Amenamevir

Amenamevir, also known as ASP2151, is a herpes virus helicase-primase inhibitor. ASP2151 had significantly better anti-HSV activity against herpes simplex keratitis than valacyclovir and acyclovir after systemic or topical use. (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 (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.

841301-32-4

ASP2151 | ASP-2151 | ASP 2151 | Amenamevir

Pharmacology & Drug Discovery

>98% (HPLC)

DMSO : ≥ 50 mg/mL; 103.62 mM

Cc1c (c (ccc1) C) N (CC (=O) Nc1ccc (cc1) c1nocn1) C (=O) C1CCS (=O) (=O) CC1

C24H26N4O5S

482.56

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.