EIDD-2801

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EIDD-2801在體內(nèi)水解成為為N4-羥基胞苷，N4-羥胞苷在組織中被磷酸化為活性5'-三磷酸形式，并摻入新病毒體的基因組中，導(dǎo)致病毒失活突變的積累。

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A remdesivir resistant mutant mouse hepatitis virus has also been shown to have increased sensitivity to N4-hydroxycytidine

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EIDD-2801 is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. It has broad-spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. EIDD-2801 has the potential for COVID-19, and seasonal and pandemic influenza treatment.

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EIDD-2801是核糖核苷類似物EIDD-1931的口服生物可利用的前藥。它具有針對流感病毒和多種冠狀病毒（如SARS-CoV-2，MERS-CoV，SARS-CoV）的廣譜抗病毒活性。 EIDD-2801具有抑制COVID-19以及季節(jié)性和大流行性流感病毒的潛在能力。

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EIDD-2801 is the isopropylester prodrug of N4-hydroxycytidine.1,2 With improved oral bioavailability in non human primates, it is hydrolyzed in vivo, and distributes into tissues where it becomes the active 5’-triphosphate form.The active drug incorporates into the genome of RNA viruses, leading to an accumulation of mutations known as viral error catastrophe. Recent studies have shown EIDD-2801 inhibits replication of human and bat coronaviruses, including SARS-CoV-2, in mice and human airway epithelial cells.1 A remdesivir resistant mutant mouse hepatitis virus has also been shown to have increased sensitivity to N4-hydroxycytidine.

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In vivo：
         50, 150, or 500 mg/kg EIDD-2801 orally administered in the intranasal infection mouse-adapted SARS-CoV (SARS-MA15). The body weight loss compared to vehicle treatment was significantly diminished (50 mg/kg) or prevented (150, 500 mg/kg) with EIDD-2801 prophylaxis. Therefore, EIDD-2801 is robustly antiviral and able to prevent SARS-CoV replication and disease. Altogether, therapeutic EIDD-2801 is potently antiviral against SARS-CoV in vivo but the degree of clinical benefit was dependent on the time of initiation postinfection.

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