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Entecavir hydrate CAS 209216-23-9 ENTECAVIR MONOHYDRATE
Entecavir hydrate is a new kind of cyclopentyl acyl guanosine anti-hepatitis b virus medicine with its pharmacological effects similar as entecavir. It is clinically applied to the treatment of adult chronic hepatitis b in which there is active viral replication, increased serum transaminase ALT or active lesions showed from liver histology.
In the transfected human HepG2 cells with wild type of hepatitis b virus, the 50% inhibition concentration (EC50) of entecavir in inhibiting the virus DNA synthesis is about 0.004 μM. The median value of the EC50 of entecavir on the inhibition of lamivudine resistant strains (rtL180M rtM204V) is 0.026 μM (range: 0.01 to 0.059 μM). However, entecavir has no clinically relevant effect on the growth of the in type 1 human immunodeficiency virus (HIV) on the cell culture (EC50 > 10 μM). Daily or weekly administration of this product can reduce the DNA level of hepatitis b virus of North American marmot and duck. Long-term studies on 5 North America marmot have shown that oral administration of 0.5 mg/kg entecavir per week (equivalent to the dose of 1.0 mg to the human body) can maintain the viral DNA in undetectable level for three marmot (HBV DNA levels < 200 copies/mL, PCR method) for as long as three years. In any animals which have subject to treatment of this drug for up to three years, there have been no cases of the HBV polymerase's resistances on the entecavir.
Research reagent; API. Antiviral products; Nucleoside classes; Intermediates; Active pharmaceutical ingredients. Baraclude; Antiviral medicine; The raw material; Antiviral; Pharmaceutical raw materials; Liver diseases, the Series
Category: Antibiotic Drugs API