Lagociclovir (MIV-210), a nucleoside analogue, is an antiviral compound available for the treatment of HBV82 that inhibits the replication of wild-type hepatitis B virus (HBV) in human hepatocellular carcinoma cell lines that permanently express HBV.

HBV (3TC-R):8 μM, HBV (WT):9 μM, HBV (3TC+PMEA-R):15 μM, PMEA-R (HBV):13 μM

Lagociclovir (FLG) (6 days) demonstrated inhibitory activity against 3TC-R HBV, wt HBV, PMEA-R HBV, and 3TC+PMEA-R HBV in transiently transfected Huh7 cells, with IC50s of 8 ± 3.8, 9 ± 2.5, 13 ± 3.4, and 15 ± 6.8 μM, respectively [1]. Lagociclovir (0-100 μM; 6 days) also inhibits the replication of HBV wild-type and drug-resistant mutants in transiently transfected Huh7 cells [2].

Anti-HBV compound Oral administration of MIV-210 (20 or 60 mg/kg; body weight/day) induced a rapid virological response in chronically infected woodchucks, reducing serum WHV DNA levels by 4.75 log10 and 5.72 log10, respectively, in 2 weeks. MIV-210 at 20 or 60 mg/kg/day reduced the liver WHV DNA load 200- to 2,500-fold from pretreatment levels and, importantly, led to a 2.0 log10 drop in the hepatic content of WHV covalently closed circular DNA. Further, a daily dose of 10 mg/kg decreased the serum WHV load 400-fold after 4 weeks of treatment, and a dose of 5 mg/kg/day was sufficient to maintain this antiviral effect during the following 6-week period.[1]