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QuickView for Telbivudine (compound)

Name: telbivudine
PubChem Compound ID: 159269
Molecular formula: C10H14N2O5
Molecular weight: 242.229 g/mol
Thymine, 1-(2-deoxy-.beta.-L-erythro-pentofuranosyl)-; Telbivudine[USAN]; 2,4(1H,3H)-Pyrimidinedione, 1-(2-deoxy-b-L-erythro-pentofuranosyl)-5-methyl-; Sebivo; NV 02B; Thymine, 1-(2-deoxy-beta-L-erythro-pentofuranosyl)-; AIDS-112549; LDT600; NV-02B; 2'-Deoxy-L-thymidine.
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Name: telbivudine
Name (isomeric): DB01265
Drug Type: small molecule
2'-Deoxy-L-thymidine; L-DT; Telbivudin; L-deoxythymidine; Beta-l-thymidine; Epavudine; LDT; L-thymidine
Brand: Tyzeka, Sebivo
Category: Antiviral Agents, Reverse Transcriptase Inhibitors
CAS number: 3424-98-4
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.
Mechanism of Action:
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 in...
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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.
Protein binding: In vitro binding of telbivudine to human plasma proteins is low (3.3%).
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.
Route of elimination: Telbivudine is eliminated primarily by urinary excretion of unchanged drug.
Half Life: Approximately 15 hours.
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)]
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: Hepatitis B virus
Food interaction:
Take without regard to meals.
Drug interaction:
Peginterferon alfa-2aCo-administration of Peginterferon alpha-2a and Telbivudine may increase the risk of serious peripheral neuropathy.