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Zanamivir (INN) (IPA: ) is a neuraminidase inhibitor used in the treatment of and prophylaxis of both Influenzavirus A and Influenzavirus B. Zanamivir was the first neuraminidase inhibitor commercially developed. It is currently marketed by GlaxoSmithKline under the trade name Relenza.

Development


Zanamivir was developed in 1989 by scientists at the Australian biotechnology company Biota, working in conjunction with the CSIRO and the Victorian College of Pharmacy. The development was part of Biota's ongoing program to develop antiviral agents through rational drug design.

The strategy relied on the availability of the crystal structure of influenza neuraminidase which was achieved by x-ray crystallography. It was known as far back as 1974 that 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (DANA), a sialic acid analogue, was an inhibitor of neuraminidase.Meindl P, Bodo G, Palese P, Schulman J, Tuppy H. Inhibition of neuraminidase activity by derivatives of 2-deoxy-2,3-dehydro-N-acetylneuraminic acid. Virology 1974;58(2):457-463. PMID 4362431 Using the crystal structure of neuraminidase and DANA as a starting point, the researchers employed a computer-aided process to attempt to design a molecule which better fitted (and therefore inhibited) the active site of neuraminidase. Zanamivir, a transition-state analogue inhibitor of neuraminidase, was the result.von Itzstein M, Wu W-Y, Kok GB, Pegg MS, Dyason JC, Jin B, et al. Rational design of potent sialidase-based inhibitors of influenza virus replication. Nature 1993;363(6428):418-423. PMID 8502295

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DrugDigest: Zanamivir (Relenza) - Information on dosage, usage, side effects, interactions, and drug comparisons, including generics when available.

MEDLINEplus: Zanamivir (Inhalation--Systemic) - Fact sheet on this medication (marketed as Relenza), including proper use, contraindications, and side effects.
Meta Description: [ Zanamivir (Inhalation—Systemic) ]

500 Relenza (Zanamivir) - U.S. Food and Drug Administration information, including labeling requirements and regulatory approval documents.
Meta Description: [ Relenza (zanamivir) Information ]

Relenza Consumer Information - FDA - Patient FAQ in html format with a link to approved labeling in pdf format.

404 The development of Relenza for the treatment of Influenza - Provides information on the influenza virus and details how the drug Relenza was developed using computational chemistry. Also describes how the action of the drug prevents the flu virus replicating.
Meta Description: [ The Development of Relenza for the Treatmant of Influenza ]

Zanamivir (Relenza) - Influenza Treatment - Medinfo's patient information on this new treatment for influenza, including its use, its cost, and its availability in the United Kingdom.
Meta Description: [ Medinfo's patient information on the issues around zanamivir (Relenza), a new drug, just released in the UK, for the treatment of flu (influenza). ]

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