Entecavir is primarily indicated for the treatment of chronic hepatitis B in adults with evidence of active viral replication and either persistent elevations in serum ALT levels or evidence of histologically active disease.
Pharmacological Action
Entecavir is a guanosine nucleoside analog with potent inhibitory activity against hepatitis B virus (HBV) polymerase. It undergoes phosphorylation to the active triphosphate form, which has a half-life of approximately 15 hours within cells. Entecavir triphosphate competes with the natural substrate deoxyguanosine triphosphate, thereby inhibiting all three activities of the HBV polymerase (reverse transcriptase): 1. Initiation of HBV DNA synthesis 2. Reverse transcription of the negative strand from the pregenomic mRNA 3. Synthesis of the positive strand of HBV DNA.