For the treatment of chronic hepatitis B in adult and adolescent patients ≥16 years of age with evidence of viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease.
Telbivudine 5'–triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'–triphosphate. This leads to the chain termination of DNA synthesis, thereby inhibiting viral replication. Incorporation of telbivudine 5'–triphosphate into viral DNA also causes DNA chain termination, resulting in inhibition of HBV replication. Telbivudine inhibits anticompliment or second-strand DNA.
There is no information on intentional overdose of telbivudine, but one subject experienced an unintentional and asymptomatic overdose. Healthy subjects who received telbivudine doses up to 1800 mg/day for 4 days had no increase in or unexpected adverse events. A maximum tolerated dose for telbivudine has not been determined.
Absorbed following oral administration. Telbivudine absorption and exposure were unaffected when a single 600–mg dose was administered with a high–fat (~55 g), high–calorie (~950 kcal) meal.
Approximately 15 hours.
Telbivudine is eliminated primarily by urinary excretion of unchanged drug.
* 7.6 +/- 2.9 L/h [Normal renal function (Clcr>80 mL/min)] * 5.0 +/- 1.2 L/h [Mild renal function impairement (Clcr=50-80 mL/min)] * 2.6 +/- 1.2 L/h [Moderate renal function impairement (Clcr=30-49 mL/min)] * 0.7 +/- 0.4 L/h [Severe renal function impairement (Clcr<30 mL/min)]