Telbivudine

Telbivudine

Systematic (IUPAC) name
1-(2-deoxy-β-L-erythro-pentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione
Clinical data
Trade names	Tyzeka
AHFS/Drugs.com	monograph
MedlinePlus	a607045
License data	EU EMA: Sebivo US FDA: Tyzeka
Pregnancy category	US: B (No risk in non-human studies)
Routes of administration	Oral
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Protein binding	Low (3.3% in vitro)
Metabolism	Nil
Biological half-life	40 to 49 hours (terminal phase)
Excretion	Renal
Identifiers
CAS Number	3424-98-4
ATC code	J05AF11 (WHO)
PubChem	CID 159269
DrugBank	DB01265
ChemSpider	140081
UNII	2OC4HKD3SF
ChEMBL	CHEMBL374731
Synonyms	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
Chemical data
Formula	C10H14N2O5
Molar mass	242.23 g/mol
SMILES O=C/1NC(=O)N(\C=C\1C)[C@H]2O[C@H]([C@H](O)C2)CO
InChI 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 Key:IQFYYKKMVGJFEH-CSMHCCOUSA-N
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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 (Europe) and Tyzeka (United States). Clinical trials have shown it to be significantly more effective than lamivudine or adefovir, and less likely to cause resistance.^[1][2][3]

Telbivudine is a synthetic thymidine nucleoside analogue; it is the L-isomer of thymidine. It is taken orally in a dose of 600 mg once daily with or without food.

References

1. Lai CL, Leung N, Teo EK, et al. (2005). "A 1-year trial of telbivudine, lamivudine, and the combination in patients with hepatitis B e antigen-positive chronic hepatitis B". Gastroenterology 129 (2): 528–36. doi:10.1016/j.gastro.2005.05.053. PMID 16083710.
2. Lai CL, Gane E, Liaw YF, et al. (2007). "Telbivudine versus lamivudine in patients with chronic hepatitis B". N Engl J Med 357 (25): 2576–88. doi:10.1056/NEJMoa066422. PMID 18094378.
3. Chan HL, Heathcote EJ, Marcellin P, et al. (4 December 2007). "Treatment of hepatitis B e antigen positive chronic hepatitis with telbivudine or adefovir: a randomized trial". Ann Intern Med 147 (11): 745–54. doi:10.7326/0003-4819-147-11-200712040-00183. PMID 17909201.

External links

• Tyzeka official website run by Novartis Pharmaceuticals Corporation
• Telbivudine entry in RxList
• Sebivo Summary of Product Characteristics (from the EMEA website)