Telbivudine: Difference between revisions
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{{Telbivudine}} | {{Telbivudine}} | ||
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==Overview== | ==Overview== | ||
Telbivudine is an [[antiviral drug]] used in the treatment of [[hepatitis B]] infection. It is marketed by Swiss pharmaceutical company Novartis under the trade namesSebivo (Europe) and Tyzeka (United States). [[Clinical trial]]s have shown it to be [[statistical significance|significantly]] more effective than [[lamivudine]] or [[adefovir]], and less likely to cause resistance.<ref name=Lai1>{{cite journal |author=Lai CL, Leung N, Teo EK, ''et al.'' |title=A 1-year trial of telbivudine, lamivudine, and the combination in patients with hepatitis B e antigen-positive chronic hepatitis B |journal=Gastroenterology |volume=129 |issue=2 |pages=528–36 |year=2005 |pmid=16083710 |doi=10.1016/j.gastro.2005.05.053}}</ref><ref name=NEJM>{{cite journal |author=Lai CL, Gane E, Liaw YF, ''et al.'' |title=Telbivudine versus lamivudine in patients with chronic hepatitis B |journal=[[New England Journal of Medicine|N Engl J Med]] |volume=357 |issue=25 |pages=2576–88 |year=2007 |pmid=18094378 |doi=10.1056/NEJMoa066422}}</ref><ref>{{cite journal |author=Chan HL, Heathcote EJ, Marcellin P, ''et al'' |title=Treatment of hepatitis B e antigen positive chronic hepatitis with telbivudine or adefovir: a randomized trial |journal=[[Annals of Internal Medicine|Ann Intern Med]] |volume=147 |issue=11 |pages=745–54 |year=2007 |pmid=17909201 |url=http://www.annals.org/cgi/content/full/147/11/745}}</ref> | |||
==Category== | ==Category== | ||
Antiviral | Antiviral | ||
==US Brand Names== | ==US Brand Names== | ||
TYZEKA<sup>®</sup> | TYZEKA<sup>®</sup> | ||
==FDA Package Insert== | ==FDA Package Insert== | ||
''' [[Telbivudine description|Description]]''' | ''' [[Telbivudine description|Description]]''' | ||
'''| [[Telbivudine clinical pharmacology|Clinical Pharmacology]]''' | '''| [[Telbivudine clinical pharmacology|Clinical Pharmacology]]''' | ||
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==Mechanism of Action== | ==Mechanism of Action== | ||
Telbivudine is a synthetic thymidine nucleoside analogue with activity against [[HBV]] DNA polymerase. It is phosphorylated by cellular kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Telbivudine 5'-triphosphate inhibits [[HBV]] DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'-triphosphate. Incorporation of telbivudine 5'-triphosphate into viral DNA causes DNA chain termination. Telbivudine is an inhibitor of both [[HBV]] first strand (EC50 value = 1.3 ± 1.6 micromolar) and second strand synthesis (EC50 value = 0.2 ± 0.2 micromolar). Telbivudine 5'-triphosphate at concentrations up to 100 micromolar did not inhibit human cellular DNA polymerases α, β, or γ. No appreciable mitochondrial toxicity was observed in HepG2 cells treated with telbivudine at concentrations up to 10 micromolar. | |||
Telbivudine is a synthetic [[thymidine]] nucleoside analogue with activity against [[HBV]] [[DNA polymerase]]. It is phosphorylated by cellular kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Telbivudine 5'-triphosphate inhibits [[HBV]] DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'-triphosphate. Incorporation of telbivudine 5'-triphosphate into viral DNA causes DNA chain termination. Telbivudine is an inhibitor of both [[HBV]] first strand (EC50 value = 1.3 ± 1.6 micromolar) and second strand synthesis (EC50 value = 0.2 ± 0.2 micromolar). Telbivudine 5'-triphosphate at concentrations up to 100 micromolar did not inhibit human cellular DNA polymerases α, β, or γ. No appreciable mitochondrial toxicity was observed in HepG2 cells treated with telbivudine at concentrations up to 10 micromolar. | |||
==References== | ==References== | ||
{{Reflist|2}} | {{Reflist|2}} | ||
[[Category:Antibiotics]] | [[Category:Antibiotics]] | ||
[[Category:Wikinfect]] | [[Category:Wikinfect]] | ||
Revision as of 19:21, 2 January 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]
Overview
Telbivudine is an antiviral drug used in the treatment of hepatitis B infection. It is marketed by Swiss pharmaceutical company Novartis under the trade namesSebivo (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]
Category
Antiviral
US Brand Names
TYZEKA®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Clinical Studies | Dosage and Administration | Compatibility, Reconstitution, and Stability | Directions For Use | How Supplied | Labels and Packages
Mechanism of Action
Telbivudine is a synthetic thymidine nucleoside analogue with activity against HBV DNA polymerase. It is phosphorylated by cellular kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Telbivudine 5'-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'-triphosphate. Incorporation of telbivudine 5'-triphosphate into viral DNA causes DNA chain termination. Telbivudine is an inhibitor of both HBV first strand (EC50 value = 1.3 ± 1.6 micromolar) and second strand synthesis (EC50 value = 0.2 ± 0.2 micromolar). Telbivudine 5'-triphosphate at concentrations up to 100 micromolar did not inhibit human cellular DNA polymerases α, β, or γ. No appreciable mitochondrial toxicity was observed in HepG2 cells treated with telbivudine at concentrations up to 10 micromolar.
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.