Entecavir hydrate
China [CN] Entecavir monohydrate is a new type of cyclovaleryl guanosine anti-hepatitis B virus drug. Its pharmacological effect is similar to that of entecavir. Clinically, it is indicated for the treatment of chronic adult hepatitis B with active viral replication, persistently elevated serum transaminase ALT, or active liver histological lesions. This product is a guanine nucleoside analogue and has an inhibitory effect on hepatitis B virus (HBV) polymerase. It can be phosphorylated to become active triphosphate, and the half-life of triphosphate within cells is 15 hours. By competing with the natural substrate of HBV polymerase, deoxyguanine triphosphate Chemicalbook, entecavir triphosphate can inhibit all three activities of viral polymerase (reverse transcriptase) : (1) The initiation of HBV polymerase. (2) The formation of negative strands in reverse transcription of pregenomic mRNA. (3) Synthesis of the positive strand of HBVDNA. The inhibition constant (Ki) of entecavir triphosphate on HBVDNA polymerase is 0.0012μm. Entecavir triphosphate has a weak inhibitory effect on the α, β, δDNA polymerase of cells and mitochondrial γDNA polymerase, with a Ki value ranging from 18 to 160μm.
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