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Hepunofovir fumarate (also referred to as hepenofovir fumarate or HTS) is an orally active, liver-targeting prodrug of tenofovir developed for the treatment of chronic hepatitis B (CHB). Utilizing HepDirect technology, the prodrug is designed to remain stable in systemic circulation and undergo cleavage specifically within hepatocytes by cytochrome P450 3A4 (CYP3A4). This liver-selective activation releases tenofovir, which is subsequently phosphorylated to its active diphosphate form, a potent inhibitor of the hepatitis B virus (HBV) polymerase/reverse transcriptase. By concentrating the active drug in the liver, hepunofovir fumarate achieves robust antiviral efficacy while minimizing systemic exposure, thereby reducing the risk of tenofovir-associated renal and bone toxicities.
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