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Zanamivir

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Zanamivir, better known as Relenza, (3b7e)

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Better Known as: Relenza

  • Marketed By: GlaxoSmithKline
  • Major Indication: Influenza Infection
  • Drug Class: Neuraminidase Inhibitor
  • Date of FDA Approval (Patent Expiration): 1999 (2016)
  • 2009 Sales:$1.1 Billion
  • Importance: It was the first neuraminidase inhibitor to be approved by the FDA, followed a few months later by Oseltamivir. Newer strains of flu virus, primarily H1N1, have developed varying levels of resistance to Oseltamivir, but a lesser extent to Zanamivir. Sales have increased dramatically since 2006 with scares of bird flu and swine flu pandemics.
  • See Pharmaceutical Drugs for more information about other drugs and diseases.

Mechanism of Action

Viral Neuraminidase is found on the surface of the influenza virus. When the influenza virus replicates, it attaches itself to the host cell surface using hemagglutinin.

Pharmacokinetics

Neuraminidase Inhibitor Pharmacokinetics
Parameter Zanamivir Oseltamivir
Tmax (hr) 1.25 1.5
Cmax (ng/ml) 31.6 57
Bioavailability (%) 2 75
Protein Binding (%) 10 42
T1/2 (hr) 3 3.2
AUC (ng/ml/hr) 185 204
Clearance (L/h) 54.1 18.8
Dosage (mg) 10 300
Metabolism None Hepatic

For References to Pharmacokinetic data, see: References

References


Proteopedia Page Contributors and Editors (what is this?)

David Canner, Alexander Berchansky

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