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Tenofovir disoproxil fumarate.
Shellee A Grim1, Frank Romanelli
1University of Kentucky, Lexington, KY 40536-0293, USA. sgrim2@uky.edu
The Annals of Pharmacotherapy
|May 30, 2003
Summary
Tenofovir disoproxil fumarate effectively suppresses HIV-1 RNA and boosts CD4+ cell counts. This nucleotide analog offers advantages in toxicity and adherence for HIV treatment.
Area of Science:
- Antiviral pharmacology
- HIV virology
- Nucleotide analog reverse transcriptase inhibitors
Background:
- Tenofovir disoproxil fumarate (TDF) is a key antiretroviral medication.
- Understanding its comprehensive profile is crucial for clinical application.
Purpose of the Study:
- To review the pharmacology, virology, pharmacokinetics, efficacy, safety, resistance, and clinical use of TDF.
- To consolidate existing knowledge on TDF for healthcare professionals.
Main Methods:
- Comprehensive literature search of MEDLINE (1966-August 2002) and HIV meeting abstracts.
- Inclusion of recent and pertinent publications and abstracts regarding tenofovir.
- Systematic review of available data on tenofovir disoproxil fumarate.
Main Results:
- TDF is a nucleotide prodrug converted to tenofovir diphosphate, inhibiting HIV-1 reverse transcriptase.
- Clinical trials demonstrate TDF's efficacy in suppressing HIV-1 RNA and increasing CD4+ counts.
- TDF allows once-daily dosing due to its long intracellular half-life and has minimal drug interactions via the cytochrome P450 pathway.
Conclusions:
- Tenofovir is active against HIV-1 when used with other antiretrovirals.
- TDF is beneficial as a single-agent intensifier in highly active antiretroviral therapy for experienced patients.
- Preliminary data suggest encouraging results for treatment-naïve patients.