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。

Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC 50 of 14 ng/mL.

Solid

HSV-1 7.7-20 ng/mL (IC50) HSV-2 15-58 ng/m

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Katsumata K, et al. Pharmacokinetics and pharmacodynamics of ASP2151, a helicase-primase inhibitor, in a murine model of herpes simplex virus infection. Antimicrob Agents Chemother. 2013 Mar;57(3):1339-46.

In Vitro: DMSO : ≥ 50 mg/mL (103.62 mM)配制储备液