In vitro activity: Pritelivir (formerly known as AIC316, BAY 57-1293) is a novel and potent helicase primase inhibitor that showed antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2. It represents a new class of potent inhibitors of HSV that target the virus helicase primase complex. BAY 57-1293 exhibits anti-herpes activity through inhibiting the helicase-primase and affecting the viral DNA synthesis. In the in vitro viral replication assay, BAY 57-1293 shows inhibition against HSV-1 F, HSV-2 G and acyclovir-resistant HSV-1 F mutant with IC50 value of 20nM. Thus, BAY 57-1293 has significant potential for the treatment of HSV disease in humans, including those resistant to current medications. The mechanism of action is that BAY 57-1293 directly inhibits the ATPase activity of the viral helicase-primase enzyme complex in a dose-dependent manner. BAY 57-1293 also shows potent antiviral activity against acyclovir resistant HSV mutants. BAY 57-1293 reduces Aβ and P-tau induced by herpes simplex virus type 1 in vero cells.
Kinase Assay: Pritelivir (formerly known as AIC316, BAY 57-1293) is a novel and potent helicase primase inhibitor that showed antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.
Cell Assay: In the in vitro viral replication assay, BAY 57-1293 shows inhibition against HSV-1 F, HSV-2 G and acyclovir-resistant HSV-1 F mutant with IC50 value of 20nM. In the plaque reduction assay and the conventional cytopathogenicity assay, BAY 57-1293 shows IC50 values of 0.01-0.02μM and 0.01-0.03μM, respectively. |