恩替卡韦（Entecavir）.docVIP

恩替卡韦（Entecavir） Entecavir Entecavir English Name: Entecavir Chinese names: 2- amino -9-[(1S, 3S, 4S), -4- hydroxy -3- hydroxymethyl -2-, amyl]-1, 9- hydrogen, -6-H- purine, -6- ketone hydrate Chinese Pinyin: Entikawei Pian Molecular formula: C12H15N5O3? H2O Molecular weight: 295.3 Raw material content: greater than 99.8% (actual content above 99.9%) It is up to 0531 -pharmacology and toxicology Mechanism [1]: This product is a nucleoside analogue of guanine and 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. Antiviral activity In human HepG2 cells transfected with wild-type hepatitis B virus, the concentration required for the synthesis of entecavir 50% virus DNA (EC50) was 0.004 mu M. EN entecavir for lamivudine resistant virus strains (rtL180M, rtM204V) EC50 the median value is 0.26 M (range 0.01 to 0.059 M), and entecavir on medium growth in human immunodeficiency type 1 cells (HIV) without clinical related activity (EC50 10 M). Every day or every week using this product can reduce the long-term study of woodchuck that weekly oral entecavir 0.5mg/kg Cave (equivalent to human 1.0mg virus DNA 3 dose) can be only the soil marmots maintained at the undetectable level (level 200 virus DNA copies /ml, PCR) 3 years. No chan