Pritelivir mesylate hydrate

Names

[ CAS No. ]:
1428321-10-1

[ Name ]:
Pritelivir mesylate hydrate

Biological Activity

[Description]:

Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), 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 hydrate 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].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HSV
Research Areas >> Infection

[Target]

IC50: 0.02 μM (HSV1-2)[1]


[In Vivo]

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]. Animal Model: Female BALB/c mice[3] Dosage: 0.03 to 45 mg/kg Administration: Administered orally, twice daily at approximately 12 h intervals, for 7 days Result: Survival was significantly increased to 80-100% as compared to the vehicle treatment. Even the lowest dose of 0.3 mg/kg was effective in increasing survival to 53%.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H24N4O7S3

[ Molecular Weight ]:
516.61


Related Compounds