替比夫定

替比夫定用途

Telbivudine是特异的HBV复制抑制剂。

替比夫定作用

1.作用机制：替比夫定为天然胸腺嘧啶脱氧核苷的自然L-对映体，是人工合成的胸腺嘧啶脱氧核苷类抗乙肝病毒(HBV)DNA多聚酶药物。
替比夫定在细胞激酶的作用下被磷酸化为有活性的代谢产物--腺苷，腺苷的细胞内半衰期为14小时。替比夫定5'-腺苷通过与HBV中自然底物胸腺嘧啶5'-腺苷竞争，从而抑制HBVDNA多聚酶的活性;通过整和到HBVDNA中造成乙肝病毒(HBV)DNA链延长终止，从而抑制乙肝病毒的复制。
替比夫定同时抑制乙肝病毒(HBV)DNA第一链(EC50value=1.3±1.6μ

替比夫定名称

[ CAS 号 ]:
3424-98-4

[ 中文名 ]:
2-脱氧-L-胸苷

[ 英文名 ]:
Telbivudine

[中文别名 ]:

替比夫定

[英文别名 ]:

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

替比夫定生物活性

[ 描述 ]:

Telbivudine是特异的HBV复制抑制剂。

[ 相关类别 ]:

信号通路 >> 抗感染 >> HBV

研究领域 >> 感染

[参考文献]

[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.

[相关活性小分子]

替比夫定物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 熔点 ]:
188-190ºC

[ 分子式 ]:
C₁₀H₁₄N₂O₅

[ 分子量 ]:
242.229

[ 精确质量 ]:
242.090271

[ PSA ]:
104.55000

[ LogP ]:
-1.11

[ 外观性状 ]:
白色晶体粉末

[ 折射率 ]:
1.584

[ 储存条件 ]:
2-8°C

替比夫定安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 安全声明 (欧洲) ]:
24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
UV9048500

替比夫定文献

Cell Fusion Connects Oncogenesis with Tumor Evolution.

Am. J. Pathol. 185 , 2049-60, (2015)

Cell fusion likely drives tumor evolution by undermining chromosomal and DNA stability and/or by generating phenotypic diversity; however, whether a cell fusion event can initiate malignancy and direc...

In vitro activity and resistance profile of samatasvir, a novel NS5A replication inhibitor of hepatitis C virus.

Antimicrob. Agents Chemother. 58(8) , 4431-42, (2014)

The hepatitis C virus (HCV) nonstructural 5A (NS5A) protein is a clinically validated target for drugs designed to treat chronic HCV infection. This study evaluated the in vitro activity, selectivity,...

Telbivudine therapy may shape CD4(+) T-cell response to prevent liver fibrosis in patients with chronic hepatitis B.

Liver Int. 35(3) , 834-45, (2015)

Nucleos(t)ide analogues (NAs) can indirectly restore host immunity against hepatitis B virus (HBV) by inhibiting virus replication. We aimed to investigate whether telbivudine could prevent HBV-relate...

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