Metabolic Activation of the Anti-Hepatitis C Virus Nucleotide Prodrug PSI-352938
Antimicrobial Agents and Chemotherapy,
Niu C et al. – In addition, formation of nucleoside metabolites was observed in primary hepatocytes, and ecto–5–nucleotidase was able to dephosphorylate the monophosphate metabolites. Since CYP3A4 is highly expressed in the liver, the CYP3A4–dependent metabolism of PSI–352938 makes it an effective liver–targeted prodrug, in part accounting for the potent antiviral activity observed clinically.