Volume V of the series Biotechnology: Pharmaceutical Aspects pp 1347-1357

Case Study: Tenofovir Disoproxil Fumarate: An Oral Prodrug of Tenofovir

  • Maria FardisAffiliated withGilead Sciences Inc.
  • , Reza OliyaiAffiliated withGilead Sciences Inc.

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Tenofovir (PMPA) is a novel nucleotide analog that belongs to the class of acyclic nucleoside phosphonates. The potential antiviral effect of tenofovir was demonstrated by Hol and DeClercq (Balzarini et al., 1993). In this class of compounds, the ribose-phosphate group is replaced with the isopolar phosphonopropyl ether functionality. Tenofovir is recognized by host kinases and is phosphorylated in situ to the virologically active tenofovir diphosphate. Tenofovir diphosphate inhibits the human immunodeficiency virus (HIV-1 and HIV-2) DNA polymerase (reverse transcriptase) in addition to other viral DNA polymerases (Naesens et al., 1997). This inhibition results in DNA chain termination and impairment of viral replication. The IC50 values of tenofovir inhibition of HIV-1 reverse transcriptase is between 0.04 and 8.5 µM (Viread package insert).