巴洛昔韦是一种新型的特异性抗流感药物

N. V. Breslav, A. V. Ignatjeva, E. Mukasheva, Anastasiya S. Krepkaia, E. Burtseva
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摘要

介绍。Baloxavir marboxil是首个具有独特单剂量的抗病毒药物,于2020年9月在俄罗斯注册,商品名为xofluusa,用于治疗甲型和乙型流感病毒引起的感染。本文综述了国外有关巴洛昔韦抗流感活性的研究进展。对不同作者发表的科学论文的数据进行了分析,并考虑了体外结果和临床数据,这有助于就使用该药物治疗和接触后预防流感提出建议。审查。Baloxavir marboxil是流感病毒RNA聚合酶复合体中一种特异性酶的选择性低分子量抑制剂,对奥司他韦耐药菌株有效。结合表型分析和基于PA聚合酶蛋白序列的分析表明,对该药敏感性降低的病毒频率仍然很低。许多研究表明,在不同人群(无风险因素和高危患者)中,流感治疗的安全性和有效性。结论。Baloxavir marboxil在治疗过程的早期阶段阻止流感病毒的复制,从而在第一天终止病毒的释放,并在第二天显著缓解患者的病情。应密切监测药物的抗病毒活性,特别是在12岁以下儿童群体和免疫力较弱的人群中,以便制定临床建议,以防止甲型和乙型流感病毒在PA中形成I38 (I38T/F/M/S/L/V)替代品,从而降低其对药物的敏感性。
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BALOXAVIR MARBOXIL IS A NEW SPECIFIC ANTI–INFLUENZA DRUG
Introduction. Baloxavir marboxil is the first antiviral drug with a unique single dose, registered in Russia in September 2020 under the trade name Xoflusa for the treatment of infection caused by influenza A and B viruses. The article presents an overview of studies on the anti-influenza activity of Baloxavir marboxil by foreign colleagues. The data of scientific articles by different authors were analyzed and in vitro results and clinical data were taken into account, which can help in making recommendations for the use of the drug for the treatment and post-exposure prophylaxis of influenza. Review. Baloxavir marboxil acts as a selective low molecular weight inhibitor of an enzyme specific to the influenza virus in the viral RNA polymerase complex and is effective against strains resistant to oseltamivir. Combined phenotypic analysis and analysis based on the sequence in the protein of PA polymerase showed that the frequency of viruses showing reduced susceptibility to the drug remains low. Numerous studies have demonstrated the safe profile and productivity of influenza treatment in patients of various population groups (without risk factors and high-risk patients). Conclusions. Baloxavir marboxil stops the replication of the influenza virus in the early stages of the process, which leads to the termination of its release during the first day, and on the second day significantly relieves the patient's condition. Monitoring of the antiviral activity of the drug, especially in groups of children under the age of 12 and people with weakened immunity, should be closely monitored in order to develop clinical recommendations to prevent the formation of substitutions I38 (I38T/F/M/S/L/V) in the PA of influenza A and B viruses that reduce their sensitivity to the drug.
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