ArticleAIDS (London, England)2012
Tenofovir and tenofovir disoproxil fumarate pharmacokinetics from intravaginal rings.
Article in AIDS (London, England), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
26 citing papers in PubMed, 35 citations in OpenAlex.
- An intravaginal ring for HIV pre-exposure prophylaxis: assessment of safety and pharmacokinetics in a randomized, placebo-controlled clinical trial.Frontiers in cellular and infection microbiology · 2026Trial
- A phase 1 randomized placebo-controlled safety and pharmacokinetic trial of a tenofovir disoproxil fumarate vaginal ring.AIDS (London, England) · 2016Trial
- Preclinical Pharmacokinetics of a Triple-Combination Intravaginal Ring for HIV Prevention.Pharmaceutics · 2026Article
- Surrogate post-coital testing for contraceptive efficacy against human sperm activity in the ovine vaginal model†.Biology of reproduction · 2021Article
- Safety and pharmacokinetics of single, dual, and triple antiretroviral drug formulations delivered by pod-intravaginal rings designed for HIV-1 prevention: A Phase I trial.PLoS medicine · 2018Article
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- Combination Pod-Intravaginal Ring Delivers Antiretroviral Agents for HIV Prophylaxis: Pharmacokinetic Evaluation in an Ovine Model.Antimicrobial agents and chemotherapy · 2016Article
- Accurate measurement of female genital tract fluid dilution in cervicovaginal lavage samples.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences · 2016Article
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- An intravaginal ring for the sustained delivery of tenofovir disoproxil fumarate.International journal of pharmaceutics · 2015Article
- Lack of in vitro-in vivo correlation for a UC781-releasing vaginal ring in macaques.Drug delivery and translational research · 2015Article
- An intravaginal ring for the sustained delivery of antibodies.Journal of pharmaceutical sciences · 2014Article
- Pharmacokinetics and preliminary safety study of pod-intravaginal rings delivering antiretroviral combinations for HIV prophylaxis in a macaque model.Antimicrobial agents and chemotherapy · 2014Article
- Comparison of the vaginal microbial communities in women with recurrent genital HSV receiving acyclovir intravaginal rings.Antiviral research · 2014Article
- Sustained delivery of commensal bacteria from pod-intravaginal rings.Antimicrobial agents and chemotherapy · 2014Article
- Intravaginal ring eluting tenofovir disoproxil fumarate completely protects macaques from multiple vaginal simian-HIV challenges.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Pharmacokinetics of a multipurpose pod-intravaginal ring simultaneously delivering five drugs in an ovine model.Antimicrobial agents and chemotherapy · 2013Article
- Antiretroviral bioanalysis methods of tissues and body biofluids.Bioanalysis · 2013Review
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 1 country.
Funding
Abstract
objectivesTo compare the distribution of tenofovir in sheep vaginal lumen, tissue, and plasma following topical delivery of the antiretroviral drug from intravaginal rings, either as tenofovir or the disoproxil fumarate prodrug.
designComparative pharmacokinetic study in sheep.
methodIntravaginal rings formulated to achieve equivalent release rates of tenofovir and its disoproxil fumarate prodrug were evaluated for 28 days in sheep, with four animals in each group. Drug concentrations were measured by high-performance liquid chromatography-mass spectrometry.
resultsTenofovir levels in cervicovaginal lavage were indistinguishable (P > 0.30) in both groups, but tissue levels in animals receiving the prodrug were 86-fold higher than those receiving tenofovir, and approximately 50 times higher than the level shown to be protective of HIV infection in the CAPRISA 004 trial.
conclusionThis is the first study to compare the pharmacokinetics of tenofovir and its disoproxil fumarate prodrug administered topically to the vaginal tract. These in-vivo data show that the prodrug leads to significantly higher drug tissue levels than tenofovir, a finding that may have important implications for the development of preexposure prophylaxis strategies based on topical delivery of antivirals to the female genital tract.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.