This product is a nucleoside analogue of guanine, which has inhibitory effect on hepatitis B virus (HBV) polymerase. It can be converted into active three phosphate by phosphorylation, and the half-life of three phosphate in cells is 15 hours. The natural substrate and HBV polymerase three phosphate deoxyguanosine competition, entecavir three phosphate can inhibit the viral polymerase (reverse transcriptase) of all three activities:

(1) HBV polymerase promoter;
(2) before the formation of genomic mRNA reverse transcription negative strand synthesis;
(3) HBV DNA is the chain.

The inhibitory constant (Ki) of entecavir three phosphate against HBV DNA polymerase was 0.0012 mu M. Entecavir three phosphate inhibited the alpha, beta, Delta DNA polymerase, and mitochondrial gamma DNA polymerase of cells less, and the Ki value was 18, as far as 160 M.

Appliction

1.Entecavir is an oral antiviral drug used in the treatment of hepatitis B infection.