Telbivudine

Modify Date: 2024-01-02 19:33:01

Telbivudine Structure
Telbivudine structure
Common Name Telbivudine
CAS Number 3424-98-4 Molecular Weight 242.229
Density 1.5±0.1 g/cm3 Boiling Point N/A
Molecular Formula C10H14N2O5 Melting Point 188-190ºC
MSDS Chinese USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of Telbivudine


Telbivudine, a specific inhibitor of hepatitis B virus (HBV) replication, is an antiviral drug used in the treatment of hepatitis B infection.Target: HBVTelbivudine 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. Telbivudine is a synthetic thymidine nucleoside analogue, it is the L-isomer of thymidine. It is taken once daily.Telbivudine is a potent antiviral that provides effective and sustained viral suppression in patients with compensated CHB. In clinical trials, treatment outcomes were improved significantly more with telbivudine 600 mg once daily than with lamivudine 100 mg or adefovir 10 mg once daily, and telbivudine-treated patients had significantly less viral resistance than lamivudine-treated patients. Telbivudine is associated with a medium genetic barrier to resistance and, as patients with undetectable HBV DNA levels have significantly improved outcomes, it is recommended that HBV DNA levels are monitored at week 24 (and 6 monthly thereafter), with the addition of a nucleoside/nucleotide analogue without cross resistance (such as adefovir dipivoxil) if viraemia is present to reduce the risk of resistance (Roadmap concept). Telbivudine was generally well tolerated in clinical trials for periods of up to 4 years, and has a similar tolerability profile to that of lamivudine.

 Names

Name telbivudine
Synonym More Synonyms

 Telbivudine Biological Activity

Description Telbivudine, a specific inhibitor of hepatitis B virus (HBV) replication, is an antiviral drug used in the treatment of hepatitis B infection.Target: HBVTelbivudine 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. Telbivudine is a synthetic thymidine nucleoside analogue, it is the L-isomer of thymidine. It is taken once daily.Telbivudine is a potent antiviral that provides effective and sustained viral suppression in patients with compensated CHB. In clinical trials, treatment outcomes were improved significantly more with telbivudine 600 mg once daily than with lamivudine 100 mg or adefovir 10 mg once daily, and telbivudine-treated patients had significantly less viral resistance than lamivudine-treated patients. Telbivudine is associated with a medium genetic barrier to resistance and, as patients with undetectable HBV DNA levels have significantly improved outcomes, it is recommended that HBV DNA levels are monitored at week 24 (and 6 monthly thereafter), with the addition of a nucleoside/nucleotide analogue without cross resistance (such as adefovir dipivoxil) if viraemia is present to reduce the risk of resistance (Roadmap concept). Telbivudine was generally well tolerated in clinical trials for periods of up to 4 years, and has a similar tolerability profile to that of lamivudine.
Related Catalog
References

[1]. Lai CL, et al. A 1-year trial of telbivudine, lamivudine, and the combination in patients with hepatitis B e antigen-positive chronic hepatitis B. Gastroenterology. 2005 Aug;129(2):528-36.

[2]. Lai CL, et al. Telbivudine versus lamivudine in patients with chronic hepatitis B. N Engl J Med. 2007 Dec 20;357(25):2576-88.

[3]. McKeage K, et al. Telbivudine: a review of its use in compensated chronic hepatitis B. Drugs. 2010 Oct 1;70(14):1857-83.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Melting Point 188-190ºC
Molecular Formula C10H14N2O5
Molecular Weight 242.229
Exact Mass 242.090271
PSA 104.55000
LogP -1.11
Index of Refraction 1.584
Storage condition 2-8°C

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Hazard Codes Xn
Risk Phrases 22
Safety Phrases 24/25
RIDADR NONH for all modes of transport
RTECS UV9048500

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 Synonyms

L-Deoxythymidine
2'-DEOXY-L-THYMIDINE
Epavudine
L-Dt
NV 02B
Telbivudine
L-2'-deoxythymidine
Β-L-2'-DEOXY-THYMIDINE
β-L-Thymidine
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