Favipiravir (T-705), a broad spectrum inhibitor of viral RNA polymerase.
Favipiravir (T-705), a broad spectrum inhibitor of viral RNA polymerase.
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DOI：
10.2183/pjab.93.027
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Nakamura T
中科院分区：
文献类型：
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作者：
Furuta Y;Komeno T;Nakamura T
法匹拉韦（T-705; 6-氟-3-羟基-2-吡嗪甲酰胺）是一种选择性和有效抑制RNA病毒的RNA依赖性RNA聚合酶（RdRp）的抗病毒剂。Favipiravir是富山化学公司通过筛选针对流感病毒的抗病毒活性的化学文库而发现的，Ltd.法匹拉韦经过细胞内磷酸核糖基化成为活性形式法匹拉韦-RTP（法匹拉韦呋喃核糖基-5 ′-三磷酸），其被RdRp识别为底物，并抑制RNA聚合酶活性。由于RdRp的催化结构域在各种类型的RNA病毒中是保守的，因此这种作用机制支持了法匹拉韦更广谱的抗病毒活性。法匹拉韦对多种类型和亚型的流感病毒有效，包括对现有抗流感药物耐药的毒株。值得注意的是，法匹拉韦显示出对其他RNA病毒（如沙粒病毒、布尼亚病毒和丝状病毒）的抗病毒活性，已知所有这些病毒均可引起致死性出血热。这些独特的抗病毒特性将使法匹拉韦成为一种潜在的有前途的药物，用于治疗特定的不可治疗的RNA病毒感染。
Favipiravir (T-705; 6-fluoro-3-hydroxy-2-pyrazinecarboxamide) is an anti-viral agent that selectively and potently inhibits the RNA-dependent RNA polymerase (RdRp) of RNA viruses. Favipiravir was discovered through screening chemical library for anti-viral activity against the influenza virus by Toyama Chemical Co., Ltd. Favipiravir undergoes an intracellular phosphoribosylation to be an active form, favipiravir-RTP (favipiravir ribofuranosyl-5′-triphosphate), which is recognized as a substrate by RdRp, and inhibits the RNA polymerase activity. Since the catalytic domain of RdRp is conserved among various types of RNA viruses, this mechanism of action underpins a broader spectrum of anti-viral activities of favipiravir. Favipiravir is effective against a wide range of types and subtypes of influenza viruses, including strains resistant to existing anti-influenza drugs. Of note is that favipiravir shows anti-viral activities against other RNA viruses such as arenaviruses, bunyaviruses and filoviruses, all of which are known to cause fatal hemorrhagic fever. These unique anti-viral profiles will make favipiravir a potentially promising drug for specifically untreatable RNA viral infections.