In vitro efficacy of brincidofovir against variola virus.

Abstract

Brincidofovir (CMX001), a lipid conjugate of the acyclic nucleotide phosphonate cidofovir, is under development for smallpox treatment using "the Animal Rule," established by the FDA in 2002. Brincidofovir reduces mortality caused by orthopoxvirus infection in animal models. Compared to cidofovir, brincidofovir has increased potency, is administered orally, and shows no evidence of nephrotoxicity. Here we report that the brincidofovir half-maximal effective concentration (EC50) against five variola virus strains in vitro averaged 0.11 μM and that brincidofovir was therefore nearly 100-fold more potent than cidofovir.

• Authors: Victoria A Olson, Scott K Smith, Scott Foster, Yu Li, E Randall Lanier, Irina Gates, Lawrence C Trost, Inger K Damon
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 58 Issue 9 Pg. 5570-1 (Sep 2014) ISSN: 1098-6596 [Electronic] United States
• PMID: 24957837 (Publication Type: Journal Article)
• Copyright: Copyright © 2014, American Society for Microbiology. All Rights Reserved.

Chemical References

• Antiviral Agents
• DNA, Viral
• Organophosphonates
• brincidofovir
• Cytosine
• Cidofovir

Topics

• Animals
• Antiviral Agents (pharmacology)
• Cell Line
• Chlorocebus aethiops
• Cidofovir
• Cytosine (analogs & derivatives, pharmacology)
• DNA, Viral (analysis, genetics)
• Disease Models, Animal
• Humans
• In Vitro Techniques
• Microbial Sensitivity Tests
• Organophosphonates (pharmacology)
• Smallpox (drug therapy)
• Variola virus (drug effects, growth & development)