Entecavir monohydrate

Details:

entecavir hydrate;
Entecavir hydrate;
Entecavir monohydrate;
9-[(1S,3R,4S)-4-Hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]guanine Monohydrate;
Entecavir Monohydrate IsoMers;
Entecavir Hydrate;
Entecavirhydrate;
Entecavir (monohydrate)

Entecavir monohydrate is a new type of cyclopentanoylguanosine anti-hepatitis B virus drug. Its pharmacological action is similar to entecavir. It is clinically suitable for active virus replication, continuous increase in serum transaminase ALT or liver histology showing active lesions. Treatment of chronic adult hepatitis B. This product is a guanine nucleoside analog, which has an inhibitory effect on hepatitis B virus (HBV) polymerase. It can be phosphorylated into active triphosphate, and the half-life of triphosphate in the cell is 15 hours. By competing with the natural substrate of HBV polymerase Chemicalbook deoxyguanosine triphosphate, Entecavir triphosphate can inhibit all three activities of viral polymerase (reverse transcriptase): (1) HBV polymerase initiation. (2) Formation of reverse transcription negative strand of pregenomic mRNA. (3) Synthesis of the positive strand of HBVDNA. The inhibitory constant (Ki) of entecavir triphosphate on HBV DNA polymerase is 0.0012μm. Entecavir triphosphate has a weak inhibitory effect on cell α, β, δ DNA polymerase and mitochondrial γ DNA polymerase, with Ki values ranging from 18 to 160 μm.

Entecavir has a strong antiviral ability and a low incidence of drug resistance in long-term applications. It may have a direct inhibitory effect on cccDNA in liver cells. It can effectively treat chronic hepatitis B and has a better curative effect than lamivudine. 2. Entecavir had a resistance rate of 0 for patients who were newly treated for 1 year, but had a resistance rate of 5.8% for patients who had YMDD mutations for 1 year. 3. Entecavir's inhibitory effect on lamivudine-resistant (rtL1Chemicalbook80M and/or rtM204V/I) virus strains is 8 to 30 times weaker than that of wild strains, so the therapeutic dose for lamivudine-resistant patients should be increased to 1.0 mg. Entecavir is sensitive to viruses with adefovir resistance mutations (HBV DNA polymerase rtN236T or rtA181V mutation). Entecavir-resistant virus strains are sensitive to adefovir, but still remain resistant to lamivudine.