Idenix and Novartis
Antiviral (nucleoside analog reverse transcriptase inhibitor)
Telbivudine 600 mg; tabs.
Treatment of chronic hepatitis B in patients with evidence of viral replication and either evidence of persistent elevations of alanine aminotransferase (ALT)/aspartate aminotransferase (AST) or histologically active disease.
Telbivudine is a thymidine nucleoside analog that has activity against hepatitis B virus (HBV) reverse transcriptase. Its active form is incorporated into viral DNA, causing DNA chain termination and inhibition of HBV replication.
In a trial involving 1,367 nucleoside-naïve patients with chronic hepatitis B infection, telbivudine 600 mg once daily was compared with lamivudine 100 mg once daily for up to 104 weeks; the primary data analysis was conducted after week 52. Clinical and virological end points were evaluated separately in hepatitis B e antigen (HBeAg)-positive and HBeAg-negative patients. The percentage of patients who became HBV DNA-negative at 52 weeks using telbivudine was 60% in the HBeAg-positive cohort and 88% in the HBeAg-negative cohort compared with 40% and 71%, respectively, in the lamivudine-treated group. Telbivudine-treated patients who achieved non-detectable HBV DNA levels at 24 weeks were more likely to undergo e-antigen seroconversion, normalize ALT, and minimize resistance at one year. Optimal duration of therapy has not been established.
Telbivudine has not been studied in patients co-infected with other viruses, but it has not been shown to be active against hepatitis C or HIV-1. It was shown to have no antagonistic activity against other antiretroviral agents such as abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, and zidovudine. Telbivudine has not been shown to be effective in patients with hepatitis B infection that is resistant to either lamivudine or adefovir.
≥16 years (creatinine clearance [CrCl] ≥50 mL/min): 600 mg once daily. Renal impairment: CrCl 30-49 mL/min: 600 mg once every 48 hours; CrCl <30 mL/min (not on dialysis): 600 mg once every 72 hours; end-stage renal disease: 600 mg every 96 hours (give after dialysis session).
<16 years: not recommended.
Renal impairment. Monitor for lactic acidosis and for myopathy; suspend therapy if myopathy is suspected, discontinue if confirmed. Risk of hepatitis B reactivation (monitor after discontinuing therapy). Elderly. Pregnancy (Cat. B). Nursing mothers: not recommended.
Risk of myopathy may be increased with statins, fibrates, corticosteroids, chloroquine, hydroxychloroquine, penicillamine, zidovudine, cyclosporine, erythromycin, niacin, azole antifungals. Caution with drugs that affect renal elimination (may need to extend telbivudine dosing interval); monitor renal function with cyclosporine, tacrolimus.
Fatigue, malaise, fever, joint pain, upper respiratory symptoms, headache, abdominal pain, myalgia/myopathy, elevated creatine kinase levels, GI upset, dizziness, insomnia, post-treatment exacerbation of hepatitis B; lactic acidosis, severe hepatomegaly with steatosis.
Register pregnant patients exposed to telbivudine by calling 800.258.4263.