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Tenofovir disoproxil fumarate.
Joel E Gallant1, Stanley Deresinski
1Div. of Infectious Diseases, Johns Hopkins University School of Medicine, Baltimore, Maryland 21287, USA. jgallant@jhmi.edu
Summary
Tenofovir disoproxil fumarate (tenofovir DF) is an effective HIV and hepatitis B virus treatment. It shows good tolerability and is active against some resistant strains, though cross-resistance can occur.
Area of Science:
- Antiviral drug development
- Nucleotide analogue reverse-transcriptase inhibitors
Background:
- Tenofovir disoproxil fumarate (tenofovir DF) is a prodrug of tenofovir, a potent inhibitor of reverse transcriptase.
- It is used to treat human immunodeficiency virus (HIV) and hepatitis B virus (HBV).
Purpose of the Study:
- To review the efficacy and safety of tenofovir DF in HIV treatment.
- To examine its activity against nucleoside-resistant HIV strains.
Main Methods:
- Review of clinical trial data for tenofovir DF in HIV-infected patients.
- Analysis of resistance patterns and cross-resistance with other nucleoside analogues.
Main Results:
- Tenofovir DF demonstrated efficacy in both treatment-experienced and initial HIV therapy.
- It is active against some nucleoside-resistant HIV strains, with K65R being a key resistance mutation.
- The drug was well-tolerated in trials up to 96 weeks, with favorable lipid profiles and no observed mitochondrial toxicity.
Conclusions:
- Tenofovir DF is a well-tolerated and effective option for HIV treatment.
- Its activity against resistant strains and favorable safety profile make it a valuable therapeutic agent.