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Antiinfective agent stubs
Telbivudine
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Telbivudine

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Telbivudine
Telbivudine structure.svg
Clinical data
Trade names Tyzeka, Sebivo
Other names 1-(2-deoxy-β-L-ribofuranosyl)-5-methyluracil
β-L-2-deoxythymidine
β-L-thymidine (LdT)
1-[(2S,4R,5S)-4-hydroxy-5-hydroxymethyltetrahydrofuran-2-yl]-5-methyl-1H-pyrimidine-2,4-dione
AHFS/Drugs.com Monograph
MedlinePlus a607045
License data
Pregnancy
category
  • AU: B1
Routes of
administration		 By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU: Rx-only
Pharmacokinetic data
Protein binding Low (3.3% in vitro)
Metabolism Nil
Elimination half-life 40 to 49 hours (terminal phase)
Excretion Kidney
Identifiers
  • 1-(2-deoxy-β-L-erythro-pentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.125.511
Chemical and physical data
Formula C10H14N2O5
Molar mass 242.231 g·mol−1
3D model (JSmol)
  • Cc1cn([C@@H]2C[C@@H](O)[C@H](CO)O2)c(=O)[nH]c1=O
  • InChI=1S/C10H14N2O5/c1-5-3-12(10(16)11-9(5)15)8-2-6(14)7(4-13)17-8/h3,6-8,13-14H,2,4H2,1H3,(H,11,15,16)/t6-,7+,8+/m1/s1 checkY
  • Key:IQFYYKKMVGJFEH-CSMHCCOUSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Telbivudine is an antiviral drug used in the treatment of hepatitis B infection. It is marketed by Swiss pharmaceutical company Novartis under the trade names Sebivo (European Union) and Tyzeka (United States). Clinical trials have shown it to be significantly more effective than lamivudine or adefovir, and less likely to cause resistance. However, HBV signature resistance mutation M204I (a change from methionine to isoleucine at position 204 in the reverse transcriptase domain of the hepatitis B polymerase) or L180M+M204V have been associated with Telbivudine resistance.

Telbivudine is a synthetic thymidine β-L-nucleoside analogue; it is the L-isomer of thymidine. Telbivudine impairs hepatitis B virus (HBV) DNA replication by leading to chain termination. It differs from the natural nucleotide only with respect to the location of the sugar and base moieties, taking on an levorotatory configuration versus a dextrorotatory configuration as do the natural deoxynucleosides. It is taken orally in a dose of 600 mg once daily with or without food.

Telbivudine has no in vitro activity against HIV-1, and in a case-series of three HIV-HBV co-infected patients, telbivudine did not produce sustained HIV-1 virologic suppression or induce any resistance mutations in HIV-1.

In 2016, Novartis posted a discontinuation notice for Tyzeka.

External links

  • "Telbivudine". Drug Information Portal. U.S. National Library of Medicine.

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