Safety evaluation of telbivudine

Expert Opin Drug Saf. 2010 Sep;9(5):821-9. doi: 10.1517/14740338.2010.507190.


Importance of the field: Successful treatment of chronic hepatitis B (CHB) often requires long-term oral nucleoside/nucleotide agents which can be associated with viral resistance, patient non-compliance and adverse effects. Telbivudine is one of the more potent options available, with a 6.5- to 6.6-log copies/ml hepatitis B DNA reduction at 12 weeks in an early viral kinetic study, a potency comparable to entecavir. It is also one of the few drugs in the treatment of CHB under FDA pregnancy Category B.

Areas covered in this review: The efficacy and safety profile of telbivudine in compensated and decompensated CHB patients compared to other agents are discussed. Viral resistance, characteristic adverse effects including elevation in creatine kinase and peripheral neuropathy in telbivudine treatment are reviewed. Infrequent but significant adverse effects of other nucleoside/nucleotide analogs are highlighted.

What the reader will gain: Readers are provided the latest update on the clinical profile of long-term use of telbivudine.

Take home message: Long-term telbivudine treatment offers effective viral suppression to CHB patients with certain baseline characteristics and on-treatment virologic response. Creatine kinase elevation is not a good predictor of muscle-related adverse effects with nucleoside/nucleotide analogs. But significant myopathy and neuropathy have been reported in a small number of patients receiving telbivudine.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adult
  • Antiviral Agents / administration & dosage
  • Antiviral Agents / adverse effects*
  • Antiviral Agents / pharmacokinetics
  • Antiviral Agents / therapeutic use
  • Biomarkers
  • Creatine Kinase / blood
  • Double-Blind Method
  • Drug Resistance, Viral / genetics
  • Female
  • Hepatitis B virus / drug effects
  • Hepatitis B virus / enzymology
  • Hepatitis B virus / genetics
  • Hepatitis B, Chronic / drug therapy*
  • Humans
  • Isoenzymes / blood
  • Male
  • Multicenter Studies as Topic / statistics & numerical data
  • Muscular Diseases / blood
  • Muscular Diseases / chemically induced
  • Nucleosides / administration & dosage
  • Nucleosides / adverse effects*
  • Nucleosides / pharmacokinetics
  • Nucleosides / therapeutic use
  • Peripheral Nervous System Diseases / chemically induced
  • Predictive Value of Tests
  • Pregnancy
  • Pregnancy Complications, Infectious / drug therapy
  • Pyrimidinones / administration & dosage
  • Pyrimidinones / adverse effects*
  • Pyrimidinones / pharmacokinetics
  • Pyrimidinones / therapeutic use
  • Randomized Controlled Trials as Topic
  • Telbivudine
  • Thymidine / analogs & derivatives


  • Antiviral Agents
  • Biomarkers
  • Isoenzymes
  • Nucleosides
  • Pyrimidinones
  • Telbivudine
  • Creatine Kinase
  • Thymidine