Pritelivir mesylate (BAY 57-1293 mesylate) 是一种病毒解旋酶-引物酶复合物 (helicase-primase complex) 抑制剂,在体外和单纯疱疹病毒 (HSV) 感染的动物模型中均具有抗病毒活性。Pritelivir mesylate 对 1 型和 2 型单纯疱疹病毒 (HSV-1 和 HSV-2) 具有活性,对 HSV1-2 的 IC50 为 0.02 μM。
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Pritelivir mesylate (BAY 57-1293 mesylate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2[1].
Pritelivir is the first in a class of antiviral agents that inhibit HSV replication by targeting the viral helicase-primase enzyme complex[2]. Pritelivir (0.03-45 mg/kg) significantly increases survival. Pritelivir (0.3-30 mg/kg) reduces mortality against HSV-1, E-377. Pritelivir has potent and resistance-breaking antiviral efficacy with potential for the treatment of potentially life-threatening HSV type 1 and 2 infections, including herpes simplex encephalitis[3].Combination therapies of Pritelivir at 0.1 or 0.3 mg/kg/dose with Acyclovir (10 mg/kg/dose) are protective when compared to the vehicle treated group against HSV-2, strain MS[3].
[1]. Ligat G, et al. Identification of Amino Acids Essential for Viral Replication in the HCMV Helicase-PrimaseComplex. Front Microbiol. 2018 Oct 23;9:2483.
[2]. Wald A, et al. Helicase-primase inhibitor Pritelivir for HSV-2 infection. N Engl J Med. 2014 Jan 16;370(3):201-10.
[3]. Quenelle DC, et al. Efficacy of pritelivir and acyclovir in the treatment of herpes simplex virus infections in a mouse model of herpes simplex encephalitis. Antiviral Res. 2018 Jan;149:1-6.
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