Pritelivir (AIC316) is an inhibitor of the viral helicase-primase complex, which exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir 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].
体内研究
Pritelivir is a pioneering agent in antiviral treatment that interrupts HSV replication by targeting the viral helicase-primase enzyme complex.
Pritelivir, at dosages ranging from 0.03 to 45 mg/kg, significantly improves survival rates and, at 0.3 to 30 mg/kg, reduces mortality against HSV-1, E-377, thereby demonstrating potent and breakthrough antiviral efficiency with the potential for managing life-threatening HSV-1 and -2 infections, including herpes simplex encephalitis.
Compared with the control treatment group, 0.1 or 0.3 mg/kg/ dose of pritlivir combined with acyclovir (10 mg/kg/ dose) had a protective effect against HSV-2 MS strains [3].
Pritelivir/普瑞利韦 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary keratinocytes
0.05–15 µM
24 hours
Evaluate the cytotoxicity of Pritelivir on primary keratinocytes, showing no significant toxicity at concentrations ranging from 0.05–15 μmol/L.
J Invest Dermatol. 2019 Mar;139(3):673-682.
Vero cells
0.39 µM (EC50), 0.81 µM (EC90)
48 hours
Determine the EC50 and EC90 values of Pritelivir against resistant mutant cl-2-r1-Rec strain
To evaluate the in vivo antiviral activity of Pritelivir against HSV-1 and HSV-2, including acyclovir-resistant strains. Results showed that Pritelivir significantly improved survival rates in infected mice and remained effective even when treatment was delayed for 72 hours.
Antiviral Res. 2018 Jan;149:1-6
Mice
HSV infection model
Oral
0.5 mg/kg
Once daily for 5 days
To evaluate the therapeutic effect of Pritelivir on HSV infection, results showed that Pritelivir was more effective than valacyclovir in treating HSV infections.
J Med Chem. 2022 Oct 27;65(20):13614-13628
BALB/c mice
Murine neck skin infection model
Oral gavage
0.5, 1.0, 5.0, 10, 15, 60 mg/kg
Once daily for 4 or 8 days
Evaluate the efficacy of Pritelivir in a murine HSV-1 infection model, including treatment effects on wild-type and resistant mutant strains
To evaluate the safety and pharmacokinetics of Pritelivir in pigtailed macaques, showing median plasma concentrations of 18,700 pg/mL, and vaginal fluid concentrations of 632,327.9 pg/mL (proximal) and 171,289.3 pg/mL (distal).
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