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Curr Med Chem. 2000 Jun;7(6):663-72.

Discovery and development of GS 4104 (oseltamivir): an orally active influenza neuraminidase inhibitor.

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Gilead Sciences Inc., 333 Lakeside Drive, Foster City, California, 94404, USA.


Rational drug design utilizing available X-ray crystal structures of sialic acid analogues bound to the active site of influenza virus neuraminidase has led to the discovery of a series of potent carbocyclic influenza neuraminidase inhibitors. From this series, GS 4104 (oseltamivir, TAMIFLU ) has emerged as a promising antiviral for the treatment and prophylaxis of human influenza infection. This article will summarize the design, discovery, and development of oseltamivir as an oral therapeutic to treat influenza infection.

[Indexed for MEDLINE]

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