Peramivir (BCX-1812, RWJ-270201): potential new therapy for influenza

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Abstract
The cyclopentane peramivir (BCX-1812, RWJ-270201) is a highly selective inhibitor of influenza A and B virus neuraminidases and a potent inhibitor of influenza A and B virus replication in cell culture. The in vitro potency appears to be greater than either zanamivir or oseltamivir carboxylate based on the generally lower EC50 values seen using peramivir in studies run in parallel with each compound. In mice infected with influenza A or B viruses, oral treatment with peramivir was highly effective in preventing death, signs of the disease and in lowering lung virus titres. Similar effects were seen in influenza A virus-infected ferrets. Efficacy was seen in mice when therapy began after virus exposure. Peramivir is non-toxic in mice and rats at doses of ≥ 1000 mg/kg/day and ferrets tolerated doses of ≥ 100 mg/kg/day. Doses of 100 mg/kg/day do not appear to affect murine immune parameters. A pharmacokinetic study of this compound in influenza virus-infected mice indicates once-, twice- or thrice-daily oral...