Amenamevir阿莫奈韦,841301-32-4

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Amenamevir

CAS No. : 841301-32-4

MCE 国际站：Amenamevir

产品活性：Amenamevir 是一种 helicase-primase 抑制剂，对 HSVs 具有强效的抗病毒活性， EC₅₀ 值为 14 ng/mL。

研究领域：Anti-infection

作用靶点：HSV

In Vitro: Amenamevir (ASP2151) inhibits the replication of the HSV strains isolated in Japan and the United States as well as the laboratory-stocked strains. The mean EC₅₀s of Amenamevir against HSV-1 and HSV-2 are 14 (range, 7.7 to 20) and 30 ng/mL (range, 15 to 58), respectively, whereas those of acyclovir (ACV) are 29 (range, 18 to 38) and 71 ng/mL (range, 45 to 95), respectively. The EC₅₀s of Amenamevir against HSV strains are significantly lower than those of ACV.

In Vivo: Amenamevir (ASP2151) administration accelerates the reduction in virus titer in a dose-dependent manner in the range of 3 to 30 mg/kg/day. Amenamevir treatment decreases both lesion scores and HSV-1 titers in a dose-dependent manner, irrespective of the dosing interval. Based on the correlation curves, the PK parameters at which HSV-1 growth is completely suppressed by oral administration of Amenamevir are estimated to be 10,000 ng/mL or higher for the maximum concentration of drug in serum (C_max), 60 μg • h/ml or higher for concentration-time curve over 24 h (AUC_24h), and 21 to 24 h for T_>100 . The mean concentration of Amenamevir in plasma at 5 days postinfection increases in a dose-dependent manner, with doses of 3 mg Amenamevir/g or higher significantly reducing the intradermal HSV-1 titer.

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