ArticleAntimicrobial agents and chemotherapy2012
Pharmacokinetics of tenofovir following intravaginal and intrarectal administration of tenofovir gel to rhesus macaques.
Article in Antimicrobial agents and chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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
53 citing papers in PubMed.
- Population pharmacokinetics of tenofovir alafenamide delivered via an annual subdermal implant in South African women.Scientific reports · 2026Trial
- Phase 1 randomized pharmacokinetic and safety study of a 90-day tenofovir vaginal ring in the United States.Journal of the International AIDS Society · 2024Trial
- Trial
- Pharmacokinetics and Pharmacodynamics of Tenofovir Reduced-Glycerin 1% Gel in the Rectal and Vaginal Compartments in Women: A Cross-Compartmental Study With Directly Observed Dosing.Journal of acquired immune deficiency syndromes (1999) · 2018Trial
- Comparison of the Pharmacokinetics and Pharmacodynamics of Single-Dose Tenofovir Vaginal Film and Gel Formulation (FAME 05).Journal of acquired immune deficiency syndromes (1999) · 2018Trial
- Trial
- Trial
- Trial
- Sustained mucosal delivery of SAMT-247 via an intravaginal ring reduces the risk of SIVCell reports. Medicine · 2026Article
- Mucosal tenofovir 1% gel stimulates cell proliferation and type I/III interferon pathways.Microbiology spectrum · 2026Article
- Friend or foe: divergent immunomodulatory effects of metabolites derived from the virucidal zinc finger inhibitor SAMT-247.Frontiers in immunology · 2026Article
- Intravaginal delivery of mRNA-encoded antibodies with enhanced breadth and potency for SHIV/HIV protection.Nature communications · 2025Article
- Preclinical Considerations for Long-acting Delivery of Tenofovir Alafenamide from Subdermal Implants for HIV Pre-exposure Prophylaxis.Pharmaceutical research · 2023Article
- Translational Models to Predict Target Concentrations for Pre-Exposure Prophylaxis in Women.AIDS research and human retroviruses · 2022Review
- Article
- TheiScience · 2022Article
- Fundamental aspects of long-acting tenofovir alafenamide delivery from subdermal implants for HIV prophylaxis.Scientific reports · 2022Article
- Women for science and science for women: Gaps, challenges and opportunities towards optimizing pre-exposure prophylaxis for HIV-1 prevention.Frontiers in immunology · 2022Review
- Development, Characterization and In Vivo Pharmacokinetic Assessment of Rectal Suppositories Containing Combination Antiretroviral Drugs for HIV Prevention.Pharmaceutics · 2021Article
- Efficacy of Vaginally Administered Gel Containing Emtricitabine and Tenofovir Against Repeated Rectal Simian Human Immunodeficiency Virus Exposures in Macaques.The Journal of infectious diseases · 2018Article
Corrections and comments
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tenofovir gel (1%) is being developed as a microbicide for the prevention of human immunodeficiency virus (HIV) infection and has been shown to reduce transmission to women by 39%. The gel also prevents infection in macaques when applied intravaginally or intrarectally prior to challenge with simian-human immunodeficiency virus (SHIV), but very little pharmacokinetic information for macaques is available to help extrapolate the data to humans and thus inform future development activities. We have determined the pharmacokinetics of tenofovir in macaques following intravaginal and intrarectal administration of 0.2, 1, and 5% gels. Plasma and vaginal and rectal fluid samples were collected up to 24 h after dosing, and at 24 h postdosing biopsy specimens were taken from the vaginal wall, cervix, and rectum. Following vaginal and rectal administration, tenofovir rapidly distributed to the matrices distal to the site of administration. In all matrices, exposure increased with increasing dose, and with the 1% and 5% formulations, concentrations remained detectable in most animals 24 h after dosing. At all doses, concentrations at the dosing site were typically 1 to 2 log units higher than those in the opposite compartment and 4 to 5 log units higher than those in plasma. Exposure in vaginal fluid after vaginal dosing was 58 to 82% lower than that in rectal fluid after rectal dosing, but plasma exposure was 1- to 2-fold greater after vaginal dosing than after rectal dosing. These data suggest that a tenofovir-based microbicide may have the potential to protect when exposure is via vaginal or anal intercourse, regardless of whether the microbicide is applied vaginally or rectally.
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