal half life in perfused Sprague-Dawley rat brain at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1059382Cytotoxicity against chicken embryo fibroblasts infected with Influenza A virus (A/Chicken/Shandong/LY/08(H9N2)) preincubated for 1 hr followed by viral-infection measured after 2 days by MTS assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Further discovery of caffeic acid derivatives as novel influenza neuraminidase inhibitors.
AID581519Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 83 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID286200Antiviral activity against 10^6 EID50 influenza A/turkey/15/06 H5N1 virus inoculated ferrets assessed as weight loss at 10 mg/kg twice daily after 24 hrs inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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.
AID1222248AUC(0 to 6 hrs) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID558685AUC (0 to 24 hrs) in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system at 1 ng/ml administered as continuous infusion by LC-MS-MS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1077005Antiviral activity against Influenza A virus (A/FM/1/1947(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathicity after 40 hrs2014European journal of medicinal chemistry, Apr-09, Volume: 761,2,3-Triazole-containing derivatives of rupestonic acid: click-chemical synthesis and antiviral activities against influenza viruses.
AID582066Prodrug conversion in 86 years old male human brain S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID561140Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL1alpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
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.
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.
AID561147Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in TNFalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
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.
AID478321Antiviral activity against influenza A virus H1N1 assessed as cell viability by cell based MTS assay2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Click reaction synthesis of carbohydrate derivatives from ristocetin aglycon with antibacterial and antiviral activity.
AID1222263Cmax in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1222245Drug excretion in healthy human urine assessed as unchanged drug level at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fed conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1160750Antiviral activity against Influenza A virus H3N2 VR1679 infected in MDCK cells assessed as inhibition of virus-induced cytocidal activity compound treated 6 hrs post infection by time of addition assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
AID1473437Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 10:1 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
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.
AID1186765Inhibition of influenza B virus (B/Brisbane/60/2008) neuraminidase using MUNANA substrate pre-incubated for 30 mins before substrate addition by fluorometric assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Inhibitory potency of flavonoid derivatives on influenza virus neuraminidase.
AID1438095Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) expressing wild-type M2 proton channel infected in MDCK cells assessed as reduction in cytopathic effect after 48 hrs by crystal violet staining-based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Binding and Proton Blockage by Amantadine Variants of the Influenza M2
AID1498141Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus-induced visual cytopathicity2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
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.
AID314410Inhibition of influenza B/Memphis/3/89 neuraminidase2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
Synthesis of potent pyrrolidine influenza neuraminidase inhibitors.
AID1266211Inhibition of Influenza B virus wild type neuraminidase2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
AID581681Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in non-perfused Sprague-Dawley rat plasma at 30 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID548441Antiviral activity against Influenza A H3N2 virus subtype infected in MDCK cells assessed as inhibition of virus induced cytopathicity by visual scoring of CPE2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
AID611762Antiviral activity against Mammalian orthoreovirus 1 infected in Vero cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID1059387Inhibition of Influenza A virus (A/Chicken/Shandong/LY/08(H9N2)) neuraminidase using 4-MU-NANA as substrate incubated for 5 mins prior to substrate addition measured after 30 to 60 mins by fluorescence assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Further discovery of caffeic acid derivatives as novel influenza neuraminidase inhibitors.
AID539956Antiviral activity against influenza A virus H1N1 infected in MDCK cells assessed as cell viability after 2 days by MTS assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
AID582046Permeability from basolateral to apical side of pig LLC-PK1 cells over expressing human MDR1 in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID286186Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as increase in temperature at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
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.
AID763865Antiviral activity against Influenza A virus (A/California/07/2009(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect by cell-based neutral red uptake assay2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
AID1201115Cytotoxicity against MDCK cells after 72 hrs by microscopic analysis2015European journal of medicinal chemistry, Apr-13, Volume: 94A few atoms make the difference: synthetic, CD, NMR and computational studies on antiviral and antibacterial activities of glycopeptide antibiotic aglycon derivatives.
AID286177Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as inhibition of virus spread in liver at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID286180Survival of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1280344Antiviral activity against Influenza A virus A/WSN/1933 (H1N1) infected in MDCK cells assessed as protection against virus induced cytopathic effect after 40 hrs by Celltiter-Glo assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Spiromastilactones: A new class of influenza virus inhibitors from deep-sea fungus.
AID548438Cytotoxicity against MDCK cells assessed as altered cell morphology2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
AID286174Antiviral activity against 10 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as weight loss at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1073036Induction of fluorescence at 100 uM relative to 4-methylumbelliferone2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
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.
AID1460731Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as reduction in viral HA titer by measuring reduction in chicken RBC lysis after 24 hrs by hemagglutination test2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Boronic Acid Modifications Enhance the Anti-Influenza A Virus Activities of Novel Quindoline Derivatives.
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.
AID1365375Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 1 hr before virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
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.
AID1183511Antiviral activity against Influenza A virus A/Viet Nam/1203/2004(H5N1) infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
AID1401150Inhibition of Influenza A virus A/California/04/2009(H1N1) neuraminidase H274Y mutant using MUNANA as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis and biological evaluation of NH
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.
AID558684Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in hemagglutinination units at 1 ng/ml administered as 1 hr infusion every 8 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1266214Ratio of IC50 for Influenza A virus H1N1 wild type neuraminidase to IC50 for Influenza A virus H1N1 neuraminidase H275Y mutant2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
AID1654871Cytotoxicity in MDCK cells assessed as reduction in cell viability2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action.
AID392525Antiviral activity against influenza B 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.
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.
AID581528Cmax in non-perfused Sprague-Dawley rat plasma at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID1460745Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Kunming mouse assessed as viral titer reduction in lungs at 20 mg/kg/day, po qd for 4 days measured on day 4 post last dose by crystal violet staining based plaque assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Boronic Acid Modifications Enhance the Anti-Influenza A Virus Activities of Novel Quindoline Derivatives.
AID634751Antiviral activity against Human cytomegalovirus AD169 infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1588932Potency index, ratio of IC50 for OSV to IC50 for test compound for inhibition of Influenza A virus (A/Anhui/1/2013 (H7N9) neuraminidase expressed by HEK293 cells incubated for 1 hr using 4-MU-NANA substrate by spectrofluorometric assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases.
AID1235019Antiviral activity against Influenza A virus (A/FM/1/47(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bioactive Sesquiterpenes and Lignans from the Fruits of Xanthium sibiricum.
AID539957Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as cell viability after 2 days by MTS assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
AID581734Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 100 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1498140Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced visual cytopathicity2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
AID1266216Antiviral activity against Influenza A virus infected in MDCK cells after 72 hrs by yield reduction assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B 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.
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.
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.
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.
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.
AID350630Antiviral activity against Influenza A virus (A/Viet Nam/1203/2004(H5N1)) in MDCK cells assessed as inhibition of viral replication after 48 hrs by hemagglutinination assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
A novel small-molecule inhibitor of the avian influenza H5N1 virus determined through computational screening against the neuraminidase.
AID560895Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 6 postinfection2009Antimicrobial 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.
AID286194Inhibition of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus replication in ferrets spleen at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1234205Cytotoxic activity against MDCK cells assessed as cytopathogenic effect incubated for 48 hrs2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Antiviral Matrine-Type Alkaloids from the Rhizomes of Sophora tonkinensis.
AID634754Antiviral activity against thymidine kinase-deficient Varicella Zoster virus 07/1 infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID558674Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in hemagglutinination at 1 ng/ml administered as continuous infusion for 6 days 2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1418309Inhibition of wild type Influenza A virus (A/chicken/Hubei/327/2004(H5N1)) M2 channel expressed in yeast after 46 to 48 hrs by yeast growth restoration assay2018European journal of medicinal chemistry, Nov-05, Volume: 159Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors.
AID561351Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in MCP1 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID558682Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in hemagglutinination units at 1 ng/ml administered as 1 hr infusion every 24 hr2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1360192Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as protection against virus-induced infection at 48 umol/kg/day administered via oral gavage for 5 days2018European journal of medicinal chemistry, Jun-25, Volume: 154Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.
AID582083Prodrug conversion in commercial liver S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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).
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).
AID611628Antiviral activity against HIV 2 ROD infected in CEM cells assessed as inhibition of virus-induced giant cell formation after 4 days by microscopy2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID1365374Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 2 hrs before virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID1365373Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 6 hrs before virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
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.
AID542581Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as mortality rate at 1 mg/kg, po administered 4 hrs before infection for 5 days measured on day 5 (Rvb = 100 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
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.
AID763859Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza A virus (A/Perth/16/2009(H3N2))2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
AID1498123Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathicity by MTS assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
AID634748Antiviral activity against thymidine kinase-deficient acv-resistant Herpes simplex virus 1 KOS infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
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.
AID561150Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in TNFalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
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.
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.
AID1222296Drug uptake in CHOK1 cells at 100 uM at 4 degC after 10 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1660631Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect incubated for 48 hrs by crystal violet staining based assay2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.
AID581676Terminal half life in non-perfused Sprague-Dawley rat cerebrospinal fluid at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID582080Prodrug conversion in 77 years old male human brain S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1204727Tmax in CD1 mouse at 30 mg/kg, po2015Bioorganic & 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.
AID561349Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IFNalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID542550Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as mortality rate at 10 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 5 (Rvb = 100 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID581713Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in perfused Sprague-Dawley rat brain at 1000 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1498142Antiviral activity against Influenza B virus infected in MDCK cells assessed as inhibition of virus-induced visual cytopathicity2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
AID1365386Inhibition of neuraminidase in influenza A virus (A/Puerto Rico/8/1934(H1N1)) assessed as remaining enzyme activity at 10 ug/ml pre-incubated for 30 mins before NA-Star substrate addition for 30 mins by luminescence based assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID560883Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as survival rate at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
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.
AID1470963Inhibition of Influenza A virus (A/Puerto Rico/8/1934(H1N1)) neuraminidase H259Y mutant using 4-MU-NANA as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors.
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.
AID1372136Antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2017Bioorganic & medicinal chemistry letters, 12-15, Volume: 27, Issue:24
Design, synthesis and biological evaluation of novel oseltamivir derivatives as potent neuraminidase inhibitors.
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.
AID634838Antiviral activity against Human immunodeficiency virus 1 infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 days by microscopic analysis2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID527165Cytotoxicity against MDCK cells after 48 hrs by neutral red dye assay2010Journal of natural products, Oct-22, Volume: 73, Issue:10
C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase.
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.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID286197Inhibition of 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus replication in ferrets spleen at 25 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID582044Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222268AUC(0 to 5 hrs) in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1470966Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) harboring neuraminidase H259Y mutant infected in MDCK cells assessed as inhibition of viral replication preincubated for 36 hrs followed by reinfection in new monolayer of MDCK cell2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors.
AID753435Inhibition of Influenza A virus H1N1 A/duck/China/QJ/01 neuraminidase N1 using 4-MU-NANA as substrate after 5 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Caffeic acid derivatives: a new type of influenza neuraminidase inhibitors.
AID634756Antiviral activity against Reovirus-1 infected in african green monkey Vero cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID582056Prodrug conversion in commercial brain S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID581516Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 914 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
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.
AID458820Inhibition of Spanish flu (A/Bervig_Mission/1/18) neuraminidase2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Inhibition of neuraminidase activity by polyphenol compounds isolated from the roots of Glycyrrhiza uralensis.
AID1160744Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytocidal activity after 48 hrs by CellTiter-Glo assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
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.
AID561125Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in lung at 20 mg/kg, po BID for 5 days measured on day 6 postinfection2009Antimicrobial 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.
AID1073035Induction of fluorescence quenching at 100 uM relative to 4-methylumbelliferone2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
AID1222286Drug uptake in CHOK1 cells expressing human PEPT1 incubated for 30s to 15 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1200484Cytotoxicity against MDCK cells assessed as cell growth after 40 hrs by CellTiter-Glo assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin.
AID1409724Antiviral activity against Influenza A virus A/WSN/33 H1N1 harboring N31S mutant infected in MDCK cells assessed as reduction in virus-induced cytopathic effect by crystal violet staining based light-microscopic analysis2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Unraveling the Binding, Proton Blockage, and Inhibition of Influenza M2 WT and S31N by Rimantadine Variants.
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).
AID658747Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as reduction visual scoring of virus-induced cytopathogenicity after 4 days2012European journal of medicinal chemistry, Jun, Volume: 522-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
AID634761Antiviral activity against Coxsackievirus B4 infected in human HeLa cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID542556Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as reduction in body weight at 1 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 5 (Rvb = 22.2 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
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.
AID674870Cytotoxicity against MDCK cells incubated for 48 hrs by CPE method2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors.
AID581733Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 9918 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID582054Prodrug conversion in 77 years old male human brain S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID558673Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in viral replication after 48 to 72 hrs by plaque assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1473450Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 1:5 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]a2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
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.
AID561132Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID611757Antiviral activity against VSV infected in HeLa cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID1365383Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity at 1 ug/ml treated before virus infection and measured after 48 hrs by SRB assay relative to untreate2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
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.
AID561146Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in TNFalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
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.
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.
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.
AID581740Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 3500 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID581739Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 1750 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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]
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.
AID581736Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 350 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID582032Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 9918 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID1505283Antiviral activity against Influenza A virus (A/HK/68(H3N2)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by microscopic analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
AID560894Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 6 postinfection2009Antimicrobial 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.
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.
AID416780Antiviral activity against influenza H1N1 virus in MDCK cells assessed as reduction of virus-induced cytopathicity by visual cytopathic effect scoring method2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
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.
AID1617145Therapeutic index, ratio of CC50 for human A549 cells to IC50 for Influenza A virus (A/Puerto Rico/8/34(H1N1))2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region.
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.
AID548444Antiviral activity against Influenza B virus infected in MDCK cells assessed as inhibition of virus induced cytopathicity after 2 to 4 days by MTS assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
AID768188Antiviral activity against influenza A virus H3N3 subtype infected in dog MDCK cells assessed as reduction of virus-induced cytopathogenicity by MTS assay2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies.
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.
AID582034Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 350 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID582068Prodrug conversion in human liver S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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).
AID1470961Inhibition of Influenza A virus (A/Puerto Rico/8/1934(H1N1)) neuraminidase using 4-MU-NANA as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors.
AID561121Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 15 postinfection2009Antimicrobial 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.
AID1415636Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza A virus (A/Puerto Rico/8/34(H1N1))2017MedChemComm, May-01, Volume: 8, Issue:5
Synthesis and
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.
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.
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.
AID581529Cmax in non-perfused Sprague-Dawley rat cerebrospinal fluid at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1473439Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 1:1 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]a2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
AID548440Antiviral activity against Influenza A H1N1 virus subtype infected in MDCK cells assessed as inhibition of virus induced cytopathicity after 2 to 4 days by MTS assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
AID1266209Inhibition of Influenza A virus H1N1 wild type neuraminidase2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
AID1713958Antiviral activity against Influenza A virus (A/Puerto Rico/8/34 (H1N1) infected in MDCK cells assessed as decrease in viral titer preincubated for 1 hr followed by viral infection and cultivated for 48 hrs followed by supernatant transferred to chicken e2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Biological evaluation of tetracationic compounds based on two 1,4-diazabicyclo[2.2.2]octane moieties connected by different linkers.
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.
AID1588930Inhibition of Influenza A virus (A/Anhui/1/2013 (H7N9) neuraminidase expressed by HEK293 cells incubated for 1 hr using 4-MU-NANA substrate by spectrofluorometric assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases.
AID582078Prodrug conversion in 42 days old female rat liver S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID581716AUC ratio in cerebrospinal fluid to plasma in Sprague-Dawley rat at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1186764Inhibition of influenza A virus (A/Perth/16/2009(H3N2)) neuraminidase using MUNANA substrate pre-incubated for 30 mins before substrate addition by fluorometric assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Inhibitory potency of flavonoid derivatives on influenza virus neuraminidase.
AID582036Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 1750 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
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.
AID283467Toxicity in BALB/c mouse assessed as survival at 20 mg/kg/day, po twice daily for 5 days2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
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.
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.
AID634834Antiviral activity against Influenza B virus infected in MDCK cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1432503Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 40 hrs2017Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
Structure-activity relationship studies of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses.
AID1588931Inhibition of Influenza A virus (A/Shanghai/1/2013 (H7N9)) neuraminidase R294K mutant expressed by HEK293 cells incubated for 1 hr using 4-MU-NANA substrate by spectrofluorometric assay12019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases.
AID1226077Inhibition of oseltamivir/amantadine-resistant Influenza A virus (A/Puerto Rico/8/1934(H1N1)) hemagglutinin-mediated hemolysis of chicken RBC at 10 uM preincubated with virus for 30 mins followed by RBC addition measured after 30 mins by microplate reader2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Phenolic diterpenoid derivatives as anti-influenza a virus agents.
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.
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.
AID611767Antiviral activity against Influenza A H3N2 infected in MDCK cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID753436Inhibition of Influenza A virus (A/chicken/Sandong/Li/2008(H9N2)) neuraminidase N2 using 4-MU-NANA as substrate after 5 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Caffeic acid derivatives: a new type of influenza neuraminidase inhibitors.
AID766685Antiviral activity against Influenza B virus infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity2013European journal of medicinal chemistry, Sep, Volume: 67Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity.
AID634750Antiviral activity against Vesicular stomatitis virus infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
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.
AID1222249AUC(0 to infinity) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID766694Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity2013European journal of medicinal chemistry, Sep, Volume: 67Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity.
AID715108Octanol-water partition coefficient, log D of the compound at pH 7.4 at 1 mg after 24 hrs by HPLC analysis2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
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.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1401148Inhibition of Influenza A virus A/California/04/2009(H1N1) neuraminidase using MUNANA as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis and biological evaluation of NH
AID1266217Cytotoxicity against MDCK cells after 72 hrs by XTT assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
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.
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.
AID558675Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in viral replication at 100 ng/ml administered as continuous infusion for 6 days2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
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.
AID1365378Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity treated 2 hrs after virus infection and measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
AID1200485Antiviral activity against influenza A virus A/WSN/33 (H1N1) infected in MDCK cells assessed as inhibition of plaque formation after 3 days at 37 degC2015European journal of medicinal chemistry, Mar-26, Volume: 93Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin.
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).
AID1073045Inhibition of Influenza A virus J/8178/09 neuraminidase by chemiluminescence based assay2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
AID549518Inhibition of Influenza A H9N2 virus neuraminidase activity after 2 hrs by spectrofluorometry2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Chalcones as novel influenza A (H1N1) neuraminidase inhibitors from Glycyrrhiza inflata.
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.
AID1222252AUC(0 to 6 hrs) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1470967Cytotoxicity against MDCK cells after 72 hrs by Alamar-Blue assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors.
AID582038Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 10000 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID539958Antiviral activity against influenza B virus infected in MDCK cells assessed as cell viability after 2 days by MTS assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
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.
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.
AID582067Prodrug conversion in 77 years old male human brain S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID560890Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as mean day to death at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
AID1473438Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 5:1 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]a2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
AID1222269Cmax in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1280361Antiviral activity against oseltamivir-resistant influenza A virus LN/1109 (H1N1) infected in dog MDCK cells assessed as inhibition of virus induced cytopathic effect after 40 hrs by Cell-Titer-Glo assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Spiromastilactones: A new class of influenza virus inhibitors from deep-sea fungus.
AID611769Cytotoxicity against african green monkey Vero cells assessed as alteration of cell morphology after 3 days by microscopy2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID443299Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) in MDCK cells assessed as reduction in plaque number by plaque reduction assay2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
AID443296Inhibition of Influenza Virus A/Brest/IDT7490/08 (H1N1) neuraminidase2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
AID611759Antiviral activity against Coxsackievirus B4 infected in HeLa cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
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.
AID1385612Antiviral activity against Influenza A virus A/95-359 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect2018Journal of natural products, 08-24, Volume: 81, Issue:8
Minor Nortriterpenoids from the Twigs and Leaves of Rhododendron latoucheae.
AID1222281Drug uptake in CHOK1 cells at pH 5 by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1160753Binding affinity to recombinant Influenza A virus (A/Puerto Rico/8/1934(H1N1)) nucleoprotein in culture medium assessed as protection from Influenza A virus H3N2 VR1679-induced MDCK cytocidal activity after 2 days by CellTiter-Glo assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
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.
AID561348Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IFNalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID581741Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 7000 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID561138Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL1alpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1280345Cytotoxicity against MDCK cells after 40 hrs by Celltiter-Glo assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Spiromastilactones: A new class of influenza virus inhibitors from deep-sea fungus.
AID634749Antiviral activity against Vaccinia virus infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1384745Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in C57BL/6J mouse assessed as recovery of weight loss at 8 mg/mouse/day, ip qd treated for 1 day starting at 5 to 10 mins post infection measured up to day 122018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
From Naproxen Repurposing to Naproxen Analogues and Their Antiviral Activity against Influenza A Virus.
AID1460728Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as reduction in virus titer at 10 uM preincubated with virus for 1 hr followed by viral infection measured after 24 hrs by crystal violet staining base2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Boronic Acid Modifications Enhance the Anti-Influenza A Virus Activities of Novel Quindoline Derivatives.
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.
AID581677Terminal half life in non-perfused Sprague-Dawley rat brain at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID558672Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system assessed as decrease in viral replication at 1 ng/ml administered as continuous infusion for 6 days m2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID1588927Inhibition of Influenza A virus (A/California/04/2009 (H1N1) neuraminidase expressed by HEK293 cells incubated for 1 hr using 4-MU-NANA substrate by spectrofluorometric assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases.
AID763863Antiviral activity against Influenza B virus (B/Florida/4/2006) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect by cell-based neutral red uptake assay2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
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).
AID1222239Cmax in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fed conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID416785Antiviral activity against influenza B virus in MDCK cells assessed as reduction of virus-induced cytopathicity by MTS method2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID582081Prodrug conversion in human liver S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222247Tmax in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID286201Antiviral activity against 10^6 EID50 influenza A/turkey/15/06 H5N1 virus inoculated ferrets assessed as increase in temperature at 10 mg/kg twice daily after 24 hrs inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID561136Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL1alpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID582051Prodrug conversion assessed as oseltamivir carboxylate level in presence of Sf9 cell culture supernatant expressing human recombinant HCE1 after 30 mins2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1071443Oral bioavailability in Sprague-Dawley rat at 10 mg/kg by LC-MS/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
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.
AID286190Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as increase in temperature at 25 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID283459Inhibition of increase in lung weight of BALB/c mouse infected with influenza A virus (A/duck/Minnesota/1525/1981 (H5N1)) at 20 mg/kg/day, po twice daily for 5 days administered 1 hr after infection measured on day 6 relative to carboxymethyl cellulose2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID611771Cytotoxicity against human HeLa cells assessed as growth inhibition after 3 days by coulter counting analysis2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
AID539954Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as protection against virus-induced cytopathogenicity after 2 days2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
AID1386755Antiviral activity against oseltamivir-resistant Influenza A virus (H1N1) LN/11092018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
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.
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.
AID674872Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus (A/Guangdong-Luohu/219/2006(H1N1))2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors.
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.
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.
AID542565Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as lung viral titer at 1 mg/kg, po administered 48 hrs postinfection for 5 days measured on day 4 (Rvb = 1 x 10'6 +/- 0.3 x 10'6 PFU2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1222314Drug uptake in CHOK1 cells at 100 uM at pH 4 to 8 after 10 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1713959Cytotoxicity against MDCK cells assessed as cell death incubated for 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Biological evaluation of tetracationic compounds based on two 1,4-diazabicyclo[2.2.2]octane moieties connected by different linkers.
AID1222257AUC(0 to 6 hrs) in adult fed Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID581517Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 618 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID286170Survival of 10 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets at 5 mg/kg after 4 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1773432Selectivity index, ratio of CC50 for cytotoxicity against dog MDCK cells to EC50 for antiviral activity against Influenza A virus H1N1 (A/PR/8/34) infected in MDCK cells assessed as reduction in virus titer treated 1 hr post viral infection followed by re2021European journal of medicinal chemistry, Dec-05, Volume: 225Novel betulin dicarboxylic acid ester derivatives as potent antiviral agents: Design, synthesis, biological evaluation, structure-activity relationship and in-silico study.
AID548442Antiviral activity against Influenza A H3N2 virus subtype infected in MDCK cells assessed as inhibition of virus induced cytopathicity after 2 to 4 days by MTS assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
AID1771094Selectivity index, ratio of CC50 for cytotoxicity against dog MDCK cells to EC50 for antiviral activity against Influenza A virus (A/chicken/Hubei/327/2004(H5N1)) infected in dog MDCK cells
AID392527Antiviral activity against influenza H1N1 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.
AID1432507Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza B virus infected in MDCK cells2017Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
Structure-activity relationship studies of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses.
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.
AID286188Antiviral activity against 10^2 EID50 influenza A/Vietnam/1203/04 H5N1 virus inoculated ferrets assessed as weight loss at 25 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
AID1077004Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus (A/FM/1/1947(H1N1))2014European journal of medicinal chemistry, Apr-09, Volume: 761,2,3-Triazole-containing derivatives of rupestonic acid: click-chemical synthesis and antiviral activities against influenza viruses.
AID561347Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IFNalpha production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID1498139Cytotoxicity against MDCK cells assessed as alteration of cell morphology by microscopic analysis2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
AID582058Prodrug conversion in 7 days old male rat brain S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1160749Antiviral activity against Influenza A virus H3N2 VR1679 infected in MDCK cells assessed as inhibition of virus-induced cytocidal activity compound treated 4 hrs post infection by time of addition assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
AID1167296Inhibition of Influenza A virus H5N1 neuraminidase using 4-methylumbelliferyl-alpha-D-Nacetylneuraminic acid sodium salt hydrate as substrate by fluorometry2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Neuraminidase inhibitory activities of quaternary isoquinoline alkaloids from Corydalis turtschaninovii rhizome.
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.
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.
AID542561Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as time to death at 1 mg/kg, po administered 48 hrs postinfection for 5 days (Rvb = 5.1 days)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID1222262AUC(0 to 5 hrs) in juvenile breast-fed Sprague-Dawley rat at 30 mg/kg, po administered as water solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
AID581706Cmax in perfused Sprague-Dawley rat plasma at 1000 mg/kg, po2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID763858Selectivity index, ratio of CC50 for MDCK cells to EC50 for Influenza B virus (B/Florida/4/2006)2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
AID1432505Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus H3N2 infected in MDCK cells2017Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
Structure-activity relationship studies of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses.
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.
AID1858132Selectivity index, ratio of CC50 for human A549 cells to EC50 for group 2 influenza A virus H3N2 (A/Hong Kong-11/1968) infected in human A549 cells2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-
AID582033Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 100 uM in presence of P-gp inhibitor elacridar2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
AID560891Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 6 postinfection2009Antimicrobial 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.
AID1222274Terminal half life in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fasting conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID1289284Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs by crystal violet staining-based microplate reader analysis2016Journal of natural products, Jan-22, Volume: 79, Issue:1
Antiviral Merosesquiterpenoids Produced by the Antarctic Fungus Aspergillus ochraceopetaliformis SCSIO 05702.
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.
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.
AID1183506Antiviral activity against Influenza A virus A/Texas/48/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
AID581742Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 10000 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID455709Antiviral activity against influenza A virus H1N1 A/PR/8/34 infected in MDCK cells assessed as reduction in fluorescence positive cells at 50 uM immunofluorescence assay2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities.
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.
AID1460723Selectivity index, ratio of CC50 for MDCK cells to IC50 for Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Boronic Acid Modifications Enhance the Anti-Influenza A Virus Activities of Novel Quindoline Derivatives.
AID1280363Antiviral activity against amantadine-resistant influenza A virus HN/1222 (H3N2) infected in dog MDCK cells assessed as inhibition of virus induced cytopathic effect after 40 hrs by Cell-Titer-Glo assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Spiromastilactones: A new class of influenza virus inhibitors from deep-sea fungus.
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.
AID1432504Antiviral activity against Influenza B virus infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 40 hrs2017Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
Structure-activity relationship studies of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses.
AID581678Terminal half life in perfused Sprague-Dawley rat plasma at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1222307Cmax in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID634832Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
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.
AID1222303Cmax in adult fasted Sprague-Dawley rat at 30 mg/kg, po administered as solution in bovine milk by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID582065Prodrug conversion in 42 days old female rat liver S9 fractions assessed as oseltamivir carboxylate generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID558671Antiviral activity against influenza virus (A/Sidney/5/97 (H3N2)) R292 infected in MDCK cells expressing human ST6Gal 1 gene after 48 to 72 hrs by plaque assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
AID561343Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as decrease in virus-induced increase in IL6 production at 20 mg/kg, po BID for 5 days measured on day 3 postinfection2009Antimicrobial 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.
AID634753Antiviral activity against thymidine kinase-positive Varicella Zoster virus Oka infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID350635Antiviral activity against influenza A virus H1N1 A/HK/54/98 in MDCK cells assessed as inhibition of viral replication at 100 uM after 18 hrs by transmission electron microscopy2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
A novel small-molecule inhibitor of the avian influenza H5N1 virus determined through computational screening against the neuraminidase.
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.
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.
AID561135Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in brain at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID473066Inhibition of human neuraminidase 2 at 5 mM2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Complexity in influenza virus targeted drug design: interaction with human sialidases.
AID581683Ratio of AUC (0 to infinity) after iv dose to AUC (0 to 8 hrs) after po dose in non-perfused Sprague-Dawley rat brain at 30 mg/kg2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID286202Antiviral activity against 10^6 EID50 influenza A/turkey/15/06 H5N1 virus inoculated ferrets assessed as viral titer in lungs at 10 mg/kg after 24 hrs of inoculum for 5 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Efficacy of oseltamivir therapy in ferrets inoculated with different clades of H5N1 influenza virus.
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.
AID1415634Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as reduction in viral titer preincubated with cells for 1 hr followed by viral inoculation and measured after 48 hrs by hemagglutination test2017MedChemComm, May-01, Volume: 8, Issue:5
Synthesis and
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.
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.
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.
AID558687Half life in MDCK cells expressing human ST6Gal 1 gene in hollow fiber model system at 1 ng/ml administered as 1 hr infusion every 24 hrs by LC-MS-MS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prediction of the pharmacodynamically linked variable of oseltamivir carboxylate for influenza A virus using an in vitro hollow-fiber infection model system.
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.
AID582082Prodrug conversion in commercial brain S9 fractions assessed as conversion of oseltamivir to oseltamivir carboxylate2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1660682Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in Kunming mouse assessed as decrease in lung IL6 level at 10 mg/kg/day, po starting 4 hrs after viral challenge and continued for 4 days by ELISA2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.
AID1201118Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as cell viability after 72 hrs by MTS assay2015European journal of medicinal chemistry, Apr-13, Volume: 94A few atoms make the difference: synthetic, CD, NMR and computational studies on antiviral and antibacterial activities of glycopeptide antibiotic aglycon derivatives.
AID560896Antiviral activity against Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID763924Antiviral activity against Influenza A virus (A/duck/Minnesota/1525/1981(H5N1)) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect by cell-based neutral red uptake assay2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
AID1432506Selectivity index, ratio of TC50 for MDCK cells to IC50 for Influenza A virus H1N1 infected in MDCK cells2017Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
Structure-activity relationship studies of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses.
AID1365368Antiviral activity against Influenza A virus (A/Puerto Rico/8/1934(H1N1)) infected in MDCK cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
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).
AID1409723Antiviral activity against Influenza A virus A/Udorn/72 H3N2 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect by crystal violet staining based light-microscopic analysis2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Unraveling the Binding, Proton Blockage, and Inhibition of Influenza M2 WT and S31N by Rimantadine Variants.
AID581737Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 700 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID733270Cytotoxicity against MDCK cells after 3 days by fluorescein diacetate-based fluorimetric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Efficient synthesis of 3H,3'H-spiro[benzofuran-2,1'-isobenzofuran]-3,3'-dione as novel skeletons specifically for influenza virus type B inhibition.
AID478325Antiviral activity against influenza B virus assessed as cell viability by cell based MTS assay2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Click reaction synthesis of carbohydrate derivatives from ristocetin aglycon with antibacterial and antiviral activity.
AID542558Antiviral activity against recombinant Influenza A virus (A/WSN/1933(H1N1)) H274Y mutant infected in BALB/c mouse assessed as mortality rate at 1 mg/kg, po administered 4 hrs before infection for 5 days measured on day 5 (Rvb = 100 %)2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Activity of the oral neuraminidase inhibitor A-322278 against the oseltamivir-resistant H274Y (A/H1N1) influenza virus mutant in mice.
AID548439Antiviral activity against Influenza A H1N1 virus subtype infected in MDCK cells assessed as inhibition of virus induced cytopathicity by visual scoring of CPE2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
AID1201122Antiviral activity against Influenza B virus (B/Hong Kong/05/1972) infected in MDCK cells assessed as cell viability after 72 hrs by MTS assay2015European journal of medicinal chemistry, Apr-13, Volume: 94A few atoms make the difference: synthetic, CD, NMR and computational studies on antiviral and antibacterial activities of glycopeptide antibiotic aglycon derivatives.
AID581710AUC (0 to 8 hrs) ratio in cerebrospinal fluid to brain in perfused Sprague-Dawley rat at 1000 mg/kg, po2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID560888Antiviral activity against Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) infected in BALB/c mouse assessed as mean day to death at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
AID1498125Antiviral activity against Influenza B virus infected in MDCK cells assessed as inhibition of virus-induced cytopathicity by MTS assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
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.
AID1473448Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 5:1 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]a2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
AID478324Antiviral activity against influenza B virus assessed as inhibition of viral induced cytopathic effect2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Click reaction synthesis of carbohydrate derivatives from ristocetin aglycon with antibacterial and antiviral activity.
AID733266Antiviral activity against Influenza B virus (B/Taiwan/2/62) infected in MDCK cells assessed as inhibition of virus-induced cytopathogenicity at 1 hr post-infection measured after 3 days by fluorescein-diacetate based fluorimetric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Efficient synthesis of 3H,3'H-spiro[benzofuran-2,1'-isobenzofuran]-3,3'-dione as novel skeletons specifically for influenza virus type B inhibition.
AID1222271AUC(0 to 5 hrs) in juvenile fasted Sprague-Dawley rat at 30 mg/kg, po administered as 125 mM aqueous Gly-Sar solution by HPLC-tandem mass spectrometry2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID528273Inhibition of influenza A virus H9N2 Neuraminidase using 4-methylumbelliferyl-alpha-D-N-acetylneuraminic acid sodium salt hydrate substrate2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
New stilbenoid with inhibitory activity on viral neuraminidases from Erythrina addisoniae.
AID1473451Synergistic antiviral activity against Influenza A virus (A/WSN/33(H1N1)) infected in MDCK cells expressing ST6Gal-1 assessed as reduction in virus-induced cytopathic effect after 44 to 48 hrs in presence of 1:10 3-{[(5-Cyclopropyl-1,2-oxazol-3-yl)methyl]2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
AID1403781Antiviral activity against Influenza A virus (A/WSN/1933(H1N1)) infected in BALB/c mouse assessed as mouse survival at 0.96 umol/day, po for 5 consecutive days measured on day 14 post dose2018European journal of medicinal chemistry, Feb-10, Volume: 145Peramivir conjugates as orally available agents against influenza H275Y mutant.
AID1073034Inhibition of Clostridium perfringens neuraminidase by fluorescence based assay2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Computer-guided approach to access the anti-influenza activity of licorice constituents.
AID1200495Antiviral activity against OSV-resistant influenza A virus A/LiaoNing-ZhenXing/1109/2010 (H1N1) strain2015European journal of medicinal chemistry, Mar-26, Volume: 93Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin.
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]
AID443294Inhibition of Influenza Virus A/Belzig/2/01 (H1N1) neuraminidase2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
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.
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.
AID1460754Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in Kunming mouse assessed as survival rate at 20 mg/kg/day, po qd for 7 days measured on day 14 post infection (Rvb = 30%)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Boronic Acid Modifications Enhance the Anti-Influenza A Virus Activities of Novel Quindoline Derivatives.
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.
AID634835Antiviral activity against Felid herpesvirus 1 infected in CrFK cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
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.
AID1183508Antiviral activity against Influenza A virus A/California/07/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
AID443829Antiviral activity against Influenza A virus (A/Hong Kong/7/87(H3N2)) assessed as inhibition of virus-induced cytopathic effect by cell-based assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Diazo transfer-click reaction route to new, lipophilic teicoplanin and ristocetin aglycon derivatives with high antibacterial and anti-influenza virus activity: an aggregation and receptor binding study.
AID634836Antiviral activity against Feline coronavirus infected in CrFK cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
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.
AID658748Antiviral activity against Influenza B virus infected in MDCK cells assessed as reduction visual scoring of virus-induced cytopathogenicity after 4 days2012European journal of medicinal chemistry, Jun, Volume: 522-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
AID1222279Drug uptake in CHOK1 cells at 5 to 100 uM after 10 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID561122Antiviral activity against Influenza A virus (A/duck/Laos/25/2006(H5N1)) infected in BALB/c mouse assessed as virus-induced change body weight at 20 mg/kg, po BID for 5 days measured on day 15 postinfection2009Antimicrobial 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.
AID582049Inhibition of human MDR1-mediated digoxin permeability expressed in pig LLC-PK1 cells2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
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.
AID416778Cytotoxicity against MDCK cells assessed as drug level causing microscopically detectable alteration of normal cell morphology2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID443293Inhibition of Influenza Virus A/Potsdam/15/81 (H1N1) neuraminidase2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
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).
AID1401147Inhibition of Influenza A virus A/Anhui/1/2005(H5N1) neuraminidase at 100 uM using MUNANA as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 30 mins by fluorescence assay relative to control2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis and biological evaluation of NH
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.
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.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID581709AUC (0 to 8 hrs) ratio in brain to plasma in perfused Sprague-Dawley rat at 1000 mg/kg, po2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1505284Antiviral activity against Influenza A virus (A/Aichi/2/68 (H3N2)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by microscopic analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
AID283471Effect on weight change in BALB/c mouse at 20 mg/kg/day, po measured after 18 hrs of final treatment2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice.
AID634752Antiviral activity against Human cytomegalovirus Davis infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1858131Antiviral activity against group 2 influenza A virus LPAI H7N7 (A/Netherlands/219/2003) infected in human A549 cells assessed as inhibition of viral entry preincubated with compound for 30 mins followed by viral infection for 1 hour further incubated for 2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-
AID1612769Antiviral activity against Influenza A virus A/WSN/33/H1N1 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 40 hrs by CellTiter-Glo assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis, structure activity relationship and in vitro anti-influenza virus activity of novel polyphenol-pentacyclic triterpene conjugates.
AID611629Antiviral activity against VSV infected in HEL cells assessed as protection against virus-induced cytopathicity2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
New prodrugs of Adefovir and Cidofovir.
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.
AID581530Cmax in non-perfused Sprague-Dawley rat brain at 30 mg/kg, iv2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID634746Antiviral activity against Herpes simplex virus 1 KOS infected in human HEL cells assessed as inhibition of viral plaque formation at 250 uM2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
AID1167295Inhibition of recombinant Influenza A virus H1N1 neuraminidase using 4-methylumbelliferyl-alpha-D-Nacetylneuraminic acid sodium salt hydrate as substrate by fluorometry2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Neuraminidase inhibitory activities of quaternary isoquinoline alkaloids from Corydalis turtschaninovii rhizome.
AID1222235AUC(0 to 24 hrs) in healthy human at 150 mg, po administered as single dose by HPLC-tandem mass spectrometry under fasting conditions2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
AID416782Antiviral activity against influenza H3N2 virus in MDCK cells assessed as reduction of virus-induced cytopathicity by visual cytopathic effect scoring method2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID560889Antiviral activity against Influenza A virus (A/whooper swan/Mongolia/1/2009(H5N1)) infected in BALB/c mouse assessed as mean day to death at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
AID561126Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as decrease in viral load in lung at 20 mg/kg, po BID for 5 days measured on day 9 postinfection2009Antimicrobial 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.
AID1222280Drug uptake in CHOK1 cells expressing human PEPT1 at 5 to 100 uM after 10 mins by HPLC coupled with radiodetection analysis2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
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.
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.
AID581527Prodrug conversion in 7 days old male rat brain S9 fractions assessed as paranitrophenol generation rate assessed per mg of protein per min2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
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.
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.
AID1427858Cytotoxicity against MDCK cells assessed as growth inhibition after 48 hrs
AID1372137Cytotoxicity against MDCK cells infected with Influenza A virus (A/WSN/33(H1N1)) after 72 hrs by CellTiter-Glo assay2017Bioorganic & medicinal chemistry letters, 12-15, Volume: 27, Issue:24
Design, synthesis and biological evaluation of novel oseltamivir derivatives as potent neuraminidase inhibitors.
AID560887Antiviral activity against Influenza A virus (A/Turkey/651242/2006(H5N1)) infected in BALB/c mouse assessed as mean day to death at 20 mg/kg, po BID for 5 days measured post last dose2009Antimicrobial 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.
AID1386761Antiviral activity against influenza A virus assessed as inhibition of viral replicon activity up to 100 uM incubated for 30 hrs by firefly luciferase reporter gene assay2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1617174Invivo antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in BALB/c mouse assessed as survival rate at 10 mg/kg, po administered bid for 10 days after 48 hrs post infection and observed for 21 days relative to control2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region.
AID581732Permeability from apical to basolateral side of pig LLC-PK1 cells over expressing human MDR1 at 6918 uM2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
AID1156849Inhibition of Influenza A H1N1 virus neuraminidase at 0.8 nM after 1 hr by spectrofluorimetry using 2-(4-meythylumbelliferyl)-alpha-D-acetylneuramic acid as substrate2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
AID1505285Antiviral activity against Influenza A virus (A/duck/Guangdong/1/1996 (H7N3)) infected in MDCK cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by microscopic analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
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.
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.
AID1803041Neuraminidase Activity Assay from Article 10.3109/14756366.2011.568415: \\A screening assay for neuraminidase inhibitors using neuraminidases N1 and N3 from a baculovirus expression system.\\2012Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 27, Issue:1
A screening assay for neuraminidase inhibitors using neuraminidases N1 and N3 from a baculovirus expression system.
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.
AID1803040Neuraminidase Inhibition Assay from Article 10.3109/14756366.2011.568415: \\A screening assay for neuraminidase inhibitors using neuraminidases N1 and N3 from a baculovirus expression system.\\2012Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 27, Issue:1
A screening assay for neuraminidase inhibitors using neuraminidases N1 and N3 from a baculovirus expression system.
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.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,250)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's34 (1.05)18.2507
2000's850 (26.15)29.6817
2010's1966 (60.49)24.3611
2020's400 (12.31)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 115.88

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 Index115.88 (24.57)
Research Supply Index8.18 (2.92)
Research Growth Index5.90 (4.65)
Search Engine Demand Index215.92 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (115.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials186 (5.52%)5.53%
Reviews346 (10.27%)6.00%
Case Studies367 (10.90%)4.05%
Observational43 (1.28%)0.25%
Other2,426 (72.03%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (134)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomised Controlled Trial on the Effect of Post-exposure Oseltamivir Prophylaxis on Influenza Transmission in Nursing Homes [NCT01053377]Phase 4900 participants (Anticipated)Interventional2009-12-31Enrolling by invitation
An Observational Study on the Pharmacokinetics of Oseltamivir in the Treatment of Influenza During Lactation, Phase IV Trial [NCT01130636]Phase 46 participants (Actual)Interventional2010-06-30Completed
A Randomized, Open-label, Single-Dose, Two-Period, Crossover Study to Evaluate the Bioequivalence of Over-encapsulated Oseltamivir Capsules to Marketed Oseltamivir Capsules in Healthy Volunteers [NCT01258530]Phase 128 participants (Actual)Interventional2010-12-20Completed
Oseltamivir Versus Paracetamol for Influenza-like Illness During the Influenza Season: a Randomized Controlled Trial [NCT03754686]Phase 4436 participants (Anticipated)Interventional2019-02-10Not yet recruiting
A Multicenter, Randomized, Double-Blind, Active (Oseltamivir)-Controlled Study to Assess the Safety, Pharmacokinetics, and Efficacy of Baloxavir Marboxil in Otherwise Healthy Pediatric Patients 1 to <12 Years of Age With Influenza-Like Symptoms [NCT03629184]Phase 3173 participants (Actual)Interventional2018-11-20Completed
A Phase 3, Multicenter, Randomized, Double-blind Study of a Single Dose of S-033188 (Baloxavir Marboxil) Compared With Placebo or Oseltamivir 75 mg Twice Daily for 5 Days in Otherwise Healthy Patients With Influenza [NCT02954354]Phase 31,436 participants (Actual)Interventional2016-12-08Completed
Duration of Prophylactic Treatment With Oseltamivir: A Randomized Clinical Trial [NCT03899571]222 participants (Actual)Interventional2019-01-22Completed
A Double-blind Randomised Controlled Trial on Flufenamic Acid for Hospitalised Influenza Infection [NCT03238612]Phase 2200 participants (Anticipated)Interventional2018-01-08Recruiting
A Phase 3, Multicenter, Randomized, Double-blind Study of a Single Dose of S-033188 Compared With Placebo or Oseltamivir 75 mg Twice Daily for 5 Days in Patients With Influenza at High Risk of Influenza Complications [NCT02949011]Phase 32,184 participants (Actual)Interventional2017-01-11Completed
Phase 2b, Multicenter, Randomized, Double-blind Study to Evaluate the Efficacy and Safety of IV VIS410 in Addition to Oseltamivir Compared With Oseltamivir Alone in Hospitalized Adults With Influenza A Infection Requiring Oxygen Support [NCT03040141]Phase 289 participants (Actual)Interventional2018-01-03Completed
Convalescent Plasma Treatment in Patients With Severe 2009 H1N1 Infection: a Prospective Cohort Study [NCT01306773]80 participants (Actual)Interventional2009-12-31Completed
A Randomized Controlled Trial on the Treatment of Severe Influenza A Infection [NCT02108366]Phase 3107 participants (Actual)Interventional2014-03-31Completed
A Phase II, Global, Randomized Study to Evaluate the Efficacy and Safety of Danirixin (GSK1325756) Co-administered With a Standard-of-care Antiviral (Oseltamivir), in the Treatment of Adults Hospitalized With Influenza [NCT02927431]Phase 210 participants (Actual)Interventional2017-01-19Terminated(stopped due to The study was stopped early due to lack of enrollment.)
A Phase 1/2a Clinical Study to Evaluate the Efficacy of MEDI8852 in the Treatment of Influenza in Adults Challenged With a Wild-Type Influenza Strain [NCT03903718]Phase 20 participants (Actual)Interventional2020-04-03Withdrawn(stopped due to Terminated due to delay in site enrollment timelines)
Phase I, Open-Label Study to Evaluate Potential Pharmacokinetic of Orally Administered Oseltamivir in Healthy Obese Thai Adult Subjects [NCT01049763]Phase 124 participants (Actual)Interventional2010-01-31Completed
Comparative Open-label,Randomized, Fasting, Single Dose, Two-way Crossover Bioequivalence Study of Oseltamivir From Oseltamivir 75 mg Caps (Pharmacare PLC, Palestine) and Tamiflu® 75 mg Caps (Hoffmann-La Roche, Switzerland) [NCT02507648]Phase 124 participants (Actual)Interventional2013-03-31Completed
Banlangen Granules Anti-seasonal Influenza Study: a Randomized, Double Blind, Positive and Placebo Controlled,Clinical Study. [NCT02232945]Phase 4177 participants (Anticipated)Interventional2012-04-30Recruiting
A Randomized Open Label Study Comparing the Efficacy, Safety, and Tolerability of Oral Administration of Amantadine and Ribavirin With Oseltamivir Versus Oseltamivir to Influenza A Virus Infected Immunocompromised Subjects [NCT00979251]Phase 22 participants (Actual)Interventional2009-09-30Completed
An Adaptive Study of the Pharmacokinetics of Favipiravir in Patients With Severe [NCT03394209]Phase 234 participants (Actual)Interventional2018-02-06Completed
A Randomized Controlled Trial of Oseltamivir in Outpatients With Chronic Pulmonary Disease: a Pilot Study [NCT02282384]Phase 40 participants (Actual)Interventional2014-10-31Withdrawn(stopped due to Sites were unable to recruit participants)
A Randomized Controlled Trial of Oseltamivir in High-Risk Patients Presenting to the Emergency Department With Influenza [NCT02561169]Phase 41 participants (Actual)Interventional2015-12-31Terminated
Indian Herbal Medicine for Influenza - Randomized Controlled Study [NCT03365336]100 participants (Anticipated)Interventional2018-02-01Recruiting
A Randomized, Multicenter Trial of Oseltamivir [Tamiflu] Doses of 75 mg for 5 or 10 Days Versus 150 mg for 5 or 10 Days to Evaluate the Effect on the Duration of Viral Shedding in Influenza Patients With Pandemic (H1N1) 2009 [NCT01032837]Phase 4102 participants (Actual)Interventional2009-11-30Terminated(stopped due to Study closed prematurely due to the end of the influenza (H1N1) 2009 pandemic)
Pilot Study of Interferon Alpha Lozenges Plus Oseltamivir in the Treatment of Influenza A Infection [NCT01146535]Phase 240 participants (Actual)Interventional2011-01-31Completed
A Multicenter, Randomized, Open Label, Add-on Study to Assess Efficacy and Safety of Xiyanping Injection in Pediatric Participants With Severe Influenza-Like Symptoms [NCT03947411]72 participants (Anticipated)Interventional2019-03-04Recruiting
Prospective, Randomized, Parallel-Group, Open-Label Study to Evaluate the Efficacy and Safety of IMU-838, in Combination With Oseltamivir, in Adults With COVID-19 [NCT04516915]Phase 238 participants (Actual)Interventional2020-06-15Completed
An Open-label, Randomized, Single-dose Crossover Study to Evaluate the Pharmacokinetics of HIP1403 in Healthy Male Subjects [NCT02473900]Phase 132 participants (Actual)Interventional2015-04-30Completed
Validation of the Efficiency of Molecules Reproposed on the Basis of Their Cellular Transcriptomic Signature, Antagonist of the Signature Determined in Infection Due to Virus Influenza A. [NCT03212716]Phase 285 participants (Actual)Interventional2017-12-23Terminated(stopped due to rate of inclusion and study affected by covid-19 epidemic)
A Randomized Double-Blind Study Comparing Oseltamivir Versus Placebo for the Treatment of Influenza in Low Risk Adults [NCT01314911]716 participants (Actual)Interventional2011-04-30Completed
Efficacy of Different Regimens in Influenza Postexposure Chemoprophylaxis With Oral Neuraminidase Inhibitor in Children [NCT04297462]50 participants (Anticipated)Interventional2016-11-17Recruiting
Reduning Injection for the Treatment of Influenza in Children:a Randomized, Double-blinded, Parallel-controlled Clinical Study [NCT04183725]Phase 4240 participants (Anticipated)Interventional2019-12-01Not yet recruiting
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 Clinical Trial to Investigate the Influence of CES1 Polymorphism on Pharmacokinetic Characteristics of Oseltamivir in Healthy Korean Volunteers [NCT01902342]Phase 120 participants (Actual)Interventional2013-07-31Completed
A Phase 1, Randomized, 3-way Crossover, Open-label Study to Assess the Drug-drug Interaction Between VX-787 and Tamiflu®, Followed by a Double-blind, Randomized, Placebo-controlled Study to Collect Safety, Tolerability and Pharmacokinetics of VX-787, in H [NCT02262715]Phase 138 participants (Actual)Interventional2014-07-31Completed
A Phase III, Randomized, Double-Blind, Placebo-Controlled Trial to Evaluate the Efficacy and Safety of Nitazoxanide and Nitazoxanide Plus Oseltamivir in the Treatment of Acute Uncomplicated Influenza [NCT01610245]Phase 31,941 participants (Actual)Interventional2013-03-31Completed
A Randomized Double-blind Controlled Study of CS-8958 Versus Oseltamivir Phosphate in Patients With Influenza Virus Infection [NCT00803595]Phase 31,002 participants (Actual)Interventional2008-11-30Completed
A Randomized, Double-blind, Placebo Controlled Study to Evaluate the Safety, Tolerability and Clinical Effect of Oral Danirixin (GSK1325756) in the Treatment of Healthy Adults With Acute, Uncomplicated Influenza (201682) [NCT02469298]Phase 245 participants (Actual)Interventional2015-06-01Completed
A Four-part, Single-center, Open-label, Phase I Clinical Study to Evaluate the Drug-drug Interactions (DDIs) Between GP681 and Rosuvastatin/Digoxin/Itraconazole/Oseltamivir in Chinese Healthy Volunteers [NCT05789342]Phase 154 participants (Actual)Interventional2023-02-15Completed
Evaluation of The Efficacy of Triazavirin Versus Oseltamivir in Egyptian Patients Infected With Coronavirus Disease 2019 (COVID-19) [NCT04973462]Phase 480 participants (Anticipated)Interventional2021-08-01Recruiting
Randomized Double-blind, Placebo-controlled Single Center Pilot Study to Evaluate the Efficacy and Safety of Baloxavir in Combination With Oseltamivir in Adult Allogeneic Bone Marrow Transplant Recipients With Influenza [NCT05170009]Phase 2/Phase 330 participants (Anticipated)Interventional2022-04-22Recruiting
[NCT02572583]Phase 1/Phase 2300 participants (Anticipated)Interventional2014-11-30Recruiting
A Double-Blind, Randomized, Stratified Multi-Center Trial Evaluating Conventional and Double Dose Oseltamivir in the Treatment of Immunocompromised Patients With Influenza [NCT00545532]Phase 3228 participants (Actual)Interventional2008-02-04Completed
A Pharmacokinetic/Pharmacodynamic and Safety Evaluation of Oseltamivir (Tamiflu®) for the Treatment of Children Less Than 24 Months of Age With Confirmed Influenza Infection (CASG 114) [NCT00391768]Phase 1/Phase 287 participants (Actual)Interventional2007-01-31Completed
Phase II, Multicenter, Randomized, Double-Mask, Double-Dummy Study Comparing Efficacy and Safety of Intravenous Peramivir Once Daily Versus Oral Oseltamivir Twice Daily in Adults With Acute Serious or Potentially Life-Threatening Influenza [NCT00453999]Phase 2137 participants (Actual)Interventional2007-07-31Completed
Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia [NCT02735707]Phase 310,000 participants (Anticipated)Interventional2016-04-11Recruiting
Antiviral and Chinese Medicinal Herbs Treatment on Novel Influenza A (H1N1) Virus Pneumonia: Multi-centre, Prospective, Randomized Controlled Study [NCT00936013]Phase 4400 participants (Anticipated)Interventional2009-08-31Recruiting
Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs [NCT04278404]5,000 participants (Anticipated)Observational2020-03-05Recruiting
A Double-blind, Randomized, Placebo Controlled, Multi-center Trial of Oseltamivir for the Seasonal Prophylaxis of Influenza in Immunocompromised Patients [NCT00412737]Phase 4477 participants (Actual)Interventional2007-01-31Completed
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)
Initiating Oseltamivir in Adults Hospitalized With Influenza -- a Study on the Impact of Virological Clearance and Clinical Recovery for Higher-dose Treatment Started Within 96 Hours [NCT01052961]Phase 4157 participants (Actual)Interventional2010-01-31Completed
A Multicenter Study of the Safety of Oseltamivir Administered Intravenously for the Treatment of Influenza in Patients Aged Greater Than or Equal to 13 Years [NCT01050257]Phase 3118 participants (Actual)Interventional2010-01-31Completed
Influenza Resistance Information Study (IRIS) [NCT00884117]4,561 participants (Actual)Observational2009-01-31Completed
Efficacy of Clarithromycin-Naproxen-Oseltamivir Combination Therapy vs. Oseltamivir Alone for Hospitalised Paediatric Influenza Patients [NCT04315194]54 participants (Actual)Observational [Patient Registry]2017-12-18Completed
A Single-Center, Randomized, Double-Blind, Single and Multiple Doses, Placebo-Controlled Study,To Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics, Food Effects of HEC116094HCl•3H2O and the Interaction With Oseltamivir Phosphate Capsules [NCT04982913]Phase 1118 participants (Actual)Interventional2021-08-24Completed
A Randomized Controlled Trial of Adjunctive Sirolimus and Oseltamivir Versus Oseltamivir Alone for Treatment of Influenza [NCT03901001]Phase 3160 participants (Anticipated)Interventional2023-05-08Recruiting
A Study of the Pharmacology of Oseltamivir (Tamiflu) in Pregnancy [NCT00873886]Phase 10 participants (Actual)Interventional2009-04-30Withdrawn(stopped due to We will focus on other Tamiflu research studies. No subjects were enrolled.)
A Phase IIIb, Open-label, Comparative, Randomized Study on Resistance of Influenza A/H1N1 2009 Virus to Treatment With Oseltamivir at Standard Dose Versus Double Dose [NCT00949533]Phase 337 participants (Actual)Interventional2009-08-31Completed
Antiviral and Chinese Medicinal Herbs Treatment on Novel Influenza A (H1N1) Virus Infection: Multi-centre, Prospective, Randomized Controlled Study [NCT00935194]Phase 4102 participants (Actual)Interventional2009-07-31Completed
An Open Label, Prospective, Pharmacokinetic/Pharmacodynamic and Safety Evaluation of Intravenous Oseltamivir (Tamiflu) in the Treatment of Children 1 to 12 Years of Age With Influenza Infection [NCT01033734]Phase 18 participants (Actual)Interventional2010-12-31Completed
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
A Study of the Relative Oral Bioavailability of the Antiflu Medicine Oseltamivir (Tamiflu®) in Patients in the Intensive Care Unit [NCT00844155]0 participants (Actual)Interventional2009-03-31Withdrawn(stopped due to Study has been withdrawn as the H1N1 epidemic made this study redundant)
An Open, Prospective/Retrospective, Randomized Controlled Cohort Study to Compare the Efficacy of Three Antiviral Drugs(Abidol Hydrochloride, Oseltamivir and Lopinavir/Ritonavir) in the Treatment of 2019-nCoV Pneumonia. [NCT04255017]Phase 4400 participants (Anticipated)Interventional2020-02-01Recruiting
Randomized, Double-Blinded, Oseltamivir-and-Placebo-Controlled Clinical Study About Lingdancao Granules in the Treatment of Seasonal Influenza [NCT02662426]Phase 3318 participants (Anticipated)Interventional2016-04-30Not yet recruiting
Pharmacokinetics of Oseltamivir in Newborns and Infants [NCT01388439]19 participants (Actual)Observational2011-01-31Completed
Study on the Human Bioequivalence of Oseltamivir Phosphate For Oral Suspension [NCT05297968]Phase 172 participants (Actual)Interventional2021-05-13Completed
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
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)
Oseltamivir Treatment in Children Under One Year of Age With Moderate or Severe Influenza Lower Respiratory Tract Infection - a Clinical and Pharmacokinetic Study [NCT01037634]Phase 20 participants (Actual)Interventional2010-03-31Withdrawn
"A Randomized, Double-Blinded Controlled Trial Comparing High vs Standard Dose Oseltamivir in Severe, Influenza Infection in ICU. ROSII Study" [NCT01010087]Phase 259 participants (Actual)Interventional2009-11-30Terminated(stopped due to Patient population no longer available.)
Efficacy of Combination Baloxovir and Oseltamivir Therapy in Influenza Infected Immunocompromised Hosts [NCT04712539]Phase 260 participants (Anticipated)Interventional2021-10-11Recruiting
A Multicenter Randomized Open-label Study of Oseltamivir Combined With High-dose Dexamethasone Versus High-dose Dexamethasone in the Management of Immune Thrombocytopenia [NCT01965626]Phase 296 participants (Actual)Interventional2016-02-01Completed
A Randomized, Double-Blind, Placebo-Controlled, Phase 2a Study in Healthy Volunteers to Evaluate the Efficacy and Safety of MHAA4549A in an Influenza Challenge Model [NCT01980966]Phase 2101 participants (Actual)Interventional2013-11-25Completed
An Open-label, Multiple Dose, Randomized, Three-period Crossover Study in Healthy Subjects to Evaluate the Effect of Co-administration of Oseltamivir (Ro 64-0796) 75 mg Twice Daily and Rimantadine 100 mg Twice Daily on the Pharmacokinetic Properties of Os [NCT01172847]Phase 124 participants (Actual)Interventional2009-08-31Completed
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
The Effectivity and Safety of Favipiravir Compared to Oseltamivir as Adjuvant Therapy for COVID-19: An Open Label Trial [NCT04558463]Phase 3100 participants (Anticipated)Interventional2020-04-16Recruiting
Oseltamivir and Oseltamivir Carboxylate Pharmacokinetics in Obese Adults [NCT01179919]Phase 1/Phase 221 participants (Actual)Interventional2010-07-31Completed
Efficacy of Sofosbuvir Plus Ledipasvir in Egyptian Patients With COVID-19 Compared to Standard Treatment [NCT04530422]Phase 3250 participants (Actual)Interventional2020-04-15Completed
A Double-Blind, Randomized, Placebo-Controlled Study of Early Oseltamivir Treatment of Influenza in Children 1-3 Years of Age [NCT00593502]Phase 4409 participants (Actual)Interventional2008-02-29Completed
A Randomized,Open,Controlled Small Sample Clinical Study to Evaluate the Efficacy and Safety of ASC09/Ritonavir Compound Tablets and Ritonavir for 2019-nCoV Pneumonia [NCT04261270]Phase 360 participants (Anticipated)Interventional2020-02-01Recruiting
Efficacy of Oseltamivir in Reducing the Duration of Clinical Illness, Viral Shedding, and Transmissibility Reduction Within Households Among Participants in an Influenza Disease Burden Surveillance Cohort in Urban Dhaka, Bangladesh [NCT00707941]Phase 31,190 participants (Actual)Interventional2008-05-31Completed
A Phase-1, Open-label, Four Group, Fixed-Sequence Study to Evaluate the Effect of AL-794 on the Pharmacokinetics of Oseltamivir, JNJ-63623872, and Probes for P-glycoprotein, CYP3A and OATP1B1 in Healthy Volunteers [NCT02888327]Phase 168 participants (Actual)Interventional2016-07-31Completed
An Open-label, Prospective, Pharmacokinetic/Pharmacodynamic and Safety Evaluation of Intravenous Oseltamivir in the Treatment of Infants Less Than One Year of Age With Influenza Infection [NCT01053663]Phase 19 participants (Actual)Interventional2011-01-31Terminated(stopped due to The study was terminated prematurely after three influenza seasons.)
Evaluation of Alternative Oseltamivir (Tamiflu[R]) Dosing Strategies for Use During Influenza Prophylaxis [NCT00334529]Phase 248 participants Interventional2006-06-05Completed
An Open-label Study to Evaluate the Efficacy of Neuraminidase Inhibitor Treatment in ST-Elevation Myocardial Infarction (STEMI) Patients [NCT04684498]Phase 4382 participants (Anticipated)Interventional2020-03-01Recruiting
Oseltamivir Pharmacokinetics in Morbid Obesity [NCT01002729]20 participants (Actual)Interventional2009-11-30Completed
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
A Phase 2b, Randomized, Double-Blind, Placebo Controlled, Parallel-Group, Multicenter Study of 2 Dose Levels of VX 787 Administered as Monotherapy and One Dose Level of VX-787 Administered in Combination With Oseltamivir for the Treatment of Acute Uncompl [NCT02342249]Phase 2292 participants (Actual)Interventional2014-12-11Completed
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)
An Open-label, Randomized 2-period Crossover Study to Investigate the Pharmacodynamics, Pharmacokinetics, Safety and Tolerability of Warfarin in Combination With Oseltamivir in Volunteers Stabilized on Warfarin Therapy [NCT02780622]Phase 420 participants (Actual)Interventional2008-02-29Completed
Pharmacologic Study of Oseltamivir in Healthy Volunteers [NCT00439530]Phase 121 participants (Actual)Interventional2006-11-30Completed
Randomised, Open-label, Multi-Centre, Phase IV Study Assessing the Effect of Oseltamivir Treatment on Cognitive Function in Subjects With Confirmed Influenza Virus Infection [NCT01249833]Phase 4122 participants (Actual)Interventional2010-11-30Completed
A Randomized Double-Blind Phase 2 Study Comparing the Efficacy, Safety, and Tolerability of Combination Antivirals (Amantadine, Ribavirin, Oseltamivir) Versus Oseltamivir for the Treatment of Influenza in Adults at Risk for Complications [NCT01227967]Phase 2881 participants (Actual)Interventional2010-09-30Completed
An Open-Label, Multiple Dose, Randomized, Three-Period Crossover Study in Healthy Volunteers to Evaluate the Effect of co-Administration of Amantadine 100 mg BID and Oseltamivir 75 mg BID on the Pharmacokinetic Properties of Amantadine and Oseltamivir. [NCT00416962]Phase 118 participants Interventional2006-08-31Completed
Title: Effectiveness of Empiric Antiviral Treatment for Hospitalized Community Acquired Pneumonia During the Influenza Season (U18) [NCT01248715]Phase 41,107 participants (Actual)Interventional2010-11-30Completed
A Randomized, Open Label Study to Evaluate the Effect of Tamiflu on Viral Shedding and on Serum and Cytoplasmic Inflammatory Cytokine Concentrations in Patients With Laboratory-confirmed Influenza [NCT00436124]Phase 40 participants Interventional2007-01-31Terminated(stopped due to poor recruitment, no patients were enrolled)
An Open-label, Randomized, Single-dose Crossover Study to Evaluate the Pharmacokinetics of HIP1403 in Healthy Male Subjects [NCT02941731]Phase 132 participants (Actual)Interventional2015-04-30Completed
SEA022 Oseltamivir Treatment in Children Under One Year of Age With Moderate or Severe Influenza Lower Respiratory Tract Infection - a Clinical and Pharmacokinetic Study. [NCT01546935]Phase 2/Phase 30 participants (Actual)Interventional2012-12-31Withdrawn(stopped due to Study drugs (Oseltamivir suspension from Roche) were unavailable)
Comparative Effectiveness of Baloxavir Versus Oseltamivir for Influenza Outbreak Management in U.S. Nursing Homes [NCT05012189]Phase 41,000 participants (Anticipated)Interventional2021-08-06Active, not recruiting
An Open-label Multi-center Trial of Oseltamivir for the Seasonal Prophylaxis of Influenza in Children. [NCT00412555]Phase 452 participants (Actual)Interventional2006-12-31Completed
Pakistan Randomized and Observational Trial to Evaluate Coronavirus Treatment [NCT04338698]Phase 3550 participants (Actual)Interventional2020-04-22Completed
A Phase 1, Open-label, Randomized, Crossover Study in Two Panels of Healthy Adult Subjects to Assess the Relative Oral Bioavailability of a Single Dose of JNJ-63623872/Oseltamivir Fixed-dose Combination Tablet and Single Agent Concept Formulations of JNJ- [NCT03023852]Phase 145 participants (Actual)Interventional2017-02-14Completed
Monitoring Influenza Severity on Tamiflu (MIST) [NCT00555893]194 participants (Actual)Interventional2008-01-31Completed
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
Randomized, Open Label, Balanced, Two-Treatment, Two-Period, Two-Sequence, Single Dose, Crossover, Bioequivalence Study of Oseltamivir Phosphate 75 mg Capsule of Yangtze River Pharmaceutical (Group) Co., Ltd., China and TAMIFLU® (Oseltamivir Phosphate) Ca [NCT04536415]Phase 496 participants (Actual)Interventional2020-08-25Completed
Oseltamivir (Tamiflu) Dosing Strategies for Use During Influenza Prophylaxis (VA01) [NCT00304434]Phase 448 participants (Anticipated)Interventional2005-02-28Completed
Efficacy of Early Oseltamivir Phosphate Treatment at Hospital Admission to Reduce Severity of Illness Among Children Aged Less Than 10 Years Hospitalized With Influenza in El Salvador and Panama [NCT01690637]Phase 4721 participants (Actual)Interventional2012-09-30Terminated(stopped due to Slower than anticipated participant accrual)
Inhibition of Carboxylesterase Metabolism by Ethanol [NCT01708369]Phase 119 participants (Actual)Interventional2012-02-29Completed
An Open-Label, Randomized, Adaptive, Two-Arm, Multicenter Trial to Evaluate Pharmacokinetics And Pharmacodynamics of Two Doses of Oseltamivir (Tamiflu®) in The Treatment Of Influenza in Immunocompromised Children Less Than 13 Years Of Age, With Confirmed [NCT01715909]Phase 120 participants (Anticipated)Interventional2014-01-22Completed
Multicentre Open Label Comparative Parallel-group Randomized Clinical Trial of Clinical Efficiency and Safety of Ergoferon in Treatment of Influenza [NCT01804946]Phase 4161 participants (Actual)Interventional2011-02-28Completed
A Phase 1, Open-Label, Three-Period, Single-center Study to Assess the Pharmacokinetic Interactions Between ZSP1273 and Oseltamivir in Healthy Subjects [NCT05108051]Phase 136 participants (Actual)Interventional2020-11-19Completed
Characterisation of the Human Carboxylesterase 1 (CES1) Mutation(s) Which May be Responsible for Markedly Reduced Conversion of Oseltamivir Phosphate to Oseltamivir Carboxylate [NCT01443806]Phase 41 participants (Actual)Interventional2011-07-31Completed
Pharmacokinetics of Tamiflu® (Oseltamivir) in Patients Receiving CVVHD and/or ECMO [NCT01048879]Phase 415 participants (Actual)Interventional2009-10-31Completed
An Open Label, Prospective, Pharmacokinetic/Pharmacodynamic and Safety Evaluation of Oseltamivir (Tamiflu®) in the Treatment of Infants 0 to <12 Months of Age With Confirmed Influenza Infection [NCT00988325]Phase 165 participants (Actual)Interventional2011-01-31Completed
A Phase 2a Double-Blind, Randomized, Placebo-Controlled Study to Evaluate the Efficacy and Safety of MK-4482 in Healthy Participants Inoculated With Experimental Influenza Virus [NCT05818124]Phase 1160 participants (Anticipated)Interventional2023-08-21Recruiting
A Phase 2a, Randomized, Partial Double-blind, Single Dose, Active-controlled, Dose Ranging Study to Evaluate the Safety of MEDI8852 in Adults With Acute, Uncomplicated Influenza [NCT02603952]Phase 1/Phase 2126 participants (Actual)Interventional2015-12-07Completed
A Phase 2b, Randomized, Double-blind, Single-dose, Active-controlled, Dose Ranging Study to Evaluate the Efficacy and Safety of MEDI8852 in Adults Who Are Hospitalized With Influenza Caused by Type A Strains [NCT03028909]Phase 20 participants (Actual)Interventional2017-07-24Withdrawn(stopped due to Study is withdrawn due to company decision.)
Safety and Effectiveness of Mesenchymal Stem Cells in the Treatment of Pneumonia of Coronavirus Disease 2019 [NCT04371601]Early Phase 160 participants (Actual)Interventional2020-03-01Active, not recruiting
Comparative Parallel-group Randomized Clinical Trial of Efficacy and Safety of Ergoferon Versus Oseltamivir in Treatment of Influenza [NCT01850446]Phase 4184 participants (Actual)Interventional2015-02-20Completed
A Phase 3, Randomized, Open Label, Active-controlled Study to Evaluate the Safety, Pharmacokinetics and Effectiveness of IV Peramivir Compared to Oral Oseltamivir in Pediatric Subjects With Acute Uncomplicated Influenza [NCT02369159]Phase 3137 participants (Actual)Interventional2015-03-11Completed
A Randomized, Double-blind Phase III Clinical Study of ZSP1273 Tablets Compared With Placebo or Oseltamivir Patients With Acute Uncomplicated Influenza A [NCT04683406]Phase 3750 participants (Actual)Interventional2020-12-28Completed
A Single Center, Open Label, Multiple-Dose Oral Oseltamivir Suspension Study in End-Stage-Renal Disease (ESRD) Patients on Hemodialysis (HD) and Continuous Ambulatory Peritoneal Dialysis (CAPD) [NCT02617784]Phase 124 participants (Actual)Interventional2001-10-31Completed
High-Dose Versus Standard-Dose Oseltamivir for the Treatment of Severe Influenza and Avian Influenza: A Phase II Double-Blind, Randomized Clinical Trial [NCT00298233]Phase 2326 participants (Actual)Interventional2006-02-28Completed
Bioavailability of a Formulation of Oseltamivir Phosphate 75 mg Capsules With Regards to the Reference Product [NCT05083325]Phase 136 participants (Actual)Interventional2021-10-08Completed
The Effects of Neuraminidase Inhibitor Oseltamivir in Patients With Chronic Heart Failure: an Open Label, Randomized, Blank-controlled Study. [NCT05008679]388 participants (Anticipated)Interventional2021-02-25Recruiting
An Open Label, Prospective, Single Oral Dose Study Evaluating the Pharmacokinetics, Safety, and Tolerability of Oseltamivir in Adult Subjects on Peritoneal Dialysis (PD) Using a Rapid Cycle Regimen to Simulate APD and in Adult Subjects With Creatinine Cle [NCT01556633]Phase 116 participants (Actual)Interventional2012-03-31Completed
A Phase 2, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Pharmacokinetics, Safety, and Antiviral Activity of JNJ-63623872 in Combination With Oseltamivir in Adult and Elderly Hospitalized Patients With Influenza A Infection [NCT02532283]Phase 2102 participants (Actual)Interventional2015-12-11Completed
Comparison of Time From Symptom Onset to Oseltamivir Access When Oseltamivir is Prescribed by Pharmacists vs. Physicians and the Impact on Symptoms, Oseltamivir Resistance, and Patient Safety [NCT01456234]Phase 448 participants (Actual)Interventional2011-11-30Terminated(stopped due to Insufficient recruitment)
A Study to Evaluate Drug-drug Interaction of ZX-7101A Tablets and Oseltamivir Phosphate Capsules in Healthy Adult Subjects -a Single-center, Open-labelled, Six-sequence, Three-cycle Crossover Design [NCT06057103]Phase 118 participants (Anticipated)Interventional2023-08-25Recruiting
Influenza Therapeutic Trial: A Pilot Randomized Controlled Trial for Feasibility of Enrolling Subjects for Influenza Therapeutic Trials and Administering Influenza Antivirals in the Emergency Department to High Risk Subjects [NCT02609399]Phase 4180 participants (Actual)Interventional2015-11-01Completed
[NCT02989012]Phase 296 participants (Anticipated)InterventionalNot yet recruiting
A Multiple-Center, Randomized, Double-blind, Multiple-Dose, Placebo-Controlled, Parallel-Group Study to Investigate the Safety, Tolerability, and Pharmacokinetics of RO0640796 (Oseltamivir) and Its Carboxylate Metabolite, RO0640802, Following Intravenous [NCT02717754]Phase 199 participants (Actual)Interventional2009-12-31Completed
Proof of Concept; A Pilot, Randomized, Double-Blind Study of Oseltamivir Versus Placebo for Immune Thrombocytopenia [NCT03520049]Phase 330 participants (Anticipated)Interventional2016-11-30Recruiting
Application of Umbilical Cord Mesenchymal Stem Cells as Adjuvant Therapy for Critically-Ill COVID-19 Patients [NCT04457609]Phase 140 participants (Anticipated)Interventional2020-07-31Recruiting
[NCT02293863]Phase 2168 participants (Actual)Interventional2015-01-14Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00298233 (6) [back to overview]Participants Meeting Criteria for Day 5 Clinical Failure
NCT00298233 (6) [back to overview]Proportion of All Participants Negative for Viral RNA on Day 5
NCT00298233 (6) [back to overview]Median Time (Days) Receipt of Oxygen
NCT00298233 (6) [back to overview]Median Time (Days) on Ventilation
NCT00298233 (6) [back to overview]Median Time (Days) in ICU
NCT00298233 (6) [back to overview]In-hospital Mortality Rates
NCT00391768 (8) [back to overview]Incidence of Treatment Emergent AEs and Drug Related AEs by Cohort Leading to Discontinuation of Study Medication
NCT00391768 (8) [back to overview]Correlation of Clearance of Viral RNA by Polymerase Chain Reaction (PCR) to Pharmacokinetic Parameters by Cohort.
NCT00391768 (8) [back to overview]Correlation of Clearance of Viral RNA by Culture With Pharmacokinetic Parameters by Cohort
NCT00391768 (8) [back to overview]Incidence of All Serious Adverse Events by Cohort and System Organ Class (SOC)
NCT00391768 (8) [back to overview]Incidence of Treatment Emergent AEs and Drug Related AEs by Cohort and Toxicity Grade
NCT00391768 (8) [back to overview]Number and Characteristics of Adverse Events (AEs) Described as Neurological Events.
NCT00391768 (8) [back to overview]Oseltamivir Carboxylate AUC12 (Area Under the Curve).
NCT00391768 (8) [back to overview]Overall Reported Adverse Events (AEs) Thought to be Associated With Study Therapy.
NCT00412737 (7) [back to overview]Number of Participants With Laboratory Confirmed Clinical Influenza, Intent-to-treat Virus Negative at Baseline (ITTNAB) Population
NCT00412737 (7) [back to overview]Number of Participants With Laboratory Confirmed Clinical Influenza, Per Protocol (PP) Population
NCT00412737 (7) [back to overview]Number of Participants With Laboratory-Confirmed Clinical Influenza, ITT Population
NCT00412737 (7) [back to overview]Number of Participants With Reverse Transcriptase Polymerase Chain Reaction (RT-PCR) Confirmed Clinical Influenza, ITT Population
NCT00412737 (7) [back to overview]Number of Participants With RT-PCR Confirmed Clinical Influenza, ITTNAB Population
NCT00412737 (7) [back to overview]Number of Participants With RT-PCR, or Serology/Viral Culture Confirmed Clinical Influenza, ITT Population
NCT00412737 (7) [back to overview]Number of Participants With RT-PCR, or Serology/Viral Culture Confirmed Clinical Influenza, ITTNAB Population
NCT00453999 (6) [back to overview]Change in Amount of Influenza Virus in Nose and Throat (Influenza A and B Combined)
NCT00453999 (6) [back to overview]Incidence of Clinical Relapse of Influenza After Treatment (Number of Participants Experiencing Relapse During the Study)
NCT00453999 (6) [back to overview]Time to Clinical Stability (Kaplan-Meier Estimate)
NCT00453999 (6) [back to overview]Time to Hospital Discharge (Kaplan-Meier Estimate)
NCT00453999 (6) [back to overview]Time to Resumption of Ability to Perform Usual Activities (Kaplan-Meier Estimate)
NCT00453999 (6) [back to overview]Change From Baseline in Scores of Symptoms of Influenza
NCT00545532 (46) [back to overview]Change From Baseline in Viral Load Assessed by Reverse Transcription Polymerase Chain Reaction (RT-PCR)
NCT00545532 (46) [back to overview]Time to Cessation of Viral Shedding by RT-PCR
NCT00545532 (46) [back to overview]Change From Baseline in Viral Load Assessed by Culture
NCT00545532 (46) [back to overview]Percentage of Participants Who Initiated Antibiotic Treatment
NCT00545532 (46) [back to overview]Total Symptom Score Area Under the Efficacy Curve (AUE)
NCT00545532 (46) [back to overview]Pharmacokinetics: Trough Plasma Concentration (Ctrough) of Oseltamivir in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Tmax of Oseltamivir Carboxylate in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Time to Maximum Concentration (Tmax) of Oseltamivir in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Elimination Constant (ke) of Oseltamivir in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Maximum Plasma Concentration (Cmax) of Oseltamivir in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Elimination Constant (ke) of Oseltamivir Carboxylate in Adults
NCT00545532 (46) [back to overview]Percentage of Participants Hospitalized
NCT00545532 (46) [back to overview]Pharmacokinetics: Ctrough of Oseltamivir Carboxylate in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Cmax of Oseltamivir Carboxylate in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Apparent Volume of Distribution (Vc/F) of Oseltamivir in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Apparent Volume of Distribution (Vc/F) of Oseltamivir Carboxylate in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Apparent Clearance (CL/F) of Oseltamivir in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics: Apparent Clearance (CL/F) of Oseltamivir Carboxylate in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics : AUC0-12 at Steady State of Oseltamivir Carboxylate in Adults
NCT00545532 (46) [back to overview]Pharmacokinetics : Area Under the Concentration-Time Curve From 0 to 12 Hours (AUC0-12) at Steady State of Oseltamivir in Adults
NCT00545532 (46) [back to overview]Percentage of Participants With Tissue Rejection or Graft Versus Host Disease (GVHD)
NCT00545532 (46) [back to overview]Percentage of Participants With Persistent Viral Shedding
NCT00545532 (46) [back to overview]Pharmacokinetics: Tmax of Oseltamivir in Adolescents and Children
NCT00545532 (46) [back to overview]Time to Cessation of Viral Shedding by Cell Culture
NCT00545532 (46) [back to overview]Time to Resolution (TTR) of All Clinical Influenza Symptoms
NCT00545532 (46) [back to overview]Time to Resolution of Fever
NCT00545532 (46) [back to overview]Percentage of Participants With Viral Shedding Assessed by RT-PCR Over Time
NCT00545532 (46) [back to overview]Percentage of Participants With Viral Shedding Assessed by Culture Over Time
NCT00545532 (46) [back to overview]Percentage of Participants With Adverse Events
NCT00545532 (46) [back to overview]Change From Baseline in Viral Load Assessed by Reverse Transcription Polymerase Chain Reaction (RT-PCR)
NCT00545532 (46) [back to overview]Percentage of Participants Who Developed Viral Resistance to Oseltamivir
NCT00545532 (46) [back to overview]Percentage of Participants Who Developed Secondary Illness
NCT00545532 (46) [back to overview]Duration of Hospitalization
NCT00545532 (46) [back to overview]Pharmacokinetics: Tmax of Oseltamivir Carboxylate in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Elimination Constant (ke) of Oseltamivir in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Elimination Constant (ke) of Oseltamivir Carboxylate in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Ctrough of Oseltamivir in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Ctrough of Oseltamivir Carboxylate in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Cmax of Oseltamivir in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Cmax of Oseltamivir Carboxylate in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: AUC0-12 at Steady State of Oseltamivir in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: AUC0-12 at Steady State of Oseltamivir Carboxylate in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Apparent Volume of Distribution (Vc/F) of Oseltamivir in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Apparent Volume of Distribution (Vc/F) of Oseltamivir Carboxylate in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Apparent Clearance (CL/F), of Oseltamivir Carboxylate in Adolescents and Children
NCT00545532 (46) [back to overview]Pharmacokinetics: Apparent Clearance (CL/F) of Oseltamivir in Adolescents and Children
NCT00555893 (4) [back to overview]Mean Influenza Well-being Score
NCT00555893 (4) [back to overview]Mean Illness Severity Score
NCT00555893 (4) [back to overview]Duration of Influenza Illness
NCT00555893 (4) [back to overview]Viral Shedding on Day 3-4 of Treatment
NCT00803595 (2) [back to overview]Time for Body Temperature to Return to Normal
NCT00803595 (2) [back to overview]Time to Alleviation of Influenza Illness
NCT00867139 (12) [back to overview]Days on Supplemental Oxygen
NCT00867139 (12) [back to overview]Number of Patients Not Shedding Virus at Day 5 +/-1 and Day 10 +/- 1
NCT00867139 (12) [back to overview]Pharmacokinetics (AUC0-last) of TCAD
NCT00867139 (12) [back to overview]Number of Deaths
NCT00867139 (12) [back to overview]Number of Participants With Viral Resistance as a Function of Drug Exposure
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 Intubations
NCT00867139 (12) [back to overview]Number of Participants With ICU Admissions
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]Frequency of Confirmed Pneumonia
NCT00867139 (12) [back to overview]Duration of Symptoms
NCT00867139 (12) [back to overview]Duration of Hospitalization
NCT00884117 (25) [back to overview]Number of Participants With Viral RNA Detected by RT-PCR on Day 1 Among Children Treated With Oseltamivir
NCT00884117 (25) [back to overview]Number of Participants With Viral RNA Detected by RT-PCR on Day 10 Among Children Treated With Oseltamivir
NCT00884117 (25) [back to overview]Number of Participants With Viral RNA Detected by RT-PCR on Day 3 Among Adults Treated With Oseltamivir
NCT00884117 (25) [back to overview]Number of Participants With Viral RNA Detected by RT-PCR on Day 3 Among Children Treated With Oseltamivir
NCT00884117 (25) [back to overview]Number of Participants With Viral RNA Detected by RT-PCR on Day 6 Among Adults Treated With Oseltamivir
NCT00884117 (25) [back to overview]Number of Participants With Viral RNA Detected by RT-PCR on Day 6 Among Children Treated With Oseltamivir
NCT00884117 (25) [back to overview]Percentage of Participants by Day of Viral RNA First Not Detected Comparing Resistant and Susceptible Viruses
NCT00884117 (25) [back to overview]Number of Participants With Viral RNA Detected by RT-PCR on Day 10 Among Adults Treated With Oseltamivir
NCT00884117 (25) [back to overview]Percentage of Participants With Resistant Versus Susceptible Viruses by Baseline Viral Load
NCT00884117 (25) [back to overview]Percentage of Participants With Symptom Resolution on Day 6 Comparing Resistant and Susceptible Viruses
NCT00884117 (25) [back to overview]Viral Load Among Children Treated With Oseltamivir
NCT00884117 (25) [back to overview]Viral Load Among Adults Treated With Oseltamivir
NCT00884117 (25) [back to overview]Total Daily Symptom Score According to Global Assessment by the Investigator Among Children Treated With Oseltamivir
NCT00884117 (25) [back to overview]Total Daily Symptom Score According to Global Assessment by the Investigator Among Adults Treated With Oseltamivir
NCT00884117 (25) [back to overview]Change From Baseline in Body Temperature Among Adults Treated With Oseltamivir
NCT00884117 (25) [back to overview]Body Temperature Among Adults Treated With Oseltamivir
NCT00884117 (25) [back to overview]Time to Non-Detection of Viral RNA Among Participants With Influenza B Infections
NCT00884117 (25) [back to overview]Time to Non-Detection of Viral RNA Among Participants With H3N2 Infections
NCT00884117 (25) [back to overview]Time to Non-Detection of Viral RNA
NCT00884117 (25) [back to overview]Percentage of Participants Exhibiting Treatment-Emergent Resistance by Study Year Among Participants With H3N2 or H1N1pdm09 Infections
NCT00884117 (25) [back to overview]Change From Baseline in Body Temperature Among Children Treated With Oseltamivir
NCT00884117 (25) [back to overview]Number of Participants With Genotypic Resistance
NCT00884117 (25) [back to overview]Number of Participants With Viral RNA Detected by RT-PCR on Day 1 Among Adults Treated With Oseltamivir
NCT00884117 (25) [back to overview]Body Temperature Among Children Treated With Oseltamivir
NCT00884117 (25) [back to overview]Time to Non-Detection of Viral RNA Among Participants With H1N1pdm09 Infections
NCT00949533 (4) [back to overview]Percentage of Participants With A Reduction in Viral Load
NCT00949533 (4) [back to overview]Percentage of Participants Excreting Resistant Virus
NCT00949533 (4) [back to overview]Number of Participants With Various Clinical Signs and Symptoms
NCT00949533 (4) [back to overview]Number of Participants With Various Clinical Signs and Symptoms in Whom Resistant Virus Were Detected
NCT00988325 (16) [back to overview]Time to the Maximum Observed Plasma Concentration of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Total Plasma Clearance as a Function of Bioavailability and Apparent Plasma Clearance of the Metabolite as a Function of Bioavailability (CLm/F) of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Time of the Last Measurable Plasma Concentration for Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]The Volume of Distribution as a Function of Bioavailability of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Steady-state Minimum Observed Plasma Concentration of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Steady-state Maximum Observed Plasma Concentration of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Steady-state Area Under the Plasma Concentration Versus Time Curve From Time Zero to 12 Hours of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Percentage of Participants With Decline of Body Temperature to the Afebrile State
NCT00988325 (16) [back to overview]Number of Participants With Virus Shedding by Virus Type
NCT00988325 (16) [back to overview]Number of Participants With Change From Baseline in Neurological Assessment Scores
NCT00988325 (16) [back to overview]Number of Participants With Adverse Events, Serious Adverse Events and Secondary Illness
NCT00988325 (16) [back to overview]Clast of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Apparent First-order Elimination Rate Constant of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Apparent Elimination Half Life of Oseltamivir and Oseltamivir Carboxylate
NCT00988325 (16) [back to overview]Time to Resolution of Fever in Participants With Fever at the Baseline
NCT00988325 (16) [back to overview]Median Time to Cessation of Viral Shedding in Participants With Positive Culture at Baseline
NCT01032837 (10) [back to overview]Number of Participants With Development of Oseltamivir-Resistant Influenza Virus
NCT01032837 (10) [back to overview]Time to Cessation of Viral Shedding
NCT01032837 (10) [back to overview]Time to Alleviation of All Clinical Symptoms - Children
NCT01032837 (10) [back to overview]Time to Alleviation of All Clinical Symptoms - Adults
NCT01032837 (10) [back to overview]Number of Participants Who Developed Secondary Illnesses That Were Treated With Antibiotics
NCT01032837 (10) [back to overview]Percentage of Participants With Viral Shedding by Clinic Visit as Measured by Reverse Transcriptase Polymerase Chain Reaction
NCT01032837 (10) [back to overview]Change From Baseline in Influenza Titer Measured by Viral Culture
NCT01032837 (10) [back to overview]Time to Resolution of Fever
NCT01032837 (10) [back to overview]Number of Participants Who Developed Secondary Illnesses During the Study
NCT01032837 (10) [back to overview]Percentage of Participants With Viral Shedding by Clinic Visit as Measured by Viral Culture
NCT01033734 (14) [back to overview]Last Measurable Plasma Concentration (Clast) of Oseltamivir and Oseltamivir Carboxylate
NCT01033734 (14) [back to overview]Cmax of Oseltamivir and Oseltamivir Carboxylate Day 5
NCT01033734 (14) [back to overview]Cmax of Oseltamivir and Oseltamivir Carboxylate Day 4
NCT01033734 (14) [back to overview]Cmax of Oseltamivir and Oseltamivir Carboxylate Day 3
NCT01033734 (14) [back to overview]Cmax of Oseltamivir and Oseltamivir Carboxylate Day 2
NCT01033734 (14) [back to overview]AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 5
NCT01033734 (14) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Oseltamivir and Oseltamivir Carboxylate Day 1
NCT01033734 (14) [back to overview]AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 3
NCT01033734 (14) [back to overview]AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 2
NCT01033734 (14) [back to overview]Area Under the Concentration Versus Time Curve From Time Zero to Last Measurable Plasma Concentration (AUClast) of Oseltamivir and Oseltamivir Carboxylate on Day 1
NCT01033734 (14) [back to overview]AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 4
NCT01033734 (14) [back to overview]Time of the Last Measurable Plasma Concentration (Tlast) of Oseltamivir and Oseltamivir Carboxylate
NCT01033734 (14) [back to overview]Time to the Maximum Observed Plasma Concentration (Tmax) of Oseltamivir and Oseltamivir Carboxylate
NCT01033734 (14) [back to overview]Participants With Greater Than or Equal to (>=) 5-Fold Change in Neuraminidase Inhibition (NAI) Assay 50 Percent (%) Inhibitory Concentration (IC50) Values
NCT01048879 (2) [back to overview]Continuous Venovenous Hemodialysis (CVVHD)Oseltamivir Carboxylate Transmembrane Clearance
NCT01048879 (2) [back to overview]Oseltamivir Carboxylate Removal by ECMO
NCT01050257 (10) [back to overview]Number of Participants With Viral Resistance
NCT01050257 (10) [back to overview]Percentage of Participants With Viral Shedding by Reverse Transcriptase Polymerase Chain Reaction (RT-PCR)
NCT01050257 (10) [back to overview]Change From Baseline in Influenza Titer by Culture at Day 4
NCT01050257 (10) [back to overview]Percentage of Participants With Viral Shedding by Culture or RT-PCR
NCT01050257 (10) [back to overview]Percentage of Participants With Viral Shedding by Culture
NCT01050257 (10) [back to overview]Percentage of Participants With Influenza Symptoms
NCT01050257 (10) [back to overview]Percentage of Participants Who Had a Fever During the Study
NCT01050257 (10) [back to overview]Number of Participants With Adverse Events (AEs), Serious Adverse Events(SAEs, AEs Leading to Withdrawal, and Death
NCT01050257 (10) [back to overview]Change From Baseline in Influenza Titer by Reverse Transcriptase Polymerase Chain Reaction (RT-PCR) at Day 4
NCT01050257 (10) [back to overview]Time to Resolution of Fever for Participants Who Had a Fever at Baseline
NCT01053663 (11) [back to overview]Time of the Last Measurable Plasma Concentration (Tlast) of Oseltamivir and Oseltamivir Carboxylate
NCT01053663 (11) [back to overview]Number of Participants With Greater Than or Equal to (≥) 5-Fold Change in Neuraminidase Inhibition (NAI) Assay 50 Percent (%) Inhibitory Concentration (IC50) Values
NCT01053663 (11) [back to overview]Number of Participants With Oseltamivir Resistance Mutation
NCT01053663 (11) [back to overview]Area Under the Concentration Versus Time Curve From Time Zero to Last Measurable Plasma Concentration (AUClast) of Oseltamivir and Oseltamivir Carboxylate on Day 1
NCT01053663 (11) [back to overview]AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 4
NCT01053663 (11) [back to overview]Cmax of Oseltamivir and Oseltamivir Carboxylate on Day 4
NCT01053663 (11) [back to overview]Last Measurable Plasma Concentration (Clast) of Oseltamivir and Oseltamivir Carboxylate
NCT01053663 (11) [back to overview]Time to the Maximum Observed Plasma Concentration (Tmax) of Oseltamivir and Oseltamivir Carboxylate
NCT01053663 (11) [back to overview]Cmax of Oseltamivir and Oseltamivir Carboxylate on Day 2
NCT01053663 (11) [back to overview]AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 2
NCT01053663 (11) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Oseltamivir and Oseltamivir Carboxylate on Day 1
NCT01172847 (8) [back to overview]Steady State Area Under the Plasma Concentration Versus Time Curve From 0 to 12 Hours After Dosing (AUC0-12) of Oseltamivir and Oseltamivir Carboxylate
NCT01172847 (8) [back to overview]Number of Participants With Marked Abnormality in Laboratory Parameters
NCT01172847 (8) [back to overview]Number of Participants With Abnormal Vital Signs
NCT01172847 (8) [back to overview]Steady State Area Under the Plasma Concentration Versus Time Curve From 0 to 12 Hours After Dosing (AUC0-12) of Rimantadine
NCT01172847 (8) [back to overview]Number of Participants With Clinically Significant or Treatment Related Changes in Electrocardiogram (ECG)
NCT01172847 (8) [back to overview]Number of Participants With Any Adverse Events (AEs) and Any Serious Adverse Events (SAEs)
NCT01172847 (8) [back to overview]Maximum Plasma Concentration (Cmax) of Rimantadine
NCT01172847 (8) [back to overview]Maximum Plasma Concentration (Cmax) of Oseltamivir and Oseltamivir Carboxylate
NCT01179919 (2) [back to overview]Steady-State AUC of Oseltamivir Carboxylate
NCT01179919 (2) [back to overview]Steady-State Cmax and Cmin of Oseltamivir Carboxylate
NCT01227967 (14) [back to overview]28-day Mortality
NCT01227967 (14) [back to overview]Percentage of Participants Who Required Hospitalization.
NCT01227967 (14) [back to overview]Percentage of Participants Who Required New or Increased Use of Supplemental Oxygen
NCT01227967 (14) [back to overview]Percentage of Participants With Clinical Failure at Day 5
NCT01227967 (14) [back to overview]Percentage of Participants With Virus Detectable by Quantitative PCR (qPCR) in Nasopharyngeal (NP) Swabs
NCT01227967 (14) [back to overview]Time to Absence of Fever
NCT01227967 (14) [back to overview]Time to Alleviation of Influenza Clinical Symptoms.
NCT01227967 (14) [back to overview]Time to Feeling as Good as Before the Onset of the Influenza Illness
NCT01227967 (14) [back to overview]Time to Resolution of All Symptoms AND Fever
NCT01227967 (14) [back to overview]Time to Return to Pre-influenza Function
NCT01227967 (14) [back to overview]Percentage of Participants Who Develop Bronchitis, Pneumonia, or Other Complications of Influenza After Day 0.
NCT01227967 (14) [back to overview]qPCR Viral Shedding
NCT01227967 (14) [back to overview]Number of Participants by Virus Detection Status
NCT01227967 (14) [back to overview]Time to Return of Physical Function to Pre-illness Leve
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]Median Time of Duration of Clinical Symptoms of Influenza
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]Change From Baseline in the Katz Activities of Daily Living (ADL) Score and Each ADL Activity Score
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]Serum Concentration of IV Zanamivir
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 the Indicated Ventilation Status: Modality of Invasive and Non-invasive Ventilator Support and Oxygen Supplementation
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 Any Severe or Grade 3/4 AE
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 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 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 Clinical Symptoms of Influenza
NCT01231620 (36) [back to overview]Number of Participants With the Indicated Chemistry Laboratory Values Shifts From Baseline (Day 1) and up to 42 Days
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]Change From Baseline in Quantitative Virus Culture From Nasopharyngeal Swabs Positive at Baseline
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 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]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 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 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]Serum Concentration of IV Zanamivir
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]Median Time to Virologic Improvement
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]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 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 of Duration of Invasive and Non-invasive Ventilator Support and Oxygen Supplementation
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]Median Time of Duration of Hospitalization and Intensive Care Unit (ICU) Stay
NCT01248715 (7) [back to overview]Number of Participants to Transfer to ICU After 24 h
NCT01248715 (7) [back to overview]Number of Participants That Required Re-hospitalization
NCT01248715 (7) [back to overview]Number of Participants That Had Short-term Mortality
NCT01248715 (7) [back to overview]Length of Hospital Stay
NCT01248715 (7) [back to overview]Days to Reach Clinical Stability
NCT01248715 (7) [back to overview]Number of Participants With Clinical Failure (Failure to Reach Clinical Stability)
NCT01248715 (7) [back to overview]Number of Participants With Hospital Mortality.
NCT01249833 (4) [back to overview]Change in Attention Assessment
NCT01249833 (4) [back to overview]Change in Processing Speed Assessment
NCT01249833 (4) [back to overview]Change in Working Memory Assessment
NCT01249833 (4) [back to overview]Change in Mood Assessment
NCT01314911 (16) [back to overview]Time to Return of Physical Function to Pre-illness Level
NCT01314911 (16) [back to overview]Time to Feeling as Good as Before the Onset of the Influenza Illness
NCT01314911 (16) [back to overview]28-day Mortality
NCT01314911 (16) [back to overview]Area Under The Curve (AUC) Of Viral Shedding For Self Collected Samples
NCT01314911 (16) [back to overview]Percentage of Participants With Virus Detectable by Quantitative PCR (qPCR) in Nasopharyngeal (NP) Swabs --Self Collected Samples
NCT01314911 (16) [back to overview]Percentage of Participants With Virus Detectable by Quantitative PCR (qPCR) in Nasopharyngeal (NP) Swabs at Day 3 -- Team Collected Samples
NCT01314911 (16) [back to overview]Time to Absence of Fever
NCT01314911 (16) [back to overview]Time to Alleviation of Influenza Clinical Symptoms
NCT01314911 (16) [back to overview]Number of Participants by Virus Detection Status--Team Collected Samples
NCT01314911 (16) [back to overview]Number of Participants by Virus Detection Status --Self Collected Samples
NCT01314911 (16) [back to overview]qPCR Viral Shedding -- Team Collected Samples
NCT01314911 (16) [back to overview]Percentage of Participants Who Required Hospitalization.
NCT01314911 (16) [back to overview]Time to Resolution of All Symptoms AND Fever
NCT01314911 (16) [back to overview]qPCR Viral Shedding -- Self Collected Samples
NCT01314911 (16) [back to overview]Percentage of Participants Who Develop Bronchitis, Pneumonia, or Other Complications Requiring An Antibiotic Use, After Day 0.
NCT01314911 (16) [back to overview]Time to Return to Pre-influenza Function
NCT01556633 (11) [back to overview]Renal Clearance (CLR) of Oseltamivir and Oseltamivir Carboxylate
NCT01556633 (11) [back to overview]Tmax and T1/2 of Oseltamivir and Oseltamivir Carboxylate
NCT01556633 (11) [back to overview]C120h, C168h and Clast of Oseltamivir and Oseltamivir Carboxylate for 75 mg Dose
NCT01556633 (11) [back to overview]Total Dialysate Clearance for Automated Peritoneal Dialysis (CLDAPD) of Oseltamivir and Oseltamivir Carboxylate for 75 mg Dose
NCT01556633 (11) [back to overview]Cmax of Oseltamivir and Oseltamivir Carboxylate
NCT01556633 (11) [back to overview]Number of Participants With Abnormal Shifts in Vital Signs
NCT01556633 (11) [back to overview]Number of Participants With Any Adverse Event (AEs) and Any Serious Adverse Events (SAEs)
NCT01556633 (11) [back to overview]Number of Participants With Marked Abnormality in Laboratory Measurements
NCT01556633 (11) [back to overview]Number of Participants With Change From Baseline in Marked Abnormality in Electrocardiogram (ECG) Parameters at Follow-up Visit
NCT01556633 (11) [back to overview]AUC120, AUC168 and AUCinf of Oseltamivir and Oseltamivir Carboxylate for 75 mg Dose
NCT01556633 (11) [back to overview]AUCinf of Oseltamivir and Oseltamivir Carboxylate for 30 mg Dose
NCT01804946 (9) [back to overview]Percentage of Patients With Resolution of Influenza Symptoms
NCT01804946 (9) [back to overview]Severity of Influenza Symptoms (Total Score of the Common Symptoms and Respiratory Symptoms)
NCT01804946 (9) [back to overview]The Number of the Antipyretic Intake
NCT01804946 (9) [back to overview]Time to Resolution of the Influenza
NCT01804946 (9) [back to overview]Percentage of Patients With Complications of the Influenza
NCT01804946 (9) [back to overview]Change in the Patient's Quality of Life.
NCT01804946 (9) [back to overview]Change in the Subjective Health Status
NCT01804946 (9) [back to overview]Mean Body Temperature
NCT01804946 (9) [back to overview]Percentage of Patients With Normal Body Temperature
NCT01850446 (14) [back to overview]Proportion of Patients With Negative Results of Virological Analysis.
NCT01850446 (14) [back to overview]Dynamics of Parameters of Immune Status (T-cell and B-cell Immune Response).
NCT01850446 (14) [back to overview]Percentage of Patients Who Used Antipyretics on Days 1, 2, 3, 4 and 5 of the Treatment.
NCT01850446 (14) [back to overview]Percentage of Patients With Normal Body Temperature.
NCT01850446 (14) [back to overview]Severity of Influenza Symptoms (Fever, Flu Non-specific and Nasal/Throat/Chest Symptoms) in Scores According to the Symptoms Severity Scale.
NCT01850446 (14) [back to overview]Percentage of Patients With Recovery/Improvement in Health Status.
NCT01850446 (14) [back to overview]Average Duration of Fever.
NCT01850446 (14) [back to overview]Percentage of Patients Requiring Antibiotics Administration.
NCT01850446 (14) [back to overview]The Severity of Influenza.
NCT01850446 (14) [back to overview]Changes in Fever.
NCT01850446 (14) [back to overview]Duration of Clinical Symptoms of Influenza (Fever, Non-specific Symptoms and Nasal/ Throat/ Chest Symptoms) in Days.
NCT01850446 (14) [back to overview]Dynamics of Parameters of Immune Status ( IFN-α and IFN-γ Production).
NCT01850446 (14) [back to overview]Dynamics of Parameters of Immune Status (Absolute Number of Each Type of White Blood Cells and Different Lymphocyte Phenotypes).
NCT01850446 (14) [back to overview]Dynamics of Parameters of Immune Status (Relative Percentage of Each Type of White Blood Cells and Different Lymphocyte Phenotypes).
NCT02293863 (21) [back to overview]Percentage of Participants With Clinical Resolution of Abnormal Vital Signs
NCT02293863 (21) [back to overview]Percentage of Participants With Secondary Complications of Influenza
NCT02293863 (21) [back to overview]Time to Normalization of Respiratory Function
NCT02293863 (21) [back to overview]Number of Participants With Anti-Therapeutic Antibodies (ATA) to MHAA4549A During and Following Administration of MHAA4549A
NCT02293863 (21) [back to overview]Percentage of Participants by Clinical Status Using a Categorical Ordinal Outcome
NCT02293863 (21) [back to overview]Percentage of Participants Who Died Due to Any Cause
NCT02293863 (21) [back to overview]Area Under Serum Concentration-Time Curve From Time 0 to Infinity (AUC ) of MHAA4549A
NCT02293863 (21) [back to overview]Area Under Viral Load-Time Curve (AUEC ) of Influenza A Virus
NCT02293863 (21) [back to overview]Duration of Hospitalization
NCT02293863 (21) [back to overview]Duration of Intensive Care Unit (ICU) Stay
NCT02293863 (21) [back to overview]Duration of Ventilation
NCT02293863 (21) [back to overview]Duration of Viral Shedding
NCT02293863 (21) [back to overview]Elimination Half-Life (Terminal t1/2) of MHAA4549A
NCT02293863 (21) [back to overview]Maximum Serum Concentration (Cmax ) of MHAA4549A
NCT02293863 (21) [back to overview]Observed Clearance (CL-obs) of MHAA4549A
NCT02293863 (21) [back to overview]Observed Steady State Volume of Distribution (Vss_obs) of MHAA4549A
NCT02293863 (21) [back to overview]Peak Influenza A Viral Load
NCT02293863 (21) [back to overview]Percentage of Participants Readmitted to Hospital Due to Any Cause
NCT02293863 (21) [back to overview]Percentage of Participants Using Antibiotics for Respiratory Infections
NCT02293863 (21) [back to overview]Percentage of Participants With Adverse Events
NCT02293863 (21) [back to overview]Percentage of Participants With Clinical Failure
NCT02369159 (7) [back to overview]Time to Resolution of Fever
NCT02369159 (7) [back to overview]Changes in Influenza Virus Titer in Nasopharyngeal Samples in Response to Treatment.
NCT02369159 (7) [back to overview]Influenza-Related Complications Assessment.
NCT02369159 (7) [back to overview]Plasma Exposure of IV Peramivir as Measured by the Drug Concentration Over 6 Hours Post-dose
NCT02369159 (7) [back to overview]Safety and Tolerability, as Measured by the Number of Participants Experiencing Adverse Events.
NCT02369159 (7) [back to overview]Time to Reduction in Viral Shedding
NCT02369159 (7) [back to overview]Time to Resolution of Influenza Symptoms
NCT02469298 (33) [back to overview]Change From Baseline in Hematology Parameters- Mean Corpuscle Hemoglobin (MCH)
NCT02469298 (33) [back to overview]Change From Baseline in Hematology Parameters- Hemoglobin
NCT02469298 (33) [back to overview]Change From Baseline in Hematology Parameters- Hematocrit
NCT02469298 (33) [back to overview]Number of Participants With no Detectable Influenza Viral RNA by qRT-PCR From Nasopharyngeal Swabs on Baseline (Day 1), Day 3, Day 5, Day 8 and Day 14
NCT02469298 (33) [back to overview]Change From Baseline in Clinical Chemistry- Alkaline Phosphatase (ALP), Alanine Amino Transferase (ALT), Aspartate Amino Transferase (AST) and Gamma Glutamyl Transferase (GGT)
NCT02469298 (33) [back to overview]Change From Baseline in Clinical Chemistry Parameters- Direct Bilirubin, Total Bilirubin, Creatinine and Uric Acid
NCT02469298 (33) [back to overview]Change From Baseline in Clinical Chemistry Parameters- Calcium, Carbon Dioxide (CO2) Content/ Bicarbonate, Glucose, Potassium, Sodium and Urea/Blood Urea Nitrogen (BUN)
NCT02469298 (33) [back to overview]Change From Baseline in Clinical Chemistry Parameters- Albumin and Total Protein
NCT02469298 (33) [back to overview]Time to Resolution of Fever Over Time Post Initiation of Treatment
NCT02469298 (33) [back to overview]Number of Participants With DRE of Interest-associated Antibiotic Use
NCT02469298 (33) [back to overview]Number of Participants With Disease Related Events (DREs) of Interest
NCT02469298 (33) [back to overview]Number of Hospital Admissions Due to Influenza Infection
NCT02469298 (33) [back to overview]Total Dose of Relief Medication
NCT02469298 (33) [back to overview]Change From Baseline in Electrocardiogram (ECG) Parameters
NCT02469298 (33) [back to overview]Change From Baseline in Hematology Parameters- Red Blood Cell (RBC) Count and Reticulocytes Count
NCT02469298 (33) [back to overview]Change From Baseline in Hematology Parameters-Basophils, Eosinophils, Lymphocytes, Monocytes, Total Neutrophils (Total Absolute Neutrophil Count [Total ANC]), Platelet Count and White Blood Cell (WBC) Count
NCT02469298 (33) [back to overview]Change From Baseline in Influenza Viral Load as Measured by Quantitative Reverse Transcription-polymerase Chain Reaction (qRT-PCR) From Nasopharyngeal Swabs on Day 3, Day 5, Day 8 and Day 14
NCT02469298 (33) [back to overview]Change From Baseline in Influenza Viral Load as Measured by Quantitative Virus Culture From Nasopharyngeal Swabs on Day 3, Day 5, Day 8 and Day 14
NCT02469298 (33) [back to overview]Change From Baseline in Urinalysis Parameters- Urine pH
NCT02469298 (33) [back to overview]Change From Baseline in Urinalysis Parameters- Urine Specific Gravity
NCT02469298 (33) [back to overview]Change From Baseline in Vital Signs- Diastolic Blood Pressure (DBP) and Systolic Blood Pressure (SBP)
NCT02469298 (33) [back to overview]Change From Baseline in Vital Signs- Heart Rate (HR)
NCT02469298 (33) [back to overview]Change From Baseline in Vital Signs- Percent Oxygen in Blood (POB)
NCT02469298 (33) [back to overview]Change From Baseline in Vital Signs- Respiration Rate (RR)
NCT02469298 (33) [back to overview]Change From Baseline in Vital Signs- Temperature
NCT02469298 (33) [back to overview]Number of Afebrile Participants Over Time Post Initiation of Treatment
NCT02469298 (33) [back to overview]Number of Participants Who Used Relief Medication
NCT02469298 (33) [back to overview]Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT02469298 (33) [back to overview]Number of Participants With Maximum Post-baseline Urine Dipstick Abnormalities- Urine Glucose (Dipstick)
NCT02469298 (33) [back to overview]Number of Participants With Maximum Post-baseline Urine Dipstick Abnormalities- Urine Occult Blood (Dipstick)
NCT02469298 (33) [back to overview]Number of Participants With Maximum Post-baseline Urine Dipstick Abnormalities- Urine Protein (Dipstick)
NCT02469298 (33) [back to overview]Change From Baseline in Hematology Parameters- Mean Corpuscle Volume (MCV)
NCT02469298 (33) [back to overview]Number of Participants With no Detectable Influenza Viral RNA by Quantitative Virus Culture From Nasopharyngeal Swabs on Baseline (Day 1), Day 3, Day 5, Day 8 and Day 14
NCT02532283 (22) [back to overview]Percentage of Participants With Influenza Complications
NCT02532283 (22) [back to overview]Percentage of Participants With Clinical Outcome Based on Ordinal Scale
NCT02532283 (22) [back to overview]Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Treatment-emergent Serious AEs (TESAEs)
NCT02532283 (22) [back to overview]Number of Participants With the Emergence of Drug Resistance Mutations With Oseltamivir (OST) and Pimodivir
NCT02532283 (22) [back to overview]Influenza Viral Load Over Time
NCT02532283 (22) [back to overview]Influenza Viral Load Over Time
NCT02532283 (22) [back to overview]Change From Baseline in Influenza Patient-Reported Outcome Questionnaire (FLU-PRO) Total Score
NCT02532283 (22) [back to overview]Change From Baseline in Influenza Patient-Reported Outcome Questionnaire (FLU-PRO) Total Score
NCT02532283 (22) [back to overview]Time to Significant Reduction in FLU-PRO Influenza Symptom Severity
NCT02532283 (22) [back to overview]Time to Return to Usual Health
NCT02532283 (22) [back to overview]Time to Return to Premorbid Functional Status
NCT02532283 (22) [back to overview]Time to Influenza A Viral Negativity
NCT02532283 (22) [back to overview]Time to Improvement of Vital Signs
NCT02532283 (22) [back to overview]Time to Improvement of Respiratory Status
NCT02532283 (22) [back to overview]Time to Hospital Discharge
NCT02532283 (22) [back to overview]Rate of Decline in Viral Load
NCT02532283 (22) [back to overview]Minimum Observed Plasma Concentration (Cmin) of Pimodivir
NCT02532283 (22) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Pimodivir
NCT02532283 (22) [back to overview]Area Under the Plasma Concentration-time Curve From Time of Administration to 12 Hours After Dosing (AUC [0-12]) of Pimodivir
NCT02532283 (22) [back to overview]Percentage of Participants With Significant Reduction in FLU-PRO All Influenza Symptoms (Mild or None for All Symptoms)
NCT02532283 (22) [back to overview]Area Under the Plasma Concentration-time Curve (AUC) of Viral Load
NCT02532283 (22) [back to overview]Percentage of Participants With Significant Reduction in FLU-PRO All Influenza Symptoms (Mild or None for All Symptoms)
NCT02603952 (10) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT02603952 (10) [back to overview]Quantitation of Influenza Viral Shedding as Measured by qRT-PCR
NCT02603952 (10) [back to overview]Number of Participants With Treatment Emergent Adverse Events of Special Interest (TEAESIs)
NCT02603952 (10) [back to overview]Number of Participants With Viral Susceptibility to MEDI8852 as Determined by a Cell Based Microneutralization Assay
NCT02603952 (10) [back to overview]Percentage of Participants With Amino Acid Changes in MEDI8852 Binding Site
NCT02603952 (10) [back to overview]Percentage of Participants With Virus Containing Known Oseltamivir Resistance-Associated Mutations
NCT02603952 (10) [back to overview]Number of Days of Influenza Viral Shedding as Measured by qRT-PCR
NCT02603952 (10) [back to overview]Percentage of Participants With Influenza Viral Shedding as Measured by Quantitative Reverse Transcription-Polymerase Chain Reaction (qRT-PCR)
NCT02603952 (10) [back to overview]Number of Participants With Treatment-Emergent Serious Adverse Events (TESAEs)
NCT02603952 (10) [back to overview]Quantitation of Influenza Viral Shedding as Measured by qRT-PCR
NCT02609399 (4) [back to overview]Mean Symptom Severity Score During the 2015-2016 Influenza Season for Symptom Domains as Assessed Using the Influenza-Patient Reported Outcome (FLU-PRO™) Questionnaire
NCT02609399 (4) [back to overview]Mean Karnofsky Performance Scale Score During the 2016-2017 Influenza Season
NCT02609399 (4) [back to overview]Mean Karnofsky Performance Scale Score During the 2015-2016 Influenza Season
NCT02609399 (4) [back to overview]Mean Symptom Severity Score During the 2016-2017 Influenza Season for Symptom Domains as Assessed Using the FLU-PRO™ Questionnaire
NCT02617784 (43) [back to overview]Percentage of Oseltamivir Dose Excreted as Metabolite Oseltamivir Carboxylate in HD Participants
NCT02617784 (43) [back to overview]Percentage of Oseltamivir Dose Excreted as Unchanged Drug in HD Participants
NCT02617784 (43) [back to overview]Percentage of Oseltamivir Dose Renally Excreted as Metabolite Oseltamivir Carboxylate in CAPD Participants
NCT02617784 (43) [back to overview]Percentage of Oseltamivir Dose Renally Excreted as Unchanged Drug in CAPD Participants
NCT02617784 (43) [back to overview]Renal Clearance (CLr) of Oseltamivir in HD Participants
NCT02617784 (43) [back to overview]Area Under the Concentration-Time Curve (AUC) of Oseltamivir in HD Participants During Days 1 to 5
NCT02617784 (43) [back to overview]AUC of Metabolite Oseltamivir Carboxylate in CAPD Participants During Days 1 to 6
NCT02617784 (43) [back to overview]AUC of Metabolite Oseltamivir Carboxylate in CAPD Participants During Days 36 to 43
NCT02617784 (43) [back to overview]AUC of Metabolite Oseltamivir Carboxylate in HD Participants During Days 1 to 5
NCT02617784 (43) [back to overview]AUC of Metabolite Oseltamivir Carboxylate in HD Participants During Days 38 to 43
NCT02617784 (43) [back to overview]AUC of Oseltamivir in CAPD Participants During Days 1 to 6
NCT02617784 (43) [back to overview]AUC of Oseltamivir in CAPD Participants During Days 36 to 43
NCT02617784 (43) [back to overview]AUC of Oseltamivir in HD Participants During Days 38 to 43
NCT02617784 (43) [back to overview]CL/F of Metabolite Oseltamivir Carboxylate in CAPD Participants
NCT02617784 (43) [back to overview]CL/F of Metabolite Oseltamivir Carboxylate in HD Participants
NCT02617784 (43) [back to overview]CL/F of Oseltamivir in CAPD Participants
NCT02617784 (43) [back to overview]Dialysis Clearance (CLd) of Metabolite Oseltamivir Carboxylate in HD Participants
NCT02617784 (43) [back to overview]Elimination Rate Constant of Metabolite Oseltamivir Carboxylate in CAPD Participants
NCT02617784 (43) [back to overview]Oral Plasma Clearance (CL/F) of Oseltamivir in HD Participants
NCT02617784 (43) [back to overview]Plasma Concentration of Metabolite Oseltamivir Carboxylate by Timepoint in CAPD Participants
NCT02617784 (43) [back to overview]Plasma Concentration of Metabolite Oseltamivir Carboxylate by Timepoint in HD Participants
NCT02617784 (43) [back to overview]Plasma Concentration of Metabolite Oseltamivir Carboxylate in Arterial and Venous Blood by Timepoint in HD Participants
NCT02617784 (43) [back to overview]Plasma Concentration of Oseltamivir by Timepoint in CAPD Participants
NCT02617784 (43) [back to overview]Cmax of Metabolite Oseltamivir Carboxylate in HD Participants During Days 1 to 5
NCT02617784 (43) [back to overview]Plasma Concentration of Oseltamivir by Timepoint in HD Participants
NCT02617784 (43) [back to overview]Terminal Elimination Half-Life of Metabolite Oseltamivir Carboxylate in CAPD Participants
NCT02617784 (43) [back to overview]Tmax of Metabolite Oseltamivir Carboxylate in CAPD Participants
NCT02617784 (43) [back to overview]Tmax of Metabolite Oseltamivir Carboxylate in HD Participants
NCT02617784 (43) [back to overview]Tmax of Oseltamivir in CAPD Participants
NCT02617784 (43) [back to overview]Time to Maximum Plasma Concentration (Tmax) of Oseltamivir in HD Participants
NCT02617784 (43) [back to overview]CLd of Metabolite Oseltamivir Carboxylate in CAPD Participants
NCT02617784 (43) [back to overview]CLr of Metabolite Oseltamivir Carboxylate in CAPD Participants
NCT02617784 (43) [back to overview]CLr of Metabolite Oseltamivir Carboxylate in HD Participants
NCT02617784 (43) [back to overview]CLr of Oseltamivir in CAPD Participants
NCT02617784 (43) [back to overview]Cmax of Metabolite Oseltamivir Carboxylate in CAPD Participants During Days 1 to 6
NCT02617784 (43) [back to overview]Cmax of Metabolite Oseltamivir Carboxylate in CAPD Participants During Days 36 to 43
NCT02617784 (43) [back to overview]Cmax of Metabolite Oseltamivir Carboxylate in HD Participants During Days 38 to 43
NCT02617784 (43) [back to overview]Cmax of Oseltamivir in CAPD Participants During Days 1 to 6
NCT02617784 (43) [back to overview]Cmax of Oseltamivir in CAPD Participants During Days 36 to 43
NCT02617784 (43) [back to overview]Cmax of Oseltamivir in HD Participants During Days 38 to 43
NCT02617784 (43) [back to overview]Maximum Plasma Concentration (Cmax) of Oseltamivir in HD Participants During Days 1 to 5
NCT02617784 (43) [back to overview]Percentage of Oseltamivir Dose Eliminated by Dialysis as Metabolite Oseltamivir Carboxylate in CAPD Participants
NCT02617784 (43) [back to overview]Percentage of Oseltamivir Dose Eliminated by Dialysis as Unchanged Drug in CAPD Participants
NCT02717754 (10) [back to overview]Volume of Distribution (Vd) of Oseltamivir and RO0640802
NCT02717754 (10) [back to overview]Area Under the Plasma Concentration-Time Curve From Time 0 to Last Measurable Concentration (AUC0-last) of Oseltamivir and RO0640802
NCT02717754 (10) [back to overview]Clearance (CL) of Oseltamivir and RO0640802
NCT02717754 (10) [back to overview]Cmax of Oseltamivir and RO0640802
NCT02717754 (10) [back to overview]Half-Life (t1/2) of Oseltamivir and RO0640802
NCT02717754 (10) [back to overview]Time to Reach Maximum Plasma Concentration (Tmax) of Oseltamivir and RO0640802
NCT02717754 (10) [back to overview]Minimum Plasma Concentration (Cmin) of RO0640802
NCT02717754 (10) [back to overview]Area Under the Plasma Concentration-Time Curve From Time 0 to 12 Hour (AUC0-12h) of Oseltamivir and RO0640802 at Steady State
NCT02717754 (10) [back to overview]Maximum Plasma Concentration (Cmax) of Oseltamivir and RO0640802 at Steady State
NCT02717754 (10) [back to overview]Area Under the Plasma Concentration-Time Curve From Time 0 to Infinity (AUC0-inf) of Oseltamivir and RO0640802
NCT02780622 (20) [back to overview]Oral Plasma Clearance (CL/F) for Oseltamivir
NCT02780622 (20) [back to overview]Percentage of Participants With Adverse Events
NCT02780622 (20) [back to overview]Change From Baseline in Plasma Concentration of Vitamin K1
NCT02780622 (20) [back to overview]Change From Baseline in Maximum Observed Effect (Emax) of International Normalized Ratio (INR)
NCT02780622 (20) [back to overview]Change From Baseline in Maximum Observed Effect (Emax) in Factor VII Activity
NCT02780622 (20) [back to overview]Terminal Half-life (t½) for R- and S- Warfarin
NCT02780622 (20) [back to overview]Area Under the Plasma Effect-time Curve Over 96 Hours (AUEC[0-96 h]) for International Normalized Ratio (INR)
NCT02780622 (20) [back to overview]Area Under the Plasma Effect-time Curve Over 96 Hours (AUEC[0-96 h]) for Factor VII Activity
NCT02780622 (20) [back to overview]Time to Reach Maximum Change From Baseline in Factor VII Activity (Tmax)
NCT02780622 (20) [back to overview]Time to Reach Maximum Change From Baseline in International Normalized Ratio (INR) (Tmax)
NCT02780622 (20) [back to overview]Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to 12 Hours (AUC0-12h) for Oseltamivir and Oseltamivir Carboxylate
NCT02780622 (20) [back to overview]Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to 12 Hours (AUC0-12h) for R- and S- Warfarin
NCT02780622 (20) [back to overview]Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to 24 Hours (AUC0-24h) for Oseltamivir and Oseltamivir Carboxylate
NCT02780622 (20) [back to overview]Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to 24 Hours (AUC0-24h) for R- and S- Warfarin
NCT02780622 (20) [back to overview]Maximum Plasma Concentration (Cmax) for Oseltamivir and Oseltamivir Carboxylate
NCT02780622 (20) [back to overview]Maximum Plasma Concentration (Cmax) for R- and S- Warfarin
NCT02780622 (20) [back to overview]Oral Plasma Clearance (CL/F) for R- and S- Warfarin
NCT02780622 (20) [back to overview]Terminal Half-life (t½) for Oseltamivir and Oseltamivir Carboxylate
NCT02780622 (20) [back to overview]Time to Maximum Plasma Concentration (Tmax) for Oseltamivir and Oseltamivir Carboxylate
NCT02780622 (20) [back to overview]Time to Maximum Plasma Concentration (Tmax) for R- and S- Warfarin
NCT02927431 (19) [back to overview]Time to Respiratory Response (TTRR)
NCT02927431 (19) [back to overview]Time to Clinical Response (TTCR)
NCT02927431 (19) [back to overview]Percentage of Participants With Improved Respiratory Status Over Time
NCT02927431 (19) [back to overview]Percentage of Participants With Clinical Response Over Time
NCT02927431 (19) [back to overview]Number of Participants Used Antibiotics for Complications of Influenza
NCT02927431 (19) [back to overview]Change From Baseline in White Blood Cell Count (WBC) and Absolute Neutrophil Count (ANC)
NCT02927431 (19) [back to overview]Number of Participants With Any Non-serious Adverse Event (AE); Any Serious AE (SAE); Any AEs of Special Interest (AESIs)
NCT02927431 (19) [back to overview]Change From Baseline in White Blood Cell Count (WBC) and Absolute Neutrophil Count (ANC)
NCT02927431 (19) [back to overview]Change From Baseline in White Blood Cell Count (WBC) and Absolute Neutrophil Count (ANC)
NCT02927431 (19) [back to overview]Change From Baseline in Total Bilirubin (T. Bilirubin), Creatinine and Direct Bilirubin (D. Bilirubin)
NCT02927431 (19) [back to overview]Change From Baseline in Total Bilirubin (T. Bilirubin), Creatinine and Direct Bilirubin (D. Bilirubin)
NCT02927431 (19) [back to overview]Change From Baseline in Total Bilirubin (T. Bilirubin), Creatinine and Direct Bilirubin (D. Bilirubin)
NCT02927431 (19) [back to overview]Change From Baseline in Albumin and Total Protein
NCT02927431 (19) [back to overview]Change From Baseline in Albumin and Total Protein
NCT02927431 (19) [back to overview]Change From Baseline in Albumin and Total Protein
NCT02927431 (19) [back to overview]Change From Baseline in Alanine Amino Transferase (ALT), Aspartate Amino Transferase (AST) and Alkaline Phosphatase (ALP)
NCT02927431 (19) [back to overview]Change From Baseline in Alanine Amino Transferase (ALT), Aspartate Amino Transferase (AST) and Alkaline Phosphatase (ALP)
NCT02927431 (19) [back to overview]Change From Baseline in Alanine Amino Transferase (ALT), Aspartate Amino Transferase (AST) and Alkaline Phosphatase (ALP)
NCT02927431 (19) [back to overview]Number of Participants With Clinically Significant Abnormality in Electrocardiogram (ECG)
NCT02949011 (21) [back to overview]Area Under the Curve (AUC) Adjusted by Baseline in Viral RNA
NCT02949011 (21) [back to overview]Change From Baseline in Virus RNA (RT-PCR) at Each Time Point
NCT02949011 (21) [back to overview]Change From Baseline in Virus Titer at Each Time Point
NCT02949011 (21) [back to overview]Percentage of Participants Reporting Normal Temperature at Each Time Point
NCT02949011 (21) [back to overview]Percentage of Participants Whose Symptoms Were Improved at Each Time Point
NCT02949011 (21) [back to overview]Percentage of Participants With Adverse Events (AEs)
NCT02949011 (21) [back to overview]Percentage of Participants With Positive Influenza Virus by RT-PCR at Each Time Point
NCT02949011 (21) [back to overview]Body Temperature at Each Time Point
NCT02949011 (21) [back to overview]Time to Return to Preinfluenza Health Status
NCT02949011 (21) [back to overview]Time to Improvement of the Three Respiratory Symptoms
NCT02949011 (21) [back to overview]Percentage of Participants With Positive Influenza Virus Titer at Each Time Point
NCT02949011 (21) [back to overview]Time to Improvement of Individual Symptoms
NCT02949011 (21) [back to overview]Percentage of Participants With Influenza-related Complications
NCT02949011 (21) [back to overview]Time to Alleviation of Symptoms
NCT02949011 (21) [back to overview]Time to Resolution of Fever
NCT02949011 (21) [back to overview]Time to Improvement of the Four Systemic Symptoms
NCT02949011 (21) [back to overview]Time to Improvement of Influenza Symptoms
NCT02949011 (21) [back to overview]Percentage of Participants Requiring Systemic Antibiotics for Infections Secondary to Influenza Infection
NCT02949011 (21) [back to overview]Area Under the Curve (AUC) Adjusted by Baseline in Influenza Virus Titer
NCT02949011 (21) [back to overview]Time to Cessation of Viral Shedding Determined by Virus Titer
NCT02949011 (21) [back to overview]Time to Cessation of Viral Shedding Determined by Virus RNA
NCT02954354 (39) [back to overview]Percentage of Participants With Positive Influenza Virus by RT-PCR at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Percentage of Participants With Positive Influenza Virus by RT-PCR at Each Time Point in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Percentage of Participants With Positive Influenza Virus Titer at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Percentage of Participants With Positive Influenza Virus Titer at Each Time Point in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Time to Alleviation of Individual Symptoms in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Change From Baseline in Virus RNA (RT-PCR) at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Time to Alleviation of Symptoms in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Area Under the Curve (AUC) Adjusted by Baseline of Influenza Virus RNA in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Area Under the Curve (AUC) Adjusted by Baseline of Influenza Virus RNA in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Area Under the Curve (AUC) Adjusted by Baseline in Influenza Virus Titer in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Area Under the Curve (AUC) Adjusted by Baseline in Influenza Virus Titer in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Time to Return to Preinfluenza Health Status in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Time to Return to Preinfluenza Health Status in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Body Temperature at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Body Temperature at Each Time Point in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Change From Baseline in Composite Symptom Score at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Change From Baseline in Composite Symptom Score at Each Time Point in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Time to Alleviation of Individual Symptoms in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Time to Alleviation of the Three Respiratory Symptoms in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Time to Alleviation of the Three Respiratory Symptoms in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Time to Cessation of Viral Shedding Determined by Virus RNA in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Time to Cessation of Viral Shedding Determined by Virus RNA in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Time to Cessation of Viral Shedding Determined by Virus Titer in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Time to Cessation of Viral Shedding Determined by Virus Titer in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Time to Resolution of Fever in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Time to Resolution of Fever in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Time to Alleviation of the Four Systemic Symptoms in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Time to Alleviation of the Four Systemic Symptoms in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Time to Alleviation of Symptoms in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Change From Baseline in Virus RNA (RT-PCR) at Each Time Point in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Change From Baseline in Virus Titer at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Change From Baseline in Virus Titer at Each Time Point in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Percentage of Participants Reporting Normal Temperature at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Percentage of Participants Reporting Normal Temperature at Each Time Point in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Percentage of Participants Whose Symptoms Were Alleviated at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Percentage of Participants Whose Symptoms Were Alleviated at Each Time Point in Participants Randomized to Baloxavir or Placebo
NCT02954354 (39) [back to overview]Percentage of Participants With Adverse Events (AEs)
NCT02954354 (39) [back to overview]Percentage of Participants With Influenza-related Complications in Adults Randomized to Baloxavir or Oseltamivir
NCT02954354 (39) [back to overview]Percentage of Participants With Influenza-related Complications in Participants Randomized to Baloxavir or Placebo
NCT03040141 (37) [back to overview]Total Number of Days on Ventilation
NCT03040141 (37) [back to overview]Viral Nasopharyngeal AUC
NCT03040141 (37) [back to overview]Viral Nasopharyngeal AUC by TCID50
NCT03040141 (37) [back to overview]Viral Nasopharyngeal AUC by TCID50
NCT03040141 (37) [back to overview]All Cause and Attributable Mortality at Day 14
NCT03040141 (37) [back to overview]All Cause and Attributable Mortality by Day 28
NCT03040141 (37) [back to overview]The Half-life of VIS410 in Participant's Serum
NCT03040141 (37) [back to overview]All Cause and Attributable Mortality Day 56
NCT03040141 (37) [back to overview]Viral Titer in Upper Respiratory Samples by qRT-PCR
NCT03040141 (37) [back to overview]Comparison of Ordinal Scale Parameters - Days in Hospital/ICU
NCT03040141 (37) [back to overview]Comparison of Ordinal Scale Parameters - Days in ICU
NCT03040141 (37) [back to overview]Comparison of Ordinal Scale Parameters - Days in ICU
NCT03040141 (37) [back to overview]Comparison of Ordinal Scale Parameters - Days on Ventilation
NCT03040141 (37) [back to overview]Comparison of Ordinal Scale Parameters - Days on Ventilation
NCT03040141 (37) [back to overview]Negative Viral Cultures by Study Day
NCT03040141 (37) [back to overview]Number of Participants With Influenza-related Complications
NCT03040141 (37) [back to overview]The Number of Participants With Adverse Events and Serious Adverse Events Following Administration of VIS410
NCT03040141 (37) [back to overview]Area Under the Viral Load-Time Curve (VL AUC) Based on qRT-PCR From Nasopharyngeal Swabs Through Day 14
NCT03040141 (37) [back to overview]Area Under the Viral Load-Time Curve (VL AUC) Based on qRT-PCR From Nasopharyngeal Swabs Through Day 7
NCT03040141 (37) [back to overview]Clinical Status Ordinal Scale Mean Area Under the Curve Through Day 14.
NCT03040141 (37) [back to overview]Healthcare Resource Utilization. Days in Hospital and/or ICU
NCT03040141 (37) [back to overview]Median Time to Resolution of Viral Load by Treatment Arm by qRT-PCR - From End of Infusion
NCT03040141 (37) [back to overview]Median Time to Resolution of Viral Load by Treatment Arm by TCID50 - From End of Infusion
NCT03040141 (37) [back to overview]Median Time to Resolution of Viral Load by Treatment Arm by TCID50 - From Onset of Symptoms
NCT03040141 (37) [back to overview]Number of Days to Resumption of Usual Activities
NCT03040141 (37) [back to overview]Time to Cessation of Oxygen Support for Any Patient Requiring Supplemental Oxygen Therapy
NCT03040141 (37) [back to overview]Number of Participants in Whom Peak Viral Load Occurred Post Baseline Measured by qRT-PCR
NCT03040141 (37) [back to overview]Peak Viral Load by TCID50
NCT03040141 (37) [back to overview]The Area Under the Concentration/Time Curve of VIS410 in Participant's Serum
NCT03040141 (37) [back to overview]The Clearance Rate (Cl) of VIS410 in Participant's Serum
NCT03040141 (37) [back to overview]The Maximum Concentration (Cmax) of VIS410 in Participant's Serum
NCT03040141 (37) [back to overview]Time to Cessation of Oxygen Support Compared to Oseltamivir Alone Among Patients Requiring Supplemental Oxygen Therapy With Baseline Room Air <= 92%
NCT03040141 (37) [back to overview]Number of Participants in Whom Peak Viral Load Occurred Post Baseline Measured by TCID50
NCT03040141 (37) [back to overview]Clinical Status Ordinal Scale Mean Area Under the Curve Through Day 7
NCT03040141 (37) [back to overview]Time to Clinical Response (4 Out of 5 Vital Signs)
NCT03040141 (37) [back to overview]Time to Complete Clinical Response (Resolution of All Vital Signs)
NCT03040141 (37) [back to overview]Total Number of Days in ICU
NCT03629184 (29) [back to overview]Duration of Fever
NCT03629184 (29) [back to overview]Duration of Symptoms
NCT03629184 (29) [back to overview]Time to Alleviation of Influenza Signs and Symptoms
NCT03629184 (29) [back to overview]Time to Cessation of Viral Shedding by RT-PCR
NCT03629184 (29) [back to overview]Area Under the Curve in the Amount of Virus RNA (RT-PCR)
NCT03629184 (29) [back to overview]Area Under the Concentration to Time Curve From Time 0 to Infinity (AUC0-inf) of S-033447.
NCT03629184 (29) [back to overview]Area Under the Concentration to Time Curve From Time 0 to Infinity (AUC0-inf) of Baloxavir Marboxil
NCT03629184 (29) [back to overview]Time to Return to Normal Health and Activity
NCT03629184 (29) [back to overview]Plasma Concentrations of Baloxavir Marboxil by Dosage
NCT03629184 (29) [back to overview]Plasma Concentrations of Baloxavir Marboxil - Sparse PK Population
NCT03629184 (29) [back to overview]Plasma Concentrations of S-033447 - Extensive PK Population
NCT03629184 (29) [back to overview]Percentage of Participants With Positive Influenza Virus Titer at Day 2, 4, 6, 10
NCT03629184 (29) [back to overview]Percentage of Participants With Influenza-Related Complications
NCT03629184 (29) [back to overview]Percentage of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT03629184 (29) [back to overview]Percentage of Participants Requiring Antibiotics
NCT03629184 (29) [back to overview]Percentage of Participants Positive by RT-PCR at Day 2, 4, 6, 10, 15, 29
NCT03629184 (29) [back to overview]Maximum Plasma Concentration (Cmax) of S-033447
NCT03629184 (29) [back to overview]Maximum Plasma Concentration (Cmax) of Baloxavir Marboxil
NCT03629184 (29) [back to overview]Frequency of Influenza-Related Complications
NCT03629184 (29) [back to overview]Change From Baseline in the Amount of Virus RNA (RT-PCR) at Day 2, 4, 6, 10, 15, 29
NCT03629184 (29) [back to overview]Change From Baseline in the Amount of Virus RNA (RT-PCR) at Day 2, 4, 6, 10, 15, 29
NCT03629184 (29) [back to overview]Change From Baseline in Influenza Virus Titer at Day 2, 4, 6, 10, 15, 29
NCT03629184 (29) [back to overview]Plasma Concentrations of S-033447 - Sparse PK Population
NCT03629184 (29) [back to overview]Plasma Concentrations of S-033447 by Dosage
NCT03629184 (29) [back to overview]Time to Maximum Plasma Concentration (Tmax) of S-033447
NCT03629184 (29) [back to overview]Area Under the Curve in Virus Titer
NCT03629184 (29) [back to overview]Time to Cessation of Viral Shedding by Virus Titer
NCT03629184 (29) [back to overview]Time to Maximum Plasma Concentration (Tmax) of Baloxavir Marboxil
NCT03629184 (29) [back to overview]Plasma Concentrations of Baloxavir Marboxil - Extensive PK Population

Participants Meeting Criteria for Day 5 Clinical Failure

"Proportion of participants that have clinical failure by day 5. Subjects that meet one of the following on Day 5 will be classified as a clinical failure:~Severe tachypnea (respiratory rate ≥ 30 for ages ≥12 years, rate ≥ 40 for ages 6 to 12 years, rate ≥45 for ages 3 to 6 years, rate ≥ 50 for ages 1 to 3 years)~Severe dyspnea (unable to speak full sentences, or use of accessory respiratory muscles)~Arterial oxygen saturation ≤92% on room air by trans-cutaneous method~Need for mechanical ventilation or intensive care unit (ICU) admission For the purpose of endpoint definition, death prior to or on Day 5 will also be considered a clinical failure at Day 5." (NCT00298233)
Timeframe: After 5 days of treatment

Interventionparticipants (Number)
Double Dose Oseltamivir16
Standard Dose Oseltamivir20

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Proportion of All Participants Negative for Viral RNA on Day 5

Proportion of all participants with no detectable viral RNA by reverse transcriptase-polymerase chain reaction (RT-PCR) in a combined nasal and throat swab sample on day 5. (NCT00298233)
Timeframe: After 5 days of treatment

Interventionparticipants (Number)
Double Dose Oseltamivir115
Standard Dose Oseltamivir105

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Median Time (Days) Receipt of Oxygen

(NCT00298233)
Timeframe: Throughout study, 14 days

Interventiondays (Median)
Double Dose Oseltamivir3
Standard Dose Oseltamivir3.5

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Median Time (Days) on Ventilation

Use of mechanical ventilation at any time for subjects with severe influenza and avian influenza. (NCT00298233)
Timeframe: Throughout study, 14 days

Interventiondays (Median)
Double Dose Oseltamivir2.5
Standard Dose Oseltamivir5

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Median Time (Days) in ICU

(NCT00298233)
Timeframe: Throughout study, 14 days

Interventiondays (Median)
Double Dose Oseltamivir4.4
Standard Dose Oseltamivir5

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In-hospital Mortality Rates

Standard therapy with oseltamivir is five days. Those patients with persistent symptoms on day five were continued on the randomized dose for an additional five days and assessments were performed up to day 10. (NCT00298233)
Timeframe: After up to 10 days of treatment

Interventionparticipants (Number)
Double Dose Oseltamivir12
Standard Dose Oseltamivir9

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Correlation of Clearance of Viral RNA by Polymerase Chain Reaction (PCR) to Pharmacokinetic Parameters by Cohort.

The Spearman coefficient and the p-values were computed between the clearance of viral RNA and oseltamivir carboxylate Area Under the Curve from 0 to 12 hours (AUC 0-12) (NCT00391768)
Timeframe: From date of enrollment until the date of first documented absence of viral load by culture, assessed up to 10 days after enrollment.

,,,,,,
Interventioncorrelation measure (Number)
AUC0-12 (hr*ng/mL) unit: Spearman CoefficientAUC0-12 (hr*ng/mL) unit: P value
Cohort IA0.570.08
Cohort IBNANA
Cohort IIA0.210.79
Cohort IIB0.900.04
Cohort III0.280.30
Cohort IV0.040.93
Cohort V0.070.77

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Correlation of Clearance of Viral RNA by Culture With Pharmacokinetic Parameters by Cohort

The Spearman coefficient and the p-values were computed between the clearance of Viral RNA and Oseltamivir Carboxylate Area under the curve from 0 to 12 hours (AUC0-12) (NCT00391768)
Timeframe: Day to negative viral load for subjects positive at baseline

InterventionSpearman coefficient (Number)
Cohort IA0.67
Cohort IBNA
Cohort IIA0.40
Cohort IIB0.62
Cohort III0.09
Cohort IV0.30
Cohort V0.01

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Incidence of All Serious Adverse Events by Cohort and System Organ Class (SOC)

Serious Adverse Event (SAE) were classified by MedDRA System Organ Class (SOC). An SAE was reported if it met the following criteria and occurred after the first dose of study medication through the end of the study: death throughout study participation; life threatening; requires inpatient hospitalization or prolongation of existing hospitalization during the period of protocol defined surveillance; results in congenital anomaly or birth defect; results in a persistent or significant disability; and an event considered serious by the PI. (NCT00391768)
Timeframe: Duration of study, from receipt of the first dose of study drug and continuing through study visit Day 30 plus or minus 3 days

,,,,,,
InterventionParticipants (Number)
TotalGeneral Disorders & Administration Site ConditionsImmune System DisordersInfections and InfestationsInvestigationsRespiratory, thoracic & mediastinal disorders
Cohort IA200200
Cohort IB000000
Cohort IIA101000
Cohort IIB200110
Cohort III210100
Cohort IV100001
Cohort V000000

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Number and Characteristics of Adverse Events (AEs) Described as Neurological Events.

Any neurological event that occurred post first dose of drug administration that was not present at baseline was considered an AE. Expected flu symptoms were not reported as AEs but were collected separately. (NCT00391768)
Timeframe: Duration of study, from receipt of the first dose of study drug and continuing through study visit Day 30 plus or minus 3 days.

,,,,,,
Interventionparticipants (Number)
Event - LethargyEvent - Tremor
Cohort IA00
Cohort IB01
Cohort IIA00
Cohort IIB00
Cohort III10
Cohort IV00
Cohort V00

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Oseltamivir Carboxylate AUC12 (Area Under the Curve).

The oseltamivir carboxylate AUC12 was derived from a series of five blood draws over 10 to 12 hours. (NCT00391768)
Timeframe: Day 3 of drug administration

,,,,,,
Interventionparticipants (Number)
AUC12 <2660AUC12 > or = 2660 and <7700AUC12 > or =7700
Cohort IA640
Cohort IB120
Cohort IIA330
Cohort IIB070
Cohort III2191
Cohort IV0100
Cohort V3133

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Overall Reported Adverse Events (AEs) Thought to be Associated With Study Therapy.

Any event considered associated with drug that occurred post first dose of drug administration that was not present at baseline was considered an AE. Expected flu symptoms were not reported as AEs but were collected separately. (NCT00391768)
Timeframe: Duration of study, from receipt of the first dose of study drug and continuing through study visit Day 30 plus or minus 3 days.

,,,,,,
Interventionparticipants (Number)
Event - VomitingEvent - Dermatitis DiaperEvent - Rash
Cohort IA300
Cohort IB000
Cohort IIA000
Cohort IIB000
Cohort III210
Cohort IV000
Cohort V001

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Number of Participants With Laboratory Confirmed Clinical Influenza, Intent-to-treat Virus Negative at Baseline (ITTNAB) Population

Laboratory-confirmed clinical influenza was defined as a fever (oral or otic temperature greater than 37.2 °C) and a symptom score for cough and/or coryza (nasal congestion on the diary cards, where 0=absent, 1=mild, 2=moderate, and 3=severe) of 1, 2 or 3 on the same day as fever, and laboratory confirmation of influenza either by detection of viral shedding by viral culture from nasopharyngeal swabs within two days of fever and symptoms, and/or by 4-fold or greater increase in serum HAI titers measured from baseline to any point during the study. (NCT00412737)
Timeframe: From baseline up to 28 days after the last dose of study drug (maximum up to 112 days)

Interventionparticipants (Number)
Placebo7
Oseltamivir4

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Number of Participants With Laboratory Confirmed Clinical Influenza, Per Protocol (PP) Population

Laboratory-confirmed clinical influenza was defined as a fever (oral or otic temperature greater than 37.2 °C) and a symptom score for cough and/or coryza (nasal congestion on the diary cards, where 0=absent, 1=mild, 2=moderate, and 3=severe) of 1, 2 or 3 on the same day as fever, and laboratory confirmation of influenza either by detection of viral shedding by viral culture from nasopharyngeal swabs within two days of fever and symptoms, and/or by 4-fold or greater increase in serum HAI titers measured from baseline to any point during the study. (NCT00412737)
Timeframe: From baseline up to 28 days after the last dose of study drug (maximum up to 112 days)

Interventionparticipants (Number)
Placebo6
Oseltamivir4

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Number of Participants With Laboratory-Confirmed Clinical Influenza, ITT Population

Laboratory-confirmed clinical influenza was defined as a fever (oral or otic temperature greater than [>] 37.2 degrees Celsius [°C]) and a symptom score for cough and/or coryza (nasal congestion on the diary cards, where 0=absent, 1=mild, 2=moderate, and 3=severe) of 1, 2 or 3 on the same day as fever, and laboratory confirmation of influenza either by detection of viral shedding by viral culture from nasopharyngeal swabs within two days of fever and symptoms, and/or by 4-fold or greater increase in serum hemagglutination inhibition (HAI) titers measured from baseline to any point during the study. (NCT00412737)
Timeframe: From baseline up to 28 days after the last dose of study drug (maximum up to 112 days)

Interventionparticipants (Number)
Placebo7
Oseltamivir5

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Number of Participants With Reverse Transcriptase Polymerase Chain Reaction (RT-PCR) Confirmed Clinical Influenza, ITT Population

RT-PCR confirmed clinical influenza was defined as a confirmation of influenza by positive RT-PCR result within 2 days of symptoms/last dose from baseline to any point during the study. (NCT00412737)
Timeframe: From baseline up to 28 days after the last dose of study drug (maximum up to 112 days)

Interventionparticipants (Number)
Placebo7
Oseltamivir2

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Number of Participants With RT-PCR Confirmed Clinical Influenza, ITTNAB Population

RT-PCR confirmed clinical influenza was defined as a confirmation of influenza by positive RT-PCR result within 2 days of symptoms/last dose from baseline to any point during the study. (NCT00412737)
Timeframe: From baseline up to 28 days after the last dose of study drug (maximum up to 112 days)

Interventionparticipants (Number)
Placebo7
Oseltamivir1

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Number of Participants With RT-PCR, or Serology/Viral Culture Confirmed Clinical Influenza, ITT Population

RT-PCR, or serology/viral culture confirmed clinical influenza was defined as a confirmation of influenza by positive RT-PCR or culture within 2 days of symptoms/ last dose and/or positive serology result from baseline to any point during the study. (NCT00412737)
Timeframe: From baseline up to 28 days after the last dose of study drug (maximum up to 112 days)

Interventionparticipants (Number)
Placebo8
Oseltamivir5

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Number of Participants With RT-PCR, or Serology/Viral Culture Confirmed Clinical Influenza, ITTNAB Population

RT-PCR, or serology/viral culture confirmed clinical influenza was defined as a confirmation of influenza by positive RT-PCR or culture within 2 days of symptoms/ last dose and/or positive serology result from baseline to any point during the study. (NCT00412737)
Timeframe: From baseline up to 28 days after the last dose of study drug (maximum up to 112 days)

Interventionparticipants (Number)
Placebo8
Oseltamivir4

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Change in Amount of Influenza Virus in Nose and Throat (Influenza A and B Combined)

Reduction in viral shedding, assessed as the change in quantitative viral titers and defined as the time-weighted change from baseline in TCID50/mL, was summarized for each treatment group. (NCT00453999)
Timeframe: Baseline, and 12, 24, 36, 48, 72, and 96 hours

,,
Interventionlog10 TCID50/mL (Mean)
Duration <48 Hours: BaselineDuration <48 Hours: Change at 12 hoursDuration <48 Hours: Change at 24 hoursDuration <48 Hours: Change at 48 hoursDuration <48 Hours: Change at 96 hoursDuration ≥48 and ≤72 hours: BaselineDuration ≥48 and ≤72 hours: Change at 12 hoursDuration ≥48 and ≤72 hours: Change at 24 hoursDuration ≥48 and ≤72 hours: Change at 48 hoursDuration ≥48 and ≤72 hours: Change at 96 hours
Oseltamivir3.4-1.5-2.2-2.5-2.82.5-0.7-1.0-1.5-1.7
Peramivir 200 mg3.6-1.5-2.5-2.4-2.82.8-1.1-1.4-1.8-2.6
Peramivir 400 mg3.5-1.6-2.2-2.9-3.02.6-1.5-1.7-1.9-2.0

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Incidence of Clinical Relapse of Influenza After Treatment (Number of Participants Experiencing Relapse During the Study)

The number of subjects with clinical relapse, defined as changes in 2 or more signs of clinical stability to values outside the range of normalization criteria for a duration of at least 12 consecutive hours after clinical stability had been attained, were summarized by treatment group. (NCT00453999)
Timeframe: 14 days

Interventionparticipants (Number)
Peramivir 200 mg0
Peramivir 400 mg0
Oseltamivir0

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Time to Clinical Stability (Kaplan-Meier Estimate)

Time to clinical stability was summarized overall and for individual clinical signs for each treatment group using the method of Kaplan Meier. Subjects who did not experience clinical stability were censored at the date of their last non-missing assessment during the study (whether this assessment occurred as an inpatient or as an outpatient). (NCT00453999)
Timeframe: 14 days

Interventionhours (Median)
Peramivir 200 mg23.7
Peramivir 400 mg37.0
Oseltamivir28.1

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Time to Hospital Discharge (Kaplan-Meier Estimate)

Time to discharge from hospital was estimated using the method of Kaplan Meier. Subjects who were not discharged from the hospital were censored at the time of their last assessment. (NCT00453999)
Timeframe: 14 days

Interventionhours (Median)
Peramivir 200 mg4.0
Peramivir 400 mg3.8
Oseltamivir4.0

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Time to Resumption of Ability to Perform Usual Activities (Kaplan-Meier Estimate)

Changes in each subject's ability to perform usual activities as determined from the visual analog scale (0 to 10, where 0 indicated subject was unable to perform usual activities at all and 10 indicated subject was able to perform all usual activities fully) were summarized by study visit and treatment group. The time to resumption of a subject's ability to perform usual activities was estimated using the method of Kaplan Meier. Subjects who did not return to the pre-study level of performance of usual activities were censored at the time of their last assessment. (Note: N is the number of ITTI participants with available data). (NCT00453999)
Timeframe: 14 days

Interventionhours (Median)
Peramivir 200 mg8.8
Peramivir 400 mg9.0
Oseltamivir13.7

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Change From Baseline in Scores of Symptoms of Influenza

Descriptive statistics for the change from baseline in each of the 7 symptoms of influenza (cough; sore throat; nasal congestion; myalgia [aches and pains]; headache; feverishness; and fatigue, each graded on a 4-point severity scale [0, absent; 1, mild; 2, moderate; 3, severe]) were tabulated by treatment group. Missing data were excluded. (NCT00453999)
Timeframe: Baseline, Days 2, 3, 4, 5, 10, and 14

,,
Interventionunits on a scale (Mean)
Sore Throat: BaselineSore Throat: Change at Day 2Sore Throat: Change at Day 3Sore Throat: Change at Day 4Sore Throat: Change at Day 5Sore Throat: Change at Day 10Sore Throat: Change at Day 14Nasal Congestion: BaselineNasal Congestion: Change at Day 2Nasal Congestion: Change at Day 3Nasal Congestion: Change at Day 4Nasal Congestion: Change at Day 5Nasal Congestion: Change at Day 10Nasal Congestion: Change at Day 14Cough: BaselineCough: Change at Day 2Cough: Change at Day 3Cough: Change at Day 4Cough: Change at Day 5Cough: Change at Day 10Cough: Change at Day 14Aches and Pains: BaselineAches and Pains: Change at Day 2Aches and Pains: Change at Day 3Aches and Pains: Change at Day 4Aches and Pains: Change at Day 5Aches and Pains: Change at Day 10Aches and Pains: Change at Day 14Fatigue: BaselineFatigue: Change at Day 2Fatigue: Change at Day 3Fatigue: Change at Day 4Fatigue: Change at Day 5Fatigue: Change at Day 10Fatigue: Change at Day 14Headache: BaselineHeadache: Change at Day 2Headache: Change at Day 3Headache: Change at Day 4Headache: Change at Day 5Headache: Change at Day 10Headache: Change at Day 14Feeling Feverish: BaselineFeeling Feverish: Change at Day 2Feeling Feverish: Change at Day 3Feeling Feverish: Change at Day 4Feeling Feverish: Change at Day 5Feeling Feverish: Change at Day 10Feeling Feverish: Change at Day 14
Oseltamivir1.2-0.3-0.8-1.1-1.1-1.2-1.11.3-0.3-0.8-1.0-1.1-1.1-1.32.1-0.2-0.9-1.0-1.1-1.3-1.51.9-0.8-1.4-1.6-1.7-1.9-1.72.3-1.0-1.1-1.6-1.7-1.7-2.01.4-0.6-1.0-1.1-1.3-1.4-1.31.8-1.0-1.6-1.6-1.8-1.8-1.8
Peramivir 200 mg1.3-0.2-0.8-0.9-1.1-1.2-1.21.3-0.2-0.7-0.8-0.9-1.1-1.02.2-0.4-0.9-1.1-1.2-1.4-1.61.8-0.8-1.3-1.5-1.6-1.7-1.72.3-0.9-1.2-1.4-1.6-1.7-1.71.5-0.5-0.9-1.0-1.2-1.3-1.32.1-1.4-1.5-1.8-1.9-2.0-1.9
Peramivir 400 mg1.1-0.3-0.7-0.9-0.9-1.1-1.11.5-0.5-0.9-1.1-1.2-1.2-1.22.0-0.3-0.9-1.1-1.1-1.2-1.41.9-0.8-1.4-1.6-1.6-1.7-1.62.0-0.5-1.0-1.2-1.3-1.4-1.61.3-0.5-1.0-1.1-1.1-1.2-1.21.9-1.0-1.5-1.8-1.8-1.8-1.7

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Change From Baseline in Viral Load Assessed by Reverse Transcription Polymerase Chain Reaction (RT-PCR)

Nasopharyngeal swab samples were tested for influenza A and B RNA using semi-quantitative RT-PCR specific for influenza A and B matrix gene, respectively, after viral RNA isolation. Cycle threshold (Ct) value was determined for each sample. Conversion of Ct values into viral load, expressed as log10 virus particles/mL (vp/mL), was obtained using external standard curves ran in parallel in all RT-PCR experiments. A value of < 2.6 log10 vp/mL for Flu A strains and < 3.0 log10 vp/mL for Flu B strains was interpreted as a negative result. Data are reported for adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline (Day 1), Day 2/3, Day 6, Day 8, Day 11 end of treatment (EOT), follow-up (FU) Day 15 and FU Day 40.

Interventionlog10 vp/mL (Median)
>/= 18 years, Baseline (BL)>/= 18 years, Change from BL on Day 2/3>/= 18 years, Change from BL on Day 6>/= 18 years, Change from BL on Day 8>/= 18 years, Change from BL on Day 11>/= 18 years, Change from BL on Day 15>/= 18 years, Change from BL on Day 40< 18 years, BL< 18 years, Change from BL on Day 2/3< 18 years, Change from BL on Day 6< 18 years, Change from BL on Day 8< 18 years, Change from BL on Day 11< 18 years, Change from BL on Day 15
Conventional Dose6.47-1.20-2.36-2.66-3.51-3.63-4.805.88-0.66-1.971.56-0.891.26

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Time to Cessation of Viral Shedding by RT-PCR

Viral shedding was determined by direct viral load measurement from nasopharyngeal swabs by RT-PCR assay and expressed in log10 vp/mL. Reported is the time to cessation of viral shedding over time in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionhours (Median)
>/= 18 years< 18 years
Conventional Dose178.0181.0
Double Dose154.1180.5

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Change From Baseline in Viral Load Assessed by Culture

Nasopharyngeal swab samples were cultured in Madin-Darby Canine Kidney cells. Culture supernatants were harvested after 2 weeks, or after a full-blown cytopathic effect was observed. Presence of infectious viruses in the cell culture supernatants (viral titer), expressed as log10 50% Tissue Culture Infectious Dose/milliliter (TCID50/mL), was determined by hemagglutination assay using turkey erythrocytes for H1 and B viruses or by detection of the virus nucleoprotein (NP) using ELISA for H3 viruses. A value of < 0.5 log10 TCID50/mL was interpreted as negative. Data are reported for adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline (Day 1), Day 2/3, Day 6, Day 8, Day 11 end of treatment (EOT), follow-up (FU) Day 15 and FU Day 40.

,
InterventionTCID50/mL (Median)
>/= 18 years, Baseline (BL)>/= 18 years, Change from BL on Day 2/3>/= 18 years, Change from BL on Day 6>/= 18 years, Change from BL on Day 8>/= 18 years, Change from BL on Day 11>/= 18 years, Change from BL on Day 15>/= 18 years, Change from BL on Day 40< 18 years, BL< 18 years, Change from BL on Day 2/3< 18 years, Change from BL on Day 6< 18 years, Change from BL on Day 8< 18 years, Change from BL on Day 11< 18 years, Change from BL on Day 15< 18 years, Change from BL on Day 40
Conventional Dose3.38-1.50-2.50-2.75-2.88-3.00-3.003.13-1.00-2.00-2.50-2.50-2.50-2.50
Double Dose3.75-1.50-3.00-3.25-3.25-3.25-3.254.00-2.00-3.50-3.50-3.50-3.50-3.50

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Percentage of Participants Who Initiated Antibiotic Treatment

Secondary illness included bronchitis, pneumonia, acute sinusitis, sinusitis, lower respiratory infection or otitis media. Reported is the percentage of participants with secondary illness, who initiated antibiotic treatment, in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionpercentage of participants (Number)
>/= 18 years< 18 years
Conventional Dose8.214.3
Double Dose5.00.0

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Total Symptom Score Area Under the Efficacy Curve (AUE)

The overall extent and severity of illness was quantified by the AUE of the total symptom scores over the duration of illness, i.e., from the start of treatment to the time symptoms first alleviated. Total symptom scores were calculated from the sum of seven individual symptom scores with each individual symptom scored from 0 (healthy) to 3 (worst sickness) and a maximum total symptom score of 21. The AUE of these average scores was then calculated for each participant using the trapezoidal rule (the trapezoidal rule calculates the area under any curve by adding up all trapezoids under such a curve). A larger area indicates more severe disease. In this study participants were treated for 10 days. If a participant had scored 21 on every visit then AUE would have been 21 score x 10 days x 24 hours/day =5040 score x hours units, which is the highest possible score. The lowest possible score is 0. Reported are results for adults >/= 18 years in the mITTi population. (NCT00545532)
Timeframe: Baseline up to Day 40

Interventionscore * hour (Median)
Conventional Dose774.7
Double Dose811.5

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Pharmacokinetics: Trough Plasma Concentration (Ctrough) of Oseltamivir in Adults

Reported here are oseltamivir Ctrough data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionng/mL (Mean)
Conventional Dose2.33
Double Dose6.98

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Pharmacokinetics: Tmax of Oseltamivir Carboxylate in Adults

Reported here are oseltamivir carboxylate tmax data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionhour (Mean)
Conventional Dose3.83
Double Dose3.96

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Pharmacokinetics: Time to Maximum Concentration (Tmax) of Oseltamivir in Adults

Reported here are oseltamivir tmax data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionhour (Mean)
Conventional Dose1.08
Double Dose1.08

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Pharmacokinetics: Elimination Constant (ke) of Oseltamivir in Adults

Reported here are oseltamivir ke data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Intervention1/hr (Mean)
Conventional Dose5.15
Double Dose4.79

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Pharmacokinetics: Maximum Plasma Concentration (Cmax) of Oseltamivir in Adults

Reported here are oseltamivir Cmax data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionnanograms per milliliter (ng/mL) (Mean)
Conventional Dose65.5
Double Dose149

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Pharmacokinetics: Elimination Constant (ke) of Oseltamivir Carboxylate in Adults

Reported here are oxeltamivir carboxylate ke data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Intervention1/hr (Mean)
Conventional Dose1.67
Double Dose1.61

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Percentage of Participants Hospitalized

Reported is the percentage of participants, who required hospitalization at any time between treatment initiation and the end of the study period, in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionpercentage of participants (Number)
>/= 18 years< 18 years
Conventional Dose6.811.1
Double Dose7.70.0

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Pharmacokinetics: Ctrough of Oseltamivir Carboxylate in Adults

Reported here are oseltamivir carboxylate Ctrough data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionng/mL (Mean)
Conventional Dose363
Double Dose831

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Pharmacokinetics: Cmax of Oseltamivir Carboxylate in Adults

Reported here are oseltamivir carboxylate Cmax data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionng/mL (Mean)
Conventional Dose655
Double Dose1420

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Pharmacokinetics: Apparent Volume of Distribution (Vc/F) of Oseltamivir in Adults

Reported here are oseltamivir Vc/F data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionliter (L) (Mean)
Conventional Dose77.5
Double Dose75.4

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Pharmacokinetics: Apparent Volume of Distribution (Vc/F) of Oseltamivir Carboxylate in Adults

Reported here are oseltamivir carboxylate Vc/F data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionliter (L) (Mean)
Conventional Dose8.39
Double Dose8.39

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Pharmacokinetics: Apparent Clearance (CL/F) of Oseltamivir in Adults

Reported here are oseltamivir CL/F data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionliter/hour (L/hr) (Mean)
Conventional Dose402
Double Dose367

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Pharmacokinetics: Apparent Clearance (CL/F) of Oseltamivir Carboxylate in Adults

Reported here are oseltamivir carboxylate CL/F data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

InterventionL/hr (Mean)
Conventional Dose14.0
Double Dose13.5

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Pharmacokinetics : AUC0-12 at Steady State of Oseltamivir Carboxylate in Adults

Reported here are oseltamivir carboxylate AUC0-12 data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionng*hr/mL (Mean)
Conventional Dose6240
Double Dose13800

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Pharmacokinetics : Area Under the Concentration-Time Curve From 0 to 12 Hours (AUC0-12) at Steady State of Oseltamivir in Adults

AUC0-12 was reported at steady state as nanograms per hour per milliliter. (ng*hr/mL). Reported here are oseltamivir AUC0-12 data for adults >/= 18 years. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours on Day 6 or any day after the 11th dose

Interventionng*hr/mL (Mean)
Conventional Dose197
Double Dose501

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Percentage of Participants With Tissue Rejection or Graft Versus Host Disease (GVHD)

The percentage of transplant patients in the safety population who experienced tissue rejection and/or GvHD is reported. (NCT00545532)
Timeframe: Baseline up to Day 40

Interventionpercentage of participants (Number)
Conventional Dose0
Double Dose0

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Percentage of Participants With Persistent Viral Shedding

Persistent shedding was defined as a viral load reduction <1 log10 vp/mL at end of treatment compared with baseline. Reported is the percentage of participants with persistent viral shedding at end of treatment in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline to Day 11 (EOT)

Interventionpercentage of participants (Number)
Conventional Dose1.2
Double Dose4.7

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Pharmacokinetics: Tmax of Oseltamivir in Adolescents and Children

Reported here are oseltamivir data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionhour (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation1111.25

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Time to Cessation of Viral Shedding by Cell Culture

Viral shedding was determined through measurement of the viral titer after viral culture in Madin-Darby Canine Kidney cells by hemagglutination assay (for Flu A/H1N1 and Flu B) and NP-ELISA (for Flu A/H3N2) and expressed in log10 TCID50/mL. Reported is the time to cessation of viral shedding over time in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionhours (Median)
>/= 18 years< 18 years
Conventional Dose105.0150.3
Double Dose105.494.9

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Time to Resolution (TTR) of All Clinical Influenza Symptoms

TTR of all clinical influenza symptoms was defined as the time from treatment initiation to the start of the 24-hour period in which all 7 influenza symptoms had scores /= 18 years, adults and adolescents >/= 13 years and children <13 years in the mITTi population. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionhours (Median)
Adults >/= 18 yearsAdults and adolescents >/= 13 yearsChildren < 13 years
Conventional Dose103.3103.432.1
Double Dose103.6107.2115.9

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Time to Resolution of Fever

Fever was defined as temperature >/= 37.8 degrees Celsius at any time point during the study. TTR of fever was determined in Adults >/= 18 years, Adults and adolescents >/= 13 years and Children < 13 years of the mITTi population. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionhours (Median)
Adults >/= 18 yearsAdults and adolescents >/= 13 yearsChildren < 13 years
Conventional Dose11.011.0NA
Double Dose0.50.526.0

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Percentage of Participants With Viral Shedding Assessed by RT-PCR Over Time

Viral shedding was determined by direct viral load measurement from nasopharyngeal swabs by RT-PCR assay and expressed in log10 vp/mL. Reported is the percentage of subjects with viral shedding over time in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline (Day 1), Day 2/3, Day 6, Day 8, Day 11 end of treatment (EOT), follow-up (FU) Day 15 and FU Day 40.

,
Interventionpercentage of participants (Number)
>/= 18 years, Baseline>/= 18 years, Day 2/3>/= 18 years, Day 6>/= 18 years, Day 8>/= 18 years, Day 11>/= 18 years, Day 15>/= 18 years, Day 40< 18 years, Baseline< 18 years, Day 2/3< 18 years, Day 6< 18 years, Day 8< 18 years, Day 11< 18 years, Day 15< 18 years, Day 40
Conventional Dose100.092.856.741.525.410.61.5100.085.785.720.028.642.90.0
Double Dose97.488.049.323.421.99.01.5100.075.057.142.914.30.00.0

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Percentage of Participants With Viral Shedding Assessed by Culture Over Time

Viral shedding was determined through measurement of the viral titer after viral culture in Madin-Darby Canine Kidney cells by hemagglutination assay (for Flu A/H1N1 and Flu B) and NP-ELISA (for Flu A/H3N2) and expressed in log10 TCID50/mL. Reported is the percentage of participants with viral shedding over time in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline (Day 1), Day 2/3, Day 6, Day 8, Day 11 end of treatment (EOT), follow-up (FU) Day 15 and FU Day 40.

,
Interventionpercentage of participants (Number)
>/= 18 years, Baseline>/= 18 years, Day 2/3>/= 18 years, Day 6>/= 18 years, Day 8>/= 18 years, Day 11>/= 18 years, Day 15>/= 18 years, Day 40< 18 years, Baseline< 18 years, Day 2/3< 18 years, Day 6< 18 years, Day 8< 18 years, Day 11< 18 years, Day 15< 18 years, Day 40
Conventional Dose91.467.215.43.21.57.90.0100.071.442.90.014.328.60.0
Double Dose84.258.918.34.84.21.50.0100.075.00.00.00.00.00.0

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Percentage of Participants With Adverse Events

An adverse event is any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with the treatment. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a pharmaceutical product, whether or not considered related to the pharmaceutical product. Preexisting conditions which worsen during a study are also considered as adverse events. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionpercentage of participants (Number)
On TreatmentOff Treatment
Conventional Dose40.025.7
Double Dose47.329.1

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Change From Baseline in Viral Load Assessed by Reverse Transcription Polymerase Chain Reaction (RT-PCR)

Nasopharyngeal swab samples were tested for influenza A and B RNA using semi-quantitative RT-PCR specific for influenza A and B matrix gene, respectively, after viral RNA isolation. Cycle threshold (Ct) value was determined for each sample. Conversion of Ct values into viral load, expressed as log10 virus particles/mL (vp/mL), was obtained using external standard curves ran in parallel in all RT-PCR experiments. A value of < 2.6 log10 vp/mL for Flu A strains and < 3.0 log10 vp/mL for Flu B strains was interpreted as a negative result. Data are reported for adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline (Day 1), Day 2/3, Day 6, Day 8, Day 11 end of treatment (EOT), follow-up (FU) Day 15 and FU Day 40.

Interventionlog10 vp/mL (Median)
>/= 18 years, Baseline (BL)>/= 18 years, Change from BL on Day 2/3>/= 18 years, Change from BL on Day 6>/= 18 years, Change from BL on Day 8>/= 18 years, Change from BL on Day 11>/= 18 years, Change from BL on Day 15>/= 18 years, Change from BL on Day 40< 18 years, BL< 18 years, Change from BL on Day 2/3< 18 years, Change from BL on Day 6< 18 years, Change from BL on Day 8< 18 years, Change from BL on Day 11
Double Dose6.52-1.35-2.34-2.62-2.96-2.60-7.715.96-0.71-1.73-2.26-2.41

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Percentage of Participants Who Developed Viral Resistance to Oseltamivir

Resistance was defined as the presence of oseltamivir resistance mutations in viruses isolated from nasopharyngeal swab samples, identified by sequencing of the neuraminidase (NA) and hemagglutinin (HA) genes (genotypic resistance) and/or determination of the oseltamivir concentration at which the response is reduced by half (IC50) in an NA inhibition assay (phenotypic resistance). Reported are post-baseline phenotypic and genotypic resistance in adults >/= 18 years and children and adolescents <18 years in the modified Intent-to-Treat infected (mITTi) population. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionpercentage of participants (Number)
Post-BL Phenotypic Resist, >/= 18 yearsPost-BL Genotypic Resist, >/= 18 yearsPost-BL Phenotypic Resist, < 18 yearsPost-BL Genotypic Resist, < 18 years
Conventional Dose8.29.625.025.0
Double Dose1.32.6012.5

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Percentage of Participants Who Developed Secondary Illness

Secondary illness included bronchitis, pneumonia, acute sinusitis, sinusitis, lower respiratory infection or otitis media. Reported is the percentage of participants with at least one event in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventionpercentage of participants (Number)
>/=18 years< 18 years
Conventional Dose8.212.5
Double Dose5.10.0

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Duration of Hospitalization

Reported is the duration of hospitalization at any time between treatment initiation and the end of the study period, in adults >/= 18 years and adolescents and children < 18 years. (NCT00545532)
Timeframe: Baseline up to Day 40

,
Interventiondays (Median)
>/= 18 years< 18 years
Conventional Dose7.05.0
Double Dose6.50NA

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Pharmacokinetics: Tmax of Oseltamivir Carboxylate in Adolescents and Children

Reported here are oseltamivir carboxylate tmax data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionhour (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation3.75444

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Pharmacokinetics: Elimination Constant (ke) of Oseltamivir in Adolescents and Children

Reported here are oseltamivir ke data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Intervention1/hr (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation4.224.563.405.74

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Pharmacokinetics: Elimination Constant (ke) of Oseltamivir Carboxylate in Adolescents and Children

Reported here are oseltamivir carboxylate ke data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Intervention1/hr (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation2.011.121.442.12

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Pharmacokinetics: Ctrough of Oseltamivir in Adolescents and Children

Reported here are oseltamivir Ctrough data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionng/mL (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation2.843.376.653.88

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Pharmacokinetics: Ctrough of Oseltamivir Carboxylate in Adolescents and Children

Reported here are oseltamivir carboxylate Ctrough data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionng/mL (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation215459445464

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Pharmacokinetics: Cmax of Oseltamivir in Adolescents and Children

Reported here are oseltamivir Cmax data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionng/mL (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation61.945.910786.6

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Pharmacokinetics: Cmax of Oseltamivir Carboxylate in Adolescents and Children

Reported here are oseltamivir carboxylate Cmax data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

Interventionng/mL (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation363848770906

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Pharmacokinetics: AUC0-12 at Steady State of Oseltamivir in Adolescents and Children

AUC0-12 will be reported at steady state as ng*hr/mL. Reported here are oseltamivir AUC0-12 data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours on Day 6 or any day after the 11th dose

Interventionng*hr/mL (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation229171425339

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Pharmacokinetics: AUC0-12 at Steady State of Oseltamivir Carboxylate in Adolescents and Children

AUC0-12 will be reported at steady state as ng*hr/mL. Reported here are oseltamivir carboxylate AUC0-12 data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours on Day 6 or any day after the 11th dose

Interventionng*hr/mL (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation3550801074608420

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Pharmacokinetics: Apparent Volume of Distribution (Vc/F) of Oseltamivir in Adolescents and Children

Reported here are oseltamivir Vc/F data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

InterventionLiter (L) (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation62.396.462.376.9

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Pharmacokinetics: Apparent Volume of Distribution (Vc/F) of Oseltamivir Carboxylate in Adolescents and Children

Reported here are oseltamivir carboxylate Vc/F data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

InterventionLiter (L) (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation8.398.398.398.39

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Pharmacokinetics: Apparent Clearance (CL/F), of Oseltamivir Carboxylate in Adolescents and Children

Reported here are oseltamivir carboxylate CL/F data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

InterventionL/hr (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation16.99.3612.117.8

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Pharmacokinetics: Apparent Clearance (CL/F) of Oseltamivir in Adolescents and Children

Reported here are oseltamivir CL/F data for adolescents and children < 18 years. Individual data are provided as participants received different drug doses. Drug dose is indicated in the row title for each participant. (NCT00545532)
Timeframe: Pre-dose (30 minutes), 1.5, 4, 8 hours postdose on Day 6 or any day after the 11th dose

InterventionL/hr (Number)
Conventional Dose: 60 mgConventional Dose: 75 mgDouble Dose: 90 mgDouble Dose: 150 mg
Adolescents and Children With Pharmacokinetic Evaluation263439212442

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Mean Influenza Well-being Score

Mean influenza wellbeing score is calculated by first summing the daily scores for overall health (0-9 points), ability to perform usual activities (0-9 points), and sleep quality (0-9 points) from initial enrollment (randomization) up to (and including) the first day of symptom resolution. This is divided by the number of reporting days to yield the mean daily influenza wellbeing score for each person. Minimum score is 0 and maximum is 27. Higher scores indicate better outcome. (NCT00555893)
Timeframe: Randomization to resolution

Interventionscore on a scale (Mean)
Active Drug19.54
Placebo20.04

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Mean Illness Severity Score

Mean severity score will be calculated by first summing the symptom severity scores for all reporting periods from initial enrollment (randomization) up to (and including) the first period of symptom resolution, as defined above. The summed total will be divided by the number of reporting periods to yield the mean severity score for each participant. For each reporting period, the possible symptom scores will range from 0 (all symptoms absent) to 24 (all symptoms severe). For children less than 2 years old, the possible scores will range from 0 to 15. (NCT00555893)
Timeframe: Calculated from initial enrollment (randomization) up to first period of symptom resolution (minimum of 7 days, maximum of 14 days)

Interventionmean severity score (Median)
Active Drug6.1
Placebo5.8

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Duration of Influenza Illness

Resolution is defined as occurring at the start of the first 24-hour period in which the total symptom score was less than or equal to 2 with no symptom rated higher than mild. Time to resolution was calculated from the time of randomization to symptom resolution in 12 hour increments. (NCT00555893)
Timeframe: Interval (in 12 hour blocks) from time of randomization until resolution (minimum 7 days, maximum 14 days)

Interventiondays (Median)
Active Drug4
Placebo4

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Viral Shedding on Day 3-4 of Treatment

Proportion of participants with positive PCR on day 3-4 of treatment (NCT00555893)
Timeframe: 3-4 days after treatment initiation

InterventionParticipants (Count of Participants)
Active Drug12
Placebo4

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Time for Body Temperature to Return to Normal

Time for return to normal axillary temperature was was defined as the time until the beginning of the first 21.5-hour period in which the axillary temperature returned to 36.9°C. Patients recorded their axillary temperature 4 times daily for 15 days. Patients whose axillary temperature had not been returned to 36.9°C at the time of their withdrawal from the study or at the end of the observation period were censored. (NCT00803595)
Timeframe: 15 days

Interventionhours (Median)
CS-8958 High Dose 40 mg55.3
CS-8958 Low Dose 20 mg58.0
Oseltamivir 75 mg54.7

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Time to Alleviation of Influenza Illness

"The time to illness alleviation which was defined as the time from the initiation of trial treatment to the beginning of the first 21.5-h period in which all influenza symptoms were absent or mild. Patients recorded their severity of influenza symptoms (headache, myalgia/arthralgia, fatigue, chills/sweats, nasal symptom, sore throat, and cough) 4 times daily for 15 days. Patients whose influenza symptoms had not been alleviated at the time of their withdrawal from the study or at the end of the observation period were censored." (NCT00803595)
Timeframe: 15 days

Interventionhours (Median)
CS-8958 High Dose 40 mg73.0
CS-8958 Low Dose 20 mg85.8
Oseltamivir 75 mg73.6

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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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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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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 Deaths

(NCT00867139)
Timeframe: 58 days

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

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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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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 Intubations

(NCT00867139)
Timeframe: 58 days

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

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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 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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Frequency of Confirmed Pneumonia

(NCT00867139)
Timeframe: 58 days

Interventionparticipants (Number)
TCAD0
Neuraminidase Inihibitor Monotherapy0
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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Duration of Hospitalization

(NCT00867139)
Timeframe: from baseline up to 58 days

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

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Number of Participants With Viral RNA Detected by RT-PCR on Day 1 Among Children Treated With Oseltamivir

(NCT00884117)
Timeframe: Baseline (Day 1)

Interventionparticipants (Number)
TotalH3N2H1N1pdm09Influenza B
Children Treated With Oseltamivir1283583371329

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Number of Participants With Viral RNA Detected by RT-PCR on Day 10 Among Children Treated With Oseltamivir

(NCT00884117)
Timeframe: Day 10

Interventionparticipants (Number)
Total (n=1228)H3N2 (n=560)H1N1pdm09 (n=351)Influenza B (n=317)
Children Treated With Oseltamivir197736460

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Number of Participants With Viral RNA Detected by RT-PCR on Day 3 Among Adults Treated With Oseltamivir

(NCT00884117)
Timeframe: Day 3

Interventionparticipants (Number)
Total (n=912)H1N1 Seasonal (n=11)H3N2 (n=398)H1N1pdm09 (n=308)Influenza B (n=195)
Adults Treated With Oseltamivir78110341258172

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Number of Participants With Viral RNA Detected by RT-PCR on Day 3 Among Children Treated With Oseltamivir

(NCT00884117)
Timeframe: Day 3

Interventionparticipants (Number)
Total (n=1238)H3N2 (n=562)H1N1pdm09 (n=358)Influenza B (n=318)
Children Treated With Oseltamivir1050453315282

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Number of Participants With Viral RNA Detected by RT-PCR on Day 6 Among Adults Treated With Oseltamivir

(NCT00884117)
Timeframe: Day 6

Interventionparticipants (Number)
Total (n=889)H1N1 Seasonal (n=9)H3N2 (n=382)H1N1pdm09 (n=308)Influenza B (n=190)
Adults Treated With Oseltamivir317414411059

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Number of Participants With Viral RNA Detected by RT-PCR on Day 6 Among Children Treated With Oseltamivir

(NCT00884117)
Timeframe: Day 6

Interventionparticipants (Number)
Total (n=1250)H3N2 (n=567)H1N1pdm09 (n=362)Influenza B (n=321)
Children Treated With Oseltamivir628271181176

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Percentage of Participants by Day of Viral RNA First Not Detected Comparing Resistant and Susceptible Viruses

Pre-defined mutations in viral RNA were noted, the presence of which was defined as genotypic resistance. Phenotypic resistance was defined as IC50 more than 10-fold higher than the median value for all viruses of the same subtype. Treatment-emergent resistance was defined as the presence of genotypic or phenotypic resistance from a post-Baseline sample in the setting of a previously non-resistant Baseline sample. Susceptible viruses were those that did not exhibit treatment-emergent resistance. The percentage of participants by earliest post-Baseline test day on which viral RNA was not detected was reported and stratified by resistant and susceptible viruses. (NCT00884117)
Timeframe: Days 3, 6, 10

Interventionpercentage of participants (Number)
Day 3, Total (n=1682)Day 3, Resistant (n=59)Day 3, Susceptible (n=1623)Day 6, Total (n=1682)Day 6, Resistant (n=59)Day 6, Susceptible (n=1623)Day 10, Total (n=1682)Day 10, Resistant (n=59)Day 10, Susceptible (n=1623)
Participants Treated With Oseltamivir15.3015.840.510.241.730.459.329.4

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Number of Participants With Viral RNA Detected by RT-PCR on Day 10 Among Adults Treated With Oseltamivir

(NCT00884117)
Timeframe: Day 10

Interventionparticipants (Number)
Total (n=833)H3N2 (n=362)H1N1pdm09 (n=283)Influenza B (n=188)
Adults Treated With Oseltamivir88443311

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Percentage of Participants With Resistant Versus Susceptible Viruses by Baseline Viral Load

Pre-defined mutations in viral RNA were noted, the presence of which was defined as genotypic resistance. Phenotypic resistance was defined as IC50 more than 10-fold higher than the median value for all viruses of the same subtype. Treatment-emergent resistance was defined as the presence of genotypic or phenotypic resistance from a post-Baseline sample in the setting of a previously non-resistant Baseline sample. Susceptible viruses were those that did not exhibit treatment-emergent resistance. The mean viral load from each sample was expressed in log10 vp/mL and stratified by resistant and susceptible viruses. (NCT00884117)
Timeframe: Baseline (Day 1)

Interventionpercentage of participants (Number)
Total, Resistant (n=1802)Total, Susceptible (n=1802)Viral Load <4.95, Resistant (n=452)Viral Load <4.95, Susceptible (n=452)Viral Load 4.95 to 5.89, Resistant (n=450)Viral Load 4.95 to 5.89, Susceptible (n=450)Viral Load 5.89 to 6.61, Resistant (n=457)Viral Load 5.89 to 6.61, Susceptible (n=457)Viral Load >6.61, Resistant (n=443)Viral Load >6.61, Susceptible (n=443)
Participants Treated With Oseltamivir3.296.82.098.03.896.23.196.93.896.2

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Percentage of Participants With Symptom Resolution on Day 6 Comparing Resistant and Susceptible Viruses

Pre-defined mutations in viral RNA were noted, the presence of which was defined as genotypic resistance. Phenotypic resistance was defined as 50% inhibitory concentration (IC50) more than 10-fold higher than the median value for all viruses of the same subtype. Treatment-emergent resistance was defined as the presence of genotypic or phenotypic resistance from a post-Baseline sample in the setting of a previously non-resistant Baseline sample. Susceptible viruses were those that did not exhibit treatment-emergent resistance. The percentage of participants with mild or absent symptoms on Day 6 was reported and stratified by resistant and susceptible viruses. (NCT00884117)
Timeframe: Day 6

Interventionpercentage of participants (Number)
Total (n=1730)Resistant (n=59)Susceptible (n=1671)
Participants Treated With Oseltamivir61.255.961.4

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Viral Load Among Children Treated With Oseltamivir

Viral load was determined for those with detectable virus above the LLQ of 1.82 for influenza A viruses and 1.99 for influenza B viruses. The viral load from each sample was averaged among all participants and expressed in log10 vp/mL. (NCT00884117)
Timeframe: Days 1, 3, 6, 10

Interventionlog10 vp/mL (Mean)
Day 1, Total (n=1283)Day 1, H3N2 (n=583)Day 1, H1N1pdm09 (n=371)Day 1, Influenza B (n=329)Day 3, Total (n=1050)Day 3, H3N2 (n=453)Day 3, H1N1pdm09 (n=315)Day 3, Influenza B (n=282)Day 6, Total (n=628)Day 6, H3N2 (n=271)Day 6, H1N1pdm09 (n=181)Day 6, Influenza B (n=176)Day 10, Total (n=197)Day 10, H3N2 (n=73)Day 10, H1N1pdm09 (n=64)Day 10, Influenza B (n=60)
Children Treated With Oseltamivir5.85.65.76.14.54.14.35.23.83.63.74.13.33.13.13.6

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Viral Load Among Adults Treated With Oseltamivir

Viral load was determined for those with detectable virus above the lower limit of quantification (LLQ) of 1.82 for influenza A viruses and 1.99 for influenza B viruses. The viral load from each sample was averaged among all participants and expressed in log10 of the number of viral particles per milliliter (log10 vp/mL). (NCT00884117)
Timeframe: Days 1, 3, 6, 10

Interventionlog10 vp/mL (Mean)
Day 1, Total (n=959)Day 1, H1N1 Seasonal (n=12)Day 1, H3N2 (n=417)Day 1, H1N1pdm09 (n=323)Day 1, Influenza B (n=207)Day 3, Total (n=781)Day 3, H1N1 Seasonal (n=10)Day 3, H3N2 (n=341)Day 3, H1N1pdm09 (n=258)Day 3, Influenza B (n=172)Day 6, Total (n=317)Day 6, H1N1 Seasonal (n=4)Day 6, H3N2 (n=144)Day 6, H1N1pdm09 (n=110)Day 6, Influenza B (n=59)Day 10, Total (n=88)Day 10, H3N2 (n=44)Day 10, H1N1pdm09 (n=33)Day 10, Influenza B (n=11)
Adults Treated With Oseltamivir5.85.75.85.75.94.24.23.94.14.73.34.13.23.13.93.02.92.83.7

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Total Daily Symptom Score According to Global Assessment by the Investigator Among Children Treated With Oseltamivir

Symptoms were assessed on Days 1, 6, and 10. The Investigator rated seven symptoms of fever, sore throat, nasal congestion, cough, aches/pains, headache, and energy/tiredness on a scale of 0 (absent/no problem) to 3 (severe/major problem). The global score was calculated as a sum of all individual symptom scores. Global scores may range from 0 to 21, with higher scores indicating worse or more pronounced symptoms. (NCT00884117)
Timeframe: Days 1, 6, 10

Interventionunits on a scale (Mean)
Day 1, Total (n=1283)Day 1, H3N2 (n=583)Day 1, H1N1pdm09 (n=371)Day 1, Influenza B (n=329)Day 6, Total (n=1252)Day 6, H3N2 (n=567)Day 6, H1N1pdm09 (n=364)Day 6, Influenza B (n=321)Day 10, Total (n=1228)Day 10, H3N2 (n=562)Day 10, H1N1pdm09 (n=350)Day 10, Influenza B (n=316)
Children Treated With Oseltamivir12.412.311.913.03.33.23.23.51.31.31.41.3

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Total Daily Symptom Score According to Global Assessment by the Investigator Among Adults Treated With Oseltamivir

Symptoms were assessed on Days 1, 6, and 10. The Investigator rated seven symptoms of fever, sore throat, nasal congestion, cough, aches/pains, headache, and fatigue on a scale of 0 (absent/no problem) to 3 (severe/major problem). The global score was calculated as a sum of all individual symptom scores. Global scores may range from 0 to 21, with higher scores indicating worse or more pronounced symptoms. (NCT00884117)
Timeframe: Days 1, 6, 10

Interventionunits on a scale (Mean)
Day 1, Total (n=960)Day 1, H1N1 Seasonal (n=12)Day 1, H3N2 (n=419)Day 1, H1N1pdm09 (n=323)Day 1, Influenza B (n=206)Day 6, Total (n=890)Day 6, H1N1 Seasonal (n=9)Day 6, H3N2 (n=383)Day 6, H1N1pdm09 (n=307)Day 6, Influenza B (n=191)Day 10, Total (n=827)Day 10, H3N2 (n=357)Day 10, H1N1pdm09 (n=281)Day 10, Influenza B (n=189)
Adults Treated With Oseltamivir12.311.411.213.213.43.72.83.43.84.12.02.11.92.1

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Change From Baseline in Body Temperature Among Adults Treated With Oseltamivir

Body temperature was measured by the Investigator using an oral or tympanic thermometer at Baseline and Day 10. The change in body temperature between visits was averaged among all participants and expressed in degrees Celsius. (NCT00884117)
Timeframe: Baseline (Day 1) to Day 10

Interventiondegrees Celsius (Mean)
Total (n=826)H3N2 (n=355)H1N1pdm09 (n=282)Influenza B (n=189)
Adults Treated With Oseltamivir-1.4-1.2-1.7-1.4

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Body Temperature Among Adults Treated With Oseltamivir

Body temperature was measured by the Investigator using an oral or tympanic thermometer at Baseline and Day 10. Body temperature at each visit was averaged among all participants and expressed in degrees Celsius. (NCT00884117)
Timeframe: Days 1, 10

Interventiondegrees Celsius (Mean)
Day 1, Total (n=960)Day 1, H1N1 Seasonal (n=12)Day 1, H3N2 (n=418)Day 1, H1N1pdm09 (n=323)Day 1, Influenza B (n=207)Day 10, Total (n=827)Day 10, H3N2 (n=356)Day 10, H1N1pdm09 (n=282)Day 10, Influenza B (n=189)
Adults Treated With Oseltamivir38.037.837.838.238.036.636.636.636.6

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Time to Non-Detection of Viral RNA Among Participants With Influenza B Infections

Time to non-detection/viral clearance was the time between symptom onset and the day on which viral RNA was no longer detected, or the last visit date if the participant was not RNA-negative at that visit. Time to non-detection/viral clearance was estimated using Kaplan-Meier analysis and expressed in days. (NCT00884117)
Timeframe: From Baseline (Day 1) to Day 10 (assessed on Days 1, 3, 6, 10)

Interventiondays (Median)
Children ≤5 Years of Age Treated With Oseltamivir9.8
Children 6 to 12 Years of Age Treated With Oseltamivir10.0
Adults Treated With Oseltamivir7.4

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Time to Non-Detection of Viral RNA Among Participants With H3N2 Infections

Time to non-detection/viral clearance was the time between symptom onset and the day on which viral RNA was no longer detected, or the last visit date if the participant was not RNA-negative at that visit. Time to non-detection/viral clearance was estimated using Kaplan-Meier analysis and expressed in days. (NCT00884117)
Timeframe: From Baseline (Day 1) to Day 10 (assessed on Days 1, 3, 6, 10)

Interventiondays (Median)
Children ≤5 Years of Age Treated With Oseltamivir9.5
Children 6 to 12 Years of Age Treated With Oseltamivir8.0
Adults Treated With Oseltamivir8.0

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Time to Non-Detection of Viral RNA

Time to non-detection/viral clearance was the time between symptom onset and the day on which viral RNA was no longer detected, or the last visit date if the participant was not RNA-negative at that visit. Time to non-detection/viral clearance was estimated using Kaplan-Meier analysis and expressed in days. (NCT00884117)
Timeframe: From Baseline (Day 1) to Day 10 (assessed on Days 1, 3, 6, 10)

Interventiondays (Median)
Children ≤5 Years of Age Treated With Oseltamivir9.7
Children 6 to 12 Years of Age Treated With Oseltamivir8.2
Adults Treated With Oseltamivir7.9

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Percentage of Participants Exhibiting Treatment-Emergent Resistance by Study Year Among Participants With H3N2 or H1N1pdm09 Infections

Pre-defined mutations in viral RNA were noted, the presence of which was defined as genotypic resistance. Treatment-emergent resistance was defined as the presence of genotypic or phenotypic resistance from a post-Baseline sample in the setting of a previously non-resistant Baseline sample. The percentage of participants with treatment-emergent resistance was reported by study year for participants with H3N2 or H1N1pdm09 infections. Only data with evaluable participants were reported. (NCT00884117)
Timeframe: From Baseline (Day 1) to Day 10 (assessed on Days 1, 3, 6, 10) during Study Years 1, 2, 3, 4, 5, 6, 7

,,,,,
Interventionpercentage of participants (Number)
Year 1, H3N2 (n=0,1,1,2,2,4)Year 2, H1N1pdm09 (n=0,54,81,135,108,243)Year 2, H3N2 (n=0,0,0,0,22,22)Year 3, H1N1pdm09 (n=0,58,30,88,148,236)Year 3, H3N2 (n=0,37,43,80,122,202)Year 4, H1N1pdm09 (n=0,6,6,12,16,28)Year 4, H3N2 (n=0,19,17,36,67,103)Year 5, H1N1pdm09 (n=0,29,8,37,41,78)Year 5, H3N2 (n=0,82,80,162,187,349)Year 6, H1N1pdm09 (n=11,33,25,69,0,69)Year 6, H3N2 (n=1,45,27,73,0,73)Year 7, H1N1pdm09 (n=0,15,5,20,0,20)Year 7, H3N2 (n=8,94,115,217,0,217)
Adults Treated With Oseltamivir00.901.40.8004.91.1NANANANA
Children <1 Year of Age Treated With OseltamivirNANANANANANANANANA36.40NA0
Children 1 to 5 Years of Age Treated With Oseltamivir01.9NA20.72.716.710.520.78.56.1033.31.1
Children 6 to 12 Years of Age Treated With Oseltamivir00NA3.30011.812.51.34.0000.9
Children Treated With Oseltamivir00.7NA14.81.38.311.118.94.910.1025.00.9
Participants Treated With Oseltamivir00.806.41.03.63.911.52.910.1025.00.9

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Change From Baseline in Body Temperature Among Children Treated With Oseltamivir

Body temperature was measured by the Investigator using an oral or tympanic thermometer at Baseline and Day 10. The change in body temperature between visits was averaged among all participants and expressed in degrees Celsius. (NCT00884117)
Timeframe: Baseline (Day 1) to Day 10

Interventiondegrees Celsius (Mean)
Total (n=1222)H3N2 (n=560)H1N1pdm09 (n=345)Influenza B (n=317)
Children Treated With Oseltamivir-1.6-1.6-1.5-1.6

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Number of Participants With Genotypic Resistance

"Samples were analyzed using reverse transcriptase-polymerase chain reaction (RT-PCR). Pre-defined mutations in viral ribonucleic acid (RNA) were noted, the presence of which was defined as genotypic resistance. The number of participants with genotypic resistance at Baseline was reported. The number of participants with genotypic resistance post-Baseline was determined by a collective count of all participants who had a resistance mutation at least once on Days 3, 6, and/or 10. (Hereafter, H stands for hemagglutinin and N stands for neuraminidase in abbreviations of viral subtype such as H1N1, H1N1pdm09, and H3N2.)" (NCT00884117)
Timeframe: Baseline (Day 1) and post-Baseline (Days 3, 6, 10)

Interventionparticipants (Number)
Baseline, H1N1 Seasonal (n=47)Baseline, H1N1pdm09 (n=1240)Baseline, H3N2 (n=1432)Baseline, Influenza B (n=1006)Baseline, All Types/Subtypes (n=3725)Post-Baseline, H1N1 Seasonal (n=47)Post-Baseline, H1N1pdm09 (n=1240)Post-Baseline, H3N2 (n=1432)Post-Baseline, Influenza B (n=1006)Post-Baseline, All Types/Subtypes (n=3725)
Otherwise Healthy Participants Infected With Influenza441024703918057

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Number of Participants With Viral RNA Detected by RT-PCR on Day 1 Among Adults Treated With Oseltamivir

(NCT00884117)
Timeframe: Baseline (Day 1)

Interventionparticipants (Number)
TotalH1N1 SeasonalH3N2H1N1pdm09Influenza B
Adults Treated With Oseltamivir96112419323207

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Body Temperature Among Children Treated With Oseltamivir

Body temperature was measured by the Investigator using an oral or tympanic thermometer at Baseline and Day 10. Body temperature at each visit was averaged among all participants and expressed in degrees Celsius. (NCT00884117)
Timeframe: Days 1, 10

Interventiondegrees Celsius (Mean)
Day 1, Total (n=1282)Day 1, H3N2 (n=583)Day 1, H1N1pdm09 (n=370)Day 1, Influenza B (n=329)Day 10, Total (n=1223)Day 10, H3N2 (n=560)Day 10, H1N1pdm09 (n=346)Day 10, Influenza B (n=317)
Children Treated With Oseltamivir38.338.338.338.236.736.636.736.6

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Time to Non-Detection of Viral RNA Among Participants With H1N1pdm09 Infections

Time to non-detection/viral clearance was the time between symptom onset and the day on which viral RNA was no longer detected, or the last visit date if the participant was not RNA-negative at that visit. Time to non-detection/viral clearance was estimated using Kaplan-Meier analysis and expressed in days. (NCT00884117)
Timeframe: From Baseline (Day 1) to Day 10 (assessed on Days 1, 3, 6, 10)

Interventiondays (Median)
Children ≤5 Years of Age Treated With Oseltamivir9.9
Children 6 to 12 Years of Age Treated With Oseltamivir8.0
Adults Treated With Oseltamivir8.0

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Percentage of Participants With A Reduction in Viral Load

Viral load is defined as the amount of H1N1 virus in blood. As per investigator, a participant was considered as having viral load reduction at Day 5 if the Day 5 viral load was lower than the Baseline viral load. (NCT00949533)
Timeframe: Baseline, Day 5

Interventionpercentage of participants (Number)
Standard Dose100
Double Dose100

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Percentage of Participants Excreting Resistant Virus

Resistant virus included new influenza A virus subtype hemagglutinin type 1 and neuraminidase type 1 (New AH1N1). (NCT00949533)
Timeframe: Day 5

Interventionpercentage of participants (Number)
Standard Dose26.3
Double Dose35.3

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Number of Participants With Various Clinical Signs and Symptoms

"Number of participants with various clinical signs and symptoms, as per investigator's discretion, were reported. Same participants were reported in more than 1 category. Other in the category included abdominal pain, breathlessness, thoracic pain and tired." (NCT00949533)
Timeframe: Day 5

,
Interventionparticipants (Number)
CoughRhinorrheaSore throatShortness of breathDiarrheaHeadacheConjunctivitisVomitingOther
Double Dose952102000
Standard Dose10102221114

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Number of Participants With Various Clinical Signs and Symptoms in Whom Resistant Virus Were Detected

Number of participants with various clinical signs and symptoms, as per investigator's discretion, in whom new AH1N1 virus was detected, were reported. Same participants were reported in more than 1 category. (NCT00949533)
Timeframe: Day 5

,
Interventionparticipants (Number)
CoughRhinorrheaShortness of breath
Double Dose431
Standard Dose330

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Time to the Maximum Observed Plasma Concentration of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is an active metabolite of oseltamivir.Tmax was estimated using non-compartmental methods (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
Interventionhours (Median)
OseltamivirOseltamivir carboxylate
Oseltamivir 2 mg/kg1.085.83
Oseltamivir 2.5 mg/kg1.082.88
Oseltamivir 3 mg/kg1.085.04

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Total Plasma Clearance as a Function of Bioavailability and Apparent Plasma Clearance of the Metabolite as a Function of Bioavailability (CLm/F) of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is active metabolite of oseltamivir. CL/F was calculated as dose/AUCinf, where AUCinf represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
InterventionmL/hour (Mean)
Oseltamivir, n= 37, 17, 4Oseltamivir carboxylate, n=18,11, 2
Oseltamivir 2 mg/kg50600NA
Oseltamivir 2.5 mg/kg630002180
Oseltamivir 3 mg/kg805003940

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Time of the Last Measurable Plasma Concentration for Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is an active metabolite of oseltamivir. (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
Interventionhours (Geometric Mean)
OseltamivirOseltamivir carboxylate
Oseltamivir 2 mg/kg6.9410.45
Oseltamivir 2.5 mg/kg8.5310.64
Oseltamivir 3 mg/kg9.2310.11

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The Volume of Distribution as a Function of Bioavailability of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is active metabolite of oseltamivir. V/F is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
InterventionmL (Geometric Mean)
Oseltamivir, n= 37, 17, 4Oseltamivir carboxylate, n=18,11, 2
Oseltamivir 2 mg/kg121000NA
Oseltamivir 2.5 mg/kg18300035400
Oseltamivir 3 mg/kg23400053700

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Steady-state Minimum Observed Plasma Concentration of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is active metabolite of oseltamivir. Cmin was estimated for both oseltamivir and oseltamivir carboxylate by non-compartmental analysis (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir carboxylate
Oseltamivir 2 mg/kg2.56169
Oseltamivir 2.5 mg/kg2.09248
Oseltamivir 3 mg/kg2.88238

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Steady-state Maximum Observed Plasma Concentration of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is an active metabolite of oseltamivir. Cmax was estimated for both oseltamivir and Oseltamivir carboxylate by non-compartmental analysis. (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir carboxylate
Oseltamivir 2 mg/kg25.2501
Oseltamivir 2.5 mg/kg62.5530
Oseltamivir 3 mg/kg80.8464

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Steady-state Area Under the Plasma Concentration Versus Time Curve From Time Zero to 12 Hours of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is active metabolite of oseltamivir. AUC0-12 was estimated for oseltamivir and oseltamivir carboxylate by linear trapezoidal rule (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
Interventionhour (h)*nanogram(ng)/milliliter (mL) (Geometric Mean)
Oseltamivir, n=37, 17, 4Oseltamivir carboxylate, n=18,11, 2
Oseltamivir 2 mg/kg142NA
Oseltamivir 2.5 mg/kg1944920
Oseltamivir 3 mg/kg2774990

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Percentage of Participants With Decline of Body Temperature to the Afebrile State

This was performed for all participants who had fever at baseline Fever is defined as body temperature >37.0ºC. Rectal temperature is converted by subtracting 1 ºC. The rate of decline of body temperature was calculated as the slope of body temperature between the baseline temperature and the 1st temperature below 37°C. Participants with decline in body temperature were considered to have no fever; however, participants who did not show any decline in body temperature were considered to have persisting fever. (NCT00988325)
Timeframe: Baseline (Day 1), Day3/4, Day 6, Day 11, Day 18+/-2 days, Day 30+/-2 days

,,
Interventionpercentage of participants (Number)
Baseline, n=33, 11, 4, declineBaseline, n=33, 11, 4, no declineDay 4, n=33, 11, 4, declineDay 4, n=33, 11, 4, no declineDay 11, n=33, 11, 4, declineDay 11, n=33, 11, 4, no declineDay 18, n=16, 5, 1, declineDay 18, n=16, 5, 1, no declineDay 30, n=31, 9, 4, declineDay 30, n=31, 9, 4, no decline
Oseltamivir 2 mg/kg25751000100010001000
Oseltamivir 2.5 mg/kg5545919100010008911
Oseltamivir 3 mg/kg3664946973946973

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Number of Participants With Virus Shedding by Virus Type

The viral titer was measured by culture and reported in log10 (50% tissue culture infective dose [TCID50]). The viral load was analyzed by PCR and reported as log10 particles/mL. The number of patients positive for viral shedding by virus sub-type was measured on specified days from baseline to last visit on Day 30. (NCT00988325)
Timeframe: Baseline (Day 1), Day3/4, Day 6, Day 11, Day 18+/-2 days, Day 30+/-2 days

,,
InterventionParticipants (Number)
BaselineDay 3 or 4Day 6Day 11Day 18 +-2Day 30 +-2
Type A (H1N1)pdm093220123200
Type A H31054910
Type B141471600

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Number of Participants With Change From Baseline in Neurological Assessment Scores

Neurological assessment was performed to assess the mental state of the participants through two scales: Infant face scale and Glasgow coma scale. Each scale consists of 3 subscales: eye opening (ranging 1 to 4), verbal response (ranging 1 to 5), and motor responses (ranging 1 to 6). The final score is the sum of these ranges and is scored between 3 and 15. 3 being the worst, and 15 the best. Change from baseline is change of final score post-baseline minus the final score at baseline. (NCT00988325)
Timeframe: Baseline (Day 1); Day 3 for who received two does on Day 1 or Day 4 for who received one dose on Day 1; Day 6, Day 11, Day 18, Day 30

,,
Interventionparticipants (Number)
With change in infant face scale measurement scoreWith change in Glasgow coma scale assessment score
Oseltamivir 2 mg/kg00
Oseltamivir 2.5 mg/kg21
Oseltamivir 3 mg/kg00

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Number of Participants With Adverse Events, Serious Adverse Events and Secondary Illness

An Adverse Event (AEs) is defined as any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered to be related to the medicinal product. An Serious Adverse Event (SAE) is any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or results in a congenital anomaly/birth defect. Secondary illnesses were influenza disease-related events, namely bronchitis, pneumonia, otitis media, and sinusitis that resolved without sequelae. Adverse events, serious adverse events, and secondary illness are reported for on-treatment period (from the first dose of oseltamivir upto 3 days after the last dose of oseltamivir [Approximately 14 days]. (NCT00988325)
Timeframe: Up to 3 days after the last dose of oseltamivir (Approximately 14 days)

,,
InterventionParticipants (Number)
Participants with any AEParticipants with any SAEParticipants with secondary illness
Oseltamivir 2 mg/kg200
Oseltamivir 2.5 mg/kg1211
Oseltamivir 3 mg/kg1330

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Clast of Oseltamivir and Oseltamivir Carboxylate

The last measurable plasma concentration of oseltamivir and oseltamivir carboxylate was the last quantifiable concentration of oseltamivir or oseltamivir carboxylate, respectively. (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir carboxylate
Oseltamivir 2 mg/kg84.33940
Oseltamivir 2.5 mg/kg1764410
Oseltamivir 3 mg/kg2623800

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Apparent First-order Elimination Rate Constant of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is active metabolite of oseltamivir.The apparent first-order elimination rate constant (Lambda Z) was determined by linear regression analysis of terminal data points. A minimum of 3 data points were used for lambda Z estimation. By reporting tool convention, if n<3, no summary statistics were calculated (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
Intervention1/hour (Geometric Mean)
Oseltamivir, n= 33, 11, 4Oseltamivir carboxylate, n=17, 7, 2
Oseltamivir 2 mg/kg0.418NA
Oseltamivir 2.5 mg/kg0.3380.0475
Oseltamivir 3 mg/kg0.3490.0735

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Apparent Elimination Half Life of Oseltamivir and Oseltamivir Carboxylate

Elimination half-life is defined as the time required for elimination of a drug to half its plasma concentration and was computed using non-compartmental method (NCT00988325)
Timeframe: 15 minutes pre-dose; 1 hour +/- 15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 3 if two doses taken on Day 1 or 15 minutes pre-dose; 1 hour +/-15 minutes, 2-3, 5-7, 10-12 hours post-dose on Day 4 if one dose taken on Day 1

,,
Interventionhours (Geometric Mean)
Oseltamivir, n= 37, 17, 4Oseltamivir carboxylate, n=18, 11, 2
Oseltamivir 2 mg/kg1.66NA
Oseltamivir 2.5 mg/kg2.0111.3
Oseltamivir 3 mg/kg2.029.45

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Time to Resolution of Fever in Participants With Fever at the Baseline

This was performed for all participants who had fever at baseline. Fever is defined as body temperature >37.0 degree Celsius. Rectal temperature is converted by subtracting 1 degree Celsius. Time to Resolution of Fever was defined as the time from the initiation of treatment to first time the afebrile state was reached and maintained for at least 21.5 hours, where afebrile state was defined as axillary temperature ≤ 37 degree Celsius. (NCT00988325)
Timeframe: Days 1 to 11; Day 18; Day 30

Interventionhours (Median)
Oseltamivir 3 mg/kg12.0
Oseltamivir 2.5 mg/kg20.5
Oseltamivir 2 mg/kg24.0

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Median Time to Cessation of Viral Shedding in Participants With Positive Culture at Baseline

Median time to cessation of viral shedding was calculated for all patients with positive by culture / by polymerase chain reaction (PCR) at baseline using all data points between the start of the treatment and the 1st time point of negative culture without subsequent positive culture results. These time-to event analyses were only performed for the viral titre. (NCT00988325)
Timeframe: Days 1, 3 or 4, 6, 11, 18, and 30

Interventionhours (Median)
Oseltamivir 3 mg/kg228.5
Oseltamivir 2.5 mg/kg113.0
Oseltamivir 2 mg/kg113.0

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Number of Participants With Development of Oseltamivir-Resistant Influenza Virus

The last positive viral isolate from each patient was tested for reduced sensitivity to oseltamivir. Phenotypic assay was performed to determine the susceptibility of the last positive viral isolate from each patient. If required, a genotypic assay to determine the contribution of both the neuraminidase (NA) and hemagglutinin (HA) genes to decreased susceptibility was also performed. (NCT01032837)
Timeframe: 40 days

Interventionparticipants (Number)
Oseltamivir Standard Dose 5 Days0
Oseltamivir Standard Dose 10 Days1
Oseltamivir High Dose 5 Days1
Oseltamivir High Dose 10 Days0

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Time to Cessation of Viral Shedding

The time to cessation of viral shedding was measured by viral culture and defined as the time from treatment initiation to the time of the first negative culture with no subsequent positive cultures. Any patient with a positive culture at the last sample time was censored at that time point. Median time to cessation was estimated from the Kaplan-Meier curve. (NCT01032837)
Timeframe: Day 1 to Day 40

Interventionhours (Median)
Oseltamivir Standard Dose 5 Days65.6
Oseltamivir Standard Dose 10 Days70.8
Oseltamivir High Dose 5 Days58.1
Oseltamivir High Dose 10 Days74.1

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Time to Alleviation of All Clinical Symptoms - Children

Daily influenza-like symptoms (such as poor appetite, irritability, low energy, nasal congestion, runny nose etc) were recorded in a diary on a scale from 0 (no problem) to 3 (major problem). A patient is considered free of all clinical influenza symptoms if all symptoms were checked as 'no problem' or 'minor problem' (i.e., symptom score ≤1). Time to alleviation of all clinical symptoms was defined as the number of hours from the first dose to the first time the patient had alleviation of all symptoms. Patients without alleviation of symptoms were censored at the last available assessment. (NCT01032837)
Timeframe: Day 1 to Day 40

Interventionhours (Median)
Oseltamivir Standard Dose 5 Days176.8
Oseltamivir Standard Dose 10 Days127.7
Oseltamivir High Dose 5 Days118.8
Oseltamivir High Dose 10 Days123.1

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Time to Alleviation of All Clinical Symptoms - Adults

Daily influenza-like symptoms (such as nasal congestion, sore throat, cough, aches and pains, fatigue, headache, chills) were recorded in a diary on a scale from 0 (absent) to 3 (severe). A patient is considered free of all clinical influenza symptoms if all symptoms were checked as 'absent' or 'mild' (i.e., symptom score ≤1). Time to alleviation of all clinical symptoms was defined as the number of hours from the first dose to the first time the patient had alleviation of all symptoms. Patients without alleviation of symptoms were censored at the last available assessment. (NCT01032837)
Timeframe: Day 1 to Day 40

Interventionhours (Median)
Oseltamivir Standard Dose 5 Days140.0
Oseltamivir Standard Dose 10 Days181.8
Oseltamivir High Dose 5 Days146.8
Oseltamivir High Dose 10 Days94.9

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Number of Participants Who Developed Secondary Illnesses That Were Treated With Antibiotics

The number of participants who developed secondary illnesses due to influenza, including otitis media, bronchitis, pneumonia, or sinusitis at any time during the study which were treated with antibiotics. (NCT01032837)
Timeframe: Day 1 through Day 40

Interventionparticipants (Number)
Oseltamivir Standard Dose 5 Days0
Oseltamivir Standard Dose 10 Days0
Oseltamivir High Dose 5 Days0
Oseltamivir High Dose 10 Days2

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Percentage of Participants With Viral Shedding by Clinic Visit as Measured by Reverse Transcriptase Polymerase Chain Reaction

Viral shedding was measured by reverse transcriptase polymerase chain reaction (RT-PCR) from samples obtained from nasal and throat swabs and performed by the central laboratory. (NCT01032837)
Timeframe: Baseline and Days 3, 6, 8, 11, 15 and 40

,,,
Interventionpercentage of participants (Number)
Baseline (n=19, 18, 16, 17)Day 3 (n=19, 17, 15, 15)Day 6 (n=19, 17, 16, 15)Day 8 (n=18, 17, 15, 15)Day 11 (n=18, 18, 15, 14)Day 15 (n=18, 14, 15, 12)Day 40 (n=16, 15, 16, 14)
Oseltamivir High Dose 10 Days1007647121860
Oseltamivir High Dose 5 Days1006950132506
Oseltamivir Standard Dose 10 Days100832811666
Oseltamivir Standard Dose 5 Days89792611505

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Change From Baseline in Influenza Titer Measured by Viral Culture

Influenza virus titer measured by viral culture and expressed on a Log10 scale of the 50% Tissue Culture Infective Dose (TCID50; amount of virus required to kill 50% of inoculated tissue culture cells). (NCT01032837)
Timeframe: Baseline, Days 2 through 15

,,,
InterventionLog10 TCID50 (Mean)
Baseline (n=19, 18, 16, 17)Day 2 (n=19, 18, 15, 17)Day 3 (n=19, 18, 15, 17)Day 4 (n=19, 18, 15, 17)Day 5 (n=19, 18, 16, 17)Day 6 (n=19, 18, 15, 17)Day 7 (n=19, 18, 16, 17)Day 8 (n=19, 18, 15, 17)Day 9 (n=19, 18, 14, 16)Day 10 (n=19, 18, 15, 16)Day 11 (n=19, 16, 16, 15)Day 12 (n=19, 18, 15, 15)Day 13 (n=19, 18, 16, 15)Day 14 (n=18, 18, 15, 15)Day 15 (n=18, 17, 14, 15)
Oseltamivir High Dose 10 Days4.54-1.15-2.88-3.76-3.91-3.99-4.04-4.04-4.08-4.14-4.08-4.10-4.10-4.10-4.10
Oseltamivir High Dose 5 Days4.14-1.97-2.95-3.33-3.45-3.45-3.58-3.65-3.57-3.55-3.64-3.63-3.64-3.55-3.55
Oseltamivir Standard Dose 10 Days4.06-1.17-2.18-3.29-3.43-3.56-3.53-3.56-3.53-3.50-3.42-3.47-3.43-3.56-3.50
Oseltamivir Standard Dose 5 Days3.74-1.82-2.38-3.18-3.00-3.22-3.22-3.18-3.24-3.21-3.22-3.11-3.17-3.17-3.14

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Time to Resolution of Fever

Temperature was recorded by the patient in a diary twice daily for 10 days and once daily thereafter. Fever was defined as a body temperature greater than or including 37.8 degrees Celsius (or ≥ 100.04 Fahrenheit). Time to resolution of fever was defined as the total number of hours from the first dose of study medication to the first time at which temperature is ≤ 37.2 degrees Celsius and lasts at least 21.5 hours. Patients who were still febrile at the end of the study period were censored at that time. (NCT01032837)
Timeframe: Day 1 through Day 40

Interventionhours (Median)
Oseltamivir Standard Dose 5 Days19.3
Oseltamivir Standard Dose 10 Days35.5
Oseltamivir High Dose 5 Days24.9
Oseltamivir High Dose 10 Days20.0

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Number of Participants Who Developed Secondary Illnesses During the Study

The number of participants who developed secondary illnesses due to influenza, including four pre-defined adverse events: otitis media, bronchitis, pneumonia, or sinusitis at any time during the study. (NCT01032837)
Timeframe: Day 1 through Day 40

,,,
Interventionparticipants (Number)
BronchitisOtitis mediaPneumoniaSinusitisAny secondary illness
Oseltamivir High Dose 10 Days00022
Oseltamivir High Dose 5 Days00000
Oseltamivir Standard Dose 10 Days00000
Oseltamivir Standard Dose 5 Days10001

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Percentage of Participants With Viral Shedding by Clinic Visit as Measured by Viral Culture

Viral shedding was measured by viral culture from samples obtained from nasal and throat swabs and performed by the central laboratory. (NCT01032837)
Timeframe: Baseline and Days 3, 6, 8, 11, 15 and 40

,,,
Interventionpercentage of participants (Number)
Baseline (n=19, 18, 16, 17)Day 3 (n=19, 17, 15, 15)Day 6 (n=19, 17, 15, 15)Day 8 (n=18, 17, 15, 15)Day 11 (n=18, 18, 15, 14)Day 15 (n=18, 14, 15, 12)Day 40 (n=16, 15, 16, 14)
Oseltamivir High Dose 10 Days100531260012
Oseltamivir High Dose 5 Days1004460000
Oseltamivir Standard Dose 10 Days100610011011
Oseltamivir Standard Dose 5 Days1003705505

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Last Measurable Plasma Concentration (Clast) of Oseltamivir and Oseltamivir Carboxylate

(NCT01033734)
Timeframe: Day 1: 15 minutes pre-infusion start, 1, 2, 3, 4, 6, 8, 12 hours post start of infusion; Day 2, 3 (with or after fifth dose), 4 or 5: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

,,
Interventionng/mL (Geometric Mean)
Day 1: Oseltamivir (n = 1, 3, 0)Day 1: Oseltamivir Carboxylate (n = 1, 3, 0)Day 2: Oseltamivir (n = 0, 2, 1)Day 2: Oseltamivir Carboxylate (n = 0, 2, 1)Day 3: Oseltamivir (n = 1, 0, 0)Day 3: Oseltamivir Carboxylate (n = 1, 0, 0)Day 4: Oseltamivir (n = 0, 1, 0)Day 4: Oseltamivir Carboxylate (n = 0, 1, 0)Day 5: Oseltamivir (n = 1, 0, 0)Day 5: Oseltamivir Carboxylate (n = 1, 0, 0)
Oseltamivir: 1 to 2 YearsNANA4.76484NANANANANANA
Oseltamivir: 3 to 5 Years2.4130825.2319NANA25.1549NANA
Oseltamivir: 6 to 12 Years4.40237NANA2.60149NANA15.1339

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Cmax of Oseltamivir and Oseltamivir Carboxylate Day 5

(NCT01033734)
Timeframe: Day 5: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 6 to 12 Years403408

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Cmax of Oseltamivir and Oseltamivir Carboxylate Day 4

(NCT01033734)
Timeframe: Day 4: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 3 to 5 Years915549

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Cmax of Oseltamivir and Oseltamivir Carboxylate Day 3

(NCT01033734)
Timeframe: Day 3 (with or after fifth dose): 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 6 to 12 Years404237

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Cmax of Oseltamivir and Oseltamivir Carboxylate Day 2

(NCT01033734)
Timeframe: Day 2: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

,
Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 1 to 2 Years1270725
Oseltamivir: 3 to 5 Years500663

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AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 5

(NCT01033734)
Timeframe: Day 5: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

Interventionhr*ng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 6 to 12 Years10102820

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Maximum Observed Plasma Concentration (Cmax) of Oseltamivir and Oseltamivir Carboxylate Day 1

(NCT01033734)
Timeframe: Day 1: 15 minutes pre-infusion start, 1, 2, 3, 4, 6, 8, 12 hours post start of infusion

,
Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 3 to 5 Years753499
Oseltamivir: 6 to 12 Years360311

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AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 3

(NCT01033734)
Timeframe: Day 3 (with or after fifth dose): 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

Interventionhr*ng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 6 to 12 Years9432000

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AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 2

(NCT01033734)
Timeframe: Day 2: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

,
Interventionh*ng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 1 to 2 Years19206760
Oseltamivir: 3 to 5 Years10705970

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Area Under the Concentration Versus Time Curve From Time Zero to Last Measurable Plasma Concentration (AUClast) of Oseltamivir and Oseltamivir Carboxylate on Day 1

(NCT01033734)
Timeframe: Day 1: 15 minutes pre-infusion start, 1, 2, 3, 4, 6, 8, 12 hours post start of infusion.

,
Interventionhour*nanogram/milliliter (h*ng/mL) (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 3 to 5 Years14604550
Oseltamivir: 6 to 12 Years8291700

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AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 4

(NCT01033734)
Timeframe: Day 4: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

Interventionhr*ng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: 3 to 5 Years24803800

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Time of the Last Measurable Plasma Concentration (Tlast) of Oseltamivir and Oseltamivir Carboxylate

(NCT01033734)
Timeframe: Day 1: 15 minutes pre-infusion start, 1, 2, 3, 4, 6, 8, 12 hours post start of infusion; Day 2, 3 (with or after fifth dose), 4 or 5: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

,,
Interventionhours (Geometric Mean)
Day 1: Oseltamivir (n = 1, 3, 0)Day 1: Oseltamivir Carboxylate (n = 1, 3, 0)Day 2: Oseltamivir (n = 0, 2, 1)Day 2: Oseltamivir Carboxylate (n = 0, 2, 1)Day 3: Oseltamivir (n = 1, 0, 0)Day 3: Oseltamivir Carboxylate (n = 1, 0, 0)Day 4: Oseltamivir (n = 0, 1, 0)Day 4: Oseltamivir Carboxylate (n = 0, 1, 0)Day 5: Oseltamivir (n = 1, 0, 0)Day 5: Oseltamivir Carboxylate (n = 1, 0, 0)
Oseltamivir: 1 to 2 YearsNANA12.0012.00NANANANANANA
Oseltamivir: 3 to 5 Years10.5011.983.503.50NANA8.058.05NANA
Oseltamivir: 6 to 12 Years7.427.42NANA10.1310.13NANA7.927.92

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Time to the Maximum Observed Plasma Concentration (Tmax) of Oseltamivir and Oseltamivir Carboxylate

(NCT01033734)
Timeframe: Day 1: 15 minutes pre-infusion start, 1, 2, 3, 4, 6, 8, 12 hours post start of infusion; Day 2, 3 (with or after fifth dose), 4 or 5: 15 minutes pre-infusion start, 2, 4, 8 hours after start of infusion

,,
Interventionhours (Geometric Mean)
Day 1: Oseltamivir (n = 1, 3, 0)Day 1: Oseltamivir Carboxylate (n = 1, 3, 0)Day 2: Oseltamivir (n = 0, 1, 1)Day 2: Oseltamivir Carboxylate (n = 0, 1, 1)Day 3: Oseltamivir (n = 1, 0, 0)Day 3: Oseltamivir Carboxylate (n = 1, 0, 0)Day 4: Oseltamivir (n = 0, 1, 0)Day 4: Oseltamivir Carboxylate (n = 0, 1, 0)Day 5: Oseltamivir (n = 1, 0, 0)Day 5: Oseltamivir Carboxylate (n = 1, 0, 0)
Oseltamivir: 1 to 2 YearsNANA1.006.00NANANANANANA
Oseltamivir: 3 to 5 Years1.264.612.004.62NANA2.508.05NANA
Oseltamivir: 6 to 12 Years2.004.00NANA1.053.05NANA2.004.08

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Participants With Greater Than or Equal to (>=) 5-Fold Change in Neuraminidase Inhibition (NAI) Assay 50 Percent (%) Inhibitory Concentration (IC50) Values

IC50 was defined as the concentration that causes 50% inhibition of viral activity. IC50 values were calculated using NAI assay. The 5-fold change was calculated as either >=5 times change in the NAI IC50 visit value from the Reference value at a visit, >=5 times change in the NAI IC50 Visit value from the Baseline value. (NCT01033734)
Timeframe: Baseline, Day 1, 6 and 30

,,,
InterventionParticipants (Number)
Day 1 (n=6, 2, 3, 1)Day 6 (n=1, 0, 1, 0)Day 30 (n=1, 1, 0, 0)
Oseltamivir: 1 to 2 Years0NANA
Oseltamivir: 3 to 5 Years11NA
Oseltamivir: 6 to 12 Years0NA0
Oseltamivir: Overall110

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Continuous Venovenous Hemodialysis (CVVHD)Oseltamivir Carboxylate Transmembrane Clearance

Oseltamivir Carboxylate Transmembrane Clearance by Continuous Venovenous Hemodialysis (Reported in mL/min). (NCT01048879)
Timeframe: 12 hours

InterventionmL/min (Mean)
CVVHD Alone52.2
CVVHD + ECMO43.3

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Oseltamivir Carboxylate Removal by ECMO

Mean percent change in oseltamivir carboxylate concentration pre- and post-oxygenator. (NCT01048879)
Timeframe: 12 hours

Interventionpercent change in concentration (Mean)
CVVHD + ECMO-0.008
ECMO Alone-0.033

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Number of Participants With Viral Resistance

Nasal and Throat swabs were collected on Days 1, 4, 6, 11, 15 and 30 and were sent to a central laboratory for testing. Viral resistance was determined by phenotypic and genotypic testing. (NCT01050257)
Timeframe: 30 days

InterventionParticipants (Number)
Oseltamivir (TAMIFLU®) 100 mg1
Oseltamivir (TAMIFLU®) 200 mg1
Oseltamivir Open Label0

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Percentage of Participants With Viral Shedding by Reverse Transcriptase Polymerase Chain Reaction (RT-PCR)

Nasal and throat swabs were collected on Days 1, 4, 6, 11, 15, and 30 and were sent to a central laboratory for analysis. The presence of viral shedding was determined by detection by RT-PCR (log 10 copies/mL). (NCT01050257)
Timeframe: Days 1, 4, 6, 11, 15 and 30

,,
InterventionPercentage of participants (Number)
Day 1 (n=29, 30, 10)Day 4 (n=28, 28, 10)Day 6 (n=22, 28, 8)Day 11 (n=22, 26, 8)Day 15 (n=17, 24, 7)Day 30 (n=22, 28, 6)
Oseltamivir (TAMIFLU®) 100 mg866441905
Oseltamivir (TAMIFLU®) 200 mg9371361244
Oseltamivir Open Label9060631300

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Change From Baseline in Influenza Titer by Culture at Day 4

Nasal and throat swabs collected at Baseline and Day 4 were sent to a laboratory for analysis. Viral influenza titer (amount of virus present) was determined by culture. A log 10 median tissue culture infective dose (TCID50) > 0.5= Positive culture. A negative change from Baseline indicated improvement (less virus present). (NCT01050257)
Timeframe: Baseline, Day 4

Interventionlog10 TCID50 (Mean)
Oseltamivir (TAMIFLU®) 100 mg-1.38
Oseltamivir (TAMIFLU®) 200 mg-2.19
Oseltamivir Open Label-3.00

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Percentage of Participants With Viral Shedding by Culture or RT-PCR

Nasal and throat swabs were collected on Days 1, 4, 6, 11, 15, and 30 and were sent to a central laboratory for analysis. The presence of viral shedding was determined by a positive culture [log10 median tissue culture infective dose (TCID50) > 0.5) or detection by RT-PCR (log 10 copies/mL). (NCT01050257)
Timeframe: Days 1, 4, 6, 11, 15 and 30

,,
InterventionPercentage of participants (Number)
Day 1 (n=29, 30, 10)Day 4 (n=28, 28, 10)Day 6 (n=22, 28, 8)Day 11 (n=22, 26, 8)Day 15 (n=17, 24, 7)Day 30 (n=22, 28, 6)
Oseltamivir (TAMIFLU®) 100 mg906441905
Oseltamivir (TAMIFLU®) 200 mg9775361584
Oseltamivir Open Label90606313140

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Percentage of Participants With Viral Shedding by Culture

Nasal and throat swabs were collected on Days 1, 4, 6, 11, 15, and 30 and were sent to a central laboratory for analysis. The presence of viral shedding was determined by a positive culture=log10 median tissue culture infective dose (TCID50) > 0.5. (NCT01050257)
Timeframe: Days 1, 4, 6, 11, 15, 30

,,
InterventionPercentage of participants (Number)
Day 1 (n=29, 30, 10)Day 4 (n=28, 28, 10)Day 6 (n=22, 28, 8)Day 11 (n=22, 26, 8)Day 15 (n=17, 24, 7)Day 30 (n=22, 28, 6)
Oseltamivir (TAMIFLU®) 100 mg76145005
Oseltamivir (TAMIFLU®) 200 mg80290444
Oseltamivir Open Label903000140

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Percentage of Participants With Influenza Symptoms

Influenza (flu) symptoms were nasal congestion, sore throat, cough, aches and pains, fatigue, headache or chills. (NCT01050257)
Timeframe: Days 1, 11, 15, 30

,,
InterventionPercentage of participants (Number)
Day 1Day 11Day 15Day 30
Oseltamivir (TAMIFLU®) 100 mg100635133
Oseltamivir (TAMIFLU®) 200 mg100644426
Oseltamivir Open Label93796464

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Percentage of Participants Who Had a Fever During the Study

Fever was defined as a temperature of ≥ 37.8 C (degrees Celcius). (NCT01050257)
Timeframe: Baseline and Hours 12, 24, 36, 48, 60, 72, 84, 96 and 108

,,
InterventionPercentage of participants (Number)
BaselineHour 12Hour 24Hour 36Hour 48Hour 60Hour 72Hour 84Hour 96Hour 108
Oseltamivir (TAMIFLU®) 100 mg23773300000
Oseltamivir (TAMIFLU®) 200 mg19903663030
Oseltamivir Open Label2010020000000

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Number of Participants With Adverse Events (AEs), Serious Adverse Events(SAEs, AEs Leading to Withdrawal, and Death

"Safety was assessed by adverse events (AEs) as measured by the collection of AEs, vital signs, electrocardiograms and laboratory parameters. An AE was considered any unfavorable and unintended sign, symptom, or disease associated with the use of the study drug, whether or not considered related to the study drug. Preexisting conditions that worsened during the study were reported as adverse events. A serious adverse event is any experience that suggests a significant hazard, contraindication, side effect or precaution that: results in death, is life-threatening, required in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or is medically significant.~On treatment = AEs that started between the day of first dose and within 2 days after the last dose. Off treatment = AEs that started more than 2 days after the last dose of study drug." (NCT01050257)
Timeframe: Up to 30 days

,,
InterventionPartipants (Number)
DeathAEs on treatment: IV doseAEs on treatment: Oral doseAEs off treatmentSAEs on treatment: IV doseSAEs on treatment: Oral doseSAEs off treatmentAEs leading to withdrawal on treatment: IV dosingAEs leading to withdrawal on treatment: Oral doseAEs leading to withdrawal off treatment
Oseltamivir (TAMIFLU®) 100 mg1241013325310
Oseltamivir (TAMIFLU®) 200 mg127913401310
Oseltamivir Open Label31145223210

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Change From Baseline in Influenza Titer by Reverse Transcriptase Polymerase Chain Reaction (RT-PCR) at Day 4

Nasal and throat swabs were collected at Baseline and Day 4 and were sent to a central laboratory for analysis. Influenza Viral titers (amount of virus present) were determined by RT-PCR for Flu A and Flu B and were reported in log 10 copies/milliliter (mL). A negative change from Baseline indicated improvement (less virus present). (NCT01050257)
Timeframe: Baseline, Day 4

,,
Interventionlog 10 copies/mL (Mean)
Flu A (n=14, 14, 5)Flu B (n=3, 5, 1)
Oseltamivir (TAMIFLU®) 100 mg-1.04-0.70
Oseltamivir (TAMIFLU®) 200 mg-1.30-1.51
Oseltamivir Open Label-1.53-2.27

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Time to Resolution of Fever for Participants Who Had a Fever at Baseline

Fever was defined as a temperature of ≥ 37.8 C (degrees Celsius). Resolution of fever was a temperature ≤ 37.2 for at least 21.5 hours. (NCT01050257)
Timeframe: Baseline, Up to 30 Days

InterventionHours (Median)
Oseltamivir (TAMIFLU®) 100 mg11.8
Oseltamivir (TAMIFLU®) 200 mg18.6
Oseltamivir Open Label47.7

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Time of the Last Measurable Plasma Concentration (Tlast) of Oseltamivir and Oseltamivir Carboxylate

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2, 3-4, 5-7, and 10-12 hours post-dose on Day 1 and Day 2, pre-dose (Hour 0), 2 and 4 hours post-dose on Day 4

,,
Interventionhours (Geometric Mean)
Day 1: Oseltamivir (n = 3, 0, 1)Day 1: Oseltamivir Carboxylate (n = 3, 0, 1)Day 2: Oseltamivir (n = 3, 1, 0)Day 2: Oseltamivir Carboxylate (n = 3, 1, 0)Day 4: Oseltamivir (n = 2, 0, 1)Day 4: Oseltamivir Carboxylate (n = 2, 0, 1)
Oseltamivir: Age 0 to 30 Days10.5810.58NANA3.983.98
Oseltamivir: Age 31 to 90 DaysNANA6.476.47NANA
Oseltamivir: Age 91 to < 365 Days9.629.628.558.553.853.85

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Number of Participants With Greater Than or Equal to (≥) 5-Fold Change in Neuraminidase Inhibition (NAI) Assay 50 Percent (%) Inhibitory Concentration (IC50) Values

IC50 was defined as the concentration that causes 50% inhibition of viral activity. IC50 values were calculated using NAI assay. The 5-fold change was calculated as either ≥5 times change in the NAI IC50 visit value from the Reference value at a visit or ≥5 times change in the NAI IC50 Visit value from the Baseline value. (NCT01053663)
Timeframe: Baseline, Days 1, 3, 4, 6, 15

,,
Interventionparticipants (Number)
Day 1 (n=4, 0, 1, 5)Day 3 (n=0, 0, 1, 1)Day 4 (n=3, 0, 0, 3)Day 6 (n=0, 0, 1, 1)Day 15 (n=1, 0, 0, 1)
Oseltamivir: Age 0 to 30 Days00NA0NA
Oseltamivir: Age 91 to < 365 Days1NA1NA0
Oseltamivir: All Participants10100

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Number of Participants With Oseltamivir Resistance Mutation

Resistance was assessed by neuraminidase (NA) and hemagglutinin (HA) genes sequencing analysis, using Reverse Transcription Polymerase Chain Reaction (RT-PCR). (NCT01053663)
Timeframe: Up to Day 30

Interventionparticipants (Number)
Oseltamivir: Age 91 to < 365 Days1
Oseltamivir: Age 31 to 90 Days0
Oseltamivir: Age 0 to 30 Days0
Oseltamivir: All Participants1

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Area Under the Concentration Versus Time Curve From Time Zero to Last Measurable Plasma Concentration (AUClast) of Oseltamivir and Oseltamivir Carboxylate on Day 1

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2, 3-4, 5-7, and 10-12 hours post-dose on Day 1

,
Interventionhour*nanogram/milliliter (h*ng/mL) (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: Age 0 to 30 Days4947510
Oseltamivir: Age 91 to < 365 Days7775200

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AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 4

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2 and 4 hours post-dose on Day 4

,
Interventionh*ng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: Age 0 to 30 Days3892070
Oseltamivir: Age 91 to < 365 Days15203880

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Cmax of Oseltamivir and Oseltamivir Carboxylate on Day 4

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2 and 4 hours post-dose on Day 4

,
Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: Age 0 to 30 Days189727
Oseltamivir: Age 91 to < 365 Days7421370

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Last Measurable Plasma Concentration (Clast) of Oseltamivir and Oseltamivir Carboxylate

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2, 3-4, 5-7, and 10-12 hours post-dose on Day 1 and Day 2, pre-dose (Hour 0), 2 and 4 hours post-dose on Day 4

,,
Interventionng/mL (Geometric Mean)
Day 1: Oseltamivir (n = 3, 0, 1)Day 1: Oseltamivir Carboxylate (n = 3, 0, 1)Day 2: Oseltamivir (n = 3, 1, 0)Day 2: Oseltamivir Carboxylate (n = 3, 1, 0)Day 4: Oseltamivir (n = 2, 0, 1)Day 4: Oseltamivir Carboxylate (n = 2, 0, 1)
Oseltamivir: Age 0 to 30 Days2.76503NANA10.7727
Oseltamivir: Age 31 to 90 DaysNANA6.84948NANA
Oseltamivir: Age 91 to < 365 Days5.585058.2284966.21370

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Time to the Maximum Observed Plasma Concentration (Tmax) of Oseltamivir and Oseltamivir Carboxylate

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2, 3-4, 5-7, and 10-12 hours post-dose on Day 1 and Day 2, pre-dose (Hour 0), 2 and 4 hours post-dose on Day 4

,,
Interventionhours (Geometric Mean)
Day 1: Oseltamivir (n = 3, 0, 1)Day 1: Oseltamivir Carboxylate (n = 3, 0, 1)Day 2: Oseltamivir (n = 3, 1, 0)Day 2: Oseltamivir Carboxylate (n = 3, 1, 0)Day 4: Oseltamivir (n = 2, 0, 1)Day 4: Oseltamivir Carboxylate (n = 2, 0, 1)
Oseltamivir: Age 0 to 30 Days2.005.58NANA1.933.98
Oseltamivir: Age 31 to 90 DaysNANA2.134.30NANA
Oseltamivir: Age 91 to < 365 Days2.514.572.023.402.023.85

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Cmax of Oseltamivir and Oseltamivir Carboxylate on Day 2

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2, 3-4, 5-7, and 10-12 hours post-dose on Day 2

,
Interventionng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: Age 31 to 90 Days1941050
Oseltamivir: Age 91 to < 365 Days4191080

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AUClast of Oseltamivir and Oseltamivir Carboxylate on Day 2

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2, 3-4, 5-7, and 10-12 hours post-dose on Day 2

,
Interventionh*ng/mL (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: Age 31 to 90 Days4815330
Oseltamivir: Age 91 to < 365 Days9887270

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Maximum Observed Plasma Concentration (Cmax) of Oseltamivir and Oseltamivir Carboxylate on Day 1

(NCT01053663)
Timeframe: Pre-dose (Hour 0), 2, 3-4, 5-7, and 10-12 hours post-dose on Day 1

,
Interventionnanogram/milliliter (ng/mL) (Geometric Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir: Age 0 to 30 Days203871
Oseltamivir: Age 91 to < 365 Days307736

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Steady State Area Under the Plasma Concentration Versus Time Curve From 0 to 12 Hours After Dosing (AUC0-12) of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is active metabolite of oseltamivir. AUC0-12 of oseltamivir and oseltamivir carboxylate were calculated following the administration of oseltamivir alone or in combination with rimantadine, using the linear trapezoidal rule. (NCT01172847)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 12 hours post-dose on Day 5

,
Interventionhours (h)*nanogram (ng)/milliliter (mL) (Least Squares Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir5.0928.008
Oseltamivir + Rimantadine5.0707.990

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Number of Participants With Marked Abnormality in Laboratory Parameters

"Laboratory analysis included hematology (hemoglobin, hematocrit, erythrocytes, platelets counts, leukocytes counts, neutrophils, eosinophils, lymphocytes, basophils, and monocytes);, biochemistry (aspartate aminotransferase , alanine aminotransferase, gamma glutamyl trans peptidase, total bilirubin, alkaline phosphatase, lactate dehydrogenase, albumin, creatinine, urea, creatine phosphokinase, total protein, sodium, chloride, calcium, phosphate, potassium, glucose (fasting), amylase, lipase, total cholesterol, and calculated creatinine clearance); and urinalysis.~Marked laboratory test values (high and low) falling outside the marked reference range and which also represents a clinically relevant change from baseline of at least a designated amount were recoded. In this study, marked abnormality ranges for phosphate as 0.75 - 1.60 millimole (mmol)/L and proteinuria (0 to 4+, and 1)." (NCT01172847)
Timeframe: Screening; Day -1 and Day 5 (pre-dose) of each treatment period; Follow-up visit

,,
Interventionparticipants (Number)
Phosphate HighPhosphate LowProteinuria
Oseltamivir111
Oseltamivir + Rimantadine100
Rimantadine100

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Number of Participants With Abnormal Vital Signs

Vital signs included heart rate (HR), blood pressure (systolic blood pressure [SBP] and diastolic blood pressure [DBP]), and body temperature. Blood pressure and pulse rate were recorded when participants were rested in a supine position for at least 5 minutes and after standing for 2 minutes. Vital signs values that fall outside the investigator's normal ranges were recorded. (NCT01172847)
Timeframe: Screening (Days -28 to -2); pre-dose and 2h post-dose on D1 and D5 of each treatment period; at Follow-up visit (10 -14 days after last dose) for blood pressure and HR; Screening; Day -1 of each treatment period; Follow-up visit for temperature

,,
Interventionparticipants (Number)
High- SBPHigh- DBPHigh- DBP standingHigh- SBP standingHigh- HRHigh- HR standingLow- Temperature
Oseltamivir6287227
Oseltamivir + Rimantadine2023028
Rimantadine10640111

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Steady State Area Under the Plasma Concentration Versus Time Curve From 0 to 12 Hours After Dosing (AUC0-12) of Rimantadine

AUC0-12 of rimantadine was calculated following the administration of rimantadine alone or in combination with oseltamivir, using the linear trapezoidal rule. (NCT01172847)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 12 hours post-dose on Day 5

Interventionh*ng/mL (Least Squares Mean)
Rimantadine8.371
Oseltamivir + Rimantadine8.398

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Number of Participants With Any Adverse Events (AEs) and Any Serious Adverse Events (SAEs)

An AE is defined as any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered to be related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or results in a congenital anomaly/birth defect. (NCT01172847)
Timeframe: Up to 11 weeks

Interventionparticipants (Number)
Oseltamivir8
Rimantadine6
Oseltamivir + Rimantadine4

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Maximum Plasma Concentration (Cmax) of Rimantadine

Cmax of rimantadine was calculated following the administration of rimantadine alone or in combination with oseltamivir and was directly observed from the data. (NCT01172847)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 12 hours post-dose on Day 5

Interventionng/mL (Least Squares Mean)
Oseltamivir6.036
Oseltamivir + Rimantadine6.062

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Maximum Plasma Concentration (Cmax) of Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is active metabolite of oseltamivir. Cmax of oseltamivir and oseltamivir carboxylate were calculated following the administration of oseltamivir alone or in combination with rimantadine and was directly observed from the data. (NCT01172847)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 12 hours post-dose on Day 5

,
Interventionng/mL (Least Squares Mean)
OseltamivirOseltamivir Carboxylate
Oseltamivir4.3955.940
Oseltamivir + Rimantadine4.2495.921

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Steady-State AUC of Oseltamivir Carboxylate

AUC is the area under the concentration-time curve. This is measured as concentration in nanograms of oseltamivir carboxylate per milliliter of plasma multiplied by time in hours (hour*ng/mL) (NCT01179919)
Timeframe: 6 days

Interventionhour*ng/mL (Mean)
Oseltamivir Dosed Group2579

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Steady-State Cmax and Cmin of Oseltamivir Carboxylate

Cmax is the maximum concentration and Cmin in the minimum concentration of oseltamivir carboxylate measured in nanogram of oseltamivir carboxylate per milliliter of plasma (ng/mL) (NCT01179919)
Timeframe: 6 days

Interventionng/mL (Mean)
CmaxCmin
Oseltamivir Dosed Group316113

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28-day Mortality

Number of deaths (NCT01227967)
Timeframe: From treatment initiation to Day 28

Interventionparticipants (Number)
Combination Therapy0
Oseltamivir Monotherapy1

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Percentage of Participants Who Required Hospitalization.

The percentage of participants hospitalized by 28 days was estimated from the Kaplan-Meier curves. (NCT01227967)
Timeframe: From treatment initiation to Day 28

Interventionpercentage of participants analyzed (Number)
Combination Therapy4.28
Oseltamivir Monotherapy0.98

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Percentage of Participants Who Required New or Increased Use of Supplemental Oxygen

Percentage of participants who required new or increased use of supplemental oxygen (NCT01227967)
Timeframe: From treatment initiation to Day 28

Interventionpercentage of participants analyzed (Number)
Combination Therapy1.91
Oseltamivir Monotherapy1.6

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Percentage of Participants With Clinical Failure at Day 5

Clinical failure at Day 5 is defined as the need for continued (non-study) antiviral use after Day 5. (NCT01227967)
Timeframe: From treatment initiation to Day 28

Interventionpercentage of participants analyzed (Number)
Combination Therapy7.0
Oseltamivir Monotherapy7.7

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Percentage of Participants With Virus Detectable by Quantitative PCR (qPCR) in Nasopharyngeal (NP) Swabs

The central laboratory performed a qualitative PCR test on the NP sample from Day 0 in order to confirm influenza infection and to determine the influenza type and subtype. For participants with a positive influenza test result at Day 0 from this qualitative PCR testing, the laboratory then performed qPCR testing of subsequent samples to quantify viral shedding. (NCT01227967)
Timeframe: At Day 3

Interventionpercentage of participants analyzed (Number)
Combination Therapy40
Oseltamivir Monotherapy50

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Time to Absence of Fever

Fever was considered present based on the diary cards if a subject reported a maximal temperature ≥38.0°C (for the period since the diary card was previously completed) or reported having taken an antipyretic drug (also for the period since the diary card was previously completed). Otherwise, fever was considered not present during the period since the diary card was previously completed, except that the evaluation was considered missing if either the temperature or the antipyretic drug use entry was not completed on the diary card. The duration of fever was defined as the time from Day 0 to the first of two successive assessments (through to Day 7) or to the first assessment (Day 8 onwards) at which no fever was present according to this definition.For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with fever evaluated. (NCT01227967)
Timeframe: From treatment initiation to Day 28

InterventionDays (Median)
Combination Therapy0.5
Oseltamivir Monotherapy0.5

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Time to Alleviation of Influenza Clinical Symptoms.

The assessed symptoms were cough, nasal obstruction (stuffy nose), sore throat, fatigue, headache, muscle aches, feverishness, rhinorrhea, nausea, vomiting, diarrhea. Duration of clinical symptoms is defined as the time from Day 0 to the first of two successive measurements at which all clinical symptoms are grade 0 (absent) or 1 (mild). A measurement is considered to be the 8AM or 8PM assessment during Days 0 to 7 (so two measurements are obtained per day) and then the daily assessment thereafter. Time will then be calculated in half-days through to Day 7. If a subject's first two assessments on (baseline assessment and first subsequent diary card assessment) satisfy this criterion, then the duration will be set to zero. For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with symptoms evaluated. (NCT01227967)
Timeframe: From treatment initiation to Day 28

InterventionDays (Median)
Combination Therapy4.5
Oseltamivir Monotherapy4.0

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Time to Feeling as Good as Before the Onset of the Influenza Illness

Time to feeling as good as before influenza is defined as time to the first of two successive 'yes' responses to the question of 'feeling as good as you did before you had the flu'.For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with question answered. (NCT01227967)
Timeframe: From treatment initiation to Day 28

InterventionDays (Median)
Combination Therapy7.5
Oseltamivir Monotherapy6.5

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Time to Resolution of All Symptoms AND Fever

The assessed symptoms were cough, nasal obstruction (stuffy nose), sore throat, fatigue, headache, muscle aches, feverishness, rhinorrhea, nausea, vomiting, diarrhea. Fever was considered present based on the diary cards if a subject reported a maximal temperature ≥38.0°C (for the period since the diary card was previously completed) or reported having taken an antipyretic drug (also for the period since the diary card was previously completed). Time to resolution of all clinical symptoms and fever is defined as the time from Day 0 to the first of two successive measurements at which all clinical symptoms are grade 0 (absent) or 1(mild) and no fever >=38.0 C or antipyretic drug is reported. For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with symptoms and fever evaluated. (NCT01227967)
Timeframe: From treatment initiation to Day 28

InterventionDays (Median)
Combination Therapy4.5
Oseltamivir Monotherapy4.5

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Time to Return to Pre-influenza Function

Time to return to pre-influenza function is defined as the time from Day 0 to the first of two successive 'Yes' answers to the global assessment question 'Are you functioning as well as you were before you had the flu'.For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with question answered. (NCT01227967)
Timeframe: From treatment initiation to Day 28

InterventionDays (Median)
Combination Therapy7.0
Oseltamivir Monotherapy6.0

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Percentage of Participants Who Develop Bronchitis, Pneumonia, or Other Complications of Influenza After Day 0.

Participants were assessed for the signs/symptoms suggestive of one of the following complications: Sinusitis, Otitis Media ,Bronchitis / Bronchiolitis, Pneumonia and antibiotic use for reason other than above. (NCT01227967)
Timeframe: From treatment initiation to Day 28

,
Interventionpercentage of participants analyzed (Number)
SinustisOtitis MediaBronchitis BronchiolitisPneumoniaAntibiotic use for other reasonsAt least one complication and/or use of antibiotic
Combination Therapy4.50.35.72.28.616.6
Oseltamivir Monotherapy4.51.03.51.99.315.4

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qPCR Viral Shedding

Median, 25% and 75% percentile of the value of viral shedding (Results = LOD, NCT01227967)
Timeframe: At Day 0, 3 and 7

,
InterventionLog10 copies/mL (Median)
Day 0Day 3Day 7
Combination Therapy6.43.43.2
Oseltamivir Monotherapy6.73.93.2

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Number of Participants by Virus Detection Status

Number of participants who had undetectable values (less than the limit of detection [LOD]), who had values between the LOD and the lower limit of quantification (LLOQ), and who had values ≥LLOQ (NCT01227967)
Timeframe: At Day 0, 3 and 7.

InterventionParticipants (Count of Participants)
Day 072298058Day 072298059Day 372298059Day 372298058Day 772298058Day 772298059
>=LOD, Missing>=LLOQ
Combination Therapy221
Oseltamivir Monotherapy200
Oseltamivir Monotherapy9
Combination Therapy5
Oseltamivir Monotherapy15
Combination Therapy0
Oseltamivir Monotherapy0
Combination Therapy65
Oseltamivir Monotherapy87
Combination Therapy22
Oseltamivir Monotherapy25
Combination Therapy134
Oseltamivir Monotherapy104
Combination Therapy9
Oseltamivir Monotherapy8
Combination Therapy19
Oseltamivir Monotherapy24
Combination Therapy4
Oseltamivir Monotherapy7
Combination Therapy193
Oseltamivir Monotherapy184
Combination Therapy14

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Time to Return of Physical Function to Pre-illness Leve

Time to return of physical function to pre-illness level was defined as the time from Day 0 to the first of two successive measurements at which the physical function score equals or is better than the pre-illness score (obtained by recall at enrollment).For subjects who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with physical function evaluated. (NCT01227967)
Timeframe: From treatment initiation to Day 28

InterventionDays (Median)
Combination Therapy7.0
Oseltamivir Monotherapy6.0

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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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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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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 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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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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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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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 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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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 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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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 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 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 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 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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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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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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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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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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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 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 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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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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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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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 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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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 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 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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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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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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Number of Participants to Transfer to ICU After 24 h

Number of subjects that were transfered to an intensive care unit (ICU) after 24 hours of hospitalization. A patient transferred to ICU within 24 hours of admission was considered as a direct admission to ICU and not meeting criteria for clinical failure. (NCT01248715)
Timeframe: 24 h

InterventionParticipants (Count of Participants)
Oseltamirvir2
Standard of Care2

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Number of Participants That Required Re-hospitalization

Participants that were re-hospitalized within 30 days after enrollment. (NCT01248715)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Oseltamirvir5
Standard of Care5

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Number of Participants That Had Short-term Mortality

Number of subjects who died within 30 days of enrollment (NCT01248715)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Oseltamirvir2
Standard of Care1

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Length of Hospital Stay

Duration of hospitalization calculated as the day of discharge minus the day of admission. (NCT01248715)
Timeframe: through study completion, up to 30 days

Interventiondays (Median)
Oseltamirvir4
Standard of Care4.5

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Days to Reach Clinical Stability

Time to clinical improvement. The criteria for clinical improvement were followed during the first week from the day of admission and defined as follows: a) improvement of signs and symptoms of LRTI reported by patient b) afebrile for at least 8 hours, c) decrease in white blood cell count to more than 10% from the prior day, and d) able to tolerate oral feeding. A patient was considered clinically improved on the day that these four criteria were all met. (NCT01248715)
Timeframe: 30 days

Interventiondays (Median)
Oseltamirvir2
Standard of Care2

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Number of Participants With Clinical Failure (Failure to Reach Clinical Stability)

Number of subject that showed lack of clinical improvement within 7 days. Criteria for clinical improvement include no fever; white blood cell count decreases, or increases in the case of leukopenia, to more than 10% from the prior day; the evaluation of signs and symptoms of CAP to define when the patient is subjectively better, and the patient is able to tolerate food by mouth. (NCT01248715)
Timeframe: 7 days

InterventionParticipants (Count of Participants)
Oseltamirvir6
Standard of Care2

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Number of Participants With Hospital Mortality.

Number of subjects who died while hospitalized (NCT01248715)
Timeframe: through study completion, up to 30 days

InterventionParticipants (Count of Participants)
Oseltamirvir1
Standard of Care1

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Change in Attention Assessment

"Attention assessed using simple reaction time measured in milliseconds. Simple reaction time calculated as the mean of the following 2 sub-tests:~Reaction Time Subtest~Cued Reaction Time Subtest~The lower the value, the better the attention." (NCT01249833)
Timeframe: Change from baseline at Day 4

Interventionmilliseconds (Least Squares Mean)
Oseltamivir-70.0
Standard of Care Alone-39.7

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Change in Processing Speed Assessment

"Processing speed assessed with the animal number decoding subtest~The lower the value, the better the processing speed" (NCT01249833)
Timeframe: Change from baseline at Day 4

InterventionMillliseconds (Least Squares Mean)
Oseltamivir-551.9
Standard of Care Alone-555.8

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Change in Working Memory Assessment

"Working memory assessed with the Dot Memory Test.~The higher the value, the better the working memory." (NCT01249833)
Timeframe: Change from baseline at Day 4

InterventionNumber of correct answers (Least Squares Mean)
Oseltamivir8.2
Standard of Care Alone4.4

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Change in Mood Assessment

"Mood was assessed using the Bond-Lader 10 cm (100 mm) visual analogue scales for mood (16 scales in total); factored for alertness (mean of 9 scales), calmness (mean of 2 scales) and contentment (mean of 5 scales).~The range in score for each scale and for each factor (alertness, calmness and contentment) was 0 - 100 mm.~Each scale was anchored such that the lower the value, the better the mood." (NCT01249833)
Timeframe: Change from baseline at Day 4

,
Interventionmillimeter (Least Squares Mean)
Change in Alertness AssessmentChange in Calmness AssessmentChange in Contentedness Assessment
Oseltamivir19.13.016.3
Standard of Care Alone17.23.613.0

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Time to Return of Physical Function to Pre-illness Level

Time to return of physical function to pre-illness level was defined as the time from Day 0 to the first of two successive measurements at which the physical function score equals or is better than the pre-illness score (obtained by recall at enrollment). For subjects who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with physical function evaluated. (NCT01314911)
Timeframe: From treatment initiation to Day 28

Interventiondays (Median)
Oseltamivir7.0
Placebo7.0

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Time to Feeling as Good as Before the Onset of the Influenza Illness

Time to feeling as good as before influenza is defined as time to the first of two successive 'yes' responses to the question of 'feeling as good as you did before you had the flu'.For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with question answered. (NCT01314911)
Timeframe: From treatment initiation to Day 28

Interventiondays (Median)
Oseltamivir6.0
Placebo6.0

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28-day Mortality

Number of deaths (NCT01314911)
Timeframe: From treatment initiation to Day 28

InterventionParticipants (Count of Participants)
Oseltamivir0
Placebo0

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Area Under The Curve (AUC) Of Viral Shedding For Self Collected Samples

This AUC was calculated using the trapezoidal rule and the units of measurement are (days*log10 copies/mL) with the fact that it was the level of virus above the LLOQ being considered. The calculation of AUC was undertaken using measurements from Day 0 to Day 3 which were collected under all versions of the protocol (i.e. evening measurements on Days 0, 1 and 2 were not used as these were collected for only about 20% of subjects). Missing values during follow-up were ignored. This is equivalent to imputing a missing value using linear interpolation between the preceding and succeeding available values. For the five subjects with missing values following a last available measurement which was above the LLOQ, the remaining values were assumed to be the mean of preceding value and LLOQ in calculating the AUC. (NCT01314911)
Timeframe: From Day 0 to Day 3

Interventiondays*log10 copies/mL (Median)
Oseltamivir12.5
Placebo13.18

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Percentage of Participants With Virus Detectable by Quantitative PCR (qPCR) in Nasopharyngeal (NP) Swabs --Self Collected Samples

For participants with a positive influenza test result at Day 0 from qualitative PCR testing on the team collected sample, the laboratory then performed qPCR testing of self-collected samples to quantify viral shedding. (NCT01314911)
Timeframe: At Day 3

InterventionParticipants (Count of Participants)
Oseltamivir56
Placebo89

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Percentage of Participants With Virus Detectable by Quantitative PCR (qPCR) in Nasopharyngeal (NP) Swabs at Day 3 -- Team Collected Samples

The central laboratory performed a qualitative PCR test on the NP sample from Day 0 team collected swap in order to confirm influenza infection and to determine the influenza type and subtype. For participants with a positive influenza test result at Day 0 from this qualitative PCR testing, the laboratory then performed qPCR testing of subsequent samples to quantify viral shedding. (NCT01314911)
Timeframe: At Day 3

InterventionParticipants (Count of Participants)
Oseltamivir99
Placebo131

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Time to Absence of Fever

Fever was considered present based on the diary cards if a subject reported a maximal temperature ≥38.0°C (for the period since the diary card was previously completed) or reported having taken an antipyretic drug (also for the period since the diary card was previously completed). Otherwise, fever was considered not present during the period since the diary card was previously completed, except that the evaluation was considered missing if either the temperature or the antipyretic drug use entry was not completed on the diary card. The duration of fever was defined as the time from Day 0 to the first of two successive assessments (through to Day 7) or to the first assessment (Day 8 onwards) at which no fever was present according to this definition.For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with fever evaluated. (NCT01314911)
Timeframe: From treatment initiation to Day 28

Interventiondays (Median)
Oseltamivir1
Placebo1

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Time to Alleviation of Influenza Clinical Symptoms

The assessed symptoms were cough, nasal obstruction (stuffy nose), sore throat, fatigue, headache, muscle aches, feverishness, rhinorrhea, nausea, vomiting, diarrhea. Duration of clinical symptoms was defined as the time from Day 0 to the first of two successive measurements at which all clinical symptoms were grade 0 (absent) or 1 (mild). A measurement was considered to be the 8AM or 8PM assessment during Days 0 to 7 (so two measurements were obtained per day) and then the daily assessment thereafter. Time was calculated in half-days through to Day 7. If a subject's first two assessments on (baseline assessment and first subsequent diary card assessment) satisfied this criterion, then the duration was set to zero. For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with symptoms evaluated. (NCT01314911)
Timeframe: From treatment initiation to Day 28

Interventiondays (Median)
Oseltamivir4
Placebo4

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Number of Participants by Virus Detection Status--Team Collected Samples

Number of participants who had undetectable values (less than the limit of detection [LOD]), who had values between the LOD and the lower limit of quantification (LLOQ), and who had values ≥LLOQ (NCT01314911)
Timeframe: At Day 0, 3 and 7

InterventionParticipants (Count of Participants)
Day 072311918Day 072311919Day 372311919Day 372311918Day 772311918Day 772311919
< LODMissing>= LLOQ>= LOD, < LLOQ
Oseltamivir237
Placebo245
Oseltamivir6
Placebo5
Oseltamivir0
Placebo0
Oseltamivir85
Placebo109
Oseltamivir24
Placebo36
Oseltamivir134
Placebo107
Oseltamivir3
Placebo3
Oseltamivir16
Placebo21
Oseltamivir11
Oseltamivir214
Placebo224
Oseltamivir5

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Number of Participants by Virus Detection Status --Self Collected Samples

Number of participants who had undetectable values (less than the limit of detection [LOD]), who had values between the LOD and the lower limit of quantification (LLOQ), and who had values ≥LLOQ. Evening samples on Day 0, 1 and 2 were only required under protocol versions 1.0-4.0 and so were only collected for about 20% of participants. (NCT01314911)
Timeframe: At Day 0, Day 0 evening, Day 1, Day 1 evening, Day 2, Day 2 evening and Day 3

InterventionParticipants (Count of Participants)
Day 072311918Day 072311919Day 0 evening72311918Day 0 evening72311919Day 172311918Day 172311919Day 1 evening72311918Day 1 evening72311919Day 272311918Day 272311919Day 2 evening72311918Day 2 evening72311919Day 372311918Day 372311919
>= LOD, < LLOQ>= LLOQ< LODMissing
Oseltamivir217
Placebo225
Placebo6
Oseltamivir17
Placebo23
Oseltamivir1
Oseltamivir37
Placebo48
Placebo1
Oseltamivir8
Placebo201
Oseltamivir138
Placebo147
Oseltamivir30
Placebo27
Oseltamivir75
Placebo76
Oseltamivir3
Placebo5
Oseltamivir23
Placebo29
Placebo9
Oseltamivir24
Placebo13
Oseltamivir195
Placebo204
Oseltamivir70
Placebo92
Oseltamivir26
Placebo31
Oseltamivir146
Placebo129
Placebo3
Oseltamivir11
Placebo12
Oseltamivir6
Placebo4
Oseltamivir32
Placebo41
Oseltamivir197
Placebo198
Oseltamivir39
Placebo65
Oseltamivir25
Placebo35
Oseltamivir178
Placebo149
Oseltamivir4

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qPCR Viral Shedding -- Team Collected Samples

Median, 25% and 75% percentile of the value of viral shedding (Results = LOD, NCT01314911)
Timeframe: At Day 0, 3 and 7

,
Interventionlog10 copies/mL (Median)
Day 0Day 3Day 7
Oseltamivir6.853.43.2
Placebo6.93.93.2

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Percentage of Participants Who Required Hospitalization.

The percentage of participants hospitalized by 28 days was constructed by inverting an exact binomial test of the actual percentages (ignoring loss to follow-up). (NCT01314911)
Timeframe: From treatment initiation to Day 28

Interventionpercentage of participants (Number)
Oseltamivir1.4
Placebo0.7

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Time to Resolution of All Symptoms AND Fever

The assessed symptoms were cough, nasal obstruction (stuffy nose), sore throat, fatigue, headache, muscle aches, feverishness, rhinorrhea, nausea, vomiting, diarrhea. Fever was considered present based on the diary cards if a subject reported a maximal temperature ≥38.0°C (for the period since the diary card was previously completed) or reported having taken an antipyretic drug (also for the period since the diary card was previously completed). Time to resolution of all clinical symptoms and fever is defined as the time from Day 0 to the first of two successive measurements at which all clinical symptoms are grade 0 (absent) or 1(mild) and no fever >=38.0 C or antipyretic drug is reported. For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with symptoms and fever evaluated. (NCT01314911)
Timeframe: From treatment initiation to Day 28

Interventiondays (Median)
Oseltamivir4.0
Placebo4.0

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qPCR Viral Shedding -- Self Collected Samples

Median, 25% and 75% percentile of the value of viral shedding (Results = LOD, NCT01314911)
Timeframe: At Day 0, Day 0 evening, Day 1, Day 1 evening, Day 2, Day 2 evening and Day 3

,
Interventionlog10 copies/mL (Median)
Day 0Day 0 eveningDay 1Day 1 eveningDay 2Day 2 eveningDay 3
Oseltamivir6.15.54.23.93.43.23.2
Placebo6.26.04.54.03.43.23.4

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Percentage of Participants Who Develop Bronchitis, Pneumonia, or Other Complications Requiring An Antibiotic Use, After Day 0.

Participants were assessed for the signs/symptoms suggestive of one of the following complications: Sinusitis, Otitis Media ,Bronchitis / Bronchiolitis, Pneumonia and antibiotic use for reason other than above. (NCT01314911)
Timeframe: From treatment initiation to Day 28

,
Interventionpercentage of participants (Number)
SinusitisOtitis MediaBronchitis BronchiolitisPneumoniaAntibiotic useIf have at least one Complication
Oseltamivir3.20.42.50.42.57.2
Placebo1.80.42.20.43.66.8

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Time to Return to Pre-influenza Function

Time to return to pre-influenza function is defined as the time from Day 0 to the first of two successive 'Yes' answers to the global assessment question 'Are you functioning as well as you were before you had the flu'.For participants who did not have two successive records meeting this criterion, follow-up was censored for analysis purposes at the time of the last but one diary card record with question answered. (NCT01314911)
Timeframe: From treatment initiation to Day 28

Interventiondays (Median)
Oseltamivir3.5
Placebo5.0

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Renal Clearance (CLR) of Oseltamivir and Oseltamivir Carboxylate

CLR is calculated as the cumulative amount of drug excreted into urine from 0 to time t hours (Ae0-tlast) / area under the concentration-time curve from time zero through the last quantifiable concentration time (AUC0-t). (NCT01556633)
Timeframe: Pre-dose; 0.5, 1.33, 2, 2.5, 3, 4, 5, 6.67, 8, 10, 12, 14, 16, 20, 24, 28, 32, 48, 72, 96, 120, 144, and 168 hrs post-dose for blood; pre-dose and 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hrs post-dose for urine.

,
InterventionL/h (Geometric Mean)
CLR, oseltamivir (n = 4, 5)CLR, oseltamivir carboxylate (n = 4, 6)
Dialysis (Oseltamivir 75 mg)0.5720.655
Reduced Creatinine Clearance (Oseltamivir 30 mg)3.302.28

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Tmax and T1/2 of Oseltamivir and Oseltamivir Carboxylate

"The Time of observed maximum plasma concentration (Tmax) is defined as actual sampling time to reach maximum observed analyte concentration.~The Elimination Half-Life Period (T1/2) is the time measured for the plasma concentration to decrease by 1 half to its original concentration. Oseltamivir carboxylate is a clinically active metabolite of oseltamivir." (NCT01556633)
Timeframe: Pre-dose; 0.5, 1.33, 2, 2.5, 3, 4, 5, 6.67, 8, 10, 12, 14, 16, 20, 24, 28, 32, 48, 72, 96, 120, 144, and 168 hrs post-dose

,
Interventionh (Median)
Tmax, Oseltamivir (n = 9, 5)T1/2, Oseltamivir (n = 6,3)Tmax, Oseltamivir carboxylate (n = 9, 6)T1/2, Oseltamivir Carboxylate (n = 9,6)
Dialysis (Oseltamivir 75 mg)2.501.9220.0035.3
Reduced Creatinine Clearance (Oseltamivir 30 mg)1.332.257.3410.7

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C120h, C168h and Clast of Oseltamivir and Oseltamivir Carboxylate for 75 mg Dose

"C120h is defined as the plasma concentration at 120 hours post-dose. C168h is defined as the plasma concentration at 168 hours post-dose. Clast is defined as the plasma concentration corresponding to the time of the last measureable (positive) plasma concentration.~Oseltamivir carboxylate is a clinically active metabolite of oseltamivir." (NCT01556633)
Timeframe: Pre-dose; 0.5, 1.33, 2, 2.5, 3, 4, 5, 6.67, 8, 10, 12, 14, 16, 20, 24, 28, 32, 48, 72, 96, 120, 144, and 168 hrs post-dose

Interventionng/mL (Mean)
C120h, oseltamivirC168h,oseltamivirClast, oseltamivirC120h, oseltamivir carboxylateC168h,oseltamivir carboxylateClast, oseltamivir carboxylate
Dialysis (Oseltamivir 75 mg)NANA1.30301.0138.0140.0

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Total Dialysate Clearance for Automated Peritoneal Dialysis (CLDAPD) of Oseltamivir and Oseltamivir Carboxylate for 75 mg Dose

"CLDAPD is the total dialysate clearance for automated peritoneal dialysis, attributable to both continuous cycler-assisted peritoneal dialysis (CCPD) and continuous ambulatory peritoneal dialysis (CAPD), which was calculated with the recovery method over the dense blood sampling collection interval from 0 to 48 hours post-dose.~CLDAPD = the amount excreted into dialysate from 0 to 48 hours (Aed[0-48])/ plasma area under the concentration-time curve from time zero through 48 hours (AUC[0-48])~CLDCCPD = mean of CLDCCPD from the 2 CCPD sessions, calculated as CLDCCPD = (Aed[0-8]/AUC[0-8] + Aed[24-32]/AUC[24-32]) / 2~CLDCAPD = mean of CLDCAPD from the 3 CAPD sessions, calculated as CLDCAPD = (Aed[8-16]/AUC[8-16] + Aed[16-24]/AUC[16-24] + Aed[32-48]/AUC[32-48]) / 3" (NCT01556633)
Timeframe: CCPD: pre-dose (0)-2.67, 2.67-5.33, 5.33-8; CAPD: 8-16, 16-24; CCPD: 24-26.67, 26.67-29.33, 29.33-32; CAPD: 32-40, 40-48 hrs post-dose for urine; CCPD and CAPD:0.5, 1.33, 2, 2.5, 3, 4, 5, 6.67, 8, 10, 12, 14, 16, 20, 24, 28, 32, 48 hrs post-dose for blood

InterventionLitre (L)/hour (h) (Geometric Mean)
Oseltamivir, CLDAPDOseltamivir, CLDCAPDOseltamivir, CLDCCPDOseltamivir Carboxylate CLDAPDOseltamivir Carboxylate, CLDCAPDOseltamivir Carboxylate, CLDCCPD
Dialysis (Oseltamivir 75 mg)NANA0.1830.2300.1870.326

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Cmax of Oseltamivir and Oseltamivir Carboxylate

The Plasma Concentration (Cmax) is defined as maximum observed analyte concentration. Oseltamivir carboxylate is a clinically active metabolite of oseltamivir. (NCT01556633)
Timeframe: Pre-dose; 0.5, 1.33, 2, 2.5, 3, 4, 5, 6.67, 8, 10, 12, 14, 16, 20, 24, 28, 32, 48, 72, 96, 120, 144, and 168 hrs post-dose

,
Interventionng/mL (Geometric Mean)
Oseltamivir (n = 9,5)Oseltamivir carboxylate (n = 9,6)
Dialysis (Oseltamivir 75 mg)67.11710
Reduced Creatinine Clearance (Oseltamivir 30 mg)22.1361

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Number of Participants With Abnormal Shifts in Vital Signs

"Vital signs included pulse rate, systolic blood pressure (SBP), diastolic blood pressure (DBP), and body temperature.~Vital sign with abnormal shifts from normal at baseline to high or low at post-baseline time points were recorded. Blood pressure was recorded in millimeter of mercury (mmHg), and temperature in degrees Celsius. Low blood pressure defined as <=70 mmHg (SBP) and <=40 mmHg (DBP); high blood pressure defined as >=140 mmHg (SBP) and >=90 mmHg (DBP); low temperature defined as <=36.5 degrees Celsius and high temperature defined as >=37.5 degrees Celsius." (NCT01556633)
Timeframe: Days 1 (post-dose), 2, 3, 4, 5, 6, 7, 8; and Follow-up visit (Days 15 to 22)

,
Interventionparticipants (Number)
SBP , Day 1 - postdose, HighSBP, Day 2, HighSBP, Day 3, HighSBP, Day 4, HighSBP, Day 5, HighSBP, Day 7, HighSBP, Day 8, HighSBP, Follow Up, HighDBP, Day 2, HighDBP, Day 3, HighDBP, Day 7, HighDBP, Day 8, HighDBP, Follow Up, HighTemperature, Day 4, LowTemperature, Day 6, LowTemperature, Day 7, LowTemperature, Day 8, LowTemperature, Follow Up, Low
Dialysis (Oseltamivir 75 mg)122221120200321112
Reduced Creatinine Clearance (Oseltamivir 30 mg)011111001011000000

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Number of Participants With Any Adverse Event (AEs) and Any Serious Adverse Events (SAEs)

An AE is defined as any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with the intervention. An SAE is any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or results in a congenital anomaly/birth defect. (NCT01556633)
Timeframe: Approximately 7 weeks

,
Interventionparticipants (Number)
Any AEsAny SAEs
Dialysis (Oseltamivir 75 mg)91
Reduced Creatinine Clearance (Oseltamivir 30 mg)20

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Number of Participants With Marked Abnormality in Laboratory Measurements

"Laboratory analysis included: hematology (hemoglobin, hematocrit, reticulocyte, red blood cell, platelet and white blood cell count, mean corpuscular volume, mean corpuscular hemoglobin), prothrombin and activated partial thromboplastin time, biochemistry (sodium, potassium, bicarbonate, phosphate, chloride, calcium, urea, serum creatinine, bilirubin, cholesterol, alkaline phosphatase, aspartate aminotransferase, alanine aminotransferase [ALT], gamma-glutamyl transferase, protein, albumin, amylase, creatinine, lipase), random glucose, and urinalysis.~Laboratory test result values falling outside of the marked abnormality range that also represent a defined change from baseline were considered as marked laboratory abnormalities. A marked reference range for sodium is 130-150 millimole (mmol)/L, chloride is 95-115 mmol/L, phosphate is 0.75-1.60 mmol/L, calcium is 2-2.90 mmol/L, glucose is 2.8-11.10 mmol/L, bicarbonate is 18-28 mmol/L, and ALT is 0-110 Unit/L." (NCT01556633)
Timeframe: Approximately 7 weeks

,
Interventionparticipants (Number)
Sodium chlorideChloridePhosphateCalciumGlucose (random)BicarbonateALT
Dialysis (Oseltamivir 75 mg)1331111
Reduced Creatinine Clearance (Oseltamivir 30 mg)0000000

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Number of Participants With Change From Baseline in Marked Abnormality in Electrocardiogram (ECG) Parameters at Follow-up Visit

ECG parameter included QT interval, QTcB interval and QTcF interval (all intervals are measured in millisecond [msec]). Marked abnormality in ECG is predefined for QT, QTcB, and QTcF interval as <=30, >30-60, and >60 msec increase from baseline. (NCT01556633)
Timeframe: From Baseline (Day -1) to Follow-up visit (Days 15 to 22)

,
Interventionparticipants (Number)
QT, <= 30QT, > 30 - 60QTcB, <= 30QTcF, <= 30QTcF, > 30 - 60
Dialysis (Oseltamivir 75 mg)821091
Reduced Creatinine Clearance (Oseltamivir 30 mg)60660

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AUC120, AUC168 and AUCinf of Oseltamivir and Oseltamivir Carboxylate for 75 mg Dose

AUC120 is defined as the area under the plasma concentration-time curve from time zero through 120 hours post-dose, AUC168 is defined as the area under the plasma concentration-time curve from time zero through 168 hours post-dose, and AUCinf is defined as the area under the plasma concentration-time curve from time zero extrapolated to infinity. Oseltamivir carboxylate is a clinically active metabolite of oseltamivir. (NCT01556633)
Timeframe: Pre-dose; 0.5, 1.33, 2, 2.5, 3, 4, 5, 6.67, 8, 10, 12, 14, 16, 20, 24, 28, 32, 48, 72, 96, 120, 144, and 168 hrs post-dose

Interventionnanogram (ng)*h/ milliliter (mL) (Geometric Mean)
AUC120 oseltamivir (n = 6)AUC168 oseltamivir (n = 6)AUCinf oseltamivir (n = 6)AUC120 oseltamivir carboxylate (n = 9)AUC168 oseltamivir carboxylate (n = 9)AUCinf oseltamivir carboxylate (n = 9)
Dialysis (Oseltamivir 75 mg)175175175834008920093800

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AUCinf of Oseltamivir and Oseltamivir Carboxylate for 30 mg Dose

AUCinf is defined as the area under the plasma concentration-time curve from time zero extrapolated to infinity. Oseltamivir carboxylate is a clinically active metabolite of oseltamivir. (NCT01556633)
Timeframe: Pre-dose; 0.5, 1.33, 2, 2.5, 3, 4, 5, 6.67, 8, 10, 12, 14, 16, 20, 24, 28, 32, 48, 72, 96, 120, 144, and 168 hrs post-dose

Interventionng*h/mL (Geometric Mean)
AUCinf, oseltamivir (n = 3)AUCinf, oseltamivir carboxylate (n = 6)
Reduced Creatinine Clearance (Oseltamivir 30 mg)64.78630

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Percentage of Patients With Resolution of Influenza Symptoms

Assessment of the proportion of subjects with no clinical symptoms of the disease (fever, common and respiratory symptoms) at Study Day 7 (Visit 3). The severity of influenza symptoms was assessed by a physician with 0 to 3 point scale, where 0 means no symptom, 1=mild symptom, 2=moderate symptom, and 3=severe symptom (NCT01804946)
Timeframe: on the day 7 of the observation

,
InterventionPercentage of participants (Number)
FeverCommon symptomsRespiratory symptomsAll symptoms
Ergoferon Group100618347
Oseltamivir Group100647649

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Severity of Influenza Symptoms (Total Score of the Common Symptoms and Respiratory Symptoms)

The severity of influenza symptoms was assessed during a physical examination at Day 1, 3 and 7; common (10 symptoms) and respiratory (5 symptoms) symptom's total score was assessed with using the point scale: 0=No symptom; 1=Mild symptom; 2=Moderate symptom ; 3=Severe symptom. The Common Symptoms total score ranged from 0 (no symptoms) to 30 (severe symptoms). The Respiration Symptoms total score ranged from 0 (no symptoms) to 15 (severe symptoms) (NCT01804946)
Timeframe: on days 1, 3 and 7 of the observation

,
InterventionScores on a scale (Mean)
Common symptoms, Day 1Common symptoms, Day 3Common symptoms, Day 7Respiratory symptoms, Day 1Respiratory symptoms, Day 3Respiratory symptoms, Day 7
Ergoferon Group19.09.22.36.14.31.3
Oseltamivir Group18.67.81.95.94.01.4

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The Number of the Antipyretic Intake

A subject recorded the number of antipyretic intake in patient diary. (NCT01804946)
Timeframe: Day 1 to Day 5

,
InterventionNumber of Doses (Mean)
Day 1Day 2Day 3Day 4Day 5
Ergoferon Group0.650.400.190.010.00
Oseltamivir Group0.720.490.150.030.01

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Time to Resolution of the Influenza

"Time to resolution was considered as time to the absence of any flu symptom. Absence of symptoms was considered as axillary temperature decline to or below 37.0 ºС without subsequent rise, resolution of the common and respiratory symptoms.~The duration of a symptom was defined by physician recorded presence/absence of the symptoms during a physical examination at Day 1 to Day 7." (NCT01804946)
Timeframe: Day 1 to Day 7

,
InterventionDays (Mean)
FeverCommon symptomsRespiratory symptomsAll influenza symptoms
Ergoferon Group2.12.62.72.6
Oseltamivir Group2.32.42.62.5

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Percentage of Patients With Complications of the Influenza

Pneumonia, sinusitis, otitis media are examples of the influenza complications (NCT01804946)
Timeframe: Day 1 to Day 7

InterventionPercentage of participants (Number)
Ergoferon Group0
Oseltamivir Group2

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Change in the Patient's Quality of Life.

The quality of life was assessed in influenza patients at baseline and at the end of the treatment period using the European Quality of Life Questionnaire (EQ5D) measuring the health status by five dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression (each dimension is assessed by 1 to 3 point scale; the minimum score 5 points refers to the best status, 15 points refers to the worst status). (NCT01804946)
Timeframe: Day 7 vs. Day 1

,
InterventionScores on a scale (Mean)
Day 1Day 7
Ergoferon Group9.55.4
Oseltamivir Group9.45.4

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Change in the Subjective Health Status

The patient subjective health status assessment was based on Visual Analogue Scale - VAS). VAS includes a rating of current health status from 0 (worst) to 100 (best). (NCT01804946)
Timeframe: Day 7 vs. Day 1

,
InterventionScores on a scale (Mean)
Day 1Day 7
Ergoferon Group41.687.7
Oseltamivir Group46.288.0

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Mean Body Temperature

The axillary temperature was assessed during a physical examination at Day 1, 3 and 7; axillary temperature was assessed in degrees (Celsius, °С) (NCT01804946)
Timeframe: on days 1, 3 and 7 of the observation

,
Intervention°C (Mean)
Axillary temperature, Day 1Axillary temperature, Day 3Axillary temperature, Day 7
Ergoferon Group38.337.036.5
Oseltamivir Group38.337.036.6

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Percentage of Patients With Normal Body Temperature

Axillary temperature (morning and evening) decline to or below 37.0 ºС (without subsequent increase during ≥24 h) (NCT01804946)
Timeframe: Day 1 to Day 5

,
InterventionPercentage of participants (Number)
Evening, Day 1Evening, Day 2Evening, Day 3Evening, Day 4Evening, Day 5
Ergoferon Group (EG)415416884
Oseltamivir Goup (OG)115437288

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Proportion of Patients With Negative Results of Virological Analysis.

Based on medical records of patients whose nasopharyngeal swabs submitted for Reverse Transcription Polymerase Chain Reaction (RT-PCR) were negative for influenza A/B virus. (NCT01850446)
Timeframe: On days 3, 5, 7 of observation.

,
InterventionParticipants (Count of Participants)
Day 3Day 5Day 7
Ergoferon (1 Tablet 3 Times a Day)455765
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day507075

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Dynamics of Parameters of Immune Status (T-cell and B-cell Immune Response).

The concentration of regulators of the T-cell immune response (IL2, IFN -γ, IL-18), and regulators of В-cell immune response (IL-4, IL-16). (NCT01850446)
Timeframe: On days1, 3 and 7 of observation.

,
Interventionpg/mL (Mean)
IL-2/Day1IL-2/Day3IL-2/Day7IFN-γ/Day1IFN-γ/Day3IFN-γ/Day7IL-18/Day1IL-18/Day3IL-18/Day7IL-4/Day1IL-4/Day3IL-4/Day7IL-16/Day1IL-16/Day3IL-16/Day7
Ergoferon (1 Tablet 3 Times a Day)3.254.404.655.117.219.00238.99277.74239.841.261.541.5128.4044.2645.36
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day4.263.524.399.917.766.63192.15220.64195.011.391.211.3260.4158.1564.45

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Percentage of Patients Who Used Antipyretics on Days 1, 2, 3, 4 and 5 of the Treatment.

"Antipyretics, which are allowed for use during clinical trial, are:~Paracetamol;~Metamizole sodium (if hyperthermia was not stopped by usage of paracetamol)." (NCT01850446)
Timeframe: Days 1, 2, 3, 4 and 5 of the treatment

,
InterventionParticipants (Count of Participants)
Day 1Day 2Day 3Day 4Day 5
Ergoferon (1 Tablet 3 Times a Day)64391410
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day59381132

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Percentage of Patients With Normal Body Temperature.

Based on patient's diary. Normal body temperature is no more than 37.0ºС. (NCT01850446)
Timeframe: Days 2-7 of the observation

,
InterventionParticipants (Count of Participants)
Morning, day 2Morning, day 3Morning, day 4Morning, day 5Morning, day 6Morning, day 7Evening, day 2Evening, day 3Evening, day 4Evening, day 5Evening, day 6
Ergoferon (1 Tablet 3 Times a Day)112143688390917456983
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day1231497281882029486978

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Severity of Influenza Symptoms (Fever, Flu Non-specific and Nasal/Throat/Chest Symptoms) in Scores According to the Symptoms Severity Scale.

"The symptoms severity scale includes 14 symptoms: body temperature, non-specific symptoms (headache, chills, sweating, weakness, muscle pain, drowsiness), nasal/throat/chest symptoms (runny nose, stuffy nose, sneezing, sore throat, hoarseness, cough, chest pain).~The severity of each non-specific and nasal/throat/chest symptom is scored on a 4-point scale (0=no symptom; 1=mild symptom; 2=moderate symptom; 3=severe symptom). The minimum value of each symptom is 0 points, and the maximum value is 4 points.~The absolute body temperature (in degrees Celsius) is converted to relative units (or scores) using the following scale: ≤37.2С=0 points; 37.3-38.0С=1 point; 38.1-39.0С=2 points; ≥39.1С=3 points.~The severity of symptoms is based on the physical examination of the patient by the physician on days 1, 3, and 7 and on the patient diary data on days 1-7. The minimum symptoms severity score is 0 points, the maximum score is 42 points." (NCT01850446)
Timeframe: On 1-7 days of observation

,
Interventionscore on a scale (Mean)
Morning, day 1 (patient diary data)Morning, day 2 (patient diary data)Morning, day 3 (patient diary data)Morning, day 4 (patient diary data)Morning, day 5 (patient diary data)Morning, day 6 (patient diary data)Morning, day 7 (patient diary data)Evening, day 1 (patient diary data)Evening, day 2 (patient diary data)Evening, day 3 (patient diary data)Evening, day 4 (patient diary data)Evening, day 5 (patient diary data)Evening, day 6 (patient diary data)Day 1 (based on physician's objective examination)Day 3 (based on physician's objective examination)Day 7 (based on physician's objective examination)
Ergoferon (1 Tablet 3 Times a Day)20.416.313.08.75.43.62.318.815.611.47.24.92.919.712.72.0
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day20.915.712.28.05.73.72.518.214.710.17.34.63.220.111.32.0

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Percentage of Patients With Recovery/Improvement in Health Status.

Based on days 2-7 days of observation according to the patient's diary, and on days 3 and 7 according to the physician's examination. (NCT01850446)
Timeframe: On 2-7 days of observation

,
InterventionParticipants (Count of Participants)
Morning, day 2 (patient diary data)Morning, day 3 (patient diary data)Morning, day 4 (patient diary data)Morning, day 5 (patient diary data)Morning, day 6 (patient diary data)Morning, day 7 (patient diary data)Evening, day 2 (patient diary data)Evening, day 3 (patient diary data)Evening, day 4 (patient diary data)Evening, day 5 (patient diary data)Evening, day 6 (patient diary data)Day 3 (physician's examination)Day 7 (physician's examination)
Ergoferon (1 Tablet 3 Times a Day)22731496813123660269
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day3392149624693153568

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Average Duration of Fever.

Criteria of no fever - body temperature lower than 37.0° C for 24 hours (NCT01850446)
Timeframe: From the time of randomization until the time of recovery/improvement (days 1-7)

Interventiondays (Mean)
Ergoferon (1 Tablet 3 Times a Day)3.77
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day3.54

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Percentage of Patients Requiring Antibiotics Administration.

"Based on patient's diary, objective examination (according to physician's objective examination).~The patients with the development of disease complications and exacerbation of the disease course (the development of severe influenza)." (NCT01850446)
Timeframe: On 1-7 days of observation.

InterventionParticipants (Count of Participants)
Ergoferon (1 Tablet 3 Times a Day)1
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day1

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The Severity of Influenza.

"Based on the patient diary. The severity of influenza based on the data on the Area Under Curve for total index of influenza severity." (NCT01850446)
Timeframe: On days 1-7 of the observation.

Interventionscore*day (Mean)
Ergoferon (1 Tablet 3 Times a Day)59.88
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day57.88

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Changes in Fever.

Fever changes over time (body temperature change on days 2-7 compared to baseline, based on patient diary data). (NCT01850446)
Timeframe: Baseline and days 2-7 of the observation

,
Intervention°C (Mean)
Morning, day 1Morning, day 2Morning, day 3Morning, day 4Morning, day 5Morning, day 6Morning, day 7Evening, day 1Evening, day 2Evening, day 3Evening, day 4Evening, day 5Evening, day 6
Ergoferon (1 Tablet 3 Times a Day)38.837.837.437.036.836.636.538.337.837.337.036.836.6
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day38.737.837.236.936.736.636.538.337.737.237.036.836.7

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Duration of Clinical Symptoms of Influenza (Fever, Non-specific Symptoms and Nasal/ Throat/ Chest Symptoms) in Days.

Duration of clinical symptoms of influenza (fever, non-specific symptoms and nasal/ throat/ chest symptoms) in days based on the result of the patient's diary data (NCT01850446)
Timeframe: On 1-7 days of observation

,
Interventiondays (Mean)
FeverNon-specific symptomsNasal/ throat/ chest symptoms
Ergoferon (1 Tablet 3 Times a Day)2.964.824.83
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day2.865.05.08

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Dynamics of Parameters of Immune Status ( IFN-α and IFN-γ Production).

Level of spontaneous and induced production of IFN-α and IFN-γ (in vitro). (NCT01850446)
Timeframe: On day 1, 3 and 7 of observation.

,
Interventionpg/mL (Mean)
Spontaneous IFN-α/Day1Spontaneous IFN-α/Day3Spontaneous IFN-α/Day7Induced IFN-α/Day1Induced IFN-α/Day3Induced IFN-α/Day7Spontaneous IFN-γ/Day1Spontaneous IFN-γ/Day3Spontaneous IFN-γ/Day7Induced IFN-γ/Day1Induced IFN-γ/Day3Induced IFN-γ/Day7
Ergoferon (1 Tablet 3 Times a Day)11.4212.398.0413.3012.989.0614.2720.7910.34113.3184.1695.16
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day8.256.196.1213.589.738.5510.7311.9917.00164.92177.92154.31

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Dynamics of Parameters of Immune Status (Absolute Number of Each Type of White Blood Cells and Different Lymphocyte Phenotypes).

The absolute number of each type of white blood cells (WBC): Absolut Count (AC) of leukocytes, neutrophils, lymphocytes, monocytes, eosinophils, basophils, and CD3, CD4, CD8, CD4/CD8, CD16, CD119 leukocytes. (NCT01850446)
Timeframe: On days 1, 3 and 7 of observation.

,
Intervention10^9 cells/L (Mean)
AC of leukocytes/Day1AC of leukocytes/Day3AC of leukocytes/Day7AC of neutrophils/Day1AC of neutrophils/Day3AC of neutrophils/Day7AC of lymphocytes/Day1AC of lymphocytes/Day3AC of lymphocytes/Day7AC of monocytes/Day1AC of monocytes/Day3AC of monocytes/Day7AC of eosinophils/Day1AC of eosinophils/Day3AC of eosinophils/Day7AC of basophils/Day1AC of basophils/Day3AC of basophils/Day7AC of CD3+/Day1AC of CD3+/Day3AC of CD3+/Day7AC of CD3+CD4+/Day1AC of CD3+CD4+/Day3AC of CD3+CD4+/Day7AC of CD3+CD8+/Day1AC of CD3+CD8+/Day3AC of CD3+CD8+/Day7AC of CD3+CD16+CD56+/Day1AC of CD3+CD16+CD56+/Day3AC of CD3+CD16+CD56+/Day7AC of CD3-CD16+CD56+/Day1AC of CD3-CD16+CD56+/Day3AC of CD3-CD16+CD56+/Day7AC of CD3-CD8+/Day1AC of CD3-CD8+/Day3AC of CD3-CD8+/Day7AC of CD19+CD3-/Day1AC of CD19+CD3-/Day3AC of CD19+CD3-/Day7AC of CD3+CD119+/Day1AC of CD3+CD119+/Day3AC of CD3+CD119+/Day7
Ergoferon (1 Tablet 3 Times a Day)5.474.985.813.392.322.731.371.982.460.620.580.470.060.070.110.030.020.041.061.591.890.661.021.240.360.520.610.070.110.100.150.190.170.050.080.090.190.200.311.391.982.37
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day5.334.616.503.232.133.451.261.862.410.730.500.490.070.100.120.040.030.031.171.481.860.740.951.220.380.470.590.090.070.070.160.160.170.060.070.070.200.200.331.531.852.39

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Dynamics of Parameters of Immune Status (Relative Percentage of Each Type of White Blood Cells and Different Lymphocyte Phenotypes).

The relative percentage of each type of white blood cells (WBC): Relative Count (AC) of leukocytes, neutrophils, lymphocytes, monocytes, eosinophils, basophils, and CD3, CD4, CD8, CD4/CD8, CD16, CD119 leukocytes. (NCT01850446)
Timeframe: On days 1, 3 and 7 of observation.

,
InterventionPercentage of total white blood cells (Mean)
RC of neutrophils/Day1RC of neutrophils/Day3RC of neutrophils/Day7RC of lymphocytes/Day1RC of lymphocytes/Day3RC of lymphocytes/Day7RC of monocytes/Day1RC of monocytes/Day3RC of monocytes/Day7RC of eosinophils/Day1RC of eosinophils/Day3RC of eosinophils/Day7RC of basophils/Day1RC of basophils/Day3RC of basophils/Day7RC of CD3+/Day1RC of CD3+/Day3RC of CD3+/Day7RC of CD3+CD4+/Day1RC of CD3+CD4+/Day3RC of CD3+CD4+/Day7RC of CD3+CD8+/Day1RC of CD3+CD8+/Day3RC of CD3+CD8+/Day7RC of CD3+CD16+CD56+/Day1RC of CD3+CD16+CD56+/Day3RC of CD3+CD16+CD56+/Day7RC of CD3-CD16+56+/Day1RC of CD3-CD16+56+/Day3RC of CD3-CD16+56+/Day7RC of CD3-CD8+/Day1RC of CD3-CD8+/Day3RC of CD3-CD8+/Day7RC of CD19+CD3-/Day1RC of CD19+CD3-/Day3RC of CD19+CD3-/Day7
Ergoferon (1 Tablet 3 Times a Day)60.5947.5947.9425.9740.7242.9511.5311.768.361.051.281.860.480.460.6174.0880.6280.0746.6351.8752.0625.8026.3626.494.995.444.2412.339.687.154.384.063.5513.709.7112.82
Oseltamivir (Tamiflu) - 1 Capsule (75mg) Two Times a Day55.6045.8352.5324.4241.9938.6913.9710.927.641.322.071.850.760.580.4175.6979.7578.4448.3251.3351.5523.9225.2124.704.663.783.249.208.887.353.483.733.1814.9610.7914.56

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Percentage of Participants With Clinical Resolution of Abnormal Vital Signs

Description: Clinical resolution of abnormal vital signs was defined as meeting three out of five of the following criteria: 1. SpO2 ≥ 95% without supplemental O2; 2. Respiratory rate < 24 breaths per minute without supplemental O2; 3. Core temperature < 37.2 Celsius (C) immediately prior to receipt of any antipyretic drug, and at least 6-8 hours from the last dose of antipyretic or core temperature > 36 C in participants who are initially hypothermic; 4. Heart rate (HR) < 100 beats/minute; 5. Systolic blood pressure (SBP) >90 mmHg. Reported here is the percentage of participants who had clinical resolution of at least three out of five abnormal vital signs by the end of study. (NCT02293863)
Timeframe: From randomization up to 60 days

Interventionpercentage of participants (Number)
Placebo + Oseltamivir81.3
MHAA4549A 3600 mg + Oseltamivir73.3
MHAA4549A 8400 mg + Oseltamivir66.7

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Percentage of Participants With Secondary Complications of Influenza

The following were considered secondary complications of influenza: pneumonia, including hospital-acquired pneumonia (HAP) and ventilation-acquired pneumonia (VAP), exacerbations of chronic lung disease, myocarditis, acute respiratory distress syndrome (ARDS), otitis media, or other related complications. (NCT02293863)
Timeframe: From randomization up to 60 days

Interventionpercentage of participants (Number)
Placebo + Oseltamivir13.0
MHAA4549A 3600 mg + Oseltamivir15.4
MHAA4549A 8400 mg + Oseltamivir13.6

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Time to Normalization of Respiratory Function

The time to normalization of respiratory function was defined as the time to removal of the participant from oxygen (O2) supplementation in order to maintain a blood oxygen saturation level (SpO2) equal to or greater than 95% as measured by pulse oximetry. (NCT02293863)
Timeframe: From randomization up to 60 days

Interventiondays (Median)
Placebo + Oseltamivir4.28
MHAA4549A 3600 mg + Oseltamivir2.78
MHAA4549A 8400 mg + Oseltamivir2.65

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Number of Participants With Anti-Therapeutic Antibodies (ATA) to MHAA4549A During and Following Administration of MHAA4549A

Reported are the number of participants positive for ATAs at baseline, the number of participants with treatment-induced ATAs and the number of participants with treatment-enhanced ATAs. (NCT02293863)
Timeframe: From randomization up to 60 days

,,
Interventionparticipants (Number)
Positive for ATAs at baselineTreatment-induced ATAsTreatment-enhanced ATAs
MHAA4549A 3600 mg + Oseltamivir100
MHAA4549A 8400 mg + Oseltamivir100
Placebo + Oseltamivir000

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Percentage of Participants by Clinical Status Using a Categorical Ordinal Outcome

The clinical status of participants was defined by five mutually exclusive categories: 1. Death; 2. In the Intensive Care Unit (ICU); 3. Non-ICU hospitalization, requiring supplemental oxygen (O2); 4. Non-ICU hospitalization, not requiring supplemental oxygen (O2); 5. Not hospitalized. (NCT02293863)
Timeframe: Days 1-7, 14 and 30

,,
Interventionpercentage of participants (Number)
Day 1: DeathDay 1: In ICUDay 1: Non-ICU, requiring supplemental O2Day 1: Non-ICU, not requiring supplemental O2Day 1: Not hospitalizedDay 2: DeathDay 2: In ICUDay 2: Non-ICU, requiring supplemental O2Day 2: Non-ICU, not requiring supplemental O2Day 2: Not hospitalizedDay 3: DeathDay 3: In ICUDay 3: Non-ICU, requiring supplemental O2Day 3: Non-ICU, not requiring supplemental O2Day 3: Not hospitalizedDay 4: DeathDay 4: In ICUDay 4: Non-ICU, requiring supplemental O2Day 4: Non-ICU, not requiring supplemental O2Day 4: Not hospitalizedDay 5: DeathDay 5: In ICUDay 5: Non-ICU, requiring supplemental O2Day 5: Non-ICU, not requiring supplemental O2Day 5: Not hospitalizedDay 6: DeathDay 6: In ICUDay 6: Non-ICU, requiring supplemental O2Day 6: Non-ICU, not requiring supplemental O2Day 6: Not hospitalizedDay 7: DeathDay 7: In ICUDay 7: Non-ICU, requiring supplemental O2Day 7: Non-ICU, not requiring supplemental O2Day 7: Not hospitalizedDay 14: DeathDay 14: In ICUDay 14: Non-ICU, requiring supplemental O2Day 14: Non-ICU, not requiring supplemental O2Day 14: Not hospitalizedDay 30: DeathDay 30: In ICUDay 30: Non-ICU, requiring supplemental O2Day 30: Non-ICU, not requiring supplemental O2Day 30: Not hospitalized
MHAA4549A 3600 mg + Oseltamivir0.038.561.50.00.00.038.551.97.71.90.032.742.319.25.80.030.821.236.511.50.026.919.234.619.21.923.115.434.625.01.921.213.528.834.63.811.53.83.876.97.73.81.93.882.7
MHAA4549A 8400 mg + Oseltamivir0.043.252.34.50.02.338.631.820.56.82.334.127.325.011.42.329.518.229.520.52.327.318.227.325.02.322.715.925.034.12.320.515.925.036.46.89.16.84.572.79.14.54.50.081.8
Placebo + Oseltamivir0.042.657.40.00.00.042.640.711.15.60.037.031.520.411.10.035.225.922.216.70.027.825.924.122.21.922.222.227.825.91.918.524.114.840.71.95.67.414.870.45.61.95.61.985.2

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Percentage of Participants Who Died Due to Any Cause

(NCT02293863)
Timeframe: Days 14, 30 and 60

,,
Interventionpercentage of participants (Number)
Day 14Day 30Day 60
MHAA4549A 3600 mg + Oseltamivir3.87.79.6
MHAA4549A 8400 mg + Oseltamivir6.89.19.1
Placebo + Oseltamivir1.95.67.4

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Area Under Serum Concentration-Time Curve From Time 0 to Infinity (AUC ) of MHAA4549A

AUC0-inf is reported as day*microgram/milliliter (day*mcg/mL). (NCT02293863)
Timeframe: 30 minutes (min) before & 60 min after end of MHAA4549A infusion (infusion duration = 120 min) on Day 1; immediately prior to oseltamivir dose on Days 2, 3, 5, 7; on Days 14, 30; on day of discharge (up to Day 60); at study completion (Day 60)

Interventionday*mcg/mL (Mean)
MHAA4549A 3600 mg + Oseltamivir11400
MHAA4549A 8400 mg + Oseltamivir26700

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Area Under Viral Load-Time Curve (AUEC ) of Influenza A Virus

Influenza A viral load was measured by quantitative polymerase chain reaction (qPCR) in nasopharyngeal samples at multiple time points during the study. AUEC is the area under the viral load-time curve expressed as log10 (viral particles/milliliter x hour) = log10 (vp/mL x hour). (NCT02293863)
Timeframe: Immediately prior to MHAA4549A infusion and oseltamivir dosing on Day 1, immediately prior to oseltamivir dosing on Days 2 to 10, Days 14, 20, 25, 30, on day of discharge from hospital (up to Day 60), and at study completion (Day 60)

Interventionlog10 (vp/mL x hour). (Mean)
Placebo + Oseltamivir25.72
MHAA4549A 3600 mg + Oseltamivir21.99
MHAA4549A 8400 mg + Oseltamivir25.03

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Duration of Hospitalization

(NCT02293863)
Timeframe: From randomization up to 60 days

Interventiondays (Median)
Placebo + Oseltamivir8.95
MHAA4549A 3600 mg + Oseltamivir7.65
MHAA4549A 8400 mg + Oseltamivir6.69

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Duration of Intensive Care Unit (ICU) Stay

(NCT02293863)
Timeframe: From randomization up to 60 days

Interventiondays (Median)
Placebo + Oseltamivir4.66
MHAA4549A 3600 mg + Oseltamivir6.60
MHAA4549A 8400 mg + Oseltamivir5.29

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Duration of Ventilation

(NCT02293863)
Timeframe: From randomization up to 60 days

Interventiondays (Median)
Placebo + Oseltamivir4.11
MHAA4549A 3600 mg + Oseltamivir7.05
MHAA4549A 8400 mg + Oseltamivir5.89

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Duration of Viral Shedding

Influenza A viral load was measured by qPCR in nasopharyngeal samples at multiple time points during the study. Reported here is the duration of viral shedding. (NCT02293863)
Timeframe: Immediately prior to MHAA4549A infusion and oseltamivir dosing on Day 1, immediately prior to oseltamivir dosing on Days 2 to 10, Days 14, 20, 25, 30, on day of discharge from hospital (up to Day 60), and at study completion (Day 60)

Interventiondays (Median)
Placebo + Oseltamivir4.00
MHAA4549A 3600 mg + Oseltamivir4.63
MHAA4549A 8400 mg + Oseltamivir4.60

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Elimination Half-Life (Terminal t1/2) of MHAA4549A

(NCT02293863)
Timeframe: 30 min before & 60 min after end of MHAA4549A infusion (infusion duration = 120 min) on Day 1; immediately prior to oseltamivir dose on Days 2, 3, 5, 7; on Days 14, 30; on day of discharge (up to Day 60); at study completion (Day 60)

Interventionday (Mean)
MHAA4549A 3600 mg + Oseltamivir19.0
MHAA4549A 8400 mg + Oseltamivir17.8

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Maximum Serum Concentration (Cmax ) of MHAA4549A

(NCT02293863)
Timeframe: 30 min before & 60 min after end of MHAA4549A infusion (infusion duration = 120 min) on Day 1; immediately prior to oseltamivir dose on Days 2, 3, 5, 7; on Days 14, 30; on day of discharge (up to Day 60); at study completion (Day 60)

Interventionmcg/mL (Mean)
MHAA4549A 3600 mg + Oseltamivir916
MHAA4549A 8400 mg + Oseltamivir2220

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Observed Clearance (CL-obs) of MHAA4549A

(NCT02293863)
Timeframe: 30 min before & 60 min after end of MHAA4549A infusion (infusion duration = 120 min) on Day 1; immediately prior to oseltamivir dose on Days 2, 3, 5, 7; on Days 14, 30; on day of discharge (up to Day 60); at study completion (Day 60)

InterventionmL/day (Mean)
MHAA4549A 3600 mg + Oseltamivir288
MHAA4549A 8400 mg + Oseltamivir350

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Observed Steady State Volume of Distribution (Vss_obs) of MHAA4549A

(NCT02293863)
Timeframe: 30 min before & 60 min after end of MHAA4549A infusion (infusion duration = 120 min) on Day 1; immediately prior to oseltamivir dose on Days 2, 3, 5, 7; on Days 14, 30; on day of discharge (up to Day 60); at study completion (Day 60)

InterventionmL (Mean)
MHAA4549A 3600 mg + Oseltamivir6410
MHAA4549A 8400 mg + Oseltamivir7450

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Peak Influenza A Viral Load

Influenza A viral load was measured by qPCR in nasopharyngeal samples at multiple time points during the study. Reported here is the peak Influenza A viral load expressed as log10 vp/mL. (NCT02293863)
Timeframe: Immediately prior to MHAA4549A infusion and oseltamivir dosing on Day 1, immediately prior to oseltamivir dosing on Days 2 to 10, Days 14, 20, 25, 30, on day of discharge from hospital (up to Day 60), and at study completion (Day 60)

Interventionlog10 vp/mL (Mean)
Placebo + Oseltamivir5.70
MHAA4549A 3600 mg + Oseltamivir5.37
MHAA4549A 8400 mg + Oseltamivir5.28

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Percentage of Participants Readmitted to Hospital Due to Any Cause

(NCT02293863)
Timeframe: Days 30 and 60

Interventionpercentage of participants (Number)
Placebo + Oseltamivir1.9
MHAA4549A 3600 mg + Oseltamivir3.8
MHAA4549A 8400 mg + Oseltamivir0

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Percentage of Participants Using Antibiotics for Respiratory Infections

(NCT02293863)
Timeframe: From randomization up to 60 days

Interventionpercentage of participants (Number)
Placebo + Oseltamivir13.0
MHAA4549A 3600 mg + Oseltamivir11.5
MHAA4549A 8400 mg + Oseltamivir11.4

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Percentage of Participants With Adverse Events

An adverse event is any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with the treatment. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a pharmaceutical product, whether or not considered related to the pharmaceutical product. Preexisting conditions which worsen during a study are also considered as adverse events. (NCT02293863)
Timeframe: From randomization up to 60 days

Interventionpercentage of participants (Number)
Placebo + Oseltamivir80.4
MHAA4549A 3600 mg + Oseltamivir67.3
MHAA4549A 8400 mg + Oseltamivir74.5

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Percentage of Participants With Clinical Failure

Clinical failure after 24 hours post-infusion of study drug was defined as progression to increased O2 requirement defined by an increase in oxygen supplementation from low flow oxygen (i.e., 2-6 liters per minute [L/min]) to high flow oxygen (i.e., > 6 L/min) or from oxygen supplementation alone to any positive pressure ventilation (PPV) or extracorporeal membrane oxygenation (ECMO), progression to ICU, prolonged ventilation or O2 support defined by > 2 weeks, or death. (NCT02293863)
Timeframe: 24 hours after end of infusion (infusion duration = approximately 120 minutes) up to Day 60

Interventionpercentage of participants (Number)
Placebo + Oseltamivir14.8
MHAA4549A 3600 mg + Oseltamivir25.0
MHAA4549A 8400 mg + Oseltamivir22.7

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Time to Resolution of Fever

Time for fever resolution based on subject diary record of temperature recorded twice daily. A subject had resolution of fever if he/she had oral temperature of < 99.4°F or an axillary temperature of < 98.4°F and no antipyretic medications were taken for ≥ 12 hours. The time to resolution of fever was estimated for each age group and overall using the Kaplan-Meier method with temperature and symptom relief medication information obtained from the Subject Diary data. (NCT02369159)
Timeframe: 14 days

Interventionhours (Mean)
Peramivir (≥ 28 Days - < 2 Years)39.7
Oseltamivir (≥ 28 Days - < 2 Years)61.8
Peramivir (≥ 2 - < 7 Years)58.8
Oseltamivir (≥ 2 - < 7 Years)16.0
Peramivir (≥ 7 - < 13 Years)36.3
Oseltamivir (≥ 7 - < 13 Years)29.7
Peramivir (≥ 13 - < 18 Years)51.3
Oseltamivir (≥ 13 - < 18 Years)43.9

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Changes in Influenza Virus Titer in Nasopharyngeal Samples in Response to Treatment.

Change in influenza viral titers was defined as the time-weighted change from Baseline in log_10 tissue culture infective dose_50 (TCID50/mL) and was summarized for each treatment group. (NCT02369159)
Timeframe: Change from baseline assessed on days 3, 7 and 14.

,
Interventioninfluenza viral titer - log10 TCID50/mL (Median)
BaselineDay 3 - Change rom baselineDay 7 - Change from baselineDay 14 - Change from baseline
Oseltamivir4.50-3.25-4.00-4.00
Peramivir4.38-2.75-3.75-3.75

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Plasma Exposure of IV Peramivir as Measured by the Drug Concentration Over 6 Hours Post-dose

Up to 4 blood samples will be drawn, where possible: immediately following infusion and 30 to 60 mins, 1 to 3 hrs and 4 to 6 hrs post-infusions. AUC calculations were performed in Phoenix WinNonlin using the linear/log trapezoidal rule. AUC0-last was calculated between start of the infusion and the time of the last measurable concentration. (NCT02369159)
Timeframe: up to 6 hours post peramivir infusion

,,,
Interventionng*h/mL (Mean)
AUC0-lastAUC0-3
Peramivir (≥ 13 - < 18 Years)7240068300
Peramivir (≥ 2 - < 7 Years)7120068100
Peramivir (≥ 28 Days - < 2 Years)5620053300
Peramivir (≥ 7 - < 13 Years)8700081400

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Safety and Tolerability, as Measured by the Number of Participants Experiencing Adverse Events.

Safety evaluation included assessment of Adverse Events (AEs). (NCT02369159)
Timeframe: 14 days

,
InterventionParticipants (Count of Participants)
Adverse EventSevere or life-threatening Adverse EventAdverse Event possibly, probably, or definitely related to study drugSerious Adverse EventsAdverse Event leading to discontinuation from studyAdverse Event leading to Death
Oseltamivir504010
Peramivir2228000

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Time to Reduction in Viral Shedding

Assessment of viral shedding in bilateral, mid-nasal swab specimens taken at baseline and then on Day 3, 7 and 14. (NCT02369159)
Timeframe: 14 days

,,,,,,,
Interventionparticipants with positive viral titer (Number)
BaselineDay 3Day 7Day 14
Oseltamivir (≥ 13 - < 18 Years)5200
Oseltamivir (≥ 2 - < 7 Years)2100
Oseltamivir (≥ 28 Days - < 2 Years)1100
Oseltamivir (≥ 7 - < 13 Years)6600
Peramivir (≥ 13 - < 18 Years)12600
Peramivir (≥ 2 - < 7 Years)231220
Peramivir (≥ 28 Days - < 2 Years)8610
Peramivir (≥ 7 - < 13 Years)271310

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Time to Resolution of Influenza Symptoms

Subjects or parents or caregivers were asked to provide an assessment of age-appropriate influenza symptoms on a 4-point severity scale (0,absent; 1, mild; 2, moderate; 3, severe) twice daily beginning before screening on Day 1 until symptoms resolved or until the last follow-up visit. Time to alleviation of symptoms was the number of hours from initiation of study drug until the start of the time period in which all age-appropriate symptoms of influenza were either absent or present at a level no greater than mild for at least 21.5 (24 - 10%) hours. Subjects who did not experience alleviation of symptoms were censored at the last observed symptom assessment. (NCT02369159)
Timeframe: 14 days

Interventionhours (Mean)
Peramivir (≥ 28 Days - < 2 Years)76.1
Oseltamivir (≥ 28 Days - < 2 Years)98.9
Peramivir (≥ 2 - < 7 Years)94.1
Oseltamivir (≥ 2 - < 7 Years)20.7
Peramivir (≥ 7 - < 13 Years)66.6
Oseltamivir (≥ 7 - < 13 Years)134.4
Peramivir (≥ 13 - < 18 Years)101.3
Oseltamivir (≥ 13 - < 18 Years)75.5

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Change From Baseline in Hematology Parameters- Mean Corpuscle Hemoglobin (MCH)

Hematology parameters included Mean corpuscle hemoglobin (MCH). Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionPicogram (PG) (Mean)
Day 3Day 5Day 8Day 28/withdrawal
Danirixin (DNX) 75 mg0.03-0.11-0.160.12
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.21-0.14-0.240.18
Oseltamivir (OSV) 75 mg0.060.020.080.20
Placebo (PBO)-0.23-0.19-0.13-0.00

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Change From Baseline in Hematology Parameters- Hemoglobin

Hematology parameters included Hemoglobin. Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionGrams per Litre (G/L) (Mean)
Day 3Day 5Day 8Day 28/withdrawal
Danirixin (DNX) 75 mg0.0-1.3-5.2-5.9
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-4.4-5.9-6.1-10.1
Oseltamivir (OSV) 75 mg-8.8-7.4-7.0-4.4
Placebo (PBO)2.20.4-0.6-5.1

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Change From Baseline in Hematology Parameters- Hematocrit

Hematology parameters included Hematocrit. Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionFraction (Mean)
Day 3Day 5Day 8Day 28/withdrawal
Danirixin (DNX) 75 mg-0.0051-0.0056-0.0173-0.0224
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.0126-0.0182-0.0176-0.0331
Oseltamivir (OSV) 75 mg-0.0294-0.0250-0.0244-0.0136
Placebo (PBO)0.0050-0.0029-0.0063-0.0171

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Number of Participants With no Detectable Influenza Viral RNA by qRT-PCR From Nasopharyngeal Swabs on Baseline (Day 1), Day 3, Day 5, Day 8 and Day 14

Number of participants with no detectable influenza viral ribonucleic acid (RNA) by qRT-PCR from nasopharyngeal swabs on Baseline (Day1), Day 3, Day 5, Day 8 and Day 14 were recorded. Assessments recorded on Day 1 were considered as Baseline. (NCT02469298)
Timeframe: Up to Day 14

,,,
InterventionParticipants (Count of Participants)
Day 1Day 3Day 5Day 8Day 14
Danirixin (DNX) 75 mg00035
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg003611
Oseltamivir (OSV) 75 mg00155
Placebo (PBO)00014

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Change From Baseline in Clinical Chemistry- Alkaline Phosphatase (ALP), Alanine Amino Transferase (ALT), Aspartate Amino Transferase (AST) and Gamma Glutamyl Transferase (GGT)

Clinical chemistry parameters included Alkaline phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase and Gamma Glutamyl Transferase. Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionInternational Units per litre (IU/L) (Mean)
ALP: Day 3ALP: Day 5ALP: Day 8ALP: Day 28/withdrawalALT: Day 3ALT: Day 5ALT: Day 8ALT: Day 28/withdrawalAST: Day 3AST: Day 5AST: Day 8AST: Day 28/withdrawalGGT: Day 3GGT: Day 5GGT: Day 8GGT: Day 28/withdrawal
Danirixin (DNX) 75 mg-5.0-5.4-4.4-2.87.94.22.92.56.30.9-0.8-0.29.37.43.3-7.6
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-4.5-4.52.9-3.80.10.92.7-2.9-0.9-2.8-3.3-4.90.90.81.5-3.5
Oseltamivir (OSV) 75 mg-7.2-5.80.8-1.6-8.4-11.8-11.0-12.8-7.2-9.4-10.4-9.8-2.60.20.2-0.6
Placebo (PBO)-5.0-1.9-0.94.9-0.12.49.12.42.92.43.4-1.91.05.07.4-1.1

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Change From Baseline in Clinical Chemistry Parameters- Direct Bilirubin, Total Bilirubin, Creatinine and Uric Acid

Clinical chemistry parameters included Direct Bilirubin, Total Bilirubin, Creatinine and Uric acid. Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionMicromole per Liter (UMOL/L) (Mean)
Direct Bilirubin: Day 3Direct Bilirubin: Day 5Direct Bilirubin: Day 8Direct Bilirubin:Day 28/withdrawalTotal Bilirubin: Day 3Total Bilirubin: Day 5Total Bilirubin: Day 8Total Bilirubin:Day 28/withdrawalCreatinine: Day 3;Creatinine: Day 5Creatinine: Day 8Creatinine: Day 28/withdrawalUric acid: Day 3Uric acid: Day 5Uric acid: Day 8Uric acid: Day 28/withdrawal
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.5-0.5-0.1-0.1-1.60.00.50.5-6.58-10.16-8.87-8.24-15.1-16.30.912.5
Danirixin (DNX) 75 Milligram (mg)-0.3-0.50.10.1-1.0-1.2-0.90.1-1.47-4.38-5.79-2.54-15.1-18.020.830.1
Oseltamivir (OSV) 75 mg0.20.20.00.0-0.81.02.22.0-8.14-11.12-10.32-5.34-45.8-54.8-13.040.6
Placebo (PBO)0.0-0.6-0.1-0.1-2.0-2.7-0.9-0.3-4.39-7.39-10.70-4.99-9.9-47.4-14.3-0.4

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Change From Baseline in Clinical Chemistry Parameters- Calcium, Carbon Dioxide (CO2) Content/ Bicarbonate, Glucose, Potassium, Sodium and Urea/Blood Urea Nitrogen (BUN)

Clinical chemistry parameters included Calcium, CO2 content/ Bicarbonate, Glucose, Potassium, Sodium and Urea/(BUN). Blood samples were collected on Day 1, Day 3, Day 5 and Day 28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionMillimoles per Liter (MMOL/L) (Mean)
Calcium: Day 3Calcium: Day 5Calcium: Day 8Calcium: Day 28/withdrawalCO2 / Bicarbonate: Day 3CO2 / Bicarbonate: Day 5CO2 / Bicarbonate: Day 8CO2 / Bicarbonate: Day 28/withdrawalGlucose: Day 3Glucose: Day 5Glucose: Day 8Glucose: Day 28/withdrawalPotassium: Day 3Potassium: Day 5Potassium: Day 8Potassium: Day 28/withdrawalSodium: Day 3Sodium: Day 5Sodium: Day 8Sodium: Day 28/withdrawalUrea/BUN: Day 3Urea/BUN: Day 5Urea/BUN: Day 8Urea/BUN: Day 28/withdrawal
Danirixin (DNX) 75 mg-0.036-0.029-0.010-0.0190.10.40.6-0.40.280.130.200.27-0.12-0.070.08-0.040.50.30.9-0.30.310.470.900.60
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.046-0.0330.0300.0310.3-0.50.4-0.50.510.29-0.130.430.010.110.150.141.40.71.50.60.290.320.821.19
Oseltamivir (OSV) 75 mg-0.092-0.0520.0040.098-1.8-1.4-0.2-1.20.621.300.480.22-0.120.080.020.242.01.82.41.6-0.24-0.880.320.66
Placebo (PBO)0.0200.0190.0530.0990.90.9-0.11.10.230.13-0.160.710.130.160.210.070.11.10.30.6-0.31-0.190.170.96

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Change From Baseline in Clinical Chemistry Parameters- Albumin and Total Protein

Clinical chemistry parameters included Albumin and Total protein. Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionGrams per Litre (G/L) (Mean)
Albumin: Day 3Albumin: Day 5Albumin: Day 8Albumin: Day 28/withdrawalTotal protein: Day 3Total protein: Day 5Total protein: Day 8Total protein: Day 28/withdrawal
Danirixin (DNX) 75 mg-1.9-1.8-1.8-1.6-1.9-1.9-1.3-3.7
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-2.3-2.3-1.7-1.5-2.8-2.9-1.4-3.2
Oseltamivir (OSV) 75 mg-3.0-2.6-0.40.2-4.4-4.0-2.2-1.0
Placebo (PBO)-1.7-1.0-0.30.4-2.3-1.30.4-1.0

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Time to Resolution of Fever Over Time Post Initiation of Treatment

Time to resolution of fever was defined as the time when oral temperature was <= 37.2 degree Celsius (<=99.0 degree Fahrenheit) for at least 24 hours (with one hour window) without having taken any antipyretic medication for at least 4 hours. Temperature was taken orally and recorded in the eDiary, thrice daily from Day 1 to Day 5 (morning, noon, evening) and twice daily (morning, evening) from Day 6 to Day 14 by the participant using a digital thermometer provided by the study. For participants whose fever was not resolved by the Day 14 visit then after Day 14, participants continued to take oral temperature twice daily until temperature <=37.2 degree Celsius or <=99 degree Fahrenheit for 24 hours. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

InterventionHours (Median)
Danirixin (DNX) 75 mg119.833
Placebo (PBO)98.092
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg54.425
Oseltamivir (OSV) 75 mg76.167

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Number of Participants With DRE of Interest-associated Antibiotic Use

Use of antibiotics for DREs of interest was monitored. Roxithromycin was used for DRE sinusitis by one participant. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

InterventionParticipants (Count of Participants)
Danirixin (DNX) 75 mg0
Placebo (PBO)0
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg1
Oseltamivir (OSV) 75 mg0

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Number of Hospital Admissions Due to Influenza Infection

Number of participants admitted in hospital due to influenza infection was recorded. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

InterventionParticipants (Number)
Danirixin (DNX) 75 mg0
Placebo (PBO)0
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg0
Oseltamivir (OSV) 75 mg0

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Total Dose of Relief Medication

Use of study supplied relief medications (paracetamol and dextromethorphan for symptom relief were recorded in the eDiary and accordingly number of participants using these medications were recorded. The total dose of these relief medications used by these participants are presented. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

,,,
InterventionMilligrams (Median)
Paracetamol total doseDextromethorphan total dose
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg5500.00120.00
Danirixin (DNX) 75 Milligram (mg)5000.00150.00
Oseltamivir (OSV) 75 mg3000.0060.00
Placebo (PBO)9000.00390.00

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Change From Baseline in Electrocardiogram (ECG) Parameters

12-lead ECGs were obtained on Day 1, Day 3 and Day28/withdrawal using an ECG machine that automatically calculates and measures RR, PR, QRS, QT, and Corrected QT Interval using Bazette's formula (QTcB) and Corrected QT Interval using Fridericia forumula (QTcF) intervals. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionMillisecond (msec) (Mean)
RR Interval: Day 3RR Interval: Day 28/withdrawalQT Interval: Day 3QT Interval: Day 28/withdrawalQTcF: Day 3QTcF:Day 28/withdrawalQTcB: Day 3QTcB: Day 28/withdrawalPR Interval: Day 3PR Interval: Day 28/withdrawalQRS Duration: Day 3QRS Duration: Day 28/withdrawal
Danirixin (DNX) 75 mg-5.858.23.118.94.511.04.16.62.43.11.5-1.3
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg83.0107.417.725.36.511.00.33.50.43.0-0.50.6
Oseltamivir (OSV) 75 mg39.241.230.711.124.64.320.90.12.32.51.90.3
Placebo (PBO)49.476.925.035.918.824.814.317.0-5.49.3-5.6-5.7

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Change From Baseline in Hematology Parameters- Red Blood Cell (RBC) Count and Reticulocytes Count

Hematology parameters included RBC count and Reticulocytes count. Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionTrillion cells per Liter (TI/L) (Mean)
RBC: Day 3RBC: Day 5RBC: Day 8RBC: Day 28/withdrawalReticulocytes: Day 3Reticulocytes: Day 5Reticulocytes: Day 8Reticulocytes: Day 28/withdrawal
Danirixin (DNX) 75 mg-0.01-0.01-0.13-0.22-0.00989-0.01793-0.001580.00071
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.11-0.19-0.17-0.38-0.01735-0.02635-0.01032-0.00477
Oseltamivir (OSV) 75 mg-0.32-0.28-0.28-0.20-0.01694-0.014060.010200.01528
Placebo (PBO)0.130.060.01-0.16-0.00392-0.00314-0.005460.02313

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Change From Baseline in Hematology Parameters-Basophils, Eosinophils, Lymphocytes, Monocytes, Total Neutrophils (Total Absolute Neutrophil Count [Total ANC]), Platelet Count and White Blood Cell (WBC) Count

Hematology parameters included Basophils, Eosinophils, Lymphocytes, Monocytes, Total neutrophils (Total ANC), Platelet count and WBC count. Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionGiga cells per litre (GI/L) (Mean)
Basophils: Day 3Basophils: Day 5Basophils: Day 8Basophils: Day 28/withdrawalEosinophils: Day 3Eosinophils: Day 5Eosinophils: Day 8Eosinophils: Day 28/withdrawalLymphocytes: Day 3Lymphocytes: Day 5Lymphocytes: Day 8Lymphocytes: Day 28/withdrawalMonocytes: Day 3Monocytes: Day 5Monocytes: Day 8Monocytes: Day 28/withdrawalTotal neutrophils: Day 3Total neutrophils: Day 5Total neutrophils: Day 8Total neutrophils:Day 28/withdrawalPlatelet count: Day 3Platelet count: Day 5Platelet count: Day 8Platelet count: Day 28/withdrawalWBC count: Day 3WBC count: Day 5WBC count: Day 8WBC count: Day 28/withdrawal
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.008-0.0070.0050.030-0.0120.0120.0360.0320.4630.8130.9180.903-0.105-0.090-0.108-0.016-1.791-0.677-0.137-0.381-6.113.753.319.2-1.49-0.170.790.51
Danirixin (DNX) 75 Milligram (mg)-0.011-0.009-0.008-0.0070.0170.0340.0740.0300.0930.5570.7160.564-0.117-0.175-0.104-0.061-1.614-1.3710.463-0.217-9.516.464.328.3-1.62-0.941.140.31
Oseltamivir (OSV) 75 mg-0.008-0.0020.0080.010-0.0120.136-0.000-0.0180.4320.5760.7220.788-0.070-0.1180.0240.064-0.416-0.4241.7660.970-3.010.466.244.2-0.060.182.521.76
Placebo (PBO)-0.0020.0170.0130.0030.0260.0350.0780.1630.7781.0381.2751.619-0.178-0.128-0.097-0.011-2.276-1.223-0.830-0.2174.36.762.147.7-1.64-0.390.491.56

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Change From Baseline in Influenza Viral Load as Measured by Quantitative Reverse Transcription-polymerase Chain Reaction (qRT-PCR) From Nasopharyngeal Swabs on Day 3, Day 5, Day 8 and Day 14

Influenza viral load as measured by quantitative reverse transcription - polymerase chain reaction (qRT-PCR) from nasopharyngeal swabs on Baseline (Day 1), Day 3, Day 5, Day 8 and Day 14 was recorded. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and Day 3, Day 5, Day 8 and Day 14

,,,
InterventionLog viral particles/mL (Mean)
Day 3Day 5Day 8Day 14
Danirixin (DNX) 75 mg-0.897-1.912-3.764-4.024
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-1.620-2.962-3.862-4.518
Oseltamivir (OSV) 75 mg-1.904-2.644-4.250-4.250
Placebo (PBO)-1.415-2.812-4.063-4.992

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Change From Baseline in Influenza Viral Load as Measured by Quantitative Virus Culture From Nasopharyngeal Swabs on Day 3, Day 5, Day 8 and Day 14

Influenza viral load as measured by quantitative virus culture from nasopharyngeal swabs on Baseline (Day 1), Day 3, Day 5, Day 8 and Day 14 was recorded. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and Day 3, Day 5, Day 8 and Day 14

,,,
InterventionLog median tissue culture infective dose (Mean)
Day 3Day 5Day 8Day 14
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-1.943-2.467-2.698-2.614
Danirixin (DNX) 75 Milligram (mg)-1.810-2.534-2.885-2.564
Oseltamivir (OSV) 75 mg-2.304-3.108-3.108-3.108
Placebo (PBO)-0.753-2.172-2.843-2.260

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Change From Baseline in Urinalysis Parameters- Urine pH

Urinalysis parameters included urine pH. pH is calculated on a scale of 0 to 14, such that, the lower the number, more acidic the urine and higher the number, more alkaline the urine with 7 being neutral. Urinalysis was done on Day 1, Day 5 and Day 28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1), Day 5 and Day 28/withdrawal

,,,
InterventionPoints on a scale (Mean)
Day 5Day 28/withdrawal
Danirixin (DNX) 75 mg0.000.27
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg0.200.07
Oseltamivir (OSV) 75 mg0.400.70
Placebo (PBO)0.210.14

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Change From Baseline in Urinalysis Parameters- Urine Specific Gravity

Urinalysis parameter included Urine specific gravity and was measured on Day 1, Day 5 and Day 28. Urinary specific gravity is a measure of the concentration of solutes in the urine. It measures the ratio of urine density compared with water density and provides information on the kidney's ability to concentrate urine. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1), Day 5 and Day 28/withdrawal

,,,
InterventionRatio (Mean)
Day 5Day 28/withdrawal
Danirixin (DNX) 75 mg-0.0001-0.0045
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.0038-0.0021
Oseltamivir (OSV) 75 mg-0.0076-0.0050
Placebo (PBO)-0.00040.0013

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Change From Baseline in Vital Signs- Diastolic Blood Pressure (DBP) and Systolic Blood Pressure (SBP)

Vital signs were measured in semi-supine position after 5 minutes rest and included systolic and diastolic blood pressure. Three readings of blood pressure were taken; the first reading was rejected and the second and third readings were averaged to give the measurement to be recorded. Vital signs were obtained on Baseline (Day 1), Day 3, Day 5, Day 8, Day 14 and Day 28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionMillimeters of Mercury (mmHg) (Mean)
DBP: Day 3DBP: Day 5DBP: Day 8DBP: Day 14DBP: Day 28/withdrawalSBP: Day 3SBP: Day 5SBP: Day 8SBP: Day 14SBP: Day 28/withdrawal
Danirixin (DNX) 75 mg-2.10.3-4.4-4.5-4.4-5.73-3.00-5.86-6.20-3.36
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-1.1-2.1-2.30.8-1.1-2.87-1.93-2.60-1.20-0.80
Oseltamivir (OSV) 75 mg-4.2-5.2-0.8-7.8-3.5-5.00-3.000.60-3.80-2.83
Placebo (PBO)-0.7-1.1-4.6-0.7-0.6-5.29-0.71-9.29-4.57-0.43

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Change From Baseline in Vital Signs- Heart Rate (HR)

Vital signs were measured in semi-supine position after 5 minutes rest and included HR. Three readings of pulse rate were taken; the first reading was rejected and the second and third readings were averaged to give the measurement to be recorded. Vital signs were obtained on Day 1, Day 3, Day 5, Day 8, Day 14 and Day 28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionBeats per minute (Mean)
Heart rate: Day 3Heart rate: Day 5Heart rate: Day 8Heart rate: Day 14Heart rate: Day 28/withdrawal
Danirixin (DNX) 75 mg3.93-2.60-2.790.80-6.57
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-8.87-9.60-10.87-8.73-11.80
Oseltamivir (OSV) 75 mg-1.20-6.80-0.80-4.200.17
Placebo (PBO)-8.00-10.29-12.29-13.43-17.14

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Change From Baseline in Vital Signs- Percent Oxygen in Blood (POB)

Vital signs were measured in semi-supine position after 5 minutes rest and included POB. POB was obtained on Baseline (Day 1), Day 3, Day 5, Day 8, Day 14 and Day 28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionPercentage (%) (Mean)
POB: Day 3POB: Day 5POB: Day 8POB: Day 14POB: Day 28/withdrawal
Danirixin (DNX) 75 mg-1.7-0.7-0.8-0.7-1.1
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg0.10.4-0.10.00.2
Oseltamivir (OSV) 75 mg0.41.00.80.81.5
Placebo (PBO)1.1-0.40.40.91.1

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Change From Baseline in Vital Signs- Respiration Rate (RR)

Vital signs were measured in semi-supine position after 5 minutes rest and included RR. RR was obtained on Day 1, Day 3, Day 5, Day 8, Day 14 and Day 28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionBreaths per minute (Mean)
RR: Day 3RR: Day 5RR: Day 8RR: Day 14RR: Day 28/withdrawal
Danirixin (DNX) 75 mg-0.1-0.5-0.3-0.7-0.4
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.5-0.7-0.6-0.3-0.3
Oseltamivir (OSV) 75 mg1.41.20.60.80.8
Placebo (PBO)0.00.00.70.60.4

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Change From Baseline in Vital Signs- Temperature

Vital signs were measured in semi-supine position after 5 minutes rest and included temperature. Oral temperature was obtained on Day 1, Day 3, Day 5, Day 8, Day 14 and Day 28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionCentigrade (Mean)
Temperature: Day 3Temperature: Day 5Temperature: Day 8Temperature: Day 14Temperature: Day 28/withdrawal
Danirixin (DNX) 75 mg-0.20-0.75-0.46-0.73-0.71
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.57-0.76-0.83-0.83-0.71
Oseltamivir (OSV) 75 mg-0.08-0.14-0.16-0.28-0.22
Placebo (PBO)-1.11-1.34-1.50-1.59-1.39

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Number of Afebrile Participants Over Time Post Initiation of Treatment

Afebrile participants were defined as participants with oral temperature <=37.2 degree Celsius, <=99.0 degree Fahrenheit over time post initiation of treatment. Temperature was taken orally and recorded in the eDiary, thrice daily from Day 1 to Day 5 (morning, noon, evening) and twice daily (morning, evening) from Day 6 to Day 14 by the participant using a digital thermometer provided by the study. For participants whose fever was not resolved by the Day 14 visit then after Day 14, participants continued to take oral temperature twice daily until temperature <=37.2 degree Celsius or <=99 degree Fahrenheit for 24 hours. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

,,,
InterventionParticipants (Count of Participants)
At 0 hourAt 24 hoursAt 72 hoursAt 120 hoursAt 192 hoursAt 336 hoursAt 672 hours
Danirixin (DNX) 75 mg0124455
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg02810111111
Oseltamivir (OSV) 75 mg0123333
Placebo (PBO)0024666

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Number of Participants Who Used Relief Medication

Use of study supplied relief medications (paracetamol and dextromethorphan for symptom relief were recorded in the eDiary and accordingly number of participants using these medications were recorded. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

,,,
InterventionParticipants (Count of Participants)
Paracetamol useDextromethorphan use
Danirixin (DNX) 75 mg1212
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg1513
Oseltamivir (OSV) 75 mg77
Placebo (PBO)75

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Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)

AE is any untoward medical occurrence in a participant or clinical investigation 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. SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

,,,
InterventionParticipants (Count of Participants)
AESAE
Danirixin (DNX) 75 mg31
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg70
Oseltamivir (OSV) 75 mg00
Placebo (PBO)40

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Number of Participants With Maximum Post-baseline Urine Dipstick Abnormalities- Urine Glucose (Dipstick)

The dipstick test gives results in a semi-quantitative manner, and results for urinalysis parameter of urine glucose can be read as negative, Trace, 1+ or 1/4 gram per deciliter (G/dL), 2+ OR 1/2 G/dL, 3+ or 1 G/dL and 4+ indicating proportional concentrations in the urine sample. Assessments recorded on Day 1 were considered as Baseline. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

,,
InterventionParticipants (Count of Participants)
1+ OR 1/4 G/DL (%)2+ OR 1/2 G/DL (%)3+ OR 1 G/DL (%)4+
Danirixin (DNX) 75 mg0100
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg0010
Placebo (PBO)1000

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Number of Participants With Maximum Post-baseline Urine Dipstick Abnormalities- Urine Occult Blood (Dipstick)

The dipstick test gives results in a semi-quantitative manner, and results for urinalysis parameter of urine occult blood can be read as negative, Trace, 1+, 2+, 3+ and 4+, indicating proportional concentrations in the urine sample. Assessments recorded on Day 1 were considered as Baseline. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

,,
InterventionParticipants (Count of Participants)
1+2+3+4+
Danirixin (DNX) 75 mg2110
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg1102
Placebo (PBO)1100

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Number of Participants With Maximum Post-baseline Urine Dipstick Abnormalities- Urine Protein (Dipstick)

The dipstick test gives results in a semi-quantitative manner, and results for urinalysis parameter of urine protein can be read as negative, Trace, 1+, 2+, 3+ and 4+, indicating proportional concentrations in the urine sample. Assessments recorded on Day 1 were considered as Baseline. (NCT02469298)
Timeframe: Up to Day 28/withdrawal

,,,
InterventionParticipants (Count of Participants)
1+2+3+4+
Danirixin (DNX) 75 mg3000
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg3000
Oseltamivir (OSV) 75 mg1000
Placebo (PBO)0010

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Change From Baseline in Hematology Parameters- Mean Corpuscle Volume (MCV)

Hematology parameters included Mean corpuscle volume (MCV). Blood samples were collected on Day 1, Day 3, Day 5 and Day28/withdrawal. Assessments recorded on Day 1 were considered as Baseline. Change from Baseline was equal to Post-Dose Visit Value minus Baseline. (NCT02469298)
Timeframe: Baseline (Day 1) and up to Day 28/withdrawal

,,,
InterventionFemtoliters (FL) (Mean)
Day 3Day 5Day 8Day 28/withdrawal
Danirixin (DNX) 75 mg-0.9-0.7-0.6-0.4
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg-0.4-0.4-0.50.1
Oseltamivir (OSV) 75 mg-0.2-0.2-0.40.6
Placebo (PBO)-0.8-1.3-1.1-0.3

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Number of Participants With no Detectable Influenza Viral RNA by Quantitative Virus Culture From Nasopharyngeal Swabs on Baseline (Day 1), Day 3, Day 5, Day 8 and Day 14

Number of participants with no detectable influenza viral RNA by quantitative virus culture from nasopharyngeal swabs on Baseline (Day1), Day 3, Day 5, Day 8 and Day 14 were recorded. Assessments recorded on Day 1 were considered as Baseline. (NCT02469298)
Timeframe: Up to Day 14

,,,
InterventionParticipants (Count of Participants)
Day 1Day 3Day 5Day 8Day 14
Danirixin (DNX) 75 mg + Oseltamivir (OSV) 75 mg06101212
Danirixin (DNX) 75 Milligram (mg)15789
Oseltamivir (OSV) 75 mg23555
Placebo (PBO)02365

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Percentage of Participants With Influenza Complications

Percentage of participants with following Influenza Complications: bacterial pneumonia (culture confirmed where possible), bacterial superinfections, respiratory failure, pulmonary disease (example, asthma, chronic obstructive pulmonary disease [COPD]), cardiovascular and cerebrovascular disease (example, myocardial infarction, congestive heart failure [CHF], arrhythmia, stroke) and all complications were reported. (NCT02532283)
Timeframe: Up to 28 Days

,
InterventionPercentage of participants (Number)
All complicationsBacterial pneumoniaBacterial superinfectionsRespiratory failurePulmonary diseaseCardiovascular and Cerebrovascular disease
Pimodivir 600 mg Plus Oseltamivir 75 mg7.901.61.63.21.6
Placebo Plus Oseltamivir 75 mg15.603.106.30

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Percentage of Participants With Clinical Outcome Based on Ordinal Scale

The ordinal scale was used to assess participant's clinical outcome. It consists of 6 categories or clinical states that are exhaustive, mutually exclusive, and ordered, where 1- Death, 2- Admitted to intensive care unit (ICU) or mechanically ventilated/ extracorporeal membrane oxygenation (ECMO), 3- Non-ICU plus supplemental oxygen, 4- Non-ICU plus no supplemental oxygen, 5- Not hospitalized, but unable to continue activity, 6- Not hospitalized (NH) and continues activities. (NCT02532283)
Timeframe: Day 8

,
InterventionPercentage of Participants (Number)
Day 8: NH and Continues ActivitiesDay 8: NH, but Unable to Continue ActivityDay 8: Non-ICU+No Supplemental OxygenDay 8: Non-ICU+Supplemental OxygenDay 8: DeathDay 8: Missing
Pimodivir 600 mg Plus Oseltamivir 75 mg40.327.414.58.11.68.1
Placebo Plus Oseltamivir 75 mg29.045.26.53.2016.1

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Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Treatment-emergent Serious AEs (TESAEs)

An adverse event (AE) is any untoward medical occurrence in a clinical study participant administered a medicinal (investigational or non investigational) product. An AE does not necessarily have a causal relationship with treatment and therefore can be any unfavorable and unintended sign (including an abnormal finding), symptom, or disease temporally associated with use of a medicinal product, whether or not related to that medicinal product. TEAEs were defined as AEs that were reported or worsened on after start of study drug(s) dosing through safety follow-up visit. A serious adverse event (SAE) is any untoward medical occurrence that at any dose resulting in any of following outcomes: results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, is a suspected transmission of any infectious agent via a medicinal product. (NCT02532283)
Timeframe: Up to 28 Days

,
InterventionParticipants (Count of Participants)
TEAEsTESAEs
Pimodivir 600 mg Plus Oseltamivir 75 mg4811
Placebo Plus Oseltamivir 75 mg254

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Number of Participants With the Emergence of Drug Resistance Mutations With Oseltamivir (OST) and Pimodivir

Number of participants with emergence (from baseline) of drug resistance mutations detected by genotype or phenotype were reported. (NCT02532283)
Timeframe: Up to 28 Days

,
InterventionParticipants (Count of Participants)
Emergence of Pimodivir MutationEmergence of OST Mutation
Pimodivir 600 mg Plus Oseltamivir 75 mg00
Placebo Plus Oseltamivir 75 mg01

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Influenza Viral Load Over Time

Influenza viral load over time (Log 10 viral particles per milliliter [vp/mL]) was measured by qRT-PCR. Viral Load LOD = 2.18 log10 vp/mL. Results < LOQ and > LOD (target detected) are imputed with 2.12 log10 vp/mL and results NCT02532283)
Timeframe: Baseline, Days 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13 and 14

InterventionLog 10 vp/mL (Mean)
BaselineDay 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14
Pimodivir 600 mg Plus Oseltamivir 75 mg5.456.404.753.833.002.572.071.951.821.511.390.421.061.061.05

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Influenza Viral Load Over Time

Influenza viral load over time (Log 10 viral particles per milliliter [vp/mL]) was measured by qRT-PCR. Viral Load LOD = 2.18 log10 vp/mL. Results < LOQ and > LOD (target detected) are imputed with 2.12 log10 vp/mL and results NCT02532283)
Timeframe: Baseline, Days 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13 and 14

InterventionLog 10 vp/mL (Mean)
BaselineDay 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 14
Placebo Plus Oseltamivir 75 mg5.904.434.633.983.142.602.182.381.430.000.990.000.20

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Change From Baseline in Influenza Patient-Reported Outcome Questionnaire (FLU-PRO) Total Score

"FLU-PRO assesses 32 influenza symptoms in each of the following body areas (domains): Nose, Throat, Eyes, Chest/Respiratory, Gastrointestinal and Body/Systemic . Participants rate each symptom on a 5-point ordinal scale, with higher scores indicating a more frequent sign or symptom. For 27 of the items, the scale is as follows: 0 (Not at all), 1 (A little bit), 2 (Somewhat), 3 (Quite a bit), and 4 (Very much). For 5 items, severity is assessed in terms of numerical frequency, that is (i.e), vomiting or diarrhea (0 times, 1 time, 2 times, 3 times, or 4 or more times); with frequency of sneezing, coughing, and coughed up mucus or phlegm evaluated on a scale from 0 (Never) to 4 (Always).The FLU-PRO total score is computed as a mean score across all 32 items comprising the instrument. Total scores can range from 0 (symptom free) to 4 (very severe symptoms)." (NCT02532283)
Timeframe: Baseline, Days 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, and 33

InterventionUnits on a scale (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14Day 15Day 16Day 17Day 18Day 19Day 20Day 21Day 22Day 23Day 24Day 25Day 26Day 27Day 28Day 29Day 30Day 31Day 32Day 33
Pimodivir 600 mg Plus Oseltamivir 75 mg-0.08-0.48-0.60-0.71-0.76-0.85-0.87-0.89-0.93-0.91-0.87-0.87-0.93-0.85-0.88-0.84-0.98-1.06-1.06-1.03-1.00-1.02-1.11-0.87-0.94-0.86-1.02-0.60-1.13-0.61-0.75-0.61-0.94

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Change From Baseline in Influenza Patient-Reported Outcome Questionnaire (FLU-PRO) Total Score

"FLU-PRO assesses 32 influenza symptoms in each of the following body areas (domains): Nose, Throat, Eyes, Chest/Respiratory, Gastrointestinal and Body/Systemic . Participants rate each symptom on a 5-point ordinal scale, with higher scores indicating a more frequent sign or symptom. For 27 of the items, the scale is as follows: 0 (Not at all), 1 (A little bit), 2 (Somewhat), 3 (Quite a bit), and 4 (Very much). For 5 items, severity is assessed in terms of numerical frequency, that is (i.e), vomiting or diarrhea (0 times, 1 time, 2 times, 3 times, or 4 or more times); with frequency of sneezing, coughing, and coughed up mucus or phlegm evaluated on a scale from 0 (Never) to 4 (Always).The FLU-PRO total score is computed as a mean score across all 32 items comprising the instrument. Total scores can range from 0 (symptom free) to 4 (very severe symptoms)." (NCT02532283)
Timeframe: Baseline, Days 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, and 33

InterventionUnits on a scale (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14Day 15Day 16Day 17Day 18Day 19Day 20Day 21Day 22Day 23Day 24Day 25Day 26Day 27Day 28Day 29
Placebo Plus Oseltamivir 75 mg-0.11-0.33-0.52-0.56-0.67-0.75-0.69-0.80-0.84-0.81-0.76-0.89-0.94-0.92-0.90-0.90-0.97-1.00-1.05-1.03-0.98-0.92-0.96-0.91-0.85-0.87-0.74-0.82-1.63

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Time to Significant Reduction in FLU-PRO Influenza Symptom Severity

Time to significant reduction in influenza symptom severity (mild/none) is time from first dose of investigational drug until first of 2 successive recordings in which total score for each of 2 recordings is lower or equal to 1 and all domain scores is lower or equal to 1. FLU-PRO assesses 32 influenza symptoms in body areas (domains): Nose, throat, eyes, chest, gastrointestinal, body. Participants rate each symptom on 5-point scale, with higher scores indicates more frequent symptom. For 27 of items, scale is as follows: 0 (Not at all), 1 (A little bit), 2 (Somewhat), 3 (Quite a bit), 4 (Very much). For 5 items, severity is assessed in terms of numerical frequency, i.e, vomiting/diarrhea (0 times, 1 time, 2 times, 3 times, or 4 or more times); with frequency of sneezing, coughing and coughed up mucus or phlegm evaluated on scale from 0=Never to 4=Always. FLU-PRO total score is computed as mean score across all 32 items and ranges from 0 (symptom free) to 4 (very severe symptoms). (NCT02532283)
Timeframe: Up to Day 33

InterventionHours (Median)
Pimodivir 600 mg Plus Oseltamivir 75 mg118.45
Placebo Plus Oseltamivir 75 mg218.72

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Time to Return to Usual Health

Time to return to usual health was defined as the time in hours from the first dose of investigational product till the first one of 2 successive cases where the response is 'Yes' on FLU-PRO additional question 9 (Have you returned to your health today?). (NCT02532283)
Timeframe: Up to Day 33

InterventionHours (Median)
Pimodivir 600 mg Plus Oseltamivir 75 mg217.05
Placebo Plus Oseltamivir 75 mg338.83

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Time to Return to Premorbid Functional Status

Time to return to premorbid functional status (time to return usual activities) was defined as time in hours from the first dose of investigational product till the first one of 2 successive cases where the response is 'Yes' on FLU-PRO additional question 7 (Have you returned to your usual activities today?). (NCT02532283)
Timeframe: Up to Day 33

InterventionHours (Median)
Pimodivir 600 mg Plus Oseltamivir 75 mg142.85
Placebo Plus Oseltamivir 75 mg154.83

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Time to Influenza A Viral Negativity

Time to influenza A viral negativity was determined based on quantitative reverse transcription polymerase chain reaction (qRT-PCR). A participant was considered influenza A viral negative at the time point that the first negative nasal midturbinate (MT) swab was recorded (in days). Viral Load Limit of detection (LOD) = 2.18 log10 viral particles per milliliter (vp/mL). Results less than (<) limit of quantification (LOQ) and greater than (>) LOD (target detected) are imputed with 2.12 log10 vp/mL, results NCT02532283)
Timeframe: Up to 14 Days

InterventionDays (Median)
Pimodivir 600 mg Plus Oseltamivir 75 mg9.53
Placebo Plus Oseltamivir 75 mg9.74

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Time to Improvement of Vital Signs

Time to improvement of vital signs was defined as the time from first study treatment to when at least 4 of 5 symptoms (temperature, blood oxygen saturation, heart rate, systolic blood pressure, and respiration rate) had recovered, including normalization of temperature and blood oxygen saturation. Resolution criteria for vital signs: for Temperature: oral temperature less than or equal to (<=) 36.5 degree Celsius (C) for elderly and <=37.2 C for adults; for oxygen saturation: greater than or equal to (>=) 92 percent (%) on room air without supplemental oxygen; for respiratory rate: <= 24 per minutes; for heart rate: <= 100 per minutes and for systolic blood pressure: >= 90 millimeters of mercury (mmHg). (NCT02532283)
Timeframe: Up to 28 Days

InterventionHours (Median)
Pimodivir 600 mg Plus Oseltamivir 75 mg169.92
Placebo Plus Oseltamivir 75 mg69.90

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Time to Improvement of Respiratory Status

The time to improvement of respiratory status was defined as the time from first study treatment until the first assessment of a successive series of 3 recording where normalization of blood oxygen saturation and respiration rate occurred at respiration rate <=24 per minutes). (NCT02532283)
Timeframe: Up to 28 Days

InterventionHours (Median)
Pimodivir 600 mg Plus Oseltamivir 75 mg33.53
Placebo Plus Oseltamivir 75 mg40.57

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Time to Hospital Discharge

Time to hospital discharge was calculated from the date of first study drug intake during hospitalization up to date of discharge. (NCT02532283)
Timeframe: Up to 28 Days

InterventionDays (Median)
Pimodivir 600 mg Plus Oseltamivir 75 mg4.00
Placebo Plus Oseltamivir 75 mg4.00

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Rate of Decline in Viral Load

Rate of decline in viral load (Log10 viral particles per milliliter per day [log10 vp/mL/day]) during treatment was measured by qRT-PCR. Viral Load Limit of quantification (LOQ) = 2.18 log10 vp/mL, LOD = 2.05 log10 vp/mL. Results < LOQ and greater than > LOD (target detected) are imputed with 2.12 log10 vp/mL. Results NCT02532283)
Timeframe: Up to Day 7

InterventionLog10 vp/mL/day (Median)
Pimodivir 600 mg Plus Oseltamivir 75 mg-0.35
Placebo Plus Oseltamivir 75 mg-0.42

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Minimum Observed Plasma Concentration (Cmin) of Pimodivir

Cmin is the minimum observed plasma concentration. As per planned analysis, results are presented by age groups (65 to <= 85 years and 18 to <=64 years). (NCT02532283)
Timeframe: Pre-dose, 1, 2, 4, 6, 8, 10 and 12 hours post-dose on Day 3

Interventionng/mL (Mean)
Elderly Adults (65 to Less Than or Equal to [<=] 85 Years)738
Non-elderly Adults (18 to <=64 Years)507

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Maximum Observed Plasma Concentration (Cmax) of Pimodivir

Cmax is the maximum observed plasma concentration. As per planned analysis, results are presented by age groups (65 to less than or equal to [<=] 85 years and 18 to <=64 years). (NCT02532283)
Timeframe: Pre-dose, 1, 2, 4, 6, 8, 10 and 12 hours post-dose on Day 3

InterventionNanogram per milliliter (ng/mL) (Mean)
Elderly Adults (65 to Less Than or Equal to [<=] 85 Years)5933
Non-elderly Adults (18 to <=64 Years)5378

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Area Under the Plasma Concentration-time Curve From Time of Administration to 12 Hours After Dosing (AUC [0-12]) of Pimodivir

AUC (0-12) is the area under the plasma concentration-time curve from time zero to 12 hours after dosing of pimodivir. As per planned analysis, results are presented by age groups (65 to <= 85 years and 18 to <=64 years). (NCT02532283)
Timeframe: Pre-dose, 1, 2, 4, 6, 8, 10 and 12 hours post-dose on Day 3

Interventionnanogram hours per milliliter (ng*h/mL) (Mean)
Elderly Adults (65 to Less Than or Equal to [<=] 85 Years)27386
Non-elderly Adults (18 to <=64 Years)20101

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Percentage of Participants With Significant Reduction in FLU-PRO All Influenza Symptoms (Mild or None for All Symptoms)

Percentage of participants with significant reduction in influenza symptom severity was defined as time from first dose of investigational product until first of 2 successive recordings in which FLU-PRO total score for each of 2 recordings <= to 1 and all FLU-PRO domain scores is <=1. FLU-PRO assesses 32 influenza symptoms in body areas (domains): Nose, throat, eyes, chest, gastrointestinal, body. Participants rate each symptom on a 5-point ordinal scale, with higher scores indicates more frequent symptom. For 27 of items, scale is as follows: 0 (Not at all), 1 (A little bit), 2 (Somewhat), 3 (Quite a bit), 4 (Very much). For 5 items, severity is assessed as numerical frequency i.e, vomiting or diarrhea (0-4 or more times); with frequency of sneezing, coughing, coughed up mucus or phlegm evaluated on a scale from 0 (Never)-4 (Always). FLU-PRO total score is computed as a mean score across all 32 items comprising instrument and ranges from 0 (symptom free) to 4 (very severe symptoms). (NCT02532283)
Timeframe: Days 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32 and 33

InterventionPercentage of participants (Number)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14Day 15Day 16Day 17Day 18Day 19Day 20Day 21Day 22Day 23Day 24Day 25Day 26Day 27Day 28Day 29Day 30
Placebo Plus Oseltamivir 75 mg18.234.626.738.537.540.034.832.038.553.859.172.069.265.457.966.763.257.958.863.260.061.170.666.769.257.150.044.466.70

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Area Under the Plasma Concentration-time Curve (AUC) of Viral Load

Viral load AUC was determined by qRT-PCR assay of nasal swabs. Viral Load LOQ = 2.18 log10 vp/mL, LOD = 2.05 log10 vp/mL. Results LOD (target detected) are imputed with 2.12 log10 vp/mL. Results NCT02532283)
Timeframe: Baseline up to Day 8

InterventionDays*vp/mL (Mean)
Pimodivir 600 mg Plus Oseltamivir 75 mg22.8
Placebo Plus Oseltamivir 75 mg22.1

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Percentage of Participants With Significant Reduction in FLU-PRO All Influenza Symptoms (Mild or None for All Symptoms)

Percentage of participants with significant reduction in influenza symptom severity was defined as time from first dose of investigational product until first of 2 successive recordings in which FLU-PRO total score for each of 2 recordings <= to 1 and all FLU-PRO domain scores is <=1. FLU-PRO assesses 32 influenza symptoms in body areas (domains): Nose, throat, eyes, chest, gastrointestinal, body. Participants rate each symptom on a 5-point ordinal scale, with higher scores indicates more frequent symptom. For 27 of items, scale is as follows: 0 (Not at all), 1 (A little bit), 2 (Somewhat), 3 (Quite a bit), 4 (Very much). For 5 items, severity is assessed as numerical frequency i.e, vomiting or diarrhea (0-4 or more times); with frequency of sneezing, coughing, coughed up mucus or phlegm evaluated on a scale from 0 (Never)-4 (Always). FLU-PRO total score is computed as a mean score across all 32 items comprising instrument and ranges from 0 (symptom free) to 4 (very severe symptoms). (NCT02532283)
Timeframe: Days 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32 and 33

InterventionPercentage of participants (Number)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14Day 15Day 16Day 17Day 18Day 19Day 20Day 21Day 22Day 23Day 24Day 25Day 26Day 27Day 28Day 29Day 30Day 31Day 32Day 33
Pimodivir 600 mg Plus Oseltamivir 75 mg9.437.336.442.054.059.255.162.776.076.570.277.176.177.163.971.474.370.077.481.879.486.278.186.292.381.583.377.880.0100.0100.0100.0100

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

An adverse event (AE) is any untoward medical occurrence attributed to study drug in a participant who received study drug. Treatment-emergent events were between administration of study drug and Day 28 that were absent before treatment or that worsened relative to pre-treatment state. (NCT02603952)
Timeframe: Day 1 (post-dose) through Day 28

InterventionParticipants (Count of Participants)
Placebo + Oseltamivir 75 mg9
MEDI8852 750 mg + Oseltamivir 75 mg11
MEDI8852 3000 mg + Oseltamivir 75 mg15
MEDI8852 3000 mg12

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Quantitation of Influenza Viral Shedding as Measured by qRT-PCR

qRT-PCR was used to measure influenza viral shedding from the nasopharyngeal swabs. (NCT02603952)
Timeframe: Baseline (Day 1) and Days 3, 5, 7, 9, 11, and 13

,,
InterventionLog10 (viral copies/mL) (Mean)
Baseline (Day 1)Day 3Day 5Day 7Day 9Day 11
MEDI8852 3000 mg + Oseltamivir 75 mg6.924.893.432.972.802.80
MEDI8852 750 mg + Oseltamivir 75 mg6.624.753.313.133.762.80
Placebo + Oseltamivir 75 mg6.374.353.452.943.122.80

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Number of Participants With Treatment Emergent Adverse Events of Special Interest (TEAESIs)

An AE is any untoward medical occurrence attributed to study drug in a participant who received study drug. An AESI was one of scientific and medical interest specific to understanding of the study drug and may have required close monitoring and rapid communication by the investigator to the sponsor. Treatment-emergent events were between administration of study drug and Day 101 that were absent before treatment or that worsened relative to pre treatment state. (NCT02603952)
Timeframe: Day 1 (post-dose) through Day 101

InterventionParticipants (Count of Participants)
Placebo + Oseltamivir 75 mg0
MEDI8852 750 mg + Oseltamivir 75 mg0
MEDI8852 3000 mg + Oseltamivir 75 mg1
MEDI8852 3000 mg0

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Number of Participants With Viral Susceptibility to MEDI8852 as Determined by a Cell Based Microneutralization Assay

Viral susceptibility to MEDI8852 was measured by a Madin-Darby canine kidney (MDCK) cell-based microneutralization assay (Virospot) for viruses recovered from baseline samples and viruses recovered from samples following treatment that contain amino acid changes within the MEDI8852 binding site. Participants with detectable levels (50% tissue culture infectious dose [TCID50]) of virus were considered susceptible and were reported. Due to the fact that the number of participants with viral susceptibility to MEDI8852 binding site was zero across all participant samples analyzed, no additional per arm analyses were performed. (NCT02603952)
Timeframe: From Baseline (Day 1) to Day 13

InterventionParticipants (Count of Participants)
All MEDI8852 Participants0

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Percentage of Participants With Amino Acid Changes in MEDI8852 Binding Site

Genotypic analysis was performed to identify all amino acid changes in MEDI8852 binding site between each baseline (Day1) sample and the participant's corresponding last sample sequenced. Percentage of participants with changes in the amino acid corresponding to MEDI8852 binding site is reported. Due to the fact that the percentage of participants with amino acid changes in MEDI8852 binding site was zero across all participant samples analyzed, no additional per arm analyses were performed. (NCT02603952)
Timeframe: From Baseline (Day 1) to Day 13

InterventionPercentage of Participants (Number)
All MEDI8852 Participants0

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Percentage of Participants With Virus Containing Known Oseltamivir Resistance-Associated Mutations

Genotypic analysis was performed to identify all amino acid changes in neuraminidase (NA) gene between each baseline (Day1) sample and the participant's corresponding last sample sequenced. Percentage of participants with virus containing known oseltamivir resistance-associated mutations (change in the NA genes) is reported. Due to the fact that the percentage of participants with virus containing known oseltamivir resistance-associated mutation was zero across all participant samples analyzed, no additional per arm analyses were performed. (NCT02603952)
Timeframe: From Baseline (Day 1) to Day 13

InterventionPercentage of Participants (Number)
All Oseltamivir Participants0

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Number of Days of Influenza Viral Shedding as Measured by qRT-PCR

Number of days of viral shedding for participants who shed influenza virus is reported. qRT-PCR was used to measure influenza viral shedding from the nasopharyngeal swabs. (NCT02603952)
Timeframe: From Baseline (Day 1) to Day 7; and Day 9 to Day 13

,,,
InterventionDays (Mean)
Day 1 to Day 7Day 9 to Day 13
MEDI8852 3000 mg4.85.5
MEDI8852 3000 mg + Oseltamivir 75 mg4.96.0
MEDI8852 750 mg + Oseltamivir 75 mg5.86.3
Placebo + Oseltamivir 75 mg4.75.4

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Percentage of Participants With Influenza Viral Shedding as Measured by Quantitative Reverse Transcription-Polymerase Chain Reaction (qRT-PCR)

Quantitative real-time polymerase chain reaction (qRT-PCR) was used to measure influenza viral shedding from the nasopharyngeal swabs. Percentage of participants who shed influenza virus are reported. (NCT02603952)
Timeframe: Baseline (Day 1) and Days 3, 5, 7, 9, 11, and 13

,,,
InterventionPercentage of Participants (Number)
Baseline (Day 1)Day 3Day 5Day 7Day 9Day 11Day 13
MEDI8852 3000 mg10095.854.237.50.04.20.0
MEDI8852 3000 mg + Oseltamivir 75 mg10091.360.930.44.30.00.0
MEDI8852 750 mg + Oseltamivir 75 mg10088.985.259.37.40.00.0
Placebo + Oseltamivir 75 mg1009056.733.33.30.00.0

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Number of Participants With Treatment-Emergent Serious Adverse Events (TESAEs)

A serious adverse event (SAE) is an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent events were between administration of study drug and Day 101 that were absent before treatment or that worsened relative to pre-treatment state. (NCT02603952)
Timeframe: Day 1 (post-dose) through Day 101

InterventionParticipants (Count of Participants)
Placebo + Oseltamivir 75 mg1
MEDI8852 750 mg + Oseltamivir 75 mg0
MEDI8852 3000 mg + Oseltamivir 75 mg1
MEDI8852 3000 mg0

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Quantitation of Influenza Viral Shedding as Measured by qRT-PCR

qRT-PCR was used to measure influenza viral shedding from the nasopharyngeal swabs. (NCT02603952)
Timeframe: Baseline (Day 1) and Days 3, 5, 7, 9, 11, and 13

InterventionLog10 (viral copies/mL) (Mean)
Baseline (Day 1)Day 3Day 5Day 7Day 9Day 11Day 13
MEDI8852 3000 mg6.344.633.733.032.803.112.80

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Mean Symptom Severity Score During the 2015-2016 Influenza Season for Symptom Domains as Assessed Using the Influenza-Patient Reported Outcome (FLU-PRO™) Questionnaire

"Symptom evaluation during the 2015-2016 influenza season as recorded through FLU-PRO™: a daily diary developed to assess occurrence and severity of influenza symptoms.~Item responses:~Not at all~A little bit~Somewhat~Quite a bit~Very much" (NCT02609399)
Timeframe: ED Enrollment Visit through Day 14 ( 2015-2016 influenza season)

,
Interventionunits on a scale (Mean)
NoseThroatEyesChest/RespiratoryGastrointestinalBody/SystemicTotal/Overall
Oseltamivir1.41.31.21.91.51.71.6
Peramivir1.91.71.62.31.51.91.9

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Mean Karnofsky Performance Scale Score During the 2016-2017 Influenza Season

"The Karnofsky Performance Scale is a tool for assessing subject functional impairment.~Subjects provided or received (from a healthcare provider such as a doctor or nurse) a daily rating from 0 (Dead) to 100 (Normal - no complaints, no evidence of disease) from enrollment through Day 14 of the 2016-2017 influenza season." (NCT02609399)
Timeframe: ED Enrollment Visit through Day 14 ( 2016-2017 influenza season)

Interventionunits on a scale (Mean)
Experimental: Oseltamivir80.0
Experimental: Peramivir79.9

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Mean Karnofsky Performance Scale Score During the 2015-2016 Influenza Season

"The Karnofsky Performance Scale is a tool for assessing subject functional impairment.~Subjects provided or received (from a healthcare provider such as a doctor or nurse) a daily rating from 0 (Dead) to 100 (Normal - no complaints, no evidence of disease) from enrollment through Day 14 of the 2015-2016 influenza season." (NCT02609399)
Timeframe: ED Enrollment Visit through Day 14 ( 2015-2016 influenza season)

Interventionunits on a scale (Mean)
Experimental: Oseltamivir77.1
Experimental: Peramivir73.2

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Mean Symptom Severity Score During the 2016-2017 Influenza Season for Symptom Domains as Assessed Using the FLU-PRO™ Questionnaire

"Symptom evaluation during the 2016-2017 influenza season as recorded through FLU-PRO™: a daily diary developed to assess occurrence and severity of influenza symptoms.~Item responses:~Not at all~A little bit~Somewhat~Quite a bit~Very much" (NCT02609399)
Timeframe: ED Enrollment Visit through Day 14 ( 2016-2017 influenza season)

,
Interventionunits on a scale (Mean)
NoseThroatEyesChest/RespiratoryGastrointestinalBody/SystemicTotal/Overall
Oseltamivir1.51.31.31.71.31.51.4
Peramivir1.51.41.21.81.31.51.5

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Percentage of Oseltamivir Dose Excreted as Metabolite Oseltamivir Carboxylate in HD Participants

Urine samples up to 42 hours post-dose during the first dose analysis (Days 1 to 5) were used to calculate metabolite excretion, computed as [amount of metabolite excreted divided by the oral oseltamivir dose] multiplied by 100. The value was averaged among all participants and expressed as a percent of the oseltamivir dose administered. (NCT02617784)
Timeframe: Urine samples 0 to 42 hours from D1 dose

Interventionpercentage of osteltamivir dose (Mean)
Oseltamivir With HD1.86

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Percentage of Oseltamivir Dose Excreted as Unchanged Drug in HD Participants

Urine samples up to 42 hours post-dose during the first dose analysis (Days 1 to 5) were used to calculate drug excretion, computed as [amount of drug excreted divided by the oral oseltamivir dose] multiplied by 100. The value was averaged among all participants and expressed as a percent of the oseltamivir dose administered. (NCT02617784)
Timeframe: Urine samples 0 to 42 hours from D1 dose

Interventionpercentage of oseltamivir dose (Mean)
Oseltamivir With HD0.00982

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Percentage of Oseltamivir Dose Renally Excreted as Metabolite Oseltamivir Carboxylate in CAPD Participants

Urine samples up to 48 hours post-dose during the first dose analysis (Days 1 to 6) were used to calculate renal excretion, computed as [amount of metabolite in urine divided by the oral oseltamivir dose] multiplied by 100. The value was averaged among all participants and expressed as a percent of the oseltamivir dose administered. (NCT02617784)
Timeframe: Urine samples 0 to 48 hours from D1 dose

Interventionpercentage of oseltamivir dose (Mean)
Oseltamivir With CAPD6.44

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Percentage of Oseltamivir Dose Renally Excreted as Unchanged Drug in CAPD Participants

Urine samples up to 48 hours post-dose during the first dose analysis (Days 1 to 6) were used to calculate renal excretion, computed as [amount of drug in urine divided by the oral oseltamivir dose] multiplied by 100. The value was averaged among all participants and expressed as a percent of the oseltamivir dose administered. (NCT02617784)
Timeframe: Urine samples 0 to 48 hours from D1 dose

Interventionpercentage of oseltamivir dose (Mean)
Oseltamivir With CAPD0.0290

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Renal Clearance (CLr) of Oseltamivir in HD Participants

Plasma and urine samples up to 12 hours post-dose during the first dose analysis (Days 1 to 5) were used to calculate CLr, computed as [amount of drug excreted divided by the AUC12]. The CLr was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12 hours from D1 dose; urine samples 0 to 12 hours from D1 dose

InterventionL/h (Mean)
Oseltamivir With HD0.0521

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Area Under the Concentration-Time Curve (AUC) of Oseltamivir in HD Participants During Days 1 to 5

Plasma samples were obtained up to 90 hours post-dose during the first dose analysis (Days 1 to 5), and the AUC was determined from 0 to 12 hours (AUC12) and up to the last measurable concentration (AUClast). Values were averaged among all participants and expressed in nanograms by hours per milliliter (ng*h/mL). (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from D1 dose

Interventionng*h/mL (Mean)
AUC12AUClast
Oseltamivir With HD63.962.1

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AUC of Metabolite Oseltamivir Carboxylate in CAPD Participants During Days 1 to 6

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6), and the AUC was determined from 0 to 48 hours (AUC48) and up to the last measurable concentration (AUClast). Values were averaged among all participants and expressed in ng*h/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 dose

Interventionng*h/mL (Mean)
AUC48AUClast
Oseltamivir With CAPD3340056800

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AUC of Metabolite Oseltamivir Carboxylate in CAPD Participants During Days 36 to 43

Plasma samples were obtained up to 168 hours post-dose during the second dose analysis (Days 36 to 43), and the AUC48 and AUClast were determined. Values were averaged among all participants and expressed in ng*h/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120, 168 hours from D36 dose

Interventionng*h/mL (Mean)
AUC48AUClast
Oseltamivir With CAPD3240060800

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AUC of Metabolite Oseltamivir Carboxylate in HD Participants During Days 1 to 5

Plasma samples were obtained up to 90 hours post-dose during the first dose analysis (Days 1 to 5), and the AUC was determined from 0 to 42 hours (AUC42) and up to the last measurable concentration (AUClast). Values were averaged among all participants and expressed in ng*h/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from D1 dose

Interventionng*h/mL (Mean)
AUC42AUClast
Oseltamivir With HD3160044400

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AUC of Metabolite Oseltamivir Carboxylate in HD Participants During Days 38 to 43

Plasma samples were obtained up to 90 hours post-dose during the second dose analysis (Days 38 to 43), and the AUC42 and AUClast were determined. Values were averaged among all participants and expressed in ng*h/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from D38 dose

Interventionng*h/mL (Mean)
AUC42AUClast
Oseltamivir With HD3820060400

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AUC of Oseltamivir in CAPD Participants During Days 1 to 6

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6), and the AUC12 and AUClast were determined. Values were averaged among all participants and expressed in ng*h/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 dose

Interventionng*h/mL (Mean)
AUC12AUClast
Oseltamivir With CAPD85.678.5

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AUC of Oseltamivir in CAPD Participants During Days 36 to 43

Plasma samples were obtained up to 168 hours post-dose during the second dose analysis (Days 36 to 43), and the AUC12 and AUClast were determined. Values were averaged among all participants and expressed in ng*h/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120, 168 hours from D36 dose

Interventionng*h/mL (Mean)
AUC12AUClast
Oseltamivir With CAPD72.467.7

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AUC of Oseltamivir in HD Participants During Days 38 to 43

Plasma samples were obtained up to 90 hours post-dose during the second dose analysis (Days 38 to 43), and the AUC12 and AUClast were determined. Values were averaged among all participants and expressed in ng*h/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from D38 dose

Interventionng*h/mL (Mean)
AUC12AUClast
Oseltamivir With HD68.565.6

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CL/F of Metabolite Oseltamivir Carboxylate in CAPD Participants

Plasma samples up to 48 hours post-dose during the first (Days 1 to 6) and second (Days 36 to 43) dose analyses were used to calculate apparent clearance adjusted for oral bioavailability. The CL/F with each dose was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48 hours from D1 and D36 dose

InterventionL/h (Mean)
Days 1 to 6Days 36 to 43
Oseltamivir With CAPD0.8820.898

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CL/F of Metabolite Oseltamivir Carboxylate in HD Participants

Plasma samples up to 42 hours post-dose during the first (Days 1 to 5) and second (Days 38 to 43) dose analyses were used to calculate apparent clearance adjusted for oral bioavailability. The CL/F with each dose was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42 hours from D1 and D38 dose

InterventionL/h (Mean)
Days 1 to 5 (n=12)Days 38 to 43 (n=11)
Oseltamivir With HD1.200.779

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CL/F of Oseltamivir in CAPD Participants

Plasma samples up to 12 hours post-dose during the first (Days 1 to 6) and second (Days 36 to 43) dose analyses were used to calculate apparent clearance adjusted for oral bioavailability. The CL/F with each dose was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12 hours from D1 and D36 dose

InterventionL/h (Mean)
Days 1 to 6Days 36 to 43
Oseltamivir With CAPD424485

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Dialysis Clearance (CLd) of Metabolite Oseltamivir Carboxylate in HD Participants

Plasma samples up to 90 hours post-dose during the first (Days 1 to 5) and second (Days 38 to 43) dose analyses, in addition to dialyzer samples obtained on Days 3 and 40, were used to calculate CLd, computed as [amount of metabolite recovered in dialysate divided by the AUC over the dialysis interval]. The CLd with each dose was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from from D1 and D38 dose; dialyzer samples 1, 2, 4, 5 hours from start of dialysis on Days 3 and 40

InterventionL/h (Mean)
Days 1 to 5 (n=12)Days 38 to 43 (n=11)
Oseltamivir With HD7.428.43

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Elimination Rate Constant of Metabolite Oseltamivir Carboxylate in CAPD Participants

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6) and up to 168 hours post-dose during the second dose analysis (Days 36 to 43). Urine and dialysate samples were also obtained up to 48 hours post-dose during the first dose analysis. The elimination rate constant was calculated as [natural log (ln)(2) divided by the half-life] and expressed as inverse hours (1/h). (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 and D36 dose AND at 168 hours from D36 dose; urine samples 0 to 48 hours from D1 dose; dialysate samples 0 to 48 hours from D1 dose

Intervention1/h (Mean)
Days 1 to 6Days 36 to 43
Oseltamivir With CAPD0.02110.0200

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Oral Plasma Clearance (CL/F) of Oseltamivir in HD Participants

Plasma samples up to 12 hours post-dose during the first (Days 1 to 5) and second (Days 38 to 43) dose analyses were used to calculate apparent clearance adjusted for oral bioavailability. The CL/F with each dose was averaged among all participants and expressed in liters per hour (L/h). (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12 hours from D1 and D38 dose

InterventionL/h (Mean)
Days 1 to 5 (n=12)Days 38 to 43 (n=11)
Oseltamivir With HD677474

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Plasma Concentration of Metabolite Oseltamivir Carboxylate by Timepoint in CAPD Participants

Plasma samples were obtained up to 120 post-dose during the first dose analysis (Days 1 to 6) and up to 168 hours post-dose during the second dose analysis (Days 36 to 43). The concentration at each collection time was recorded and averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 and D36 dose AND at 168 hours from D36 dose

Interventionng/mL (Mean)
0 hours from D1 dose1 hour from D1 dose2 hours from D1 dose4 hours from D1 dose8 hours from D1 dose12 hours from D1 dose24 hours from D1 dose48 hours from D1 dose72 hours from D1 dose120 hours from D1 dose0 hours from D36 dose1 hour from D36 dose2 hours from D36 dose4 hours from D36 dose8 hours from D36 dose12 hours from D36 dose24 hours from D36 dose48 hours from D36 dose72 hours from D36 dose120 hours from D36 dose168 hours from D36 dose
Oseltamivir With CAPD0.020.312138169181287958036014769.297.018440366380283156336214963.0

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Plasma Concentration of Metabolite Oseltamivir Carboxylate by Timepoint in HD Participants

Plasma samples were obtained up to 90 hours post-dose during the first dose analysis (Days 1 to 5) and up to 114 hours post-dose during the second dose analysis (Days 38 to 43). The concentration at each collection time was recorded and averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49 hours from D1 and D38 dose AND at 90 hours from D1 dose AND at 114 hours from D38 dose

Interventionng/mL (Mean)
0 hours from D1 dose (n=12)1 hour from D1 dose (n=12)2 hours from D1 dose (n=12)4 hours from D1 dose (n=12)8 hours from D1 dose (n=12)12 hours from D1 dose (n=12)20 hours from D1 dose (n=12)32 hours from D1 dose (n=12)42 hours from D1 dose (n=12)48 hours from D1 dose (n=12)49 hours from D1 dose (n=12)90 hours from D1 dose (n=12)0 hours from D38 dose (n=11)1 hour from D38 dose (n=11)2 hours from D38 dose (n=11)4 hours from D38 dose (n=11)8 hours from D38 dose (n=11)12 hours from D38 dose (n=11)20 hours from D38 dose (n=11)32 hours from D38 dose (n=11)42 hours from D38 dose (n=11)48 hours from D38 dose (n=11)49 hours from D38 dose (n=11)114 hours from D38 dose (n=11)
Oseltamivir With HD0.90825.710727658977290892687721223324059.095.0200413745933109010801050263279283

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Plasma Concentration of Metabolite Oseltamivir Carboxylate in Arterial and Venous Blood by Timepoint in HD Participants

Dialyzer samples were obtained up to 5 hours from the start of dialysis on Days 3 and 40 (corresponding to HD sessions 2 and 18). Arterial concentrations were estimated using the inflow to the dialyzer, and venous concentrations were estimated using the outflow from the dialyzer. The concentration at each collection time was recorded and averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Dialyzer samples 1, 2, 4, 5 hours from start of dialysis on Days 3 and 40

Interventionng/mL (Mean)
Arterial: 1 hour (Day 3)Arterial: 2 hours (Day 3)Arterial: 4 hours (Day 3)Arterial: 5 hours (Day 3)Venous: 1 hour (Day 3)Venous: 2 hours (Day 3)Venous: 4 hours (Day 3)Venous: 5 hours (Day 3)Arterial: 1 hour (Day 40)Arterial: 2 hours (Day 40)Arterial: 4 hours (Day 40)Arterial: 5 hours (Day 40)Venous: 1 hour (Day 40)Venous: 2 hours (Day 40)Venous: 4 hours (Day 40)Venous: 5 hours (Day 40)
Oseltamivir With HD57041222717128420212784.366649628121831722912895.4

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Plasma Concentration of Oseltamivir by Timepoint in CAPD Participants

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6) and up to 168 hours post-dose during the second dose analysis (Days 36 to 43). The concentration at each collection time was recorded and averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 and D36 dose AND at 168 hours from D36 dose

Interventionng/mL (Mean)
0 hours from D1 dose1 hour from D1 dose2 hours from D1 dose4 hours from D1 dose8 hours from D1 dose12 hours from D1 dose24 hours from D1 dose48 hours from D1 dose72 hours from D1 dose120 hours from D1 dose0 hours from D36 dose1 hour from D36 dose2 hours from D36 dose4 hours from D36 dose8 hours from D36 dose12 hours from D36 dose24 hours from D36 dose48 hours from D36 dose72 hours from D36 dose120 hours from D36 dose168 hours from D36 dose
Oseltamivir With CAPD0.027.822.66.980.6300.1000.00.00.00.00.024.818.05.780.7540.1030.00.00.00.00.0

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Cmax of Metabolite Oseltamivir Carboxylate in HD Participants During Days 1 to 5

Plasma samples were obtained up to 90 hours post-dose during the first dose analysis (Days 1 to 5), and the maximum observed concentration was recorded. The Cmax was averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from D1 dose

Interventionng/mL (Mean)
Oseltamivir With HD943

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Plasma Concentration of Oseltamivir by Timepoint in HD Participants

Plasma samples were obtained up to 90 hours post-dose during the first dose analysis (Days 1 to 5) and up to 114 hours post-dose during the second dose analysis (Days 38 to 43). The concentration at each collection time was recorded and averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49 hours from D1 and D38 dose AND at 90 hours from D1 dose AND at 114 hours from D38 dose

Interventionng/mL (Mean)
0 hours from D1 dose (n=12)1 hour from D1 dose (n=12)2 hours from D1 dose (n=12)4 hours from D1 dose (n=12)8 hours from D1 dose (n=12)12 hours from D1 dose (n=12)20 hours from D1 dose (n=12)32 hours from D1 dose (n=12)42 hours from D1 dose (n=12)48 hours from D1 dose (n=12)49 hours from D1 dose (n=12)90 hours from D1 dose (n=12)0 hours from D38 dose (n=11)1 hour from D38 dose (n=11)2 hours from D38 dose (n=11)4 hours from D38 dose (n=11)8 hours from D38 dose (n=11)12 hours from D38 dose (n=11)20 hours from D38 dose (n=11)32 hours from D38 dose (n=11)42 hours from D38 dose (n=11)48 hours from D38 dose (n=11)49 hours from D38 dose (n=11)114 hours from D38 dose (n=11)
Oseltamivir With HD018.012.56.061.930.5130.1040.00.00.00.00.00.41321.515.46.071.300.1930.00.00.00.00.00.0

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Terminal Elimination Half-Life of Metabolite Oseltamivir Carboxylate in CAPD Participants

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6) and up to 168 hours post-dose during the second dose analysis (Days 36 to 43). Urine and dialysate samples were also obtained up to 48 hours post-dose during the first dose analysis. The time required for the concentration to decrease by one-half was recorded and averaged among all participants and expressed in hours. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 and D36 dose AND at 168 hours from D36 dose; urine samples 0 to 48 hours from D1 dose; dialysate samples 0 to 48 hours from D1 dose

Interventionhours (Mean)
Days 1 to 6Days 36 to 43
Oseltamivir With CAPD34.836.3

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Tmax of Metabolite Oseltamivir Carboxylate in CAPD Participants

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6) and up to 168 hours post-dose during the second dose analysis (Days 36 to 43), and the observed time of maximum concentration was recorded. The Tmax following each dose was averaged among all participants and expressed in hours. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 and D36 dose AND at 168 hours from D36 dose

Interventionhours (Mean)
Days 1 to 6Days 36 to 43
Oseltamivir With CAPD20.019.0

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Tmax of Metabolite Oseltamivir Carboxylate in HD Participants

Plasma samples were obtained up to 90 hours post-dose during the first (Days 1 to 5) and second (Days 38 to 43) dose analyses, and the observed time of maximum concentration was recorded. The Tmax following each dose was averaged among all participants and expressed in hours. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from D1 and D38 dose

Interventionhours (Mean)
Days 1 to 5 (n=12)Days 38 to 43 (n=11)
Oseltamivir With HD29.729.2

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Tmax of Oseltamivir in CAPD Participants

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6) and up to 168 hours post-dose during the second dose analysis (Days 36 to 43), and the observed time of maximum concentration was recorded. The Tmax following each dose was averaged among all participants and expressed in hours. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 and D36 dose AND at 168 hours from D36 dose

Interventionhours (Mean)
Days 1 to 6Days 36 to 43
Oseltamivir With CAPD1.501.28

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Time to Maximum Plasma Concentration (Tmax) of Oseltamivir in HD Participants

Plasma samples were obtained up to 90 hours post-dose during the first (Days 1 to 5) and second (Days 38 to 43) dose analyses, and the observed time of maximum concentration was recorded. The Tmax following each dose was averaged among all participants and expressed in hours. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from D1 and D38 dose

Interventionhours (Mean)
Days 1 to 5 (n=12)Days 38 to 43 (n=11)
Oseltamivir With HD1.751.18

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CLd of Metabolite Oseltamivir Carboxylate in CAPD Participants

Plasma samples up to 120 hours and dialysate samples up to 48 hours post-dose during the first dose analysis (Days 1 to 6) were used to calculate CLd, computed as [amount of metabolite recovered in dialysate divided by the AUC over the dialysis interval]. The CLd was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 dose; dialysate samples 0 to 48 hours from D1 dose

InterventionL/h (Mean)
Oseltamivir With CAPD0.425

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CLr of Metabolite Oseltamivir Carboxylate in CAPD Participants

Plasma and urine samples up to 48 hours post-dose during the first dose analysis (Days 1 to 6) were used to calculate CLr, computed as [amount of metabolite excreted divided by the AUC48]. The CLr was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48 hours from D1 dose; urine samples 0 to 48 hours from D1 dose

InterventionL/h (Mean)
Oseltamivir With CAPD0.0665

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CLr of Metabolite Oseltamivir Carboxylate in HD Participants

Plasma and urine samples up to 42 hours post-dose during the first dose analysis (Days 1 to 5) were used to calculate CLr, computed as [amount of metabolite excreted divided by the AUC42]. The CLr was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42 hours from D1 dose; urine samples 0 to 42 hours from D1 dose

InterventionL/h (Mean)
Oseltamivir With HD0.0203

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CLr of Oseltamivir in CAPD Participants

Plasma and urine samples up to 12 hours post-dose during the first dose analysis (Days 1 to 6) were used to calculate CLr, computed as [amount of drug excreted divided by the AUC12]. The CLr was averaged among all participants and expressed in L/h. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12 hours from D1 dose; urine samples 0 to 12 hours from D1 dose

InterventionL/h (Mean)
Oseltamivir With CAPD0.146

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Cmax of Metabolite Oseltamivir Carboxylate in CAPD Participants During Days 1 to 6

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6), and the maximum observed concentration was recorded. The Cmax was averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 dose

Interventionng/mL (Mean)
Oseltamivir With CAPD885

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Cmax of Metabolite Oseltamivir Carboxylate in CAPD Participants During Days 36 to 43

Plasma samples were obtained up to 168 hours post-dose during the second dose analysis (Days 36 to 43), and the maximum observed concentration was recorded. The Cmax was averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120, 168 hours from D36 dose

Interventionng/mL (Mean)
Oseltamivir With CAPD849

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Cmax of Metabolite Oseltamivir Carboxylate in HD Participants During Days 38 to 43

Plasma samples were obtained up to 90 hours post-dose during the second dose analysis (Days 38 to 43), and the maximum observed concentration was recorded. The Cmax was averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from D38 dose

Interventionng/mL (Mean)
Oseltamivir With HD1120

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Cmax of Oseltamivir in CAPD Participants During Days 1 to 6

Plasma samples were obtained up to 120 hours post-dose during the first dose analysis (Days 1 to 6), and the maximum observed concentration was recorded. The Cmax was averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120 hours from D1 dose

Interventionng/mL (Mean)
Oseltamivir With CAPD32.0

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Cmax of Oseltamivir in CAPD Participants During Days 36 to 43

Plasma samples were obtained up to 168 hours post-dose during the second dose analysis (Days 36 to 43), and the maximum observed concentration was recorded. The Cmax was averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 24, 48, 72, 120, 168 hours from Day 36 (D36) dose

Interventionng/mL (Mean)
Oseltamivir With CAPD27.7

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Cmax of Oseltamivir in HD Participants During Days 38 to 43

Plasma samples were obtained up to 90 hours post-dose during the second dose analysis (Days 38 to 43), and the maximum observed concentration was recorded. The Cmax was averaged among all participants and expressed in ng/mL. (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from Day 38 (D38) dose

Interventionng/mL (Mean)
Oseltamivir With HD22.6

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Maximum Plasma Concentration (Cmax) of Oseltamivir in HD Participants During Days 1 to 5

Plasma samples were obtained up to 90 hours post-dose during the first dose analysis (Days 1 to 5), and the maximum observed concentration was recorded. The Cmax was averaged among all participants and expressed in nanograms per milliliter (ng/mL). (NCT02617784)
Timeframe: Blood samples 0, 1, 2, 4, 8, 12, 20, 32, 42, 48, 49, 90 hours from Day 1 (D1) dose

Interventionng/mL (Mean)
Oseltamivir With HD20.2

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Percentage of Oseltamivir Dose Eliminated by Dialysis as Metabolite Oseltamivir Carboxylate in CAPD Participants

Dialysate samples up to 48 hours post-dose during the first dose analysis (Days 1 to 6) were used to calculate dialysis elimination, computed as [amount of metabolite in dialysate divided by the oral oseltamivir dose] multiplied by 100. The value was averaged among all participants and expressed as a percent of the oseltamivir dose administered. (NCT02617784)
Timeframe: Dialysate samples 0 to 48 hours from D1 dose

Interventionpercentage of oseltamivir dose (Mean)
Oseltamivir With CAPD32.6

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Percentage of Oseltamivir Dose Eliminated by Dialysis as Unchanged Drug in CAPD Participants

Dialysate samples up to 48 hours post-dose during the first dose analysis (Days 1 to 6) were used to calculate dialysis elimination, computed as [amount of drug in dialysate divided by the oral oseltamivir dose] multiplied by 100. The value was averaged among all participants and expressed as a percent of the oseltamivir dose administered. (NCT02617784)
Timeframe: Dialysate samples 0 to 48 hours from D1 dose

Interventionpercentage of oseltamivir dose (Mean)
Oseltamivir With CAPD0.00367

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Volume of Distribution (Vd) of Oseltamivir and RO0640802

Vd is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 1 and Day 5

,
InterventionLiter (Mean)
Day 1: OseltamivirDay 1: RO0640802Day 5: OseltamivirDay 5: RO0640802
Oseltamivir 100 mg171250189266
Oseltamivir 200 mg183251192280

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Area Under the Plasma Concentration-Time Curve From Time 0 to Last Measurable Concentration (AUC0-last) of Oseltamivir and RO0640802

AUC is a measure of the plasma concentration of the drug over time. RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 1 and Day 5

,
Interventionng*hour/mL (Mean)
Day 1: OseltamivirDay 1: RO0640802Day 5: OseltamivirDay 5: RO0640802
Oseltamivir 100 mg60922735804127
Oseltamivir 200 mg1136456611427932

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Clearance (CL) of Oseltamivir and RO0640802

CL is a quantitative measure of the rate at which a drug substance is removed from the body. RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 1 and Day 5

,
InterventionLiters/hour (Mean)
Day 1: OseltamivirDay 1: RO0640802Day 5: OseltamivirDay 5: RO0640802
Oseltamivir 100 mg28926.019221.7
Oseltamivir 200 mg39325.417922.6

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Cmax of Oseltamivir and RO0640802

Cmax is the maximum observed plasma concentration. RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 1

,
Interventionng/mL (Mean)
OseltamivirRO0640802
Oseltamivir 100 mg284301
Oseltamivir 200 mg503577

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Half-Life (t1/2) of Oseltamivir and RO0640802

t1/2 is the time measured for the plasma concentration to decrease by one half. RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 1 and Day 5

,
Interventionhour (Mean)
Day 1: OseltamivirDay 1: RO0640802Day 5: OseltamivirDay 5: RO0640802
Oseltamivir 100 mg1.226.891.407.97
Oseltamivir 200 mg1.537.171.888.17

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Time to Reach Maximum Plasma Concentration (Tmax) of Oseltamivir and RO0640802

Tmax is time of observed maximum plasma concentration. RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 1 and Day 5

,
Interventionhour (Mean)
Day 1: OseltamivirDay 1: RO0640802Day 5: OseltamivirDay 5: RO0640802
Oseltamivir 100 mg1.853.901.643.69
Oseltamivir 200 mg1.653.951.813.41

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Minimum Plasma Concentration (Cmin) of RO0640802

Collection of the 12-hour post-dose sample took place prior to administration of the second daily dose of drug. RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: 12-hour post dose on Day 1, 5 and predose on Day 2, 3, 4, 5

,
Interventionng/mL (Mean)
Day 1 (12-hour post dose)Day 2 (Pre dose)Day 3 (Pre dose)Day 4 (Pre dose)Day 5 (Pre dose)Day 5 (12-hour post dose)
Oseltamivir 100 mg131209235277262238
Oseltamivir 200 mg264388450443502458

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Area Under the Plasma Concentration-Time Curve From Time 0 to 12 Hour (AUC0-12h) of Oseltamivir and RO0640802 at Steady State

AUC is a measure of the plasma concentration of the drug over time. AUC is presented in nanogram times (*) hour per milliliter (ng*hour/mL). RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 5

,
Interventionng*hour/mL (Mean)
OseltamivirRO0640802
Oseltamivir 100 mg5814147
Oseltamivir 200 mg11437966

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Maximum Plasma Concentration (Cmax) of Oseltamivir and RO0640802 at Steady State

Cmax is the maximum observed plasma concentration, presented in nanogram per milliliter (ng/mL). RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 5

,
Interventionng/mL (Mean)
OseltamivirRO0640802
Oseltamivir 100 mg266488
Oseltamivir 200 mg496960

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Area Under the Plasma Concentration-Time Curve From Time 0 to Infinity (AUC0-inf) of Oseltamivir and RO0640802

AUC is a measure of the plasma concentration of the drug over time. RO0640802 is the pharmacologically active carboxylate metabolite of oseltamivir. (NCT02717754)
Timeframe: Predose (0 hour), 1, 2, 3, 3.5, 4, 5, 6, 8, 10, 12 hours post dose on Day 1

,
Interventionng*hour/mL (Mean)
OseltamivirRO0640802
Oseltamivir 100 mg6123606
Oseltamivir 200 mg11397336

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Oral Plasma Clearance (CL/F) for Oseltamivir

(NCT02780622)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 12 hours post-dose on Day 1 and 5; 18 and 24 hours post-dose on Day 5

Interventionliters per hour (L/h) (Mean)
Oseltamivir (Single Dose: Day 1)Oseltamivir (Steady State: Day 5)
Warfarin and Oseltamivir558463

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Percentage of Participants With Adverse Events

An adverse event was defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. (NCT02780622)
Timeframe: Up to Day 26

Interventionpercentage of participants (Number)
Warfarin25.0
Warfarin and Oseltamivir25.0

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Change From Baseline in Plasma Concentration of Vitamin K1

Vitamin K1 is required by proteins involved in blood clotting. Food interaction with warfarin can lead to decreases in Vitamin K1 in plasma. An increase in vitamin K1 signifies enhancement of warfarin's anticoagulant effect. (NCT02780622)
Timeframe: Pre-dose on Day 1 and 24 hours post-dose on Day 5

Interventionnanogram per liter (ng/L) (Mean)
Warfarin305
Warfarin and Oseltamivir271

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Change From Baseline in Maximum Observed Effect (Emax) of International Normalized Ratio (INR)

INR is calculated based on results of a prothrombin time (PT) test (which measures how long it takes blood to clot) and is used to monitor individuals who are being treated with the blood-thinning medication (anticoagulant) warfarin. An increase in INR signifies enhancement of warfarin's anticoagulant effect. (NCT02780622)
Timeframe: Pre-dose on Day 1, 24 hours (Day 2), 48 hours (Day 3), 72 hours (Day 4), and 96 hours (Day 5)

Interventionratio (Mean)
Warfarin0.3
Warfarin and Oseltamivir0.1

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Change From Baseline in Maximum Observed Effect (Emax) in Factor VII Activity

Factor VIIa is a protein that causes blood to clot. A decrease in factor VIIa activity signifies enhancement of warfarin's anticoagulant effect. kIU/L = 1000 * international units per liter. (NCT02780622)
Timeframe: Pre-dose on Day 1, 24 hours (Day 2), 48 hours (Day 3), 72 hours (Day 4), and 96 hours (Day 5)

InterventionkIU/L (Mean)
Warfarin-0.0505
Warfarin and Oseltamivir-0.0432

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Terminal Half-life (t½) for R- and S- Warfarin

(NCT02780622)
Timeframe: Pre-dose; 1, 2, 4, 8, 12, 24 hours post-dose on Day 5

,
Interventionhours (Mean)
Total (S)-warfarin (n = 13, 11)Total (R)-warfarin (n = 12, 12)
Warfarin45.456.1
Warfarin and Oseltamivir45.653.6

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Area Under the Plasma Effect-time Curve Over 96 Hours (AUEC[0-96 h]) for International Normalized Ratio (INR)

INR is calculated based on results of a prothrombin time (PT) test (which measures how long it takes blood to clot) and is used to monitor individuals who are being treated with the blood-thinning medication (anticoagulant) warfarin. The net AUEC(0-96 h) was calculated using the linear trapezoidal rule; this was the area under the effect-time curve and above the baseline minus the area above the curve and below the baseline during the 5-day period. An increase in INR signifies enhancement of warfarin's anticoagulant effect. (NCT02780622)
Timeframe: Pre-dose on Day 1, 24 hours (Day 2), 48 hours (Day 3), 72 hours (Day 4), and 96 hours (Day 5)

Interventionhours*ratio (Mean)
Warfarin-2.16
Warfarin and Oseltamivir-9.06

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Area Under the Plasma Effect-time Curve Over 96 Hours (AUEC[0-96 h]) for Factor VII Activity

Factor VIIa is a protein that causes blood to clot, and low levels in the blood can cause excessive or prolonged bleeding after an injury or surgery. The net AUEC(0-96 h) was calculated using the linear trapezoidal rule; this was the area under the effect-time curve and above the baseline minus the area above the curve and below the baseline during the 5-day period. A decrease in factor VIIa activity signifies enhancement of warfarin's anticoagulant effect. kIU/L = 1000 * international units per liter. (NCT02780622)
Timeframe: Pre-dose on Day 1, 24 hours (Day 2), 48 hours (Day 3), 72 hours (Day 4), and 96 hours (Day 5)

Interventionhours*kIU/L (Mean)
Warfarin0.568
Warfarin and Oseltamivir1.45

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Time to Reach Maximum Change From Baseline in Factor VII Activity (Tmax)

Factor VIIa is a protein that causes blood to clot. A decrease in factor VIIa activity signifies enhancement of warfarin's anticoagulant effect. (NCT02780622)
Timeframe: Pre-dose on Day 1, 24 hours (Day 2), 48 hours (Day 3), 72 hours (Day 4), and 96 hours (Day 5)

Interventionhours (Median)
Warfarin96.00
Warfarin and Oseltamivir72.00

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Time to Reach Maximum Change From Baseline in International Normalized Ratio (INR) (Tmax)

INR is calculated based on results of a prothrombin time (PT) test (which measures how long it takes blood to clot) and is used to monitor individuals who are being treated with the blood-thinning medication (anticoagulant) warfarin. An increase in INR signifies enhancement of warfarin's anticoagulant effect. (NCT02780622)
Timeframe: Pre-dose on Day 1, 24 hours (Day 2), 48 hours (Day 3), 72 hours (Day 4), and 96 hours (Day 5)

Interventionhours (Median)
Warfarin24.00
Warfarin and Oseltamivir0.00

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Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to 12 Hours (AUC0-12h) for Oseltamivir and Oseltamivir Carboxylate

(NCT02780622)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 12 hours post-dose on Day 1 and 5; 18 and 24 hours post-dose on Day 5

Interventionh*ng/mL (Mean)
Oseltamivir (Single Dose: Day 1)Oseltamivir Carboxylate (Single Dose: Day 1)Oseltamivir (Steady State: Day 5)Oseltamivir Carboxylate (Steady State: Day 5)
Warfarin and Oseltamivir14129901695110

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Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to 12 Hours (AUC0-12h) for R- and S- Warfarin

R- and S-warfarin are two molecular versions of warfarin with slightly different structures. The reported concentrations were normalized by dividing the AUC values (hours multiplied by nanograms, per milliliter) by the individual average dose (milligrams). (NCT02780622)
Timeframe: Pre-dose; 1, 2, 4, 8, 12, 24 hours post-dose on Day 5

,
Interventionh*ng/mL/mg (Mean)
Total (S)-warfarinFree (S)-warfarinTotal (R)-warfarinFree (R)-warfarin
Warfarin361018.6414025.9
Warfarin and Oseltamivir338017.8387024.8

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Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to 24 Hours (AUC0-24h) for Oseltamivir and Oseltamivir Carboxylate

(NCT02780622)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 18 and 24 hours post-dose on Day 5

Interventionh*ng/mL (Mean)
Oseltamivir (Steady state: Day 5)Oseltamivir Carboxylate (Steady State: Day 5)
Warfarin and Oseltamivir1767180

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Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to 24 Hours (AUC0-24h) for R- and S- Warfarin

R- and S-warfarin are two molecular versions of warfarin with slightly different structures. The reported concentrations were normalized by dividing the AUC values (hours multiplied by nanograms, per milliliter) by the individual average dose (milligrams). (NCT02780622)
Timeframe: Pre-dose; 1, 2, 4, 8, 12, 24 hours post-dose on Day 5

,
Interventionh*ng/mL/mg (Mean)
Total (S)-warfarinFree (S)-warfarinTotal (R)-warfarinFree (R)-warfarin
Warfarin677035.2779049.4
Warfarin and Oseltamivir646033.9736048.3

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Maximum Plasma Concentration (Cmax) for Oseltamivir and Oseltamivir Carboxylate

(NCT02780622)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 12 hours post-dose on Day 1 and 5; 18 and 24 hours post-dose on Day 5

Interventionnanogram per milliliter (ng/mL) (Mean)
Oseltamivir (Single Dose: Day 1)Oseltamivir Carboxylate (Single Dose: Day 1)Oseltamivir (Steady State: Day 5)Oseltamivir Carboxylate (Steady State: Day 5)
Warfarin and Oseltamivir88.936791.2571

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Maximum Plasma Concentration (Cmax) for R- and S- Warfarin

R- and S-warfarin are two molecular versions of warfarin with slightly different structures. The reported concentrations were normalized by dividing the Cmax values (nanograms per milliliter) by the individual average dose (milligrams). (NCT02780622)
Timeframe: Pre-dose; 1, 2, 4, 8, 12, 24 hours post-dose on Day 5

,
InterventionNanogram/milliliter/milligram (ng/mL/mg) (Mean)
Total (S)-warfarinFree (S)-warfarinTotal (R)-warfarinFree (R)-warfarin
Warfarin3941.874362.70
Warfarin and Oseltamivir3301.683752.37

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Oral Plasma Clearance (CL/F) for R- and S- Warfarin

(NCT02780622)
Timeframe: Pre-dose; 1, 2, 4, 8, 12, 24 hours post-dose on Day 5

,
Interventionliters per hour (L/h) (Mean)
Total (S)-warfarinFree (S)-warfarinTotal (R)-warfarinFree (R)-warfarin
Warfarin0.19838.50.13921.7
Warfarin and Oseltamivir0.20838.20.14522

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Terminal Half-life (t½) for Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is an active metabolite of oseltamivir. (NCT02780622)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 12 hours post-dose on Day 1 and 5; 18 and 24 hours post-dose on Day 5

Interventionhours (Mean)
Oseltamivir (Single Dose: Day 1)Oseltamivir Carboxylate (Single Dose: Day 1)Oseltamivir (Steady State: Day 5)Oseltamivir Carboxylate (Steady State: Day 5)
Warfarin and Oseltamivir1.776.174.008.19

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Time to Maximum Plasma Concentration (Tmax) for Oseltamivir and Oseltamivir Carboxylate

Oseltamivir carboxylate is an active metabolite of oseltamivir. (NCT02780622)
Timeframe: Pre-dose; 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 12 hours post-dose on Day 1 and 5; 18 and 24 hours post-dose on Day 5

Interventionhours (Median)
Oseltamivir (Single Dose: Day 1)Oseltamivir Carboxylate (Single Dose: Day 1)Oseltamivir (Steady State: Day 5)Oseltamivir Carboxylate (Steady State: Day 5)
Warfarin and Oseltamivir0.504.000.754.00

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Time to Maximum Plasma Concentration (Tmax) for R- and S- Warfarin

(NCT02780622)
Timeframe: Pre-dose; 1, 2, 4, 8, 12, 24 hours post-dose on Day 5

,
Interventionhours (Median)
Total (S)-warfarinFree (S)-warfarinTotal (R)-warfarinFree (R)-warfarin
Warfarin2.0014.53.004.00
Warfarin and Oseltamivir4.003.014.003.00

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Time to Respiratory Response (TTRR)

Time to Respiratory Response was defined as meeting at least one of the following criteria, and maintained for 24 hours: return to pre-morbid oxygen requirement (participants with chronic oxygen use or ventilator support), or return to no requirement of supplemental oxygen, or respiratory rate <=24 per minute (without supplemental oxygen). Kaplan Meier estimates for the median of TTRR for each treatment group was provided. NA indicates data is not available. Due to limited data, no TTRR estimate could be calculated for any of the treatment groups. (NCT02927431)
Timeframe: Up to 45 Days

InterventionDays (Median)
Placebo + OSVNA
DNX 15 mg + OSVNA
DNX 50 mg + OSVNA

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Time to Clinical Response (TTCR)

The clinical response was defined as Hospital discharge due to clinical improvement OR normalization of temperature; and oxygen saturation; and respiratory status/heart rate/systolic blood pressure (normalization of 2 out of these 3 parameters). The clinical response based on vital signs/ventilation status required 24-hour confirmation. Considering 2-hour assessment window, the response confirmation period was 22 hours. Kaplan Meier estimates for the median of TTCR was provided. One participant had vital sign resolution at Baseline and was counted as having a clinical response but was not included in the Kaplan Meier Estimates. Influenza Positive Population (IPP) Population comprised of all participants in the Intent to Treat Exposed (ITT-E) Population with influenza infection (positive influenza Polymerase Chain Reaction [PCR] or culture at any time point) confirmed by central lab testing. Only those participants with data available at the indicated time point were analyzed. (NCT02927431)
Timeframe: Up to 45 Days

InterventionDays (Median)
Placebo + OSV1.33
DNX 15 mg + OSV4.53
DNX 50 mg + OSV4.76

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Percentage of Participants With Improved Respiratory Status Over Time

The Respiratory Response was defined as meeting at least one of the following criteria, and maintained for 24 hours: return to pre-morbid oxygen requirement (participants with chronic oxygen use or ventilator support), or return to no requirement of supplemental oxygen, or respiratory rate <=24 per minute (without supplemental oxygen). Percentage of participants with improved respiratory status has been presented. (NCT02927431)
Timeframe: Up to 45 Days

InterventionPercentage of Participants (Number)
Placebo + OSV50
DNX 15 mg + OSV50
DNX 50 mg + OSV50

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Percentage of Participants With Clinical Response Over Time

The clinical response was defined as Hospital discharge due to clinical improvement OR normalization of temperature; and oxygen saturation; and respiratory status/heart rate/systolic blood pressure (normalization of 2 out of these 3 parameters). The clinical response based on vital signs/ventilation status required 24-hour confirmation. Considering 2-hour assessment window, the response confirmation period was 22 hours. Percentage of participants with positive clinical response are presented. (NCT02927431)
Timeframe: Up to 45 Days

InterventionPercentage of Participants (Number)
Placebo + OSV100
DNX 15 mg + OSV100
DNX 50 mg + OSV100

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Number of Participants Used Antibiotics for Complications of Influenza

Complications of influenza such as bacterial pneumonia, pneumothorax, pleural effusion, acute respiratory distress syndrome (ARDS), myositis, encephalitis, myocarditis, and associated antibiotic use was recorded. Number of participants who reqruied use of associated antibiotics for complications of influenza is presented. (NCT02927431)
Timeframe: Up to 45 Days

InterventionParticipants (Count of Participants)
Placebo + OSV1
DNX 15 mg + OSV1
DNX 50 mg + OSV1

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Change From Baseline in White Blood Cell Count (WBC) and Absolute Neutrophil Count (ANC)

Blood samples were collected to evaluate WBC and ANC at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionGiga cells per Liter (GI/L) (Mean)
WBC, Day 2, n=1,0,0WBC, Day 3, n=1,1,0WBC, Day 5, n=1,1,1WBC, Day 6, n=1,0,0WBC, Day 7, n=1,0,0WBC, Day 8, n=1,0,0WBC, Discharge/Day 45, n=2,3,1WBC, Day 3 post last dose, n=1,4,1ANC, Day 2, n=1,0,0ANC, Day 3, n=1,1,0ANC, Day 5, n=1,1,1ANC, Day 6, n=1,0,0ANC, Day 7, n=1,0,0ANC, Day 8, n=1,0,0ANC, Discharge/Day 45, n=2,3,1ANC, Day 3 post last dose, n=1,4,1
Placebo + OSV-2.70-5.10-2.90-2.40-2.90-3.10-3.55-4.60-3.880-5.640-4.250-3.540-4.180-4.580-4.650-5.680

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Number of Participants With Any Non-serious Adverse Event (AE); Any Serious AE (SAE); Any AEs of Special Interest (AESIs)

An AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention or event associated with liver injury and impaired liver function were categorized as SAE. Participants who received any of the study treatment and had any AE or SAE or AESI were considered for analysis. Safety Population comprised of all participants who received at least 1 dose of study treatment. (NCT02927431)
Timeframe: Up to 45 Days

,,
InterventionParticipants (Count of Participants)
Any non-SAEAny SAEAny AESI
DNX 15 mg + OSV401
DNX 50 mg + OSV421
Placebo + OSV000

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Change From Baseline in White Blood Cell Count (WBC) and Absolute Neutrophil Count (ANC)

Blood samples were collected to evaluate WBC and ANC at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionGiga cells per Liter (GI/L) (Mean)
WBC, Day 4, n=0,2,1WBC, Day 5, n=1,1,1WBC, Discharge/Day 45, n=2,3,1WBC, Day 3 post last dose, n=1,4,1ANC, Day 4, n=0,2,1ANC, Day 5, n=1,1,1ANC, Discharge/Day 45, n=2,3,1ANC, Day 3 post last dose, n=1,4,1
DNX 50 mg + OSV-7.10-5.30-9.50-8.00-7.420-6.260-9.720-9.060

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Change From Baseline in White Blood Cell Count (WBC) and Absolute Neutrophil Count (ANC)

Blood samples were collected to evaluate WBC and ANC at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionGiga cells per Liter (GI/L) (Mean)
WBC, Day 3, n=1,1,0WBC, Day 4, n=0,2,1WBC, Day 5, n=1,1,1WBC, Discharge/Day 45, n=2,3,1WBC, Day 3 post last dose, n=1,4,1ANC, Day 3, n=1,1,0ANC, Day 4, n=0,2,1ANC, Day 5, n=1,1,1ANC, Discharge/Day 45, n=2,3,1ANC, Day 3 post last dose, n=1,4,1
DNX 15 mg + OSV-3.001.15-3.703.971.95-4.0701.410-4.2503.0501.033

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Change From Baseline in Total Bilirubin (T. Bilirubin), Creatinine and Direct Bilirubin (D. Bilirubin)

Blood samples were collected to evaluate T. Bilirubin, creatinine and D. Bilirubin at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionMicromole per Liter (µmol/L) (Mean)
D. Bilirubin, Day 2, sample 2, n=0,0,1D. Bilirubin, Day 3, n=1,2,2D. Bilirubin, Day 3, sample 2, n=0,1,2D. Bilirubin, Day 4, n=0,1,2D. Bilirubin, Day 4, sample 2, n=0,1,1D. Bilirubin, Day 5, n=1,1,3D. Bilirubin, Day 6, n=1,1,4D. Bilirubin, Day 7, n=1,1,1D. Bilirubin, Discharge/Day 45, n=2,2,3D. Bilirubin, Day 3 post last dose, n=1,3,3T. Bilirubin, Day 2, sample 2, n=0,0,1T. Bilirubin, Day 3, n=1,2,2T. Bilirubin, Day 3, sample 2, n=0,1,2T. Bilirubin, Day 4, n=0,1,2T. Bilirubin, Day 4, sample 2, n=0,1,1T. Bilirubin, Day 5, n=1,1,3T. Bilirubin, Day 6, n=1,1,4T. Bilirubin, Day 7, n=1,1,1T. Bilirubin, Discharge/Day 45, n=2,2,3T. Bilirubin, Day 3 post last dose, n=1,3,3Creatinine, Day 2, n=2,2,4Creatinine, Day 2, sample 2, n=1,1,2Creatinine, Day 3, n=1,2,3Creatinine, Day 3, sample 2, n=0,2,4Creatinine, Day 4, n=1,3,4Creatinine, Day 4, sample 2, n=0,2,3Creatinine, Day 5, n=1,2,3Creatinine, Day 6, n=1,1,4Creatinine, Day 7, n=1,1,1Creatinine, Discharge/Day 45, n=2,2,3Creatinine, Day 3 post last dose, n=1,3,3
DNX 50 mg + OSV0.00.00.00.0-2.00.0-0.52.0-0.70.7-4.00-1.00-2.00-2.000.000.67-0.500.00-0.67-4.60-3.35-8.40-4.771.32-4.20-2.40-2.673.52-1.806.502.93

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Change From Baseline in Total Bilirubin (T. Bilirubin), Creatinine and Direct Bilirubin (D. Bilirubin)

Blood samples were collected to evaluate T. Bilirubin, creatinine and D. Bilirubin at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionMicromole per Liter (µmol/L) (Mean)
D. Bilirubin, Day 3, n=1,2,2D. Bilirubin, Day 3, sample 2, n=0,1,2D. Bilirubin, Day 4, n=0,1,2D. Bilirubin, Day 4, sample 2, n=0,1,1D. Bilirubin, Day 5, n=1,1,3D. Bilirubin, Day 6, n=1,1,4D. Bilirubin, Day 7, n=1,1,1D. Bilirubin, Discharge/Day 45, n=2,2,3D. Bilirubin, Day 3 post last dose, n=1,3,3T. Bilirubin, Day 3, n=1,2,2T. Bilirubin, Day 3, sample 2, n=0,1,2T. Bilirubin, Day 4, n=0,1,2T. Bilirubin, Day 4, sample 2, n=0,1,1T. Bilirubin, Day 5, n=1,1,3T. Bilirubin, Day 6, n=1,1,4T. Bilirubin, Day 7, n=1,1,1T. Bilirubin, Discharge/Day 45, n=2,2,3T. Bilirubin, Day 3 post last dose, n=1,3,3Creatinine, Day 2, n=2,2,4Creatinine, Day 2, sample 2, n=1,1,2Creatinine, Day 3, n=1,2,3Creatinine, Day 3, sample 2, n=0,2,4Creatinine, Day 4, n=1,3,4Creatinine, Day 4, sample 2, n=0,2,3Creatinine, Day 5, n=1,2,3Creatinine, Day 5, sample 2, n=0,1,0Creatinine, Day 6, n=1,1,4Creatinine, Day 7, n=1,1,1Creatinine, Discharge/Day 45, n=2,2,3Creatinine, Day 3 post last dose, n=1,3,3
DNX 15 mg + OSV-2.0-2.00.0-2.00.00.00.0-1.00.0-2.0-6.00.0-6.0-2.02.02.00.00.0-0.507.90-3.60-9.30-5.900.45-1.35-15.90-10.60-10.60-3.55-4.47

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Change From Baseline in Total Bilirubin (T. Bilirubin), Creatinine and Direct Bilirubin (D. Bilirubin)

Blood samples were collected to evaluate T. Bilirubin, creatinine and D. Bilirubin at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionMicromole per Liter (µmol/L) (Mean)
D. Bilirubin, Day 2, n=1,0,0D. Bilirubin, Day 3, n=1,2,2D. Bilirubin, Day 5, n=1,1,3D. Bilirubin, Day 6, n=1,1,4D. Bilirubin, Day 7, n=1,1,1D. Bilirubin, Day 8, n=1,0,0D. Bilirubin, Discharge/Day 45, n=2,2,3D. Bilirubin, Day 3 post last dose, n=1,3,3T. Bilirubin, Day 2, n=1,0,0T. Bilirubin, Day 3, n=1,2,2T. Bilirubin, Day 5, n=1,1,3T. Bilirubin, Day 6, n=1,1,4T. Bilirubin, Day 7, n=1,1,1T. Bilirubin, Day 8, n=1,0,0T. Bilirubin, Discharge/Day 45, n=2,2,3T. Bilirubin, Day 3 post last dose, n=1,3,3Creatinine, Day 2, n=2,2,4Creatinine, Day 2, sample 2, n=1,1,2Creatinine, Day 3, n=1,2,3Creatinine, Day 4, n=1,3,4Creatinine, Day 5, n=1,2,3Creatinine, Day 6, n=1,1,4Creatinine, Day 7, n=1,1,1Creatinine, Day 8, n=1,0,0Creatinine, Discharge/Day 45, n=2,2,3Creatinine, Day 3 post last dose, n=1,3,3
Placebo + OSV-2.0-2.00.00.00.0-2.0-3.00.00.0-2.00.0-2.0-6.0-6.0-1.0-4.0-7.953.50-33.60-39.80-40.60-44.20-38.00-26.50-16.80-23.00

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Change From Baseline in Albumin and Total Protein

Blood samples were collected to evaluate albumin and total protein at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionGram per Liter (G/L) (Mean)
Albumin, Day 2, sample 2, n=0,0,1Albumin, Day 3, n=1,2,2Albumin, Day 3, sample 2, n=0,1,2Albumin, Day 4, n=0,1,2Albumin, Day 4, sample 2, n=0,1,1Albumin, Day 5, n=1,1,3Albumin, Day 6, n=1,1,4Albumin, Day 7, n=1,1,1Albumin, Discharge/Day 45, n=2,2,3Albumin, Day 3 post last dose, n=1,3,3Total Protein, Day 2, n=1,0,1Total Protein, Day 3, n=1,2,2Total Protein, Day 3, sample 2, n=0,1,2Total Protein, Day 4, n=0,1,2Total Protein, Day 4, sample 2, n=0,1,1Total Protein, Day 5, n=1,1,3Total Protein, Day 6, n=1,1,4Total Protein, Day 7, n=1,1,1Total Protein, Discharge/Day 45, n=2,2,3Total Protein, Day 3 post last dose, n=1,3,3
DNX 50 mg + OSV0.0-2.0-4.5-3.0-5.0-3.7-2.8-3.05.7-2.3-1.0-3.0-4.0-4.0-7.0-5.7-4.0-2.06.7-3.3

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Change From Baseline in Albumin and Total Protein

Blood samples were collected to evaluate albumin and total protein at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionGram per Liter (G/L) (Mean)
Albumin, Day 3, n=1,2,2Albumin, Day 3, sample 2, n=0,1,2Albumin, Day 4, n=0,1,2Albumin, Day 4, sample 2, n=0,1,1Albumin, Day 5, n=1,1,3Albumin, Day 6, n=1,1,4Albumin, Day 7, n=1,1,1Albumin, Discharge/Day 45, n=2,2,3Albumin, Day 3 post last dose, n=1,3,3Total Protein, Day 3, n=1,2,2Total Protein, Day 3, sample 2, n=0,1,2Total Protein, Day 4, n=0,1,2Total Protein, Day 4, sample 2, n=0,1,1Total Protein, Day 5, n=1,1,3Total Protein, Day 6, n=1,1,4Total Protein, Day 7, n=1,1,1Total Protein, Discharge/Day 45, n=2,2,3Total Protein, Day 3 post last dose, n=1,3,3
DNX 15 mg + OSV-5.0-9.0-1.0-8.0-5.0-6.0-5.0-0.5-1.3-5.5-13.0-1.0-10.0-7.0-7.0-5.0-1.5-3.0

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Change From Baseline in Albumin and Total Protein

Blood samples were collected to evaluate albumin and total protein at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionGram per Liter (G/L) (Mean)
Albumin, Day 2, n=1,0,0Albumin, Day 3, n=1,2,2Albumin, Day 5, n=1,1,3Albumin, Day 6, n=1,1,4Albumin, Day 7, n=1,1,1Albumin, Day 8, n=1,0,0Albumin, Discharge/Day 45, n=2,2,3Albumin, Day 3 post last dose, n=1,3,3Total Protein, Day 2, n=1,0,1Total Protein, Day 3, n=1,2,2Total Protein, Day 5, n=1,1,3Total Protein, Day 6, n=1,1,4Total Protein, Day 7, n=1,1,1Total Protein, Day 8, n=1,0,0Total Protein, Discharge/Day 45, n=2,2,3Total Protein, Day 3 post last dose, n=1,3,3
Placebo + OSV2.00.00.01.0-2.00.02.50.01.01.0-1.00.0-3.00.00.0-0.3

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Change From Baseline in Alanine Amino Transferase (ALT), Aspartate Amino Transferase (AST) and Alkaline Phosphatase (ALP)

Blood samples were collected to evaluate ALT, AST and ALP at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionInternational unit per Liter (IU/L) (Mean)
ALT, Day 2, sample 2, n=0,0,1ALT, Day 3, n=1,2,2ALT, Day 3, sample 2, n=0,1,2ALT, Day 4, n=0,1,2ALT, Day 4, sample 2, n=0,1,1ALT, Day 5, n=1,1,3ALT, Day 6, n=1,1,4ALT, Day 7, n=1,1,1ALT, Discharge/Day 45, n=2,2,3ALT, Day 3 post last dose, n=1,3,3AST, Day 2, sample 2, n=0,0,1AST, Day 3, n=1,2,2AST, Day 3, sample 2, n=0,1,2AST, Day 4, n=0,1,2AST, Day 4, sample 2, n=0,1,1AST, Day 5, n=1,1,3AST, Day 6, n=1,1,4AST, Day 7, n=1,1,1AST, Discharge/Day 45, n=2,2,3AST, Day 3 post last dose, n=1,3,3ALP, Day 2,sample 2, n=0,0,1ALP, Day 3, n=1,2,2ALP, Day 3, sample 2, n=0,1,2ALP, Day 4, n=0,1,2ALP, Day 4, sample 2, n=0,1,1ALP, Day 5, n=1,1,3ALP, Day 6, n=1,1,4ALP, Day 7, n=1,1,1ALP, Discharge/Day 45, n=2,2,3ALP, Day 3 post last dose, n=1,3,3
DNX 50 mg + OSV-1.02.0-1.0-3.510.0-0.3-2.3-6.00.7-4.0-4.0-2.0-1.5-8.00.0-7.3-5.8-11.0-3.0-10.7-3.0-8.0-14.0-5.5-4.0-11.0-9.517.02.0-9.3

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Change From Baseline in Alanine Amino Transferase (ALT), Aspartate Amino Transferase (AST) and Alkaline Phosphatase (ALP)

Blood samples were collected to evaluate ALT, AST and ALP at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionInternational unit per Liter (IU/L) (Mean)
ALT, Day 3, n=1,2,2ALT, Day 3, sample 2, n=0,1,2ALT, Day 4, n=0,1,2ALT, Day 4, sample 2, n=0,1,1ALT, Day 5, n=1,1,3ALT, Day 6, n=1,1,4ALT, Day 7, n=1,1,1ALT, Discharge/Day 45, n=2,2,3ALT, Day 3 post last dose, n=1,3,3AST, Day 3, n=1,2,2AST, Day 3, sample 2, n=0,1,2AST, Day 4, n=0,1,2AST, Day 4, sample 2, n=0,1,1AST, Day 5, n=1,1,3AST, Day 6, n=1,1,4AST, Day 7, n=1,1,1AST, Discharge/Day 45, n=2,2,3AST, Day 3 post last dose, n=1,3,3ALP, Day 3, n=1,2,2ALP, Day 3, sample 2, n=0,1,2ALP, Day 4, n=0,1,2ALP, Day 4, sample 2, n=0,1,1ALP, Day 5, n=1,1,3ALP, Day 6, n=1,1,4ALP, Day 7, n=1,1,1ALP, Discharge/Day 45, n=2,2,3ALP, Day 3 post last dose, n=1,3,3
DNX 15 mg + OSV3.0-1.0-18.01.0-2.0-37.0-42.0-30.0-17.06.08.0-29.016.0-9.0-46.0-51.0-27.5-21.7-6.0-23.0-25.0-22.0-8.0-51.0-50.0-25.5-19.7

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Change From Baseline in Alanine Amino Transferase (ALT), Aspartate Amino Transferase (AST) and Alkaline Phosphatase (ALP)

Blood samples were collected to evaluate ALT, AST and ALP at indicated time points. Values at Day 1 were considered as Baseline values. Change from Baseline at each visit was calculated by subtracting Baseline value from post-dose visit value. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles). NA indicates data is not available. (NCT02927431)
Timeframe: Baseline and up to 45 days

InterventionInternational unit per Liter (IU/L) (Mean)
ALT, Day 2, n=1,0,0ALT, Day 3, n=1,2,2ALT, Day 5, n=1,1,3ALT, Day 6, n=1,1,4ALT, Day 7, n=1,1,1ALT, Day 8, n=1,0,0ALT, Discharge/Day 45, n=2,2,3ALT, Day 3 post last dose, n=1,3,3AST, Day 2, n=1,0,0AST, Day 3, n=1,2,2AST, Day 5, n=1,1,3AST, Day 6, n=1,1,4AST, Day 7, n=1,1,1AST, Day 8, n=1,0,0AST, Discharge/Day 45, n=2,2,3AST, Day 3 post last dose, n=1,3,3ALP, Day 2, n=1,0,0ALP, Day 3, n=1,2,2ALP, Day 5, n=1,1,3ALP, Day 6, n=1,1,4ALP, Day 7, n=1,1,1ALP, Day 8, n=1,0,0ALP, Discharge/Day 45, n=2,2,3ALP, Day 3 post last dose, n=1,3,3
Placebo + OSV10.04.00.0-1.0-2.0-1.0-6.02.014.011.0-10.0-12.0-11.0-12.0-12.0-10.08.02.06.05.02.03.010.01.0

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Number of Participants With Clinically Significant Abnormality in Electrocardiogram (ECG)

Single 12-lead ECGs were obtained at Baseline and on the day of last dose during the study using an ECG machine that automatically calculates the heart rate (HR) and measures PR, QRS, QT, and QT duration corrected for heart rate (QTc). Number of participants with clinically significant abnormality in ECG are presented. (NCT02927431)
Timeframe: Up to 6 days

InterventionParticipants (Count of Participants)
Placebo + OSV0
DNX 15 mg + OSV0
DNX 50 mg + OSV1

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Area Under the Curve (AUC) Adjusted by Baseline in Viral RNA

This endpoint was defined as AUC of change from baseline in the amount of virus RNA (RT-PCR) from Day 1 to Day 9. The AUC was calculated using the trapezoidal method. (NCT02949011)
Timeframe: Day 1 to Day 9

Interventionlog₁₀ virus particles/mL*hours (Mean)
Baloxavir Marboxil-490.9
Placebo-434.9
Oseltamivir-482.2

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Change From Baseline in Virus RNA (RT-PCR) at Each Time Point

Nasopharyngeal swabs (or throat swabs, if nasopharyngeal swabbing was not feasible) were obtained for viral quantitation. Virus RNA was measured by reverse transcription polymerase chain reaction (RT-PCR). (NCT02949011)
Timeframe: Day 1 pretreatment (Baseline) and Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,,
Interventionlog₁₀ virus particles/mL (Mean)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir Marboxil-1.13-2.09-2.77-3.09-3.33-3.89
Oseltamivir-0.76-1.77-2.34-3.04-3.41-3.99
Placebo-0.62-1.57-2.09-2.77-3.19-3.78

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Change From Baseline in Virus Titer at Each Time Point

"Virus titer was quantified from nasopharyngeal swabs (or throat swabs if nasopharyngeal swabbing was not feasible) by tissue culture methods.~If virus titer was less than the lower limit of quantification, the virus titer was imputed 0.7 (TCID₅₀/mL)." (NCT02949011)
Timeframe: Day 1 pretreatment (Baseline) and Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,,
Interventionlog₁₀[TCID₅₀/mL] (Mean)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir Marboxil-3.36-3.92-3.99-4.32-4.07-4.53
Oseltamivir-1.76-3.26-3.75-4.41-4.39-4.78
Placebo-1.25-2.99-3.79-4.38-4.68-4.91

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Percentage of Participants Reporting Normal Temperature at Each Time Point

Defined as the percentage of patrticipants whose axillary body temperature dropped to less than 37ºC after the initiation of the study treatment. (NCT02949011)
Timeframe: 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 hours after the initial dose of study treatment

,,
Interventionpercentage of participants (Number)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours144 hours168 hours192 hours216 hours
Baloxavir Marboxil29.751.168.177.484.087.586.290.087.989.089.1
Oseltamivir25.954.364.176.482.685.888.487.487.790.589.6
Placebo24.643.247.459.371.779.886.686.188.187.589.9

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Percentage of Participants Whose Symptoms Were Improved at Each Time Point

"Participants assessed the severity of 7 influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (0 = no symptoms, 1= mild, 2 = moderate, and 3 = severe).~Improvement of symptoms was defined as all influenza symptoms alleviated, maintained, or improved, as defined below, for a duration of at least 21.5 hours:~Preexisting symptoms (cough, fatigue, or muscle/joint pain that existed prior to influenza) judged to be worse at baseline must have improved at least 1 point from baseline severity~Preexisting symptoms judged not to be worse at baseline must have maintained baseline severity~New symptoms at baseline must have alleviated, defined as a symptom score of none (0) or mild (1)." (NCT02949011)
Timeframe: 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 hours after the initial dose of study treatment

,,
Interventionpercentage of participants (Number)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours144 hours168 hours192 hours216 hours
Baloxavir Marboxil9.118.833.938.056.065.972.378.180.183.685.8
Oseltamivir8.119.631.039.956.061.172.477.679.685.688.2
Placebo8.614.221.128.841.853.464.669.672.778.078.7

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Percentage of Participants With Adverse Events (AEs)

(NCT02949011)
Timeframe: From first dose of study drug to Day 22

,,
Interventionpercentage of participants (Number)
Any adverse event (AE)Fatal adverse eventsSerious adverse eventsAEs leading to withdrawal of study drugTreatment-related adverse events (TRAEs)Fatal treatment-related adverse eventsTreatment-related serious adverse eventsTRAEs leading to withdrawal of study drug
Baloxavir Marboxil25.10.00.70.75.60.00.00.3
Oseltamivir28.00.11.10.67.90.00.30.4
Placebo29.70.01.20.78.30.00.30.3

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Percentage of Participants With Positive Influenza Virus by RT-PCR at Each Time Point

Influenza virus ribonucleic acid (RNA) was quantified from nasopharyngeal swabs (or throat swabs, if nasopharyngeal swabbing was not feasible). The percentage of participants with detectable virus RNA (2.05 for flu A and 2.83 for flu B log₁₀ virus particles/mL) measured by reverse transcription polymerase chain reaction (RT-PCR) among those assessed on Days 2, 3, 4, 5, 6 and 9. (NCT02949011)
Timeframe: Days 2, 3, 4 (optional), 5, 6 (optional), and 9.

,,
Interventionpercentage of participants (Number)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir Marboxil96.092.586.584.971.854.5
Oseltamivir96.095.186.486.171.857.7
Placebo96.395.491.088.678.064.9

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Body Temperature at Each Time Point

Participant's self-measured axillary temperature using an electronic thermometer. (NCT02949011)
Timeframe: 12, 24, 36, 48, 72, 96 and 120 hours after the initial dose of study treatment

,,
Intervention°C (Least Squares Mean)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours
Baloxavir Marboxil37.3936.8436.5836.4436.3036.2636.26
Oseltamivir37.4336.8036.6236.5036.2936.2436.21
Placebo37.5337.0236.9436.7736.4636.3536.27

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Time to Return to Preinfluenza Health Status

"Participants were asked to record their preinfluenza health status on a scale from 0 (worst possible health) to 10 (normal health [for someone your age and condition]), and their health status at baseline and every day after initiation of study treatment on the same scale. Return to preinfluenza health status was defined as time from the initiation of the study treatment to the first time when the health status score was equal to or higher than the preinfluenza health status score.~Time to return to preinfluenza health status was analyzed using KM methods; participants with a smaller number on the scale for health status by the last observation time point were censored at that time point." (NCT02949011)
Timeframe: Baseline to Day 14

Interventionhours (Median)
Baloxavir Marboxil126.4
Placebo149.8
Oseltamivir126.9

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Time to Improvement of the Three Respiratory Symptoms

"Participants assessed the severity of 7 influenza-associated symptoms on a 4-point scale (from 0 = no symptoms to 3 = severe symptoms). Time to improvement of the 3 respiratory symptoms was defined as the time from the start of study treatment to the time when all 3 respiratory symptoms (cough, sore throat, and nasal congestion) were alleviated, maintained, or improved, as defined below, for a duration of at least 21.5 hours:~Preexisting symptoms (cough, fatigue, or muscle/joint pain that existed prior to influenza) that were worse at baseline must have improved at least 1 point from baseline~Preexisting symptoms not worse at baseline must have maintained baseline severity~New symptoms at baseline must have alleviated, defined as a symptom score of none (0) or mild (1).~Time to improvement of the 3 respiratory symptoms was analyzed using KM methods; participants who did not experience improvement of symptoms were censored at the last observation time point." (NCT02949011)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir Marboxil63.6
Placebo87.8
Oseltamivir62.1

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Percentage of Participants With Positive Influenza Virus Titer at Each Time Point

Virus titer was quantified from nasopharyngeal swabs (or throat swabs if nasopharyngeal swabbing was not feasible) using tissue culture methods. Positive influenza virus titer was defined as virus titer not less than the lower limit of quantification (0.7 log₁₀ of the 50% tissue culture infective dose (TCID₅₀/mL) among those assessed for virus titer on Days 2, 3, 4, 5, 6, and 9. (NCT02949011)
Timeframe: Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,,
Interventionpercentage of participants (Number)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir Marboxil58.631.718.516.04.32.8
Oseltamivir86.960.033.120.411.40.9
Placebo86.972.750.030.716.05.3

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Time to Improvement of Individual Symptoms

"Participants assessed the severity of 7 influenza-associated symptoms on a 4-point scale (0 = no symptoms to 3 = severe). Time to improvement of cough, fatigue, and muscle/joint pain was defined as the time from the start of treatment to the time when each symptom was alleviated, maintained, or improved, as defined below, for at least 21.5 hours:~Preexisting symptoms that were worse at baseline must have improved at least 1 point from baseline~Preexisting symptoms not worse at baseline must have maintained baseline severity~New symptoms must have alleviated, defined as a score of 0 (None) or 1 (Mild). Time to improvement of sore throat, headache, nasal congestion, and feverish/chills was defined as the time from the start of treatment to the time when the symptom was assessed as 0 (None) or 1 (Mild) for at least 21.5 hours.~Time to improvement of symptoms was analyzed using KM methods; participants with no improvement of symptoms were censored at the last observation." (NCT02949011)
Timeframe: Initiation of study treatment up to Day 14

,,
Interventionhours (Median)
CoughSore ThroatHeadacheNasal CongestionFeverishness or ChillsMuscle or Joint PainFatigue
Baloxavir Marboxil47.340.233.445.628.337.241.3
Oseltamivir47.539.331.344.029.133.243.2
Placebo70.446.543.957.731.944.948.8

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Time to Alleviation of Symptoms

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~Time to alleviation of symptoms was defined as the time from the start of the study treatment to the time when all seven influenza-related symptoms were assessed by the participant as absent (0) or mild (1) for at least 21.5 hours.~Time to alleviation of symptoms was analyzed using Kaplan-Meier (KM) methods; participants who did not experience alleviation of symptoms were censored at the last observation time point." (NCT02949011)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir Marboxil77.0
Placebo102.8
Oseltamivir85.6

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Time to Resolution of Fever

Time to resolution of fever was defined as the time between the initiation of the study treatment and the resolution of fever. The resolution of fever was defined as the time when the participant's self-measured axillary temperature became less than 37ºC and was maintained at less than 37ºC for at least 12 hours. Time to resolution of fever was analyzed using KM methods; participants who did not experience resolution of fever by the last observation time point were censored at that time point. (NCT02949011)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir Marboxil30.8
Placebo50.7
Oseltamivir34.3

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Time to Improvement of the Four Systemic Symptoms

"Participants assessed the severity of 7 influenza-associated symptoms on a 4-point scale (from 0 = no symptoms to 3 = severe symptoms). Time to improvement of the 4 systemic symptoms was defined as the time between the initiation of study treatment to the time when all 4 systemic symptoms (headache, feverishness or chills, muscle or joint pain, and fatigue) were alleviated, maintained, or improved, as defined below, for a duration of at least 21.5 hours:~Preexisting symptoms (cough, fatigue, or muscle/joint pain that existed prior to influenza) that were worse at baseline must have improved at least 1 point from baseline~Preexisting symptoms not worse at baseline must have maintained baseline severity~New symptoms at baseline must have alleviated, defined as a symptom score of none (0) or mild (1).~Time to improvement of the 4 systemic symptoms was analyzed using KM methods; participants who did not experience improvement of symptoms were censored at the last observation." (NCT02949011)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir Marboxil51.7
Placebo66.8
Oseltamivir49.4

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Time to Improvement of Influenza Symptoms

"Participants assessed the severity of 7 influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness/chills, muscle/joint pain, and fatigue) on a 4-point scale (0 = no symptoms, 1= mild, 2 = moderate, and 3 = severe). Time to improvement of symptoms was defined as the time from the start of treatment to the time when all influenza symptoms were alleviated, maintained, or improved, as defined below, for a duration of at least 21.5 hours:~Preexisting symptoms (cough, fatigue, or muscle/joint pain that existed prior to influenza) that were worse at baseline must have improved at least 1 point from baseline~Preexisting symptoms not worse at baseline must have maintained baseline severity~New symptoms must have alleviated, defined as a symptom score of none (0) or mild (1).~Time to improvement of symptoms was analyzed using Kaplan-Meier (KM) methods; participants who did not experience improvement of symptom s were censored at the last observation." (NCT02949011)
Timeframe: From Day 1 pretreatment up to Day 14

Interventionhours (Median)
Baloxavir Marboxil73.2
Placebo102.3
Oseltamivir81.0

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Percentage of Participants Requiring Systemic Antibiotics for Infections Secondary to Influenza Infection

The percentage of participants who received systemic antibiotics for any of the predefined complications (sinusitis, otitis media, bronchitis and pneumonia). (NCT02949011)
Timeframe: Day 2 to Day 22

Interventionpercentage of participants (Number)
Baloxavir Marboxil3.4
Placebo7.5
Oseltamivir3.9

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Area Under the Curve (AUC) Adjusted by Baseline in Influenza Virus Titer

This endpoint was defined as AUC of change from Baseline in virus titer from Day 1 to Day 9. AUC was calculated using the trapezoidal method. (NCT02949011)
Timeframe: Day 1 to Day 9

Interventionlog₁₀[TCID₅₀/mL]*hours (Mean)
Baloxavir Marboxil-727.7
Placebo-660.2
Oseltamivir-695.5

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Time to Cessation of Viral Shedding Determined by Virus Titer

Time to cessation of viral shedding by virus titer was defined as the time between the initiation of the study treatment and first time when the virus titer was below the limit of detection (0.7 log₁₀[TCID₅₀/mL]). The median and 95% confidence interval (CI) for time to cessation of viral shedding determined by virus titer was analyzed using the Kaplan-Meier (KM) method; participants whose virus titer had not reached cessation by the last observation time point were treated as censored at that time point. (NCT02949011)
Timeframe: Day 1 to Day 9

Interventionhours (Median)
Baloxavir Marboxil48.0
Placebo96.0
Oseltamivir96.0

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Time to Cessation of Viral Shedding Determined by Virus RNA

"Time to cessation of viral shedding by RT-PCR was defined as the time between the initiation of the study treatment and first time when the virus RNA was below the limit of detection measured by RT-PCR.~Time to cessation of viral shedding by RT-PCR was analyzed using the KM method; participants whose virus RNA had not reached cessation by the last observation time point were treated as censored at that time point." (NCT02949011)
Timeframe: Day 1 to Day 9

Interventionhours (Median)
Baloxavir Marboxil216.0
Placebo240.0
Oseltamivir216.0

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Percentage of Participants With Positive Influenza Virus by RT-PCR at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir

Influenza virus RNA was quantified from nasopharyngeal swabs (or throat swabs, if nasopharyngeal swabbing was not feasible). The percentage of participants with detectable virus RNA (2.05 for flu A and 2.83 for flu B log₁₀ virus particles/mL) among those assessed measured by reverse transcription polymerase chain reaction (RT-PCR) on Days 2, 3, 4, 5, 6 and 9. (NCT02954354)
Timeframe: Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,
Interventionpercentage of participants (Number)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir97.395.393.686.669.360.2
Oseltamivir98.697.593.092.180.764.7

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Percentage of Participants With Positive Influenza Virus by RT-PCR at Each Time Point in Participants Randomized to Baloxavir or Placebo

Influenza virus ribonucleic acid (RNA) was quantified from nasopharyngeal swabs (or throat swabs, if nasopharyngeal swabbing was not feasible). The percentage of participants with detectable virus RNA (2.05 for flu A and 2.83 for flu B log₁₀ virus particles/mL) among those assessed measured by reverse transcription polymerase chain reaction (RT-PCR) on Days 2, 3, 4, 5, 6 and 9. (NCT02954354)
Timeframe: Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,
Interventionpercentage of participants (Number)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir97.395.693.487.474.861.5
Placebo97.797.291.093.977.272.4

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Percentage of Participants With Positive Influenza Virus Titer at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir

Virus titer was quantified from nasopharyngeal swabs (or throat swabs if nasopharyngeal swabbing was not feasible) by tissue culture methods. Positive influenza virus titer was defined as virus titer not less than the lower limit of quantification (0.7 log₁₀ of the 50% tissue culture infective dose (TCID₅₀/mL) among those assessed for virus titer on Days 2, 3, 4, 5, 6 and 9. (NCT02954354)
Timeframe: Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,
Interventionpercentage of participants (Number)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir47.420.016.112.95.63.0
Oseltamivir91.157.327.620.89.03.2

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Percentage of Participants With Positive Influenza Virus Titer at Each Time Point in Participants Randomized to Baloxavir or Placebo

Virus titer was quantified from nasopharyngeal swabs (or throat swabs if nasopharyngeal swabbing was not feasible) by tissue culture methods. Positive influenza virus titer was defined as virus titer not less than the lower limit of quantification (0.7 log₁₀ of the 50% tissue culture infective dose (TCID₅₀/mL) among those assessed for virus titer on Days 2, 3, 4, 5, 6 and 9. (NCT02954354)
Timeframe: Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,
Interventionpercentage of participants (Number)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir47.621.716.713.58.22.9
Placebo96.070.556.129.712.54.6

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Time to Alleviation of Individual Symptoms in Adults Randomized to Baloxavir or Oseltamivir

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~Time to alleviation of each symptom was defined as the time from the start of treatment to the start of the time period when the individual symptom was assessed by the participant as 0 (None) or 1 (Mild) for a duration of at least 21.5 hours." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

,
Interventionhours (Median)
CoughSore ThroatHeadacheNasal CongestionFeverishness or chillsMuscle or joint painFatigue
Baloxavir38.232.126.933.021.023.328.9
Oseltamivir31.430.425.631.321.224.026.6

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Change From Baseline in Virus RNA (RT-PCR) at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir

Nasopharyngeal swabs (or throat swabs, if nasopharyngeal swabbing was not feasible) were obtained for viral quantitation. Virus RNA was measured by reverse transcription polymerase chain reaction (RT-PCR). (NCT02954354)
Timeframe: Day 1 pretreatment (Baseline) and Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,
Interventionlog₁₀ virus particles/mL (Mean)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir-1.61-2.79-2.94-3.76-3.81-4.43
Oseltamivir-1.10-2.44-2.97-3.62-3.88-4.52

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Time to Alleviation of Symptoms in Adults Randomized to Baloxavir or Oseltamivir

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~Time to alleviation of symptoms was defined as the time from the start of the study treatment to the time when all seven influenza-related symptoms were assessed by the participant as absent (0) or mild (1) for at least 21.5 hours.~Time to alleviation of symptoms was analyzed using the Kaplan-Meier(KM) method; participants who did not experience alleviation of symptoms were censored at the last observation time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir53.5
Oseltamivir53.8

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Area Under the Curve (AUC) Adjusted by Baseline of Influenza Virus RNA in Participants Randomized to Baloxavir or Placebo

This endpoint was defined as AUC of change from baseline in the amount of virus RNA (RT-PCR) from Day 1 to Day 9. The AUC was calculated using the trapezoidal method. (NCT02954354)
Timeframe: Day 1 to Day 9

Interventionlog₁₀ virus particles/mL*hours (Mean)
Baloxavir-582.0
Placebo-456.8

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Area Under the Curve (AUC) Adjusted by Baseline of Influenza Virus RNA in Adults Randomized to Baloxavir or Oseltamivir

This endpoint was defined as AUC of change from baseline in the amount of virus RNA (RT-PCR) from Day 1 to Day 9. The AUC was calculated using the trapezoidal method. (NCT02954354)
Timeframe: Day 1 to Day 9

Interventionlog₁₀ virus particles/mL*hours (Mean)
Baloxavir-581.0
Oseltamivir-569.7

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Area Under the Curve (AUC) Adjusted by Baseline in Influenza Virus Titer in Participants Randomized to Baloxavir or Placebo

This endpoint was defined as AUC of change from Baseline in virus titer from Day 1 to Day 9. AUC was calculated using the trapezoidal method. (NCT02954354)
Timeframe: Day 1 to Day 9

Interventionlog₁₀[TCID₅₀/mL]*hours (Mean)
Baloxavir-836.2
Placebo-641.8

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Area Under the Curve (AUC) Adjusted by Baseline in Influenza Virus Titer in Adults Randomized to Baloxavir or Oseltamivir

This endpoint was defined as AUC of change from Baseline in virus titer from Day 1 to Day 9. AUC was calculated using the trapezoidal method. (NCT02954354)
Timeframe: Day 1 to Day 9

Interventionlog₁₀[TCID₅₀/mL]*hours (Mean)
Baloxavir-829.6
Oseltamivir-790.2

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Time to Return to Preinfluenza Health Status in Adults Randomized to Baloxavir or Oseltamivir

"Participants were asked to record their preinfluenza health status on a scale from 0 (worst possible health) to 10 (normal health [for someone your age and your health condition]), and their health status every day after initiation of study treatment on the same scale. Return to preinfluenza health status was defined as time from the initiation of the study treatment to the first time when the health status score was equal to or higher than the preinfluenza health status score.~Time to return to preinfluenza health status was analyzed using KM methods; participants with a smaller number on the scale for health status by the last observation time point were censored at that time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir127.8
Oseltamivir128.5

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Time to Return to Preinfluenza Health Status in Participants Randomized to Baloxavir or Placebo

"Participants were asked to record their preinfluenza health status on a scale from 0 (worst possible health) to 10 (normal health [for someone your age and your health condition]), and their health status every day after initiation of study treatment on the same scale. Return to preinfluenza health status was defined as time from the initiation of the study treatment to the first time when the health status score was equal to or higher than the preinfluenza health status score.~Time to return to preinfluenza health status was analyzed using KM methods; participants with a smaller number on the scale for health status by the last observation time point were censored at that time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir129.2
Placebo168.8

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Body Temperature at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir

Participant's self-measured axillary temperature using an electronic thermometer. (NCT02954354)
Timeframe: 12, 24, 36, 48, 72, 96 and 120 hours after the initial dose of study treatment

,
Intervention°C (Least Squares Mean)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours
Baloxavir37.4736.7836.5536.3436.3036.2636.27
Oseltamivir37.3536.7336.5436.3636.3136.2336.21

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Body Temperature at Each Time Point in Participants Randomized to Baloxavir or Placebo

Participant's self-measured axillary temperature using an electronic thermometer. (NCT02954354)
Timeframe: 12, 24, 36, 48, 72, 96 and 120 hours after the initial dose of study treatment

,
Intervention°C (Least Squares Mean)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours
Baloxavir37.4036.7336.4936.3236.2636.2736.28
Placebo37.4937.0736.9036.6936.4836.3136.25

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Change From Baseline in Composite Symptom Score at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~The composite symptom score is the total score of the 7 influenza symptoms as assessed by the participant, and ranges from 0 to 21." (NCT02954354)
Timeframe: Day 1 pretreatment (Baseline) and 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 hours after the initial dose of study treatment.

,
Interventionscores on a scale (Least Squares Mean)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours144 hours168 hours192 hours216 hours
Baloxavir-2.2-4.5-6.5-7.6-9.6-10.5-11.0-11.8-11.9-12.0-12.4
Oseltamivir-2.4-4.7-6.3-7.8-9.7-10.6-11.3-11.8-12.1-12.4-12.5

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Change From Baseline in Composite Symptom Score at Each Time Point in Participants Randomized to Baloxavir or Placebo

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~The composite symptom score is the total score of the 7 influenza symptoms as assessed by the participant, and ranges from 0 to 21." (NCT02954354)
Timeframe: Day 1 pretreatment (Baseline) and 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 hours after the initial dose of study treatment.

,
Interventionscores on a scale (Least Squares Mean)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours144 hours168 hours192 hours216 hours
Baloxavir-2.4-4.7-6.7-7.8-9.4-10.5-10.9-11.6-11.9-12.0-12.4
Placebo-2.5-3.6-4.9-6.0-8.0-9.5-10.6-11.2-11.8-12.0-12.4

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Time to Alleviation of Individual Symptoms in Participants Randomized to Baloxavir or Placebo

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~Time to alleviation of each symptom was defined as the time from the start of treatment to the start of the time period when the individual symptom was assessed by the participant as 0 (None) or 1 (Mild) for a duration of at least 21.5 hours." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

,
Interventionhours (Median)
CoughSore ThroatHeadacheNasal CongestionFeverishness or chillsMuscle or joint painFatigue
Baloxavir38.331.526.131.820.923.225.3
Placebo61.440.537.952.525.831.340.5

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Time to Alleviation of the Three Respiratory Symptoms in Adults Randomized to Baloxavir or Oseltamivir

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms). Time to alleviation of the 3 respiratory symptoms was defined as the time from the start of study treatment to the time when all 3 respiratory symptoms (cough, sore throat and nasal congestion) were assessed by the participant as absent (0) or mild (1) for at least 21.5 hours.~Time to alleviation of the 3 respiratory symptoms was analyzed using the KM method; participants who did not experience alleviation of symptoms were censored at the last observation time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir46.0
Oseltamivir44.6

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Time to Alleviation of the Three Respiratory Symptoms in Participants Randomized to Baloxavir or Placebo

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms). Time to alleviation of the 3 respiratory symptoms was defined as the time from the start of study treatment to the time when all 3 respiratory symptoms (cough, sore throat and nasal congestion) were assessed by the participant as absent (0) or mild (1) for at least 21.5 hours.~Time to alleviation of the 3 respiratory symptoms was analyzed using the KM method; participants who did not experience alleviation of symptoms were censored at the last observation time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir46.0
Placebo69.1

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Time to Cessation of Viral Shedding Determined by Virus RNA in Adults Randomized to Baloxavir or Oseltamivir

"Time to cessation of viral shedding by RT-PCR was defined as the time between the initiation of the study treatment and first time when the virus RNA was below the limit of detection measured by RT-PCR.~Time to cessation of viral shedding by RT-PCR was analyzed using the KM method; participants whose virus RNA had not reached cessation by the last observation time point were treated as censored at that time point." (NCT02954354)
Timeframe: Day 1 to Day 9

Interventionhours (Median)
Baloxavir216.0
Oseltamivir240.0

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Time to Cessation of Viral Shedding Determined by Virus RNA in Participants Randomized to Baloxavir or Placebo

"Time to cessation of viral shedding by RT-PCR was defined as the time between the initiation of the study treatment and first time when the virus RNA was below the limit of detection measured by RT-PCR.~Time to cessation of viral shedding by RT-PCR was analyzed using the KM method; participants whose virus RNA had not reached cessation by the last observation time point were treated as censored at that time point." (NCT02954354)
Timeframe: Day 1 to Day 9

Interventionhours (Median)
Baloxavir216.0
Placebo240.0

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Time to Cessation of Viral Shedding Determined by Virus Titer in Adults Randomized to Baloxavir or Oseltamivir

Time to cessation of viral shedding by virus titer was defined as the time between the initiation of the study treatment and first time when the virus titer was below the limit of detection (0.7 log₁₀[TCID₅₀/mL]). The time to cessation of viral shedding determined by virus titer was analyzed using the Kaplan-Meier (KM) method; participants whose virus titer had not reached cessation by the last observation time point were treated as censored at that time point. (NCT02954354)
Timeframe: Day 1 to Day 9

Interventionhours (Median)
Baloxavir24.0
Oseltamivir72.0

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Time to Cessation of Viral Shedding Determined by Virus Titer in Participants Randomized to Baloxavir or Placebo

Time to cessation of viral shedding by virus titer was defined as the time between the initiation of the study treatment and first time when the virus titer was below the limit of detection (0.7 log₁₀[TCID₅₀/mL]). The median and 95% confidence interval (CI) for time to cessation of viral shedding determined by virus titer was analyzed using the Kaplan-Meier (KM) method; participants whose virus titer had not reached cessation by the last observation time point were treated as censored at that time point. (NCT02954354)
Timeframe: Day 1 to Day 9

Interventionhours (Median)
Baloxavir24.0
Placebo96.0

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Time to Resolution of Fever in Adults Randomized to Baloxavir or Oseltamivir

"Time to resolution of fever was defined as the time between the initiation of the study treatment and the resolution of fever. The resolution of fever was defined as the time when the participant's self-measured axillary temperature became less than 37ºC and was maintained at less than 37ºC for a duration of at least 12 hours.~Time to resolution of fever was analyzed using KM methods; participants who did not experience resolution of fever by the last observation time point were censored at that time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir24.4
Oseltamivir24.0

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Time to Resolution of Fever in Participants Randomized to Baloxavir or Placebo

"Time to resolution of fever was defined as the time between the initiation of the study treatment and the resolution of fever. The resolution of fever was defined as the time when the participant's self-measured axillary temperature became less than 37ºC and was maintained at less than 37ºC for a duration of at least 12 hours.~Time to resolution of fever was analyzed using KM methods; participants who did not experience resolution of fever by the last observation time point were censored at that time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir24.5
Placebo42.0

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Time to Alleviation of the Four Systemic Symptoms in Participants Randomized to Baloxavir or Placebo

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~Time to alleviation of the 4 systemic symptoms was defined as the time between the initiation of the study treatment to the time when all 4 systemic symptoms (headache, feverishness or chills, muscle or joint pain, and fatigue) were assessed by the participant as 0 (None) or 1 (Mild) for a duration of at least 21.5 hours.~Time to alleviation of the 4 systemic symptoms was analyzed using KM methods; participants who did not experience alleviation of symptoms were censored at the last observation time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir33.8
Placebo53.5

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Time to Alleviation of the Four Systemic Symptoms in Adults Randomized to Baloxavir or Oseltamivir

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~Time to alleviation of the 4 systemic symptoms was defined as the time between the initiation of the study treatment to the time when all 4 systemic symptoms (headache, feverishness or chills, muscle or joint pain, and fatigue) were assessed by the participant as 0 (None) or 1 (Mild) for a duration of at least 21.5 hours.~Time to alleviation of the 4 systemic symptoms was analyzed using KM methods; participants who did not experience alleviation of symptoms were censored at the last observation time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir36.7
Oseltamivir37.4

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Time to Alleviation of Symptoms in Participants Randomized to Baloxavir or Placebo

"Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms).~Time to alleviation of symptoms was defined as the time from the start of the study treatment to the time when all seven influenza-related symptoms were assessed by the participant as absent (0) or mild (1) for at least 21.5 hours.~Time to alleviation of symptoms was analyzed using the Kaplan-Meier (KM) method; participants who did not experience alleviation of symptoms were censored at the last observation time point." (NCT02954354)
Timeframe: Initiation of study treatment up to Day 14

Interventionhours (Median)
Baloxavir53.7
Placebo80.2

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Change From Baseline in Virus RNA (RT-PCR) at Each Time Point in Participants Randomized to Baloxavir or Placebo

Nasopharyngeal swabs (or throat swabs, if nasopharyngeal swabbing was not feasible) were obtained for viral quantitation. Virus RNA is measured by reverse transcription polymerase chain reaction (RT-PCR). (NCT02954354)
Timeframe: Day 1 pretreatment (Baseline) and Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,
Interventionlog₁₀ virus particles/mL (Mean)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir-1.63-2.80-3.07-3.75-3.83-4.43
Placebo-0.56-1.61-1.95-3.04-3.03-4.06

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Change From Baseline in Virus Titer at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir

"Virus titer was quantified from nasopharyngeal swabs (or throat swabs if nasopharyngeal swabbing was not feasible) by tissue culture methods.~If virus titer was less than the lower limit of quantification, the virus titer was imputed 0.7 (TCID₅₀/mL)." (NCT02954354)
Timeframe: Day 1 pretreatment (Baseline) and Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,
Interventionlog₁₀[TCID₅₀/mL] (Mean)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir-4.39-4.79-4.46-4.95-4.56-5.03
Oseltamivir-2.53-4.20-4.63-4.98-4.85-5.22

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Change From Baseline in Virus Titer at Each Time Point in Participants Randomized to Baloxavir or Placebo

"Virus titer was quantified from nasopharyngeal swabs (or throat swabs if nasopharyngeal swabbing was not feasible) by tissue culture methods.~If virus titer was less than the lower limit of quantification, the virus titer was imputed 0.7 (TCID₅₀/mL)." (NCT02954354)
Timeframe: Day 1 pretreatment (Baseline) and Days 2, 3, 4 (optional), 5, 6 (optional), and 9

,
Interventionlog₁₀[TCID₅₀/mL] (Mean)
Day 2Day 3Day 4Day 5Day 6Day 9
Baloxavir-4.45-4.82-4.50-4.95-4.58-5.06
Placebo-1.19-2.88-3.31-4.47-4.68-4.87

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Percentage of Participants Reporting Normal Temperature at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir

Defined as the percentage of patients whose axillary temperature dropped to less than 37ºC after the initiation of study treatment. (NCT02954354)
Timeframe: 12, 24, 36, 48, 72, 96, 120, 144, 168, 192 and 216 hours after the initial dose of study treatment

,
Interventionpercentage of participants (Number)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours144 hours168 hours192 hours216 hours
Baloxavir25.064.381.990.193.893.993.892.893.694.692.8
Oseltamivir28.366.879.189.989.594.995.894.595.995.894.5

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Percentage of Participants Reporting Normal Temperature at Each Time Point in Participants Randomized to Baloxavir or Placebo

Defined as the percentage of patients whose axillary temperature dropped to less than 37ºC after the initiation of study treatment. (NCT02954354)
Timeframe: 12, 24, 36, 48, 72, 96, 120, 144, 168, 192 and 216 hours after the initial dose of study treatment

,
Interventionpercentage of participants (Number)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours144 hours168 hours192 hours216 hours
Baloxavir26.564.380.889.393.792.892.993.493.394.192.5
Placebo25.348.458.367.383.893.992.893.693.693.792.7

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Percentage of Participants Whose Symptoms Were Alleviated at Each Time Point in Adults Randomized to Baloxavir or Oseltamivir

Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms). Alleviation of symptoms was defined as all seven influenza-related symptoms assessed by the participant as absent (0) or mild (1) . (NCT02954354)
Timeframe: 12, 24, 36, 48, 72, 96, 120, 144, 168, 192 and 216 hours after the initial dose of study treatment

,
Interventionpercentage of participants (Number)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours144 hours168 hours192 hours216 hours
Baloxavir8.721.341.151.070.779.886.189.291.490.890.9
Oseltamivir4.922.738.754.473.080.587.091.394.395.596.3

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Percentage of Participants Whose Symptoms Were Alleviated at Each Time Point in Participants Randomized to Baloxavir or Placebo

Participants assessed the severity of seven influenza-associated symptoms (cough, sore throat, headache, nasal congestion, feverishness or chills, muscle or joint pain, and fatigue) on a 4-point scale (with 0 indicating no symptoms, 1 mild symptoms, 2 moderate symptoms, and 3 severe symptoms). Alleviation of symptoms was defined as all seven influenza-related symptoms assessed by the participant as absent (0) or mild (1) . (NCT02954354)
Timeframe: 12, 24, 36, 48, 72, 96, 120, 144, 168, 192 and 216 hours after the initial dose of study treatment

,
Interventionpercentage of participants (Number)
12 hours24 hours36 hours48 hours72 hours96 hours120 hours144 hours168 hours192 hours216 hours
Baloxavir9.723.142.450.768.978.685.589.191.690.991.1
Placebo8.112.823.126.449.569.981.685.488.391.491.9

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Percentage of Participants With Adverse Events (AEs)

(NCT02954354)
Timeframe: From first dose of study drug to Day 22

,,
Interventionpercentage of participants (Number)
Adverse events (AEs)Serious adverse events (SAEs)AEs leading to withdrawal of study drugTreatment-related adverse events (TRAEs)Treatment-related serious adverse eventsTRAEs leading to withdrawal of study drug
Baloxavir20.70.30.34.40.00.0
Oseltamivir24.80.00.48.40.00.2
Placebo24.60.00.33.90.00.3

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Total Number of Days on Ventilation

Total number of days on ventilation for participants who used ventilation, including participants on ventilation at baseline (NCT03040141)
Timeframe: 56 days

Interventiondays (Mean)
VIS410 High Dose5.2
VIS410 Low Dose7.0
VIS410 Total5.9
Placebo11.7

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Viral Nasopharyngeal AUC

The difference between VIS410 + oseltamivir and oseltamivir alone treatment groups in nasopharyngeal qRT-PCR area under the viral load-time curve (AUC) from baseline to Day 5. (NCT03040141)
Timeframe: Day 1 Predose, Day 1 End of Infusion, Day 3, Day 5

InterventionDay*Log10 virus particles/ mL (Mean)
VIS410 High Dose18.329
VIS410 Low Dose15.999
VIS410 Total17.164
Placebo17.727

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Viral Nasopharyngeal AUC by TCID50

The area under the viral load-time curve (AUC) for VIS410 + oseltamivir and oseltamivir alone treatment groups from baseline to Day 5 measured by TCID50 from nasopharyngeal swabs. (NCT03040141)
Timeframe: 5 days

InterventionDay*TCID50 log10/ml (Mean)
VIS410 High Dose3.826
VIS410 Low Dose2.823
VIS410 Total3.324
Placebo3.519

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Viral Nasopharyngeal AUC by TCID50

The area under the viral load-time curve (AUC) for VIS410 + oseltamivir and oseltamivir alone treatment groups from baseline to Day 7 measured by TCID50 from nasopharyngeal swabs. (NCT03040141)
Timeframe: 7 days

InterventionDay*TCID50 log10/ml (Mean)
VIS410 High Dose4.140
VIS410 Low Dose2.886
VIS410 Total3.513
Placebo3.711

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All Cause and Attributable Mortality at Day 14

Number of patients experiencing all-cause and attributable mortality rates at Day 14. Attributable mortality was derived from the Complication of Influenza eCRF; all-cause mortality was derived from Complication of Influenza, Seven-Level Ordinal Scale, AE and Study Completion eCRFs (NCT03040141)
Timeframe: Day 14

,,,
Interventionparticipants (Number)
All-cause mortality Day 14Attributable mortality Day 14
Placebo11
VIS410 High Dose11
VIS410 Low Dose22
VIS410 Total33

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All Cause and Attributable Mortality by Day 28

Number of patients experiencing all-cause and attributable mortality by Day 28. Attributable mortality was derived from the Complication of Influenza eCRF; all-cause mortality was derived from Complication of Influenza, Seven-Level Ordinal Scale, AE and Study Completion eCRFs (NCT03040141)
Timeframe: Day 28

,,,
Interventionparticipants (Number)
All-cause mortality Day 28Attributable mortality Day 28
Placebo22
VIS410 High Dose11
VIS410 Low Dose22
VIS410 Total33

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The Half-life of VIS410 in Participant's Serum

Summary of Serum VIS410 Pharmacokinetic Parameters in PK Population by the half-life (t1/2) of VIS410 in participant's serum. (NCT03040141)
Timeframe: PK samples were collected on days 1, 5, 14, 28 and 56.

InterventionmL/day (Mean)
VIS410 High Dose9.407
VIS410 Low Dose9.839

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All Cause and Attributable Mortality Day 56

Number of patients experiencing all-cause and attributable mortality by Day 56. Attributable mortality was derived from the Complication of Influenza eCRF; all-cause mortality was derived from Complication of Influenza, Seven-Level Ordinal Scale, AE and Study Completion eCRFs (NCT03040141)
Timeframe: Day 56

,,,
Interventionparticipants (Number)
All-cause mortality Day 56Attributable mortality Day 56
Placebo22
VIS410 High Dose11
VIS410 Low Dose22
VIS410 Total33

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Viral Titer in Upper Respiratory Samples by qRT-PCR

The difference between VIS410 + oseltamivir and oseltamivir alone treatment groups in peak viral load by qRT-PCR from nasopharyngeal swabs through Day 14 (NCT03040141)
Timeframe: Day 14

Interventionlog10 virus particles/mL (Mean)
VIS410 High Dose6.479
VIS410 Low Dose6.378
VIS410 Total6.429
Placebo6.169

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Comparison of Ordinal Scale Parameters - Days in Hospital/ICU

"Total number of days in hospital or intensive care for participations who were admitted to Hospital/ICU, including participants in Hospital/ICU at baseline. Better and worse outcome groups defined based on the Seven-Level Ordinal Scale scores, <= 4 Seven-Level Ordinal Scale Score is better; > 4 Seven-Level Ordinal Scale Score is worse group.~Seven-Level Ordinal Scale is a hierarchical scale with the classifications presented from the worst clinical outcome to the best clinical outcome in descending order with 7=death, 6=Intensive care unit (ICU) stay with mechanical ventilation , 5=ICU stay without mechanical ventilation, 4=Non-ICU hospitalization with supplemental oxygen, 3=Non-ICU hospitalization without supplemental oxygen, 2=Discharge with partial resumption of normal activities, 1=Discharge with full resumption of normal activities." (NCT03040141)
Timeframe: 56 days

,,,
Interventiondays (Mean)
> 4 Seven-Level Ordinal Scale Score<= 4 Seven-Level Ordinal Scale Score
Placebo13.88.9
VIS410 High Dose15.98.6
VIS410 Low Dose12.67.9
VIS410 Total14.38.3

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Comparison of Ordinal Scale Parameters - Days in ICU

"Total number of days in intensive care for participants who admitted to ICU, including participants in ICU at baseline. Better and worse outcome groups defined based on the Seven-Level Ordinal Scale scores, <= 4 Seven-Level Ordinal Scale Score is better; > 4 Seven-Level Ordinal Scale Score is worse group.~Seven-Level Ordinal Scale is a hierarchical scale with the classifications presented from the worst clinical outcome to the best clinical outcome in descending order with 7=death, 6=Intensive care unit (ICU) stay with mechanical ventilation , 5=ICU stay without mechanical ventilation, 4=Non-ICU hospitalization with supplemental oxygen, 3=Non-ICU hospitalization without supplemental oxygen, 2=Discharge with partial resumption of normal activities, 1=Discharge with full resumption of normal activities." (NCT03040141)
Timeframe: 56 days

,,
Interventiondays (Mean)
> 4 Seven-Level Ordinal Scale Score
VIS410 High Dose8.5
VIS410 Low Dose6.8
VIS410 Total7.7

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Comparison of Ordinal Scale Parameters - Days in ICU

"Total number of days in intensive care for participants who admitted to ICU, including participants in ICU at baseline. Better and worse outcome groups defined based on the Seven-Level Ordinal Scale scores, <= 4 Seven-Level Ordinal Scale Score is better; > 4 Seven-Level Ordinal Scale Score is worse group.~Seven-Level Ordinal Scale is a hierarchical scale with the classifications presented from the worst clinical outcome to the best clinical outcome in descending order with 7=death, 6=Intensive care unit (ICU) stay with mechanical ventilation , 5=ICU stay without mechanical ventilation, 4=Non-ICU hospitalization with supplemental oxygen, 3=Non-ICU hospitalization without supplemental oxygen, 2=Discharge with partial resumption of normal activities, 1=Discharge with full resumption of normal activities." (NCT03040141)
Timeframe: 56 days

Interventiondays (Mean)
> 4 Seven-Level Ordinal Scale Score"<= 4 Seven-Level Ordinal Scale Score is better"
Placebo10.827.0

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Comparison of Ordinal Scale Parameters - Days on Ventilation

"Total number of days on ventilation for participations who used ventilation, including participants on ventilation at baseline. Better and worse outcome groups defined based on the Seven-Level Ordinal Scale scores, <= 4 Seven-Level Ordinal Scale Score is better; > 4 Seven-Level Ordinal Scale Score is worse group.~Seven-Level Ordinal Scale is a hierarchical scale with the classifications presented from the worst clinical outcome to the best clinical outcome in descending order with 7=death, 6=Intensive care unit (ICU) stay with mechanical ventilation , 5=ICU stay without mechanical ventilation, 4=Non-ICU hospitalization with supplemental oxygen, 3=Non-ICU hospitalization without supplemental oxygen, 2=Discharge with partial resumption of normal activities, 1=Discharge with full resumption of normal activities." (NCT03040141)
Timeframe: 56 days

,,
Interventiondays (Mean)
> 4 Seven-Level Ordinal Scale Score
Total VIS4105.9
VIS410 High Dose5.2
VIS410 Low Dose7.0

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Comparison of Ordinal Scale Parameters - Days on Ventilation

"Total number of days on ventilation for participations who used ventilation, including participants on ventilation at baseline. Better and worse outcome groups defined based on the Seven-Level Ordinal Scale scores, <= 4 Seven-Level Ordinal Scale Score is better; > 4 Seven-Level Ordinal Scale Score is worse group.~Seven-Level Ordinal Scale is a hierarchical scale with the classifications presented from the worst clinical outcome to the best clinical outcome in descending order with 7=death, 6=Intensive care unit (ICU) stay with mechanical ventilation , 5=ICU stay without mechanical ventilation, 4=Non-ICU hospitalization with supplemental oxygen, 3=Non-ICU hospitalization without supplemental oxygen, 2=Discharge with partial resumption of normal activities, 1=Discharge with full resumption of normal activities." (NCT03040141)
Timeframe: 56 days

Interventiondays (Mean)
> 4 Seven-Level Ordinal Scale Score<= 4 Seven-Level Ordinal Scale Score
Placebo8.019.0

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Negative Viral Cultures by Study Day

Number of participants negative for viral titer by study day determined by TCID50 on nominal days 3, 5, 7 (NCT03040141)
Timeframe: Nominal days 3, 5, 7

,,,
InterventionParticipants (Count of Participants)
Participants with negative viral cultures by Day 3.Participants with negative viral cultures by Day 5.Participants with negative viral cultures by Day 7.
Placebo192527
VIS410 High Dose232528
VIS410 Low Dose242627
VIS410 Total475155

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The Number of Participants With Adverse Events and Serious Adverse Events Following Administration of VIS410

Safety and tolerability of 2 dose levels of a single intravenous (IV) dose of VIS410 when administered in combination with oseltamivir in hospitalized participants with influenza A infection. Data presents the count of participants who experienced an adverse event (AE) or serious treatment emergent adverse events (TEAE). (NCT03040141)
Timeframe: 56 days

,,,
InterventionParticipants (Count of Participants)
Participants with adverse eventsParticipants with at least one serious treatment emergent adverse events
Placebo166
VIS410 High Dose166
VIS410 Low Dose224
VIS410 Total3810

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Area Under the Viral Load-Time Curve (VL AUC) Based on qRT-PCR From Nasopharyngeal Swabs Through Day 14

The difference between VIS410 + oseltamivir and oseltamivir alone treatment groups in nasopharyngeal qRT-PCR area under the viral load-time curve (AUC) from baseline to Day 14. (NCT03040141)
Timeframe: Day 1 Predose, Day 1 End of Infusion, Day 3, Day 5, Day 7, Day 14

InterventionDay*vp/mL (Mean)
VIS410 High Dose37.356
VIS410 Low Dose35.172
Total VIS41036.264
Placebo36.668

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Area Under the Viral Load-Time Curve (VL AUC) Based on qRT-PCR From Nasopharyngeal Swabs Through Day 7

The difference between VIS410 + oseltamivir and oseltamivir alone treatment groups in nasopharyngeal qRT-PCR area under the viral load-time curve (AUC) from baseline to Day 7. (NCT03040141)
Timeframe: Day 1 Predose, Day 1 End of Infusion, Day 3, Day 5, Day 7

InterventionDay*vp/mL (Mean)
VIS410 High Dose25.490
VIS410 Low Dose22.394
Total VIS41023.942
Placebo24.337

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Clinical Status Ordinal Scale Mean Area Under the Curve Through Day 14.

Summary of area under the curve (AUC) over time for seven-level ordinal scale. Area under the curve (AUC) is calculated using the linear trapezoidal rule. Seven-Level Ordinal Scale is a hierarchical scale with the classifications presented from the worst clinical outcome to the best clinical outcome in descending order with 7=death, 6=Intensive care unit (ICU) stay with mechanical ventilation , 5=ICU stay without mechanical ventilation, 4=Non-ICU hospitalization with supplemental oxygen, 3=Non-ICU hospitalization without supplemental oxygen, 2=Discharge with partial resumption of normal activities, 1=Discharge with full resumption of normal activities. Time frame is from baseline to day 14. Therefore, maximum and minimum values possible for the AUC Clinical Status Ordinal Scale scores range from 14 to 98. (NCT03040141)
Timeframe: Baseline to Days 14

Interventionday*units on a scale (Mean)
VIS410 High Dose40.3
VIS410 Low Dose38.2
VIS410 Total39.3
Placebo35.8

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Healthcare Resource Utilization. Days in Hospital and/or ICU

Total number of days in hospital and/or ICU from admission to discharge (NCT03040141)
Timeframe: Day 56

InterventionDays (Mean)
VIS410 High Dose11.4
VIS410 Low Dose9.6
VIS410 Total10.5
Placebo9.6

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Median Time to Resolution of Viral Load by Treatment Arm by qRT-PCR - From End of Infusion

Number of days from the end of infusion until virus is no longer detectable (at or below the limit of detection) with no samples following that are greater than the BLQ through the Day 14 (quantitative reverse-transcription polymerase chain reaction - qRT-PCR) (NCT03040141)
Timeframe: 14 days

InterventionDays (Median)
VIS410 High Dose13.5
VIS410 Low Dose12.7
Total VIS41012.7
Placebo11.9

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Median Time to Resolution of Viral Load by Treatment Arm by TCID50 - From End of Infusion

Number of days from the end of infusion until virus is no longer detectable (at or below the limit of detection) with no samples following that are greater than the BLQ through the Day 7 (TCID50) (NCT03040141)
Timeframe: 7 Days

InterventionDays (Median)
VIS410 High Dose1.7
VIS410 Low Dose1.7
VIS410 Total1.7
Placebo1.8

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Median Time to Resolution of Viral Load by Treatment Arm by TCID50 - From Onset of Symptoms

Number of days from the onset of symptoms until virus is no longer detectable (at or below the limit of detection) with no samples following that are greater than the BLQ through the Day 7 (TCID50) (NCT03040141)
Timeframe: 7 Days

InterventionDays (Median)
VIS410 High Dose4.7
VIS410 Low Dose4.8
VIS410 Total4.8
Placebo4.4

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Number of Days to Resumption of Usual Activities

Number of days until resumption of usual activities by treatment group (NCT03040141)
Timeframe: Day 56

Interventiondays (Mean)
VIS410 High Dose11.9
VIS410 Low Dose10.3
VIS410 Total11.1
Placebo11.5

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Time to Cessation of Oxygen Support for Any Patient Requiring Supplemental Oxygen Therapy

Time to cessation of oxygen support in all patients with supplemental oxygen (regardless of oxygen saturation). (NCT03040141)
Timeframe: Baseline to Day 56

InterventionHours (Median)
VIS410 High Dose119.2
VIS410 Low Dose129.7
VIS410 Total124.7
Placebo112.2

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Number of Participants in Whom Peak Viral Load Occurred Post Baseline Measured by qRT-PCR

Number of participants in whom peak viral load is observed post-baseline based on quantitative reverse-transcription polymerase chain reaction (qRT-PCR). Post-baseline was considered the day 3 sample or later. (NCT03040141)
Timeframe: 14 days

InterventionParticipants (Count of Participants)
VIS410 High Dose5
VIS410 Low Dose1
VIS410 Total6
Placebo1

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Peak Viral Load by TCID50

Peak viral load based on TCID50 from nasopharyngeal swabs (NCT03040141)
Timeframe: Day 7

Interventionlog10 TCID50/mL (Mean)
VIS410 High Dose3.047
VIS410 Low Dose2.714
VIS410 Total2.881
Placebo2.604

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The Area Under the Concentration/Time Curve of VIS410 in Participant's Serum

Summary of Serum VIS410 Pharmacokinetic Parameters in PK Population by the area under the concentration/time curve from 0 to infinity (AUC0-inf) of VIS410 in participant's serum. (NCT03040141)
Timeframe: Baseline, end of infusion, Day 5, Day 14, Day 28, Day 56

Interventionday*µg/mL (Mean)
VIS410 High Dose11326.522
VIS410 Low Dose6934.815

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The Clearance Rate (Cl) of VIS410 in Participant's Serum

Summary of Serum VIS410 Pharmacokinetic Parameters in PK Population by the clearance rate (Cl) of VIS410 in participant's serum. (NCT03040141)
Timeframe: PK samples were collected on days 1, 5, 14, 28 and 56.

InterventionmL/day (Mean)
VIS410 High Dose401.652
VIS410 Low Dose325.926

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The Maximum Concentration (Cmax) of VIS410 in Participant's Serum

Summary of Serum VIS410 Pharmacokinetic Parameters in PK Population by maximum concentration (Cmax) of VIS410 in participant's serum. (NCT03040141)
Timeframe: Baseline, end of infusion, Day 5, Day 14, Day 28, Day 56

Interventionµg/mL (Mean)
VIS410 High Dose1301.037
VIS410 Low Dose786.393

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Time to Cessation of Oxygen Support Compared to Oseltamivir Alone Among Patients Requiring Supplemental Oxygen Therapy With Baseline Room Air <= 92%

Time to cessation of O2 support in patients with supplemental oxygen with baseline room air <= 92%. Patients with treatment resulting in a stable SpO2 by pulse oximetry. Stable SpO2 is defined as two consecutive SpO2 values of >92% on room air that are at least 8 hours apart. (NCT03040141)
Timeframe: Baseline to Day 56

InterventionHours (Median)
VIS410 High Dose92.5
VIS410 Low Dose101.3
VIS410 Total97.3
Placebo79.0

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Number of Participants in Whom Peak Viral Load Occurred Post Baseline Measured by TCID50

Number of participants in whom peak viral load occurred post-baseline measured by TCID50. Post-baseline was considered the day 3 sample or later. (NCT03040141)
Timeframe: 56 days

InterventionParticipants (Count of Participants)
VIS410 High Dose1
VIS410 Low Dose0
VIS410 Total1
Placebo1

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Clinical Status Ordinal Scale Mean Area Under the Curve Through Day 7

Summary of area under the curve (AUC) over time for seven-level ordinal scale. Area under the curve (AUC) is calculated using the linear trapezoidal rule. Seven-Level Ordinal Scale is a hierarchical scale with the classifications presented from the worst clinical outcome to the best clinical outcome in descending order with 7=death, 6=Intensive care unit (ICU) stay with mechanical ventilation , 5=ICU stay without mechanical ventilation, 4=Non-ICU hospitalization with supplemental oxygen, 3=Non-ICU hospitalization without supplemental oxygen, 2=Discharge with partial resumption of normal activities, 1=Discharge with full resumption of normal activities. Time frame is from baseline to day 7. Therefore, maximum and minimum values possible for the AUC Clinical Status Ordinal Scale scores range from 7 to 49. (NCT03040141)
Timeframe: Baseline to Day 7

Interventionday*units on a scale (Mean)
VIS410 High Dose23.6
VIS410 Low Dose22.4
VIS410 Total23.0
Placebo21.4

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Time to Clinical Response (4 Out of 5 Vital Signs)

"Median time to clinical response defined by resolution of at least 4 of 5 vital signs:~Afebrile with core temperature ≤ 37.8°C, without use of antipyretics (oral ≤ 37.2°C)~Oxygen saturation ≥ 95% on room air without support or a return to preinfection status, if pre-infection status was < 95%~Pulse rate ≤ 100/min~Systolic blood pressure ≥ 90 mm/Hg, without vasopressor use~Respiratory rate ≤ 24 beats per minute" (NCT03040141)
Timeframe: Day 56

Interventionhours (Median)
VIS410 High Dose2.6
VIS410 Low Dose2.6
VIS410 Total2.6
Placebo2.8

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Time to Complete Clinical Response (Resolution of All Vital Signs)

"Median time to clinical response defined by resolution of at all 5 vital signs:~Afebrile with core temperature ≤ 37.8°C, without use of antipyretics (oral ≤ 37.2°C)~Oxygen saturation ≥ 95% on room air without support or a return to pre-infection status, if pre-infection status was < 95%~Pulse rate ≤ 100/min~Systolic blood pressure ≥ 90 mm/Hg, without vasopressor use~Respiratory rate ≤ 24 beats per minute" (NCT03040141)
Timeframe: Day 56

Interventionhours (Median)
VIS410 High Dose103.0
VIS410 Low Dose114.6
VIS410 Total103.0
Placebo99.8

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Total Number of Days in ICU

Total number of days in intensive care (ICU) for participants who admitted to the ICU, including participants in ICU at baseline (NCT03040141)
Timeframe: 56 days

Interventiondays (Mean)
VIS410 High Dose8.5
VIS410 Low Dose6.8
VIS410 Total7.7
Placebo14.0

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Duration of Fever

Length of time taken by participants to return to afebrile state [tympanic temperature ≤ 37.2°C] and remaining so for at least 21.5 hours. (NCT03629184)
Timeframe: Up to Day 15

Interventionhours (Median)
Baloxavir Marboxil41.2
Oseltamivir46.8

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Duration of Symptoms

The clinical efficacy of baloxavir marboxil is evaluated by duration of symptoms i.e., alleviation of all symptoms as defined by a score of 0 [no problem] or 1 [minor problem] and remaining so for at least 21.5 hours, for all 18 symptoms specified in the CARIFS questionnaire. (NCT03629184)
Timeframe: Up to Day 15

Interventionhours (Median)
Baloxavir Marboxil66.4
Oseltamivir67.9

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Time to Alleviation of Influenza Signs and Symptoms

"Time to alleviation of influenza signs and symptoms is defined as the length of time taken from the start of treatment to the point at which all of the following criteria are met and remain so for at least 21.5 hours:~A score of 0 (no problem) or 1 (minor problem) for cough and nasal symptoms (items 14 and 15 of the Canadian Acute Respiratory Illness and Flu Scale [CARIFS])~A yes response to the following question on the CARIFS: Since the last assessment has the subject been able to return to day care/school, or resume his or her normal daily activity in the same way as performed prior to developing the flu?~First return to afebrile state (tympanic temperature ≤37.2 degree Celsius [°C])" (NCT03629184)
Timeframe: Up to Day 15

Interventionhours (Median)
Baloxavir Marboxil138.1
Oseltamivir150.0

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Time to Cessation of Viral Shedding by RT-PCR

Time to cessation of viral shedding by RT-PCR, in hours, is defined as the time between the initiation of any study treatment and first time when the virus RNA by RT-PCR is below the limit of detection. (NCT03629184)
Timeframe: Day 1 - Day 29

Interventionhours (Median)
Baloxavir Marboxil242.5
Oseltamivir238.9

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Area Under the Curve in the Amount of Virus RNA (RT-PCR)

AUC in virus RNA (RT-PCR) is defined as AUC of change from baseline in the amount of virus RNA (RT-PCR) from Day 1 to Day 10. AUC is calculated using the trapezoidal method similar to AUC in virus titer. (NCT03629184)
Timeframe: Day 1 - Day 10

Interventionlog₁₀ VPs/mL*hours (Mean)
Baloxavir Marboxil-381.53
Oseltamivir-353.31

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Area Under the Concentration to Time Curve From Time 0 to Infinity (AUC0-inf) of S-033447.

Dose groups correspond to body-weight groups. 2mg/kg dose was used for subjects <20 kgs and 40 mg dose was used for subjects >20 kgs. (NCT03629184)
Timeframe: Up to Day 10

Interventionng.hr/mL (Mean)
Non-Asian - 2 mg/kgAsian - 40 mgNon-Asian - 40 mg
Baloxavir Marboxil405066004390

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Area Under the Concentration to Time Curve From Time 0 to Infinity (AUC0-inf) of Baloxavir Marboxil

Dose groups correspond to body-weight groups. 2mg/kg dose was used for subjects <20 kgs and 40 mg dose was used for subjects >20 kgs. (NCT03629184)
Timeframe: Up to Day 10

Interventionng.hr/mL (Mean)
Non-Asian - 2 mg/kgAsian - 40 mgNon-Asian - 40 mg
Baloxavir MarboxilNANANA

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Time to Return to Normal Health and Activity

"Time to Return to Normal health and activity' is identified by a 'Yes' response to the following question on the CARIFS: Since the last assessment has the patient been able to return to day care/school, or resume his or her normal daily activity in the same way as performed prior to developing the flu?" (NCT03629184)
Timeframe: Up to Day 15

Interventionhours (Median)
Baloxavir Marboxil116.5
Oseltamivir111.6

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Plasma Concentrations of Baloxavir Marboxil by Dosage

Dose groups correspond to body-weight groups. 2mg/kg dose was used for subjects <20 kgs and 40 mg dose was used for subjects >20 kgs. (NCT03629184)
Timeframe: 24, 72, 96 and 240 hours post-dose

Interventionng/mL (Mean)
24 - Non-Asian - 2 mg/kg24 - Asian - 40 mg24 - Non-Asian - 40 mg72 - Non-Asian - 2 mg/kg72 - Asian - 40 mg72 - Non-Asian - 40 mg96 - Non-Asian - 2 mg/kg96 - Asian - 40 mg96 - Non-Asian - 40 mg240 - Non-Asian - 2 mg/kg240 - Asian - 40 mg240 - Non-Asian - 40 mg
Baloxavir MarboxilNANANANANANANANANANANANA

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Plasma Concentrations of Baloxavir Marboxil - Sparse PK Population

Results provided by body-weight groups for participants in the Baloxavir Marboxil arm. Values below lower limit of quantification (0.5 ng/mL) are set to zero. (NCT03629184)
Timeframe: Days 1 (Post-Dose), 2, 4, 6 and 10

Interventionng/mL (Mean)
5 - <10 kg (Day 1)5 - <10 kg (Day 2)5 - <10 kg (Day 6)10 - <15 kg (Day 1)10 - <15 kg (Day 2)10 - <15 kg (Day 4)10 - <15 kg (Day 6)10 - <15 kg (Day 10)15 - <20 kg (Day 1)15 - <20 kg (Day 2)15 - <20 kg (Day 4)15 - <20 kg (Day 6)15 - <20 kg (Day 10)>=20 kg (Day 1)>=20 kg (Day 2)>=20 kg (Day 4)>=20 kg (Day 6)>=20 kg (Day 10)
Baloxavir Marboxil0.0000.0000.0000.0730.0000.0000.0000.0000.0900.0000.0000.0000.0000.0480.0000.0000.0000.000

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Plasma Concentrations of S-033447 - Extensive PK Population

Results provided by body-weight groups for participants in the Baloxavir Marboxil arm. Values below lower limit of quantification (0.5 ng/mL) are set to zero. (NCT03629184)
Timeframe: Days 1 (Post-Dose), 2, 4, 6 and 10

Interventionng/mL (Mean)
Day 1, 0.5 - 2 hrs (10 - <15 kg)Day 1, 4 hrs (10 - <15 kg)Day 1, 6 hrs (10 - <15 kg)Day 2 (10 - <15 kg)Day 4 (10 - <15 kg)Day 6 (10 - <15 kg)Day 10 (10 - <15 kg )Day 1, 0.5 - 2 hrs (15 - <20 kg)Day 1, 4 hrs (15 - <20 kg)Day 1, 6 hrs (15 - <20 kg)Day 2 (15 - <20 kg)Day 4 (15 - <20 kg)Day 6 (15 - <20 kg)Day 1, 0.5 - 2 hrs (>=20 kg)Day 1, 4 hrs (>=20 kg)Day 1, 6 hrs ((>=20 kg)Day 2 (>=20 kg)Day 4 (>=20 kg)Day 6 (>=20 kg)
Baloxavir Marboxil10.76849.50041.00028.9332.2303.1310.00093.88372.90080.30042.64012.2002.66319.92369.19865.52757.98021.7756.240

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Percentage of Participants With Positive Influenza Virus Titer at Day 2, 4, 6, 10

(NCT03629184)
Timeframe: Baseline, Day 2, 3 (optional), 4, 6, 10

,
Interventionpercentage of participants (Number)
BaselineDay 2Day 3 (optional)Day 4Day 6Day 10
Baloxavir Marboxil10015.633.326.212.71.6
Oseltamivir10075.750.029.05.70

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Percentage of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An adverse event (AE) is any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and that does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not considered related to the medicinal (investigational) product. A serious adverse event (SAE) is any significant hazard, contraindication, side effect that is fatal or life-threatening, requires hospitalization or prolongation of an existing hospitalization, results in persistent or significant disability/ incapacity, is a congenital anomaly/ birth defect, is medically significant or requires intervention to prevent one or other of the outcomes listed above. (NCT03629184)
Timeframe: Up to Day 29

,
Interventionpercentage of participants (Number)
Adverse Events (AEs)Serious Adverse Events (SAEs)
Baloxavir Marboxil46.10
Oseltamivir53.40

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Percentage of Participants Requiring Antibiotics

(NCT03629184)
Timeframe: Up to Day 29

,
Interventionpercentage of participants (Number)
TotalBronchitisOtitis MediaPneumoniaSinusitis
Baloxavir Marboxil4.902.51.21.2
Oseltamivir4.704.700

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Percentage of Participants Positive by RT-PCR at Day 2, 4, 6, 10, 15, 29

(NCT03629184)
Timeframe: Day 2, 3 (optional), 4, 6, 10, 15 (optional), 29

,
Interventionpercentage of participants (Number)
BaselineDay 2Day 3 (optional)Day 4Day 6Day 10Day 15 (optional)Day 29
Baloxavir Marboxil10095.910089.983.146.540.025.0
Oseltamivir10010010097.075.744.125.00

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Maximum Plasma Concentration (Cmax) of S-033447

Dose groups correspond to body-weight groups. 2mg/kg dose was used for subjects <20 kgs and 40 mg dose was used for subjects >20 kgs. (NCT03629184)
Timeframe: Up to Day 10

Interventionng/mL (Mean)
Non-Asian - 2 mg/kgAsian - 40 mgNon-Asian - 40 mg
Baloxavir Marboxil10911083.2

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Maximum Plasma Concentration (Cmax) of Baloxavir Marboxil

Dose groups correspond to body-weight groups. 2mg/kg dose was used for subjects <20 kgs and 40 mg dose was used for subjects >20 kgs. (NCT03629184)
Timeframe: Up to Day 10

Interventionng/mL (Mean)
Non-Asian - 2 mg/kgAsian - 40 mgNon-Asian - 40 mg
Baloxavir MarboxilNANANA

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Change From Baseline in the Amount of Virus RNA (RT-PCR) at Day 2, 4, 6, 10, 15, 29

If the amount of virus RNA was less than the lower limit of quantification, the amount of virus RNA was imputed as 2.18 for flu A and 2.93 for flu B (log10 virus particles/mL) (NCT03629184)
Timeframe: Baseline, Day 2, 3 (optional), 4, 6, 10, 15 (optional), 29

Interventionlog10 virus particles/mL (Mean)
BaselineDay 2Day 3 (optional)Day 4Day 6Day 10Day 15 (optional)Day 29
Baloxavir Marboxil6.46-1.74-1.78-2.40-2.73-3.55-1.242.18

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Change From Baseline in the Amount of Virus RNA (RT-PCR) at Day 2, 4, 6, 10, 15, 29

If the amount of virus RNA was less than the lower limit of quantification, the amount of virus RNA was imputed as 2.18 for flu A and 2.93 for flu B (log10 virus particles/mL) (NCT03629184)
Timeframe: Baseline, Day 2, 3 (optional), 4, 6, 10, 15 (optional), 29

Interventionlog10 virus particles/mL (Mean)
BaselineDay 2Day 3 (optional)Day 4Day 6Day 10Day 15 (optional)
Oseltamivir6.86-1.12-2.21-2.47-3.32-3.81-4.44

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Change From Baseline in Influenza Virus Titer at Day 2, 4, 6, 10, 15, 29

Influenza virus titer (log10TCID50/ML) is the quantity of influenza virus in a given volume within the samples obtained from nasal swabs. If influenza virus titer was less than the lower limit of quantification, the virus titer was imputed as 0.749 (log10TCID50/mL). A lower value indicates lower viral titer. (NCT03629184)
Timeframe: Baseline, Day 2, 3 (optional), 4, 6, 10, 15 (optional), 29

,
Interventionlog10TCID50/ML (Mean)
BaselineDay 2Day 3 (optional visit)Day 4Day 6Day 10Day 15 (optional visit)Day 29
Baloxavir Marboxil4.43-3.59-2.83-3.53-3.55-3.66-3.75-3.50
Oseltamivir4.27-1.79-2.63-3.27-3.52-3.50-3.63-3.75

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Plasma Concentrations of S-033447 - Sparse PK Population

Results provided by body-weight groups for participants in the Baloxavir Marboxil arm. (NCT03629184)
Timeframe: Days 1 (Post-Dose), 2, 4, 6 and 10

Interventionng/mL (Mean)
5 - <10 kg (Day 1)5 - <10 kg (Day 2)5 - <10 kg (Day 6)10 - <15 kg (Day 1)10 - <15 kg (Day 2)10 - <15 kg (Day 4)10 - <15 kg (Day 6)10 - <15 kg (Day 10)15 - <20 kg (Day 1)15 - <20 kg (Day 2)15 - <20 kg (Day 4)15 - <20 kg (Day 6)15 - <20 kg (Day 10)>=20 kg (Day 1)>=20 kg (Day 2)>=20 kg (Day 4)>=20 kg (Day 6)>=20 kg (Day 10)
Baloxavir Marboxil45.70045.8003.11049.08442.9009.2332.9650.36764.16067.72915.8404.8291.11029.89956.28718.6747.3973.953

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Plasma Concentrations of S-033447 by Dosage

Dose groups correspond to body-weight groups. 2mg/kg dose was used for subjects <20 kgs and 40 mg dose was used for subjects >20 kgs. (NCT03629184)
Timeframe: 24, 72, 96 and 240 hours post-dose

Interventionng/mL (Mean)
24 - Non-Asian - 2 mg/kg24 - Asian - 40 mg24 - Non-Asian - 40 mg72 - Non-Asian - 2 mg/kg72 - Asian - 40 mg72 - Non-Asian - 40 mg96 - Non-Asian - 2 mg/kg96 - Asian - 40 mg96 - Non-Asian - 40 mg240 - Non-Asian - 2 mg/kg240 - Asian - 40 mg240 - Non-Asian - 40 mg
Baloxavir Marboxil55.775.253.213.228.917.907.6119.011.30.9893.311.85

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Time to Maximum Plasma Concentration (Tmax) of S-033447

Dose groups correspond to body-weight groups. 2mg/kg dose was used for subjects <20 kgs and 40 mg dose was used for subjects >20 kgs. (NCT03629184)
Timeframe: Up to Day 10

Interventionhours (Mean)
Non-Asian - 2 mg/kgAsian - 40 mgNon-Asian - 40 mg
Baloxavir Marboxil4.125.505.55

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Area Under the Curve in Virus Titer

Area under the curve (AUC) in virus titer was calculated using the trapezoidal method. (NCT03629184)
Timeframe: Day 1 - Day 29

Interventionlog₁₀[TCID₅₀/mL]*hours (Mean)
Baloxavir Marboxil-863.81
Oseltamivir-849.29

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Time to Cessation of Viral Shedding by Virus Titer

Time to cessation of viral shedding by virus titer is defined as the time, in hours, between the initiation of any study treatment and first time when the influenza virus titer is below the limit of detection. (NCT03629184)
Timeframe: Day 1 - Day 29

Interventionhours (Median)
Baloxavir Marboxil24.2
Oseltamivir75.8

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Time to Maximum Plasma Concentration (Tmax) of Baloxavir Marboxil

Dose groups correspond to body-weight groups. 2mg/kg dose was used for subjects <20 kgs and 40 mg dose was used for subjects >20 kgs. (NCT03629184)
Timeframe: Up to Day 10

Interventionhours (Mean)
Non-Asian - 2 mg/kgAsian - 40 mgNon-Asian - 40 mg
Baloxavir MarboxilNANANA

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Plasma Concentrations of Baloxavir Marboxil - Extensive PK Population

Results provided by body-weight groups for participants in the Baloxavir Marboxil arm. Values below lower limit of quantification (0.5 ng/mL) are set to zero. (NCT03629184)
Timeframe: Days 1 (Post-Dose), 2, 4, 6 and 10

Interventionng/mL (Mean)
Day 1, 0.5 - 2 hrs (10 - <15 kg)Day 1, 4 hrs (10 - <15 kg)Day 1, 6 hrs (10 - <15 kg)Day 2 (10 - <15 kg)Day 4 (10 - <15 kg)Day 6 (10 - <15 kg)Day 10 (10 - <15 kg )Day 1, 0.5 - 2 hrs (15 - <20 kg)Day 1, 4 hrs (15 - <20 kg)Day 1, 6 hrs (15 - <20 kg)Day 2 (15 - <20 kg)Day 4 (15 - <20 kg)Day 6 (15 - <20 kg)Day 1, 0.5 - 2 hrs (>=20 kg)Day 1, 4 hrs (>=20 kg)Day 1, 6 hrs ((>=20 kg)Day 2 (>=20 kg)Day 4 (>=20 kg)Day 6 (>=20 kg)
Baloxavir Marboxil0.0000.0000.0000.0000.0000.0000.0000.0000.0000.0000.0000.0000.0000.0510.0620.0000.0000.0000.000

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