| Item |
Information |
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Drug Groups
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approved; investigational |
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Description
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Telbivudine is a synthetic thymidine nucleoside analog with specific activity against the hepatitis B virus. Telbivudine is orally administered, with good tolerance, lack of toxicity and no dose-limiting side effects. |
| Indication |
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. |
| Pharmacology |
Telbivudine is a synthetic thymidine nucleoside analogue with activity against hepatitis B virus (HBV). Telbivudine is the unmodified β–L enantiomer of the naturally occurring nucleoside, thymidine. It undergoes phosphorylation via interaction with cellular kinases to form the active metabolite, telbivudine 5'-triphosphate. |
| Toxicity |
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. |
| Affected Organisms |
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| Biotransformation |
No metabolites of telbivudine were detected following administration of [14C]–telbivudine in humans. Telbivudine is not a substrate, or inhibitor of the cytochrome P450 (CYP450) enzyme system. |
| Absorption |
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. |
| Half Life |
Approximately 15 hours. |
| Protein Binding |
In vitro binding of telbivudine to human plasma proteins is low (3.3%). |
| Elimination |
Telbivudine is eliminated primarily by urinary excretion of unchanged drug. |
| Clearance |
* 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)] |
| References |
| • |
Matthews SJ: Telbivudine for the management of chronic hepatitis B virus infection. Clin Ther. 2007 Dec;29(12):2635-53.
[Pubmed]
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| • |
Amarapurkar DN: Telbivudine: a new treatment for chronic hepatitis B. World J Gastroenterol. 2007 Dec 14;13(46):6150-5.
[Pubmed]
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Dusheiko G, Danta M: Telbivudine for the treatment of chronic hepatitis B. Drugs Today (Barc). 2007 May;43(5):293-304.
[Pubmed]
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| • |
Keam SJ: Telbivudine. Drugs. 2007;67(13):1917-29.
[Pubmed]
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| • |
Ruiz-Sancho A, Sheldon J, Soriano V: Telbivudine: a new option for the treatment of chronic hepatitis B. Expert Opin Biol Ther. 2007 May;7(5):751-61.
[Pubmed]
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Marcellin P, Asselah T, Boyer N: Treatment of chronic hepatitis B. J Viral Hepat. 2005 Jul;12(4):333-45.
[Pubmed]
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| • |
Han SH: Telbivudine: a new nucleoside analogue for the treatment of chronic hepatitis B. Expert Opin Investig Drugs. 2005 Apr;14(4):511-9.
[Pubmed]
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| • |
Jones R, Nelson M: Novel anti-hepatitis B agents: A focus on telbivudine. Int J Clin Pract. 2006 Oct;60(10):1295-9.
[Pubmed]
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| External Links |
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