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首页> 外文期刊>Antiviral chemistry & chemotherapy >Laninamivir and its prodrug, CS-8958: long-acting neuraminidase inhibitors forthe treatment of influenza.
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Laninamivir and its prodrug, CS-8958: long-acting neuraminidase inhibitors forthe treatment of influenza.

机译：Laninamivir及其前药CS-8958：长效神经氨酸酶抑制剂，可用于治疗流感。

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摘要

Oseltamivir and zanamivir are currently licensed worldwide for influenzatreatment and chemoprophylaxis. Both drugs require twice-daily administration for5 days for treatment. A new influenza drug, laninamivir (code name R-125489), andits prodrug form, CS-8958 (laninamivir octanoate or laninamivir prodrug), whichare long-acting neuraminidase inhibitors, are introduced in this review.Laninamivir potently inhibited the neuraminidase activities of various influenzaA and B viruses, including subtypes N1-N9, pandemic (2009) H1N1 virus, highlypathogenic avian influenza (HPAI) H5N1 viruses and oseltamivir-resistant viruses.Because of the long retention of laninamivir in mouse lungs after an intranasaladministration of CS-8958, therapeutic administration of a single dose of CS-8958showed superior efficacy to repeated administrations of zanamivir or oseltamivirin animal infection models for influenza A and B viruses. These include pandemic(2009) H1N1 virus and HPAI H5N1 virus. Prophylactic single administration ofCS-8958, as early as 7 days prior to infection, also showed superior efficacy.Finally, the potential of a single inhalation of CS-8958 for influenza patientswas demonstrated by clinical studies, and CS-8958 has been approved and iscommercially available as Inavir(?) (Daiichi Sankyo Co., Ltd, Tokyo) in Japan.
机译：奥司他韦和扎那米韦目前在全球范围内获得流感治疗和化学预防的许可。两种药物都需要每天两次给药，连续5天进行治疗。本文介绍了一种长效神经氨酸酶抑制剂的新型流感药物拉尼米韦（代号R-125489）及其前药形式CS-8958（拉尼米韦辛酸酯或拉尼米韦前药）。拉尼米韦有效抑制了各种神经氨酸酶活性。甲型和乙型流感病毒，包括N1-N9亚型，大流行性（2009）H1N1病毒，高致病性禽流感（HPAI）H5N1病毒和耐奥司他韦的病毒。鼻内施用CS-8958后，兰尼米韦长期保留在小鼠肺中，单剂量CS-8958的治疗性给药显示出比重复给药扎那米韦或奥司他韦林动物感染模型更有效的甲型和乙型流感病毒。其中包括大流行（2009）H1N1病毒和HPAI H5N1病毒。早在感染前7天就对CS-8958进行预防性单次给药也显示出优异的疗效。最后，临床研究证明了CS-8958对流感患者单次吸入的潜力，并且CS-8958已被批准并在商业上应用在日本以Inavir（？）（东京第一化学工业有限公司）的形式提供。

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