[CAS NO. 841301-32-4] Amenamevir
PRODUCTS SPECIFICATIONS [841301-32-4]
DESCRIPTION [841301-32-4]
Overview
| MDL | MFCD19443709 |
|---|---|
| Molecular Weight | 482.55 |
| Molecular Formula | C24H26N4O5S |
| SMILES | O=C(C(CC1)CCS1(=O)=O)N(C2=C(C)C=CC=C2C)CC(NC3=CC=C(C4=NOC=N4)C=C3)=O |
Summary
Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC 50 of 14 ng/mL.
IC50 & Target
|
HSV-1 7.7-20 ng/mL (IC 50 ) |
HSV-2 15-58 ng/mL (IC 50 ) |
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 EC 50 s 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 EC 50 s of Amenamevir against HSV strains are significantly lower than those of ACV [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00487682 | Astellas Pharma Inc |
Herpes Zoster
|
November 13, 2007 | Phase 2 |
| NCT02223351 | Maruho Europe Limited |
Healthy
|
September 2014 | Phase 1 |
| NCT00870441 | Astellas Pharma Inc |
Safety of ASP2151
|
March 2009 | Phase 1 |
| NCT02403635 | Maruho Europe Limited |
Healthy
|
April 2015 | Phase 1 |
| NCT02796118 | Astellas Pharma Inc |
Healthy Subjects
|
July 2006 | Phase 1 |
| NCT01959841 | Maruho Co., Ltd. |
Herpes Zoster
|
August 2013 | Phase 3 |
| NCT02321748 | Maruho Europe Limited |
Healthy
|
December 2014 | Phase 1 |
| NCT01959295 | Maruho Co., Ltd. |
Herpes Simplex
|
August 2013 | Phase 3 |
| NCT02209324 | Maruho Co., Ltd. |
Herpes Simplex
|
November 2013 | Phase 3 |
| NCT02369172 | Maruho Europe Limited |
Healthy
|
February 2015 | Phase 1 |
| NCT02280421 | Maruho Europe Limited |
Healthy
|
October 2014 | Phase 1 |
| NCT02852876 | Astellas Pharma Europe Ltd.|Astellas Pharma Inc |
Herpes Genitalis|Herpes Zoster
|
September 2005 | Phase 1 |
| NCT00486200 | Astellas Pharma Inc |
Herpes Genitalis
|
June 21, 2007 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 103.62 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0723 mL | 10.3616 mL | 20.7232 mL |
| 5 mM | 0.4145 mL | 2.0723 mL | 4.1446 mL |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0723 mL |
Synonyms