Brivudine

Brivudine is a thymidine analog and inhibitor of herpes simplex virus 1 (HSV-1) and varicella-zoster virus (VZV) viral replication.^1,2 Following conversion to a 5'-triphosphate form by viral kinases, brivudine is incorporated into viral DNA, inhibiting viral DNA polymerases and inducing strand breakage.² Brivudine (0.02-0.04 μg/ml) inhibits VZV replication in primary human fibroblasts and inhibits cytopathogenic effects of the KOS HSV-1 strain in a panel of cell lines (MIC₅₀s = 0.007-0.4 μg/ml).^1,3 It selectively inhibits cytopathogenicity induced by HSV-1 strains over HSV-2, vaccinia virus, vesicular stomatitis virus, or deoxythymidine kinase-deficient HSV-1 strains in E₆SM cells (MIC₅₀s = 0.02, 2-10, 7, >400, and 40 μg/ml, respectively).¹ Brivudine (5 and 15 mg/kg twice per day) increases survival in a mouse model of disseminated HSV-1 infection.

WARNING This product is not for human or veterinary use.

1. De Clercq, E., Desgranges, C., Herdewijn, P., et al. Synthesis and antiviral activity of (E)-5-(2-bromovinyl)uracil and (E)-5-(2-bromovinyl)uridine. J. Med. Chem. 29(2), 213-217 (1986).

2. Kulikowski, T. Structure-activity relationships and conformational features of antiherpetic pyrimidine and purine nucleoside analogues. A review. Pharm. World Sci. 16(2), 127-138 (1994).

3. De Clercq, E., Descamps, J., Verhelst, G., et al. Antiviral activity of 5-(2-halogenovinyl)-2'-deoxyuridines. Curr. Chemother. Infect. Dis. 2, 1372-1374 (1980).