| Bioactivity | Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC50 of 14 ng/mL. | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| 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 (Cmax), 60 μg • h/ml or higher for concentration-time curve over 24 h (AUC24h), 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[1]. | ||||||||||||
| Name | Amenamevir | ||||||||||||
| CAS | 841301-32-4 | ||||||||||||
| Formula | C24H26N4O5S | ||||||||||||
| Molar Mass | 482.55 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |