Betz Ulrich A K, Fischer Rüdiger, Kleymann Gerald, Hendrix Martin, Rübsamen-Waigmann Helga
Bayer AG, Pharma Research Antiinfectives, Wuppertal, Germany.
Antimicrob Agents Chemother. 2002 Jun;46(6):1766-72. doi: 10.1128/AAC.46.6.1766-1772.2002.
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.
BAY 57-1293属于一类新型抗病毒化合物,在体外通过消除病毒引发酶-解旋酶复合物的酶活性,在纳摩尔范围内抑制1型和2型单纯疱疹病毒(HSV)的复制。在各种HSV感染的啮齿动物模型中,发现BAY 57-1293在体内的抗病毒活性优于目前用于治疗HSV感染的所有化合物。该化合物在播散性疱疹的小鼠和大鼠致死性攻击模型、皮肤疾病的小鼠带状疱疹样扩散模型以及小鼠眼部疱疹模型中显示出强大的抗病毒活性。它在肠胃外、口服和局部制剂中均有活性。当在疱疹疾病症状已经明显后开始治疗时,BAY 57-1293仍继续显示出疗效。