Antiviral activity of famciclovir and acyclovir in mice infected intraperitoneally with herpes simplex virus type 1 SC16

• Published in: Journal of antimicrobial chemotherapy 1994-08, Vol.34 (2), p.287-290
• Main Authors: Ashton, Raymond J., Abbott, Karen H., Smith, Gill M., Sutton, David
• Format: Article
• Language: English
• Subjects: 2-Aminopurine - analogs & derivatives; 2-Aminopurine - therapeutic use; Acyclovir - therapeutic use; Animals; Antiviral Agents - therapeutic use; Famciclovir; Herpes Simplex - drug therapy; Herpes Simplex - virology; herpes simplex virus; Herpesvirus 1, Human; Mice; Mice, Inbred DBA; Prodrugs - therapeutic use; varicella-zoster virus; Virus Replication - drug effects
• ISSN: 0305-7453; 1460-2091
• DOI: 10.1093/jac/34.2.287

Penciclovir (9-(4-hydroxy-3-hydroxymethylbut-1-yl)guanine; BTL 39123) exhibits potent, selective and prolonged activity against herpesviruses both in cell culture and in animals. The prolonged activity is consistent with the stability of penciclovir-triphosphate in HSV-infected cells and is a property not shared by acyclovir-trisphosphate. However, penciclovir has relatively poor oral bioavailability. Therefore an oral form, famciclovir, has been developed which is well absorbed and efficiently converted to penciclovir. Both penciclovir and famciclovir are currently undergoing clinical trials of efficacy against HSV-1, HSV-2 and varicellazoster virus (VZV) infections. In these studies, the effect of dosing frequency on the antiviral efficacy of oral famciclovir in murine infections relative to acyclovir is described.