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Antimicrobial Agents and Chemotherapy, June 2002, p. 1766-1772, Vol. 46, No. 6
0066-4804/02/$04.00+0 DOI: 10.1128/AAC.46.6.1766-1772.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.
Potent In Vivo Antiviral Activity of the Herpes Simplex Virus Primase-Helicase Inhibitor BAY 57-1293
Ulrich A. K. Betz,* Rüdiger Fischer, Gerald Kleymann, Martin Hendrix, and Helga Rübsamen-Waigmann
Bayer AG, Pharma Research Antiinfectives, Wuppertal, Germany
Received 24 October 2001/
Returned for modification 17 January 2002/
Accepted 11 March 2002
BAY 57-1293 belongs to a new class of antiviral compounds and inhibits replication of herpes simplex virus (HSV) type 1 and type 2 in the nanomolar range in vitro by abrogating the enzymatic activity of the viral primase-helicase complex. In various rodent models of HSV infection the antiviral activity of BAY 57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections. The compound shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes, in a murine zosteriform spread model of cutaneous disease, and in a murine ocular herpes model. It is active in parenteral, oral, and topical formulations. BAY 57-1293 continued to demonstrate efficacy when the onset of treatment was initiated after symptoms of herpetic disease were already apparent.
* Corresponding author. Mailing address: Bayer AG, International Pharma Research, PH-R-EU, Geb. 402, Aprather Weg 18a, D-42096 Wuppertal, Germany. Phone: 49-(0)202-364974. Fax: 49-(0)202-368171. E-mail:
ulrich.betz.ub{at}bayer-ag.de.
Antimicrobial Agents and Chemotherapy, June 2002, p. 1766-1772, Vol. 46, No. 6
0066-4804/02/$04.00+0 DOI: 10.1128/AAC.46.6.1766-1772.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.
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