Page last updated: 2024-11-12

tamiphosphor

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

tamiphosphor: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10336127
CHEMBL ID2206456
SCHEMBL ID3786197
MeSH IDM0524017

Synonyms (5)

Synonym
SCHEMBL3786197
tamiphosphor
bdbm50401399
chembl2206456 ,
[(3r,4r,5s)-4-acetamido-5-amino-3-pentan-3-yloxycyclohexen-1-yl]phosphonic acid

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" 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
)
0.56

Bioavailability

ExcerptReferenceRelevance
" The absolute oral bioavailability of these compounds was lower than 12%."( Development of oseltamivir phosphonate congeners as anti-influenza agents.
Chen, CA; Chen, CL; Cheng, TJ; Cheng, YS; Fang, JM; Hsieh, WC; Hu, OY; Huang, PW; Jan, JT; Lin, WH; Shie, JJ; Tarbet, EB; Wang, SY; Weinheimer, S; Wong, CH, 2012
)
0.38

Dosage Studied

ExcerptRelevanceReference
" 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
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))IC50 (µMol)0.00180.00000.503510.0000AID714642
NeuraminidaseInfluenza A virus (A/Wilson-Smith/1933(H1N1))IC50 (µMol)0.49770.00040.13430.9930AID713858; AID714639
Neuraminidase Influenza A virus (A/udorn/1972(H3N2))IC50 (µMol)0.00160.00160.00910.0229AID714636
Neuraminidase Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))IC50 (µMol)0.00050.00020.00130.0048AID714644
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (58)

Assay IDTitleYearJournalArticle
AID715149Oral bioavailability in Sprague-Dawley rat at 1 mg/kg2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715137AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv administered as single bolus dose2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715106Antiviral activity against Influenza A virus (A/reassortant/NIBRG-14(Viet Nam/1194/2004 x Puerto Rico/8/1934)(H5N1)) infected n BALB/c mouse assessed as protection against virus-induced mortality at 0.1 mg/kg/day, po bid for 5 days followed by viral infec2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713883Antiviral activity against oseltamivir-resistant Influenza A virus A/WSN/1933/H275Y(H1N1) infected n BALB/c mouse assessed as protection against virus-induced body weight loss at 0.1 mg/kg/day, po bid for 5 days followed by viral infection at 4 hrs post f2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714620Acute toxicity in CD1 mouse assessed as tremor at 300 to 1000 mg/kg, iv measured within 2 days2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713882Antiviral activity against oseltamivir-resistant Influenza A virus A/WSN/1933/H275Y(H1N1) infected n BALB/c mouse assessed as protection against virus-induced mortality at 0.1 mg/kg/day, po bid for 5 days followed by viral infection at 4 hrs post first do2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714624Acute toxicity in CD1 mouse assessed as hunched posture at 300 to 1000 mg/kg, iv measured within 2 days2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715136AUC (0 to t) in Sprague-Dawley rat at 1 mg/kg, iv administered as single bolus dose2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715103Antiviral activity against Influenza A virus (A/reassortant/NIBRG-14(Viet Nam/1194/2004 x Puerto Rico/8/1934)(H5N1))infected n BALB/c mouse assessed as protection against virus-induced body weight loss at 10 mg/kg/day, po bid for 5 days followed by viral 2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715102Antiviral activity against Influenza A virus (A/reassortant/NIBRG-14(Viet Nam/1194/2004 x Puerto Rico/8/1934)(H5N1))infected n BALB/c mouse assessed as protection against virus-induced mortality at 10 mg/kg/day, po bid for 5 days followed by viral infecti2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715107Antiviral activity against Influenza A virus (A/reassortant/NIBRG-14(Viet Nam/1194/2004 x Puerto Rico/8/1934)(H5N1))infected n BALB/c mouse assessed as protection against virus-induced body weight loss at 0.1 mg/kg/day, po bid for 5 days followed by viral2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715148Mean residence time in Sprague-Dawley rat at 1 mg/kg, po2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714644Inhibition of Influenza A virus (A/reassortant/NIBRG-14(Viet Nam/1194/2004 x Puerto Rico/8/1934)(H5N1)) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prio2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713862Antiviral activity against Influenza A virus A/Panama/2007/99(H3N2) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713864Antiviral activity against Influenza B virus B/Florida/4/2006 infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715139Apparent oral clearance in Sprague-Dawley rat at 1 mg/kg, iv administered as single bolus dose2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713861Antiviral activity against Influenza A virus A/Victoria/3/75(H3N2) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713859Antiviral activity against influenza A virus A/CA/07/2009 (pandemic H1N1) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714637Antiviral activity against influenza A virus A/WSN/1933(H1N1) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715142Bioavailability in Sprague-Dawley rat at 1 mg/kg, iv administered as single bolus dose2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714632Acute toxicity in CD1 mouse assessed as lesions at 300 to 1000 mg/kg, iv after 15 days by necropsy analysis2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714636Inhibition of Influenza A virus A/Udorn/1972(H3N2) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714640Inhibition of Influenza B virus B/Taiwan/70641/2004 neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713880Antiviral activity against oseltamivir-resistant Influenza A virus A/WSN/1933/H275Y(H1N1) infected n BALB/c mouse assessed as protection against virus-induced body weight loss at 10 mg/kg/day, po bid for 5 days followed by viral infection at 4 hrs post fi2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715147Apparent oral volume of distribution in Sprague-Dawley rat at 1 mg/kg2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713870Antiviral activity against Influenza A virus A/WSN/1933(H1N1) infected in BALB/c mouse assessed as protection against virus-induced body weight loss at 10 mg/kg/day, po bid for 5 days followed by viral infection at 4 hrs post first dose measured 8 days po2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715151Tmax in Sprague-Dawley rat at 1 mg/kg, po2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715138Half life in Sprague-Dawley rat at 1 mg/kg, iv administered as single bolus dose2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715105Antiviral activity against Influenza A virus (A/reassortant/NIBRG-14(Viet Nam/1194/2004 x Puerto Rico/8/1934)(H5N1))infected n BALB/c mouse assessed as partial protection against virus-induced body weight loss at 1 mg/kg/day, po bid for 5 days followed by2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715125Metabolic stability in fresh human liver microsomes assessed as compound remaining at 80 ng/mL measured at 1 hr in presence of CYP450 and NADPH2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713863Antiviral activity against Influenza A virus A/Duck/MN/1525/81(H5N1) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714622Acute toxicity in CD1 mouse assessed as body jerks at 300 to 1000 mg/kg, iv measured within 2 days2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715146Apparent oral clearance in Sprague-Dawley rat at 1 mg/kg2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714642Inhibition of Influenza A virus A/Taiwan/3446/2002(H3N2) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713881Antiviral activity against oseltamivir-resistant Influenza A virus A/WSN/1933/H275Y(H1N1) infected n BALB/c mouse assessed as protection against virus-induced mortality at 1 to 10 mg/kg/day, po bid for 5 days followed by viral infection at 4 hrs post firs2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713858Inhibition of wild type Influenza A virus A/WSN/1933(H1N1) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713871Antiviral activity against Influenza A virus A/WSN/1933(H1N1) infected in BALB/c mouse assessed as protection against virus-induced mortality at 1 mg/kg/day, po bid for 5 days followed by viral infection at 4 hrs post first dose measured after 2 to 14 day2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714625Acute toxicity in CD1 mouse assessed as piloerection at 300 to 1000 mg/kg, iv measured within 2 days2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713860Antiviral activity against Influenza A virus A/Brisbane/10/2007(H3N2) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715150Cmax in Sprague-Dawley rat at 1 mg/kg, po2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID1317961Binding affinity to Influenza A virus (A/California/07/2009(H1N1)) recombinant wild type N-terminal FLAG-tagged neuraminidase catalytic domain transfected in Drosophila Schneider S2 cells at 76 to 93 uM by isothermal titration calorimetric method2016European journal of medicinal chemistry, Oct-04, Volume: 121Kinetic, thermodynamic and structural analysis of tamiphosphor binding to neuraminidase of H1N1 (2009) pandemic influenza.
AID714641Antiviral activity against oseltamivir-resistant Influenza A virus A/Hong Kong/2369/09/H275Y(H1N1) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713865Antiviral activity against Influenza B virus B/Sichuan/379/99 infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715144AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, po2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714638Antiviral activity against oseltamivir-resistant Influenza A virus A/WSN/1933/H275Y (pandemic H1N1) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 to 72 hrs by CellTiter 96 aqueous assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714623Acute toxicity in CD1 mouse assessed as hypoactivity at 300 to 1000 mg/kg, iv measured within 2 days2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713869Antiviral activity against Influenza A virus A/WSN/1933(H1N1) infected in BALB/c mouse assessed as protection against virus-induced mortality at 10 mg/kg/day, po bid for 5 days followed by viral infection at 4 hrs post first dose measured 8 days post infe2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715145Half life in Sprague-Dawley rat at 1 mg/kg, po2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
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.
AID714621Acute toxicity in CD1 mouse assessed as convulsion at 300 to 1000 mg/kg, iv measured within 2 days2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714639Inhibition of oseltamivir-resistant Influenza A virus A/WSN/1933/H275Y(H1N1) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by 2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID714618Acute toxicity in CD1 mouse assessed as mortality at 750 mg/kg, iv2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715140Apparent oral volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv administered as single bolus dose2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715104Antiviral activity against Influenza A virus (A/reassortant/NIBRG-14(Viet Nam/1194/2004 x Puerto Rico/8/1934)(H5N1)) infected n BALB/c mouse assessed as partial protection against virus-induced mortality at 1 mg/kg/day, po bid for 5 days followed by viral2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID713868Cytotoxicity against MDCK cells at 100 uM2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
AID715141Mean residence time in Sprague-Dawley rat at 1 mg/kg, iv administered as single bolus dose2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
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.
AID715143AUC (0 to t) in Sprague-Dawley rat at 1 mg/kg, po2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Development of oseltamivir phosphonate congeners as anti-influenza agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (9.09)29.6817
2010's8 (72.73)24.3611
2020's2 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]