Entecavir CAS NO.142217-69-4

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This product is guanine nucleoside analogue, which can inhibit the polymerase of hepatitis b virus (HBV). It is phosphorylated into active triphosphates, which have a 15 hour half-life in cells. Entecavir triphosphate inhibits all three viral polymerase (reverse transcriptase) activities by competing with deoxyguanine nucleoside triphosphate, the natural substrate of HBV polymerase :(1) initiation of HBV polymerase; (2) formation of reverse transcription negative chains of progenomic mRNA; (3) synthesis of HBV DNA plus strand. The inhibition constant (Ki) of entecavir triphosphate on HBV DNA polymerase was 0.0012 mu. Entecavir triphosphate inhibited alpha, beta, delta DNA polymerase and mitochondrial gamma DNA polymerase in cells with Ki values of 18 to 160 microns.

 

Entecavir is a kind of used in the treatment of hepatitis b virus infection of a new generation of guanine nucleoside analogues for oral administration, mainly used in the treatment of adults with active viral replication and serum transaminase continues to increase, or liver histology for active pathological changes of chronic hepatitis b, it is the lowest drop viruses mutate fastest, strongest chances of nucleoside analogues.

 

Data show that different chronic hepatitis b patients, including patients with initial nucleoside treatment, nucleoside treatment and cirrhosis, can quickly control the disease by using entecavir tablets and easily reach the realistic end point of treatment, that is, hepatitis b virus cannot be detected. By adhering to treatment, a considerable number of patients can reach the satisfactory end point of treatment, that is, serological conversion of e antigen, and some patients can even reach the ideal end point of treatment, that is, surface antigen conversion.