Oseltamivir (trade name Tamiflu) is an ethyl ester prodrug of Ro 64-0802, a neuraminidase inhibitor, serving as a competitive inhibitor of the activity of the viral neuraminidase (NA) enzyme upon sialic acid, found on glycoproteins on the surface of normal host cells. By blocking the activity of the enzyme, oseltamivir prevents new viral particles from being released by infected cells. Oral administration of oseltamivir delivers the active antiviral Ro 64-0802 to the bloodstream, and thus all sites of influenza infection (lung, nasal mucosa, middle ear) are accessible. Oseltamivir (Tamiflu) was the first orally active neuraminidase inhibitor commercially developed. Treatment with oseltamivir does not seem to adversely affect the primary in vivo cellular immune responses to influenza virus infection.
Food Funct. 2016 Mar 24.
Neuraminidase inhibition of Dietary chlorogenic acids and derivatives - potential antivirals from dietary sources.
Oseltamivir purchased from AbMole
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|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Crystal structures of oseltamivir-resistant influenza virus neuraminidase mutants.
Collins PJ, et al. Nature. 2008 Jun 26;453(7199):1258-61. PMID: 18480754.
Clinical pharmacokinetics of the prodrug oseltamivir and its active metabolite Ro 64-0802.
He G, et al. Clin Pharmacokinet. 1999 Dec;37(6):471-84. PMID: 10628898.
ML-281 is a potent ans selective STK33 inhibitor with IC50 value of 14 nM.
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