2'-Deoxy-L-thymidine

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.

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.

Description

Telbivudine is a b-L-thymidine nucleoside analog launched for the once-daily oral treatment of chronic hepatitis B virus (HBV) infection. It is the fourth nucleoside or nucleotide analog to be marketed for this indication. The previous drugs from this class include lamivudine, a deoxythiacytosine analog, adefovir, a nucleotide analog, and entecavir, a guanosine analog. Adefovir, entecavir, and telbivudine are specifically indicated for HBV, whereas lamivudine is indicated for both HBV and HIV infections. Telbivudine is efficiently phosphorylated by cellular kinases to the active triphosphate derivative, which inhibits HBV DNA polymerase by competing with the natural substrate, thymidine- 5’-triphosphate.

Chemical properties

2'-Deoxy-L-thymidine is White Solid

Originator

Idenix (US)

The Uses of 2'-Deoxy-L-thymidine

Nucleoside analog; specific inhibitor of hepatitis B virus (HBV) replication. Antiviral

The Uses of 2'-Deoxy-L-thymidine

Telbivudine(Tyzeka, Sebivo) is an antiviral drug used in the treatment of hepatitis B infection. Clinical trials have shown it to be significantly more effective than lamivudine or adefovir, and less likely to cause resistance. Telbivudine is a synthetic

The Uses of 2'-Deoxy-L-thymidine

Nucleoside analog; specific inhibitor of hepatitis B virus (HBV) replication. Antiviral.

Background

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.

Indications

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.

What are the applications of Application

Telbivudine is a specific hepatitis B virus (HBV) replication inhibitor

Definition

ChEBI: A pyrimidine 2'-deoxyribonucleoside that is the L-enantiomer of thymine. A synthetic thymidine nucleoside analogue with activity against HBV DNA polymerase.

brand name

(Novirio).

Pharmacokinetics

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.

Metabolism

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.