生物活性 | |||
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描述 | Seasonal and pandemic influenza are the two faces of respiratory infections caused by influenza viruses in humans. Influenza virus infection may result in pneumonia and acute respiratory failure, frequently complicated by bacterial coinfection[1]. Baloxavir marboxil is a small molecule inhibitor of the cap-dependent endonuclease of influenza A and B viruses. Baloxavir marboxil is a prodrug that is metabolised to an active form (known as S‐033447) which is highly effective at inhibiting a number of different influenza A and B viruses in vitro[2]. In a mouse model of infection, a single dose of Baloxavir marboxil was found to reduce viral load by 2 logs and reduced mortality compared to mice being treated with oseltamivir. In a phase II study of S‐033188, patients with uncomplicated influenza were randomised to three different doses (10 mg, 20 mg and 40 mg) and compared to placebo. All three doses resulted in significant reductions in time to alleviation of symptoms and reduced virus titres at 24 and 48 hours post‐treatment compared to placebo[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.75mL 0.35mL 0.17mL |
8.75mL 1.75mL 0.87mL |
17.50mL 3.50mL 1.75mL |
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