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Pimodivir Polymerase basic protein 2 (PB2) (influenza virus) inhibitor Treatment of influenza A infection

机译:Pimodivir聚合酶碱性蛋白2(PB2)(流感病毒)抑制剂治疗流感感染

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摘要

Pimodivir (VX-787, AU-63623872) is an investigational anti-influenza drug, currently undergoing clinical development. Pimodivir is a non-nucleoside analogue that targets the cap-binding activity of the influenza A virus PB2 polymerase subunit. It is potent against influenza A, including against adamantanes and neuraminidase inhibitor-resistant strains. In a phase IIb study of naturally acquired influenza A virus infection, a statistically significant and dose-dependent decrease in virus load was observed. Diarrhea was the most common adverse event reported and was typically mild. Pimodivir is a substrate for CYP3A4 metabolism but itself has no inhibitory or induction effects on the isoenzyme. It is also a substrate for P-glycoprotein and OATP1B1 and also inhibits P-glycoprotein. Specific drug interactions have not yet been studied. Pimodivir 600 mg twice daily for 5 days has been selected and is undergoing further evaluation in phase III clinical trials.
机译:Pimodivir(VX-787,AU-63623872)是目前正在进行临床发展的研究抗流感药物。 Pimodivir是一种非核苷类似物,其靶向流感病毒PB2聚合酶亚基的帽结合活性。 它有效地对抗流感A,包括针对杀菌和神经氨酸酶抑制剂抗性菌株。 在IIB的IIB研究中,天然获得的流感病毒感染,观察到病毒载荷的统计学显着性和剂量依赖性降低。 腹泻是报告的最常见的不良事件,通常是轻微的。 Pimodivir是CYP3A4代谢的底物,但本身对同工酶没有抑制或诱导效应。 它也是p-糖蛋白和oatp1b1的基材,并且还抑制p-糖蛋白。 尚未研究具体的药物相互作用。 PimodiviR每天两次600毫克,已选择5天,并在III期临床试验中进行进一步评估。

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