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奥司他韦辛酸酯:一种新型长效神经氨酸酶抑制剂,用于治疗流感。

Laninamivir octanoate: a new long-acting neuraminidase inhibitor for the treatment of influenza.

机构信息

Department of Clinical Trials, Center for Advanced Medical Innovation, Kyushu University, 3-1-1 Maidashi Higashi-ku, Fukuoka, Japan.

出版信息

Expert Rev Anti Infect Ther. 2011 Oct;9(10):851-7. doi: 10.1586/eri.11.112.

Abstract

Oseltamivir and zanamivir are well-established and well-researched drugs for the treatment of influenza in Japan and the rest of the world. A new neuraminidase inhibitor, laninamivir octanoate, has been approved for use in Japanese clinics. Laninamivir octanoate is an inhaled drug with unique characteristics. The inhaled laninamivir octanoate is converted into its active form, laninamivir, in the lungs where a high concentration persists for a long period of time. The concentration of laninamivir exceeds the level necessary for influenza virus replication inhibition for at least 5 days, thus influenza can be treated with a single administration. The drug is delivered using one device requiring four inhalations for children and two devices requiring eight inhalations for adults. Clinical trials have shown comparable efficacy for laninamivir octanoate and oseltamivir. Laninamivir octanoate also displayed a sufficient antiviral effect to treat infection with H275Y-mutated oseltamivir-resistant virus. Laninamivir octanoate has displayed clinical efficacy comparable to that of oseltamivir and zanamivir against the H1N1 pandemic influenza strain from 2009, seasonal H3N2 influenza and influenza B viruses. The prophylactic efficacy of laninamivir octanoate has been shown in animal models. The effectiveness of laninamivir against the highly pathogenic avian influenza virus H5N1 has also been shown in vitro and in animal models. A major clinical benefit of this drug is that the single administration is very convenient for both the patient and doctor, which leads to improved compliance. Furthermore, this drug shows promise for the treatment of influenza in future pandemics.

摘要

奥司他韦和扎那米韦是日本和世界其他地区治疗流感的成熟且经过充分研究的药物。一种新型神经氨酸酶抑制剂,八戊烯酸兰尼米韦,已获准在日本临床使用。八戊烯酸兰尼米韦是一种吸入性药物,具有独特的特性。吸入的八戊烯酸兰尼米韦在肺部转化为其活性形式兰尼米韦,在肺部长时间保持高浓度。兰尼米韦的浓度超过抑制流感病毒复制所需的水平至少 5 天,因此可以单次给药治疗流感。该药物使用一种需要儿童进行四次吸入,两种设备需要成人进行八次吸入的设备进行输送。临床试验表明,八戊烯酸兰尼米韦和奥司他韦的疗效相当。八戊烯酸兰尼米韦也显示出足够的抗病毒作用,可以治疗 H275Y 突变奥司他韦耐药病毒感染。八戊烯酸兰尼米韦对 2009 年 H1N1 大流行流感株、季节性 H3N2 流感和 B 型流感病毒的临床疗效与奥司他韦和扎那米韦相当。八戊烯酸兰尼米韦在动物模型中显示出预防效果。体外和动物模型也表明兰尼米韦对高致病性禽流感病毒 H5N1 有效。该药的一个主要临床优势是单次给药对患者和医生都非常方便,从而提高了依从性。此外,该药有望在未来的流感大流行中用于治疗流感。

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