The FDA has approved two neuraminidase inhibitors, zanamivir (Relenza), and oseltamivir phosphate (Tamiflu) for the treatment of influenza. Both drugs are effective against a wide range of influenza viruses. Both compounds reduce the symptoms of the disease such as fever, headache, myalgia, and cough by 1.5-2 days if taken within 24-48 h of the onset of symptoms. The oral bioavailability of zanamivir is low. Hence, it is administered topically using a specifically designed inhaler at a dose of 10 mg twice daily for five days. Oseltamivir is given orally in 75 mg dose twice a day for five days. Zanamivir is approved only for treatment, while oseltamivir is approved both for treatment and prophylactic use.
Peramivir (BCX-1812, 24a) is another potent neuraminidase inhibitor that has been shown to be very effective in mouse influenza models [72-77]. In phase III clinical trials, the compound did not meet its primary end point probably due to its limited oral bioavailability. Using different routes of administration, intravenous and intramuscular, Phase I clinical trials have been initiated recently .
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