Telbivudine

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Telbivudine
Systematic (IUPAC) name
1-[(2S,4R,5S)-4-hydroxy-5-hydroxymethyltetrahydrofuran-2-yl]- 5-methyl-1H-pyrimidine-2,4-dione
Identifiers
CAS number	3424-98-4
ATC code	N03AX17
PubChem	159269
Chemical data
Formula	C₁₀H₁₄N₂
Mol. mass	242.23 g/mol
Synonyms	1-(2-deoxy-β-L-ribofuranosyl)-5-methyluracil β-L-2-deoxythymidine β-L-thymidine (LdT)
Pharmacokinetic data
Bioavailability	?
Protein binding	Low (3.3% in vitro)
Metabolism	Nil
Half life	40 to 49 hours (terminal phase)
Excretion	Renal
Therapeutic considerations
Licence data	EU, US
Pregnancy cat.	B(US)
Legal status	POM(UK) ℞-only(US)
Routes	Oral

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 once daily.

[edit] References

^ 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.
^ 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.
^ Chan HL, Heathcote EJ, Marcellin P, et al (2007). "Treatment of hepatitis B e antigen positive chronic hepatitis with telbivudine or adefovir: a randomized trial". Ann Intern Med 147 (11): 745–54. PMID 17909201.

[edit] External links

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

v • d • e Antivirals, other than for HIV (primarily J05, also S01AD and D06BB)

Anti-herpesvirus (DNA, I)	guanine analogues (Aciclovir, Famciclovir, Ganciclovir, Penciclovir, Valaciclovir, Valganciclovir) • nucleoside analogues (Idoxuridine, Trifluridine, Vidarabine) • Cidofovir • Docosanol • Fomivirsen • Foscarnet • Tromantadine

HPV/MC (DNA, I)	Imiquimod • Podophyllotoxin

Hepatitis B (DNA, VII)	Adefovir • Clevudine • Interferon alfa-2b • Pegylated interferon alfa-2a • Entecavir • Lamivudine • Telbivudine • Tenofovir^†

Hepatitis C (RNA, IV)	Pegylated interferon alpha • Ribavirin • Taribavirin^† • Boceprevir^†

Picornavirus (RNA, IV)	Pleconaril^†

Anti-influenza agents (RNA, V)	Arbidol adamantane derivatives/M2 inhibitors (Amantadine, Rimantadine) neuraminidase inhibitors (Oseltamivir, Zanamivir, Peramivir^†)

HIV (Reverse, VI)	See HIV pharm

Other antiviral agents	general (Inosine, Interferon)

^†Undergoing clinical trials, not FDA approved.