The Pharmacokinetics and Viral Activity of Tenofovir in the Male Genital Tract
- 1 March 2008
- journal article
- clinical trial
- Published by Wolters Kluwer Health in JAIDS Journal of Acquired Immune Deficiency Syndromes
- Vol. 47 (3) , 329-333
- https://doi.org/10.1097/qai.0b013e3181632cc3
Abstract
Objective: To measure tenofovir (TFV) concentrations in the male genital tract (GT) after single and multiple doses of tenofovir disoproxil fumarate (TDF) and evaluate the HIV-1 RNA response to monotherapy. Design and Methods: A pharmacokinetic study of blood plasma (BP) and GT TFV concentrations in 9 men was conducted after 1 and ≥14 doses of TDF. TFV concentrations were measured by validated high-performance liquid chromatography-ultraviolet or tandem mass spectrometry methods, and HIV-1 RNA was measured using Roche (Roche Molecular Systems, Branchburg, NJ) or bioMerieux (bioMerieux, Durham, NC) kits. Results: TFV GT concentrations were 4.4-fold ± 5.1-fold higher than BP after dose 1 and 5.1-fold ± 6.8-fold higher than BP after dose 14. Intracellular GT TFV-diphosphate concentrations were 9.4-fold higher than BP after dose 1 and 17.5-fold ± 22.6-fold higher after dose 7. After 14 days of TDF monotherapy, HIV-1 RNA decreased by 0.9 log10 copies/mL in blood and 1.0 log10 copies/mL in the GT. Conclusions: High TFV concentrations were achieved rapidly in the GT of all subjects after single and multiple doses and potently reduced BP and GT HIV-1 RNA levels.Keywords
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