Entecavir (ETV) Monohydrate is a first-line therapy for chronic hepatitis B virus (HBV), demonstrating potent suppression of HBV DNA and a high barrier to viral resistance[3]. Entecavir, a new deoxyguanosine analog, represents a third agent within the nucleoside/nucleotide HBV polymerase inhibitor class with distinct advantages over lamivudine and adefovir dipivoxil: it has a three-step mechanism of action, is the most potent inhibitor of HBV DNA polymerase, is not associated with any major adverse effects, and has a limited potential for resistance. In phase II and III clinical trials, entecavir was found to be superior to lamivudine for all primary endpoints evaluated in both nucleoside-naïve and lamivudine-resistant patients. Entecavir was effective in both HBeAg-positive and HBeAg-negative nucleoside-naïve patients[4]. In chronic hepatitis B patients experiencing clevudine-induced myopathy, switching to entecavir 0.5 mg per day showed a resolution of myopathy and adequate viral suppression[5]. Entecavir (ETV) resistance of hepatitis B virus (HBV) conventionally requires rt184, 202, or 250 mutations plus lamivudine-resistance mutation (rtM204V/I ± L180M)[6].
Entecavir Monohydrate/恩替卡韦 一水合物 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HepG2.2.15 cells
10 µM
48 h
To evaluate the inhibitory effect of entecavir on HBV replication
J Virol. 2023 Oct 31;97(10):e0109023.
HepAD38 cells
1 μM
To investigate the inhibitory effect of ETV on HBV DNA levels, results showed that Vpx-mediated knockdown of SAMHD1 significantly increased HBV DNA levels.
Life Sci Alliance. 2019 Mar 27;2(2):e201900355.
HepG2-NTCP (K7) cells
1 μM
72 h
To investigate the inhibitory effect of ETV on HBV DNA levels, results showed that Vpx-mediated degradation of SAMHD1 significantly increased extracellular HBV DNA levels.
Life Sci Alliance. 2019 Mar 27;2(2):e201900355.
HepG2.2.15.7 cells
1-3 nM
6 days
To investigate the effect of Entecavir on HBV-induced EV-miRNAs expression, it was found that the expression of five EV-miRNAs (miR-21, miR-192, miR-215, miR-221, miR-222) was up-regulated after Entecavir treatment.
Sci Rep. 2017 Aug 10;7(1):7780.
Entecavir Monohydrate/恩替卡韦 一水合物 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
HBV-carrier mouse model
Oral
0.3 mg/kg
Once daily for 3 weeks
To evaluate the therapeutic effect of Entecavir on HBV infection
J Exp Med. 2020 Oct 5;217(10):e20200840
FRG mice
Chronic HBV infection model
Oral gavage
1 mg/kg
Daily administration for 17 days
Suppress HBV viral load to create conditions for AAV-SaCas9 therapy
Mol Ther Methods Clin Dev. 2020 Nov 26;20:258-275
BALB/c Rag2-/-Il2rg-/-SirpaNODAlb-uPAtg/tg mice
Mouse model with humanized immune system and hepatocytes
Intraperitoneal injection or drinking water
0.3 mg/kg
Once daily for 14 weeks
Entecavir treatment effectively reduced viral loads and decreased liver inflammation
Gastroenterology. 2017 Dec;153(6):1647-1661.e9
Mice
HBV-carrier mouse model
Gavage
0.1 mg/kg
Daily for 6 weeks
To evaluate the anti-HBV effect of ETV in combination with SPD, showing significant reduction in HBsAg and pgRNA levels
Cell Rep Med. 2024 Nov 19;5(11):101822
Mice
PAAV-HBV1.2 and rAAV8-HBV1.3-transduced HBV-carrier mouse models
Oral gavage
50 μg/kg
15 consecutive days
Evaluated the therapeutic efficacy of Entecavir in HBV-carrier mouse models, showing significant reduction in serum HBV DNA copies but inability to induce anti-HBs Abs or eliminate serum HBsAg.
NPJ Vaccines. 2024 Feb 3;9(1):22
C57BL/6 mice
Chronic unpredictable mild stress (CUMS) model
Gastric administration
0.3 mg/kg
Once daily for 2 weeks
Entecavir significantly reversed chronic stress-induced negative emotional behaviors, including anxiety- and depressive-like behaviors, and improved microglial morphological activation and immuno-inflammatory responses in the BLA region.
J Neuroinflammation. 2023 Feb 15;20(1):37
C57BL/6J mice
HBV carrier mouse model
Oral gavage
0.1 mg/kg
Once daily for 15 days
To evaluate the inhibitory effect of Entecavir on HBV-DNA levels
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