tenofovir octadecyloxyethyl ester

Tenofovir octadecyloxyethyl ester is a lipid-conjugate prodrug of the nucleotide analog tenofovir, specifically designed to enhance liver-specific delivery and reduce systemic toxicity. Developed by Xinkai Pharmaceutical Chemical Intermediates (Shanghai), this small molecule utilizes an octadecyloxyethyl (ODE) moiety to exploit lipid uptake pathways, facilitating higher intracellular concentrations of the active drug in hepatocytes. Once internalized, the prodrug is enzymatically cleaved to release tenofovir, which is subsequently phosphorylated to tenofovir diphosphate. This active form acts as a potent inhibitor of the Hepatitis B virus (HBV) RNA-directed DNA polymerase (reverse transcriptase), causing premature termination of the viral DNA chain. By concentrating the drug in the liver, tenofovir octadecyloxyethyl ester aims to provide superior antiviral efficacy for chronic hepatitis B while minimizing the renal and bone density side effects typically associated with systemic tenofovir exposure.

Other names

octadecyloxyethyl tenofovir