Thursday, March 14, 2013
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Influenza virus neuraminidase
In vitro, cell culture and mouse studies suggest covalent
neuraminidase inhibitors could be useful for treating influenza infection. In
vitro, a class of 2,3-difluorosialic acid derivatives
showed longer-lasting inhibition of neuraminidase activity than the marketed
neuraminidase inhibitors Relenza
In cell culture, the lead compound showed more potent inhibition of
Relenza-resistant influenza A virus and influenza B virus than Relenza. In a
mouse model for lethal influenza infection, the lead compound decreased viral
load and increased survival with an effect comparable to that of Relenza.
Next steps include out-licensing and preclinical development of the lead
Relenza is marketed by GlaxoSmithKline
plc and Biota
Pharmaceuticals Inc. to treat and prevent influenza A.
Tamiflu is marketed by Roche
Sciences Inc. to treat and prevent influenza A.
Two other neuraminidase inhibitors are marketed outside the U.S. to treat and
prevent influenza infection: PeramiFlu
peramivir from BioCryst
Pharmaceuticals Inc., Green
Cross Corp. and Shionogi
& Co. Ltd., and Inavir
Sankyo Co. Ltd. and Biota.
Published online March 14, 2013
Patent pending; available
for licensing from CDRD
Kim, J.-H. et al.
published online Feb. 21, 2013;
Contact: Stephen G. Withers,
The University of British Columbia, Vancouver, British Columbia, Canada
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